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1

Chakraborty, Santanu, Madhusmruti Khandai, Anuradha Sharma, Ch Patra, V. Patro, and Kalyan Sen. "Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations." Acta Pharmaceutica 59, no. 3 (September 1, 2009): 313–23. http://dx.doi.org/10.2478/v10007-009-0025-8.

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Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.
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2

Dumitriu, Raluca Petronela, Ana Maria Oprea, and Cornelia Vasile. "Kinetics of Swelling and Drug Release from PNIPAAm/Alginate Stimuli Responsive Hydrogels." Solid State Phenomena 154 (April 2009): 17–22. http://dx.doi.org/10.4028/www.scientific.net/ssp.154.17.

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Stimuli responsive hydrogels are very attractive for applications in sustained and/or targeted drug delivery systems. As the release of drugs is related to the swelling behavior of hydrogels, the swelling kinetic studies become of great importance to appreciate the release kinetics from hydrogel matrices. Hydrogels with high performance properties have been prepared from N-isopropylacryl amide (NIPAAm) and sodium alginate, crosslinked with N,N`-methylene-bis-(acrylamide) (MBAAm). This study is focused on the investigation of swelling and drug release kinetics, coupled by morphological studies. The kinetic parameters of the swelling at different temperatures for hydrogels samples have been evaluated and confirmed their temperature-responsive behavior. The swelling rate constant (ksw) decreases of with increasing temperature and slight increases with the alginate content in the samples. The drug release kinetic study from the prepared hydrogel matrices was performed in twice-distilled water and ethanol for bioactive agents as vanillin and ketoprofen, respectively. An increase of alginate content results in a slower rate and smaller percentage of vanillin and ketoprofen released. It has been established that the ketoprofen occurs according with case II of transport and vanillin release behavior occurs by an anomalous transport mechanism. The values of the release rate constant (kr) decreased by increasing swelling degree in case of 75/25 NIPAAm/alginate hydrogels and decreased also by increasing content of alginate in hydrogels with various compositions. Morphological studies performed by environmental scanning electron microscopy (ESEM) evidenced a relaxed network at high relative humidity, which explain both swelling and release profiles.
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3

Arefin, Paroma, Ikramul Hasan, Md Shfiqul Islam, and Md Selim Reza. "Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres." Bangladesh Pharmaceutical Journal 19, no. 1 (August 10, 2016): 58–67. http://dx.doi.org/10.3329/bpj.v19i1.29240.

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The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016
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4

Mitran, Raul-Augustin, Daniela Berger, Jeanina Pandele-Cusu, and Cristian Matei. "Effect of Aluminum Incorporation into Mesoporous Aluminosilicate Framework on Drug Release Kinetics." Journal of Nanomaterials 2017 (2017): 1–9. http://dx.doi.org/10.1155/2017/9864396.

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Mesoporous silica materials are promising nanocarriers for the development of drug delivery systems. In this study, the influence of pore size, volume, surface area, and doping the silica framework on the release kinetics of a model drug, metoprolol, has been studied. 20% or 50% wt. therapeutic agent was loaded into the carrier mesopores through incipient wetness impregnation. The carriers and drug-loaded samples have been characterized by small- and wide-angle X-ray diffraction, FT-IR spectroscopy, scanning electron microscopy, and nitrogen adsorption-desorption isotherms. The in vitro release profiles have been fitted using a three-parameter kinetic model and they have been explained in terms of the release rate during the burst and sustained release stages and the fraction of drug molecules released during the burst stage. The silica framework doping with aluminum was found to decrease the amount of drug released in the burst stage, without affecting the other kinetic parameters. The therapeutic agent release rates depend mainly on the pore size and volume of the mesoporous carriers and drug-loaded samples.
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5

Loew, Stephan, Alfred Fahr, and Sylvio May. "Modeling the Release Kinetics of Poorly Water-Soluble Drug Molecules from Liposomal Nanocarriers." Journal of Drug Delivery 2011 (June 7, 2011): 1–10. http://dx.doi.org/10.1155/2011/376548.

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Liposomes are frequently used as pharmaceutical nanocarriers to deliver poorly water-soluble drugs such as temoporfin, cyclosporine A, amphotericin B, and paclitaxel to their target site. Optimal drug delivery depends on understanding the release kinetics of the drug molecules from the host liposomes during the journey to the target site and at the target site. Transfer of drugs in model systems consisting of donor liposomes and acceptor liposomes is known from experimental work to typically exhibit a first-order kinetics with a simple exponential behavior. In some cases, a fast component in the initial transfer is present, in other cases the transfer is sigmoidal. We present and analyze a theoretical model for the transfer that accounts for two physical mechanisms, collisions between liposomes and diffusion of the drug molecules through the aqueous phase. Starting with the detailed distribution of drug molecules among the individual liposomes, we specify the conditions that lead to an apparent first-order kinetic behavior. We also discuss possible implications on the transfer kinetics of (1) high drug loading of donor liposomes, (2) attractive interactions between drug molecules within the liposomes, and (3) slow transfer of drugs between the inner and outer leaflets of the liposomes.
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6

Ghosal, Souvik, Javon E. Walker, and Christopher A. Alabi. "Predictive Platforms of Bond Cleavage and Drug Release Kinetics for Macromolecule–Drug Conjugates." Annual Review of Chemical and Biomolecular Engineering 12, no. 1 (June 7, 2021): 241–61. http://dx.doi.org/10.1146/annurev-chembioeng-091720-030636.

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Macromolecule–drug conjugates (MDCs) occupy a critical niche in modern pharmaceuticals that deals with the assembly and combination of a macromolecular carrier, a drug cargo, and a linker toward the creation of effective therapeutics. Macromolecular carriers such as synthetic biocompatible polymers and proteins are often exploited for their inherent ability to improve drug circulation, prevent off-target drug cytotoxicity, and widen the therapeutic index of drugs. One of the most significant challenges in MDC design involves tuning their drug release kinetics to achieve high spatiotemporal precision. This level of control requires a thorough qualitative and quantitative understanding of the bond cleavage event. In this review, we highlight specific research findings that emphasize the importance of establishing a precise structure–function relationship for MDCs that can be used to predict their bond cleavage and drug release kinetic parameters.
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7

Das, Utpal, Shimul Halder, Abul Kalam Lutful Kabir, Harun Or Rashid, and Abu Shara Shamsur Rouf. "Development and in vitro Evaluation of Sustained Release Matrix Tablets of Indapamide from Methocel® K15 MCR and K100 LVCR." Dhaka University Journal of Pharmaceutical Sciences 10, no. 2 (September 3, 2012): 87–92. http://dx.doi.org/10.3329/dujps.v10i2.11785.

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Indapamide, a low-dose thiazide-type diuretic, is used for the treatment of essential hypertension. In this study, we developed an indapamide sustained release formulation using Methocel K15 MCR (a modified hydroxypropyl methylcellulose), Methocel K100 LVCR (a modified hydroxypropyl methylcellulose), magnesium stearate, talc and starch 1500 by direct compression. The powders for tableting were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity etc. The tablets were subjected to thickness, weight variation test, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out in the gastric medium (pH 1.3) for first two hours and then in the intestinal medium (pH 6.8) for 22 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus. The granules showed satisfactory flow properties, compressibility index etc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-5 and F-7 (up to 75.36 % drug release in 12 hours) could extend the drug release up to 12 hours. The drug release patterns were simulated in different kinetic orders such as Zero Order release kinetics, First Order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism. From the study we observed that Higuchi release kinetics was the predominant release mechanism than Zero Order and First Order kinetics. The drug release mechanism from the matrix tablets was found to be non Fickian mechanism. DOI: http://dx.doi.org/10.3329/dujps.v10i2.11785 Dhaka Univ. J. Pharm. Sci. 10(2): 87-92, 2011 (December)
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8

Gierszewska, Magdalena, Jadwiga Ostrowska-Czubenko, and Ewelina Chrzanowska. "CHARACTERISTICS OF ASCORBIC ACID RELEASE FROM TPP-CROSSLINKED CHITOSAN/ALGINATE POLYELECTROLYTE COMPLEX MEMBRANES." Progress on Chemistry and Application of Chitin and its Derivatives XXIII (September 10, 2018): 76–87. http://dx.doi.org/10.15259/pcacd.23.007.

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Chitosan/alginate polyelectrolyte complex membranes (Ch/Alg) additionally cross-linked with tripolyphosphate (TPP) and containing ascorbic acid (AA) were prepared. The dynamic swelling behaviour of Ch/Alg/TPP and ascorbic acid release from the membrane were characterised in different buffer solutions. It has been found that the pH of the buffer solution affects the swelling and release behaviour of AA. Ascorbic acid release, observed over a period of 360 min, exhibited a biphasic pattern, characterised by a fast initial burst release, followed by a slow, sustained release. Different mathematical models were used to study the kinetics and transport mechanism of AA from Ch/Alg/TPP hydrogels. Drug release data were fitted to the zero order kinetic model and first order kinetic model. To characterise the drug mechanism, the release data were fitted to the Higuchi and Korsmeyer-Peppas equations. The initial burst AA release followed zero order kinetics and was quasi-Fickian in nature. The second step of AA release followed first order kinetics.
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9

Kundrat, Vojtech, Nicole Cernekova, Adriana Kovalcik, Vojtech Enev, and Ivana Marova. "Drug Release Kinetics of Electrospun PHB Meshes." Materials 12, no. 12 (June 14, 2019): 1924. http://dx.doi.org/10.3390/ma12121924.

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Microbial poly(3-hydroxybutyrate) (PHB) has several advantages including its biocompatibility and ability to degrade in vivo and in vitro without toxic substances. This paper investigates the feasibility of electrospun PHB meshes serving as drug delivery systems. The morphology of the electrospun samples was modified by varying the concentration of PHB in solution and the solvent composition. Scanning electron microscopy of the electrospun PHB scaffolds revealed the formation of different morphologies including porous, filamentous/beaded and fiber structures. Levofloxacin was used as the model drug for incorporation into PHB electrospun meshes. The entrapment efficiency was found to be dependent on the viscosity of the PHB solution used for electrospinning and ranged from 14.4–81.8%. The incorporation of levofloxacin in electrospun meshes was confirmed by Fourier-transform infrared spectroscopy and UV-VIS spectroscopy. The effect of the morphology of the electrospun meshes on the levofloxacin release profile was screened in vitro in phosphate-buffered saline solution. Depending upon the morphology, the electrospun meshes released about 14–20% of levofloxacin during the first 24 h. The percentage of drug released after 13 days increased up to 32.4% and was similar for all tested morphologies. The antimicrobial efficiency of all tested samples independent of the morphology, was confirmed by agar diffusion testing.
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10

Kumar, B., and G. Jeyabalan. "Development of Anti-diabetic Niosomes Formulation Containing Metformin and Gliclazide." Indian Journal of Pharmaceutical and Biological Research 5, no. 02 (June 30, 2017): 24–28. http://dx.doi.org/10.30750/ijpbr.5.2.5.

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Metformin/Gliclazide niosomes were formulated with span 60 by ether injection method. Three batches MG1-MG3 were prepared in order to study influence of drug polymer ratio on the niosomes formation and in vitro drug release. The formulated niosomes were characterized by drug entrapment, vesicle size determination, and in vitro drug release. Optimized concentration of span 60 and cholesterol was found to be 1:1. In the in-vitro study, niosomes formulation of MG1 showed high percentage of drug release, 40.18 to 45.75% for about 8 hrs. This indicated that this batch of niosomes formulation exhibit sustained drug release pattern as the niosomes act as reservoir system for continuous delivery of drug. The quantity of Metformin/Gliclazide present in the niosomes and the release medium were estimated by a validated HPLC method. The formulated niosomes had acceptable physicochemical characters and released the drug over 6-8 h. The data obtained from in vitro release studies were fitted with various kinetic models and was found to follow Higuchi kinetics.
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11

Andreevskaya, SN, TG Smirnova, EN Antonov, LN Chernousova, SE Bogorodsky, EE Larionova, VK Popov, and A. Ergeshov. "New in vitro model to evaluate kinetics of antimycobacterial drug release from bioresorbable polymeric carriers." MicroRNA in ocular pathology, no. 2020(4) (August 2020): 10–15. http://dx.doi.org/10.24075/brsmu.2020.050.

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Sustained-release drugs against tuberculosis are a promising approach to therapy since they positively affect patient compliance with long regimens, especially when it comes to the multidrug-resistant form of the disease. Conventional UV-visible spectroscopy does not work well with multicomponential culture media used for growing M. tuberculosis. The aim of this study was to develop a method for evaluating the kinetics of anti-tuberculosis drug released from bioresorbable polymeric carriers suitable for screening a wide range of encapsulated prolonged-release drugs and identifying the best performing candidate. While studying the growth dynamics of the laboratory susceptible strain M. tuberculosis H37Rv in the presence of different levofloxacin concentrations (from 0.03 to 0.4 μg/ml), we developed a model, which is essentially a set of 2 parallel experiments evaluating the kinetics of drug release into the culture medium. The results of these 2 experiments conducted on 3 encapsulated forms of levofloxacin loaded onto bioresorbable polymeric PLGA carriers (particles sized 50 μm and 100 μm and the matrix) revealed that release kinetics of the drug largely depended on the type of polymeric carrier. The best encapsulation of the antibiotic and its gradual release into the culture medium was observed for the matrix. All experiments were run in 3 replicates. The obtained data were analyzed using descriptive statistics.
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12

Vercik, Luci Cristina de Oliveira, Andres Vercik, and Eliana Cristina da Silva Rigo. "Kinetics of silver nanoparticle release from chitosan spheres." MRS Advances 2, no. 19-20 (2017): 1089–94. http://dx.doi.org/10.1557/adv.2017.48.

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ABSTRACTThe kinetics of silver nanoparticles release from chitosan spheres is addressed experimentally and theoretically in this work. From the experimental viewpoint, the study of silver nanoparticles release is performed by measuring the time-dependent UV-Vis spectra of solutions where spheres were dispersed. The UV-VIS spectra intensity reflects the concentration of nanoparticles in the solution. Despite simple expressions for drug release are found in the literature, as those that relate the amount of drug release with the square root of time, a proper modeling might require the inclusion of several phenomena such as the presence of stagnant layers, swelling or erosion of the matrix, accumulation of particles in the medium, amongst others. The experiments show that chitosan/silver nanoparticles complexes are actually released, indicating that both swelling and erosion of the matrix takes place during the release process. The simplest model for drug release, i.e., the Higuchi’s model, fits the observed results surprisingly well, which is a relevant result due to the lack of mathematical modeling for the release of nanoparticles.
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13

Wang, Lei, and Gang Wu. "Local Delivery System Using Thermosensitive Hydrogel and Drug Loading Microspheres for Cartilage Repairing." Advanced Materials Research 898 (February 2014): 300–303. http://dx.doi.org/10.4028/www.scientific.net/amr.898.300.

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A local drug delivery system constituted by hybrid microsphere/thermosensitive hydrogel was fabricated for Osteoarthritis (OA) therapy in the research. The hydrogel were synthesized by ring-opening copolymerization. Microsphere was fabricated by O/W emulsion and solution evaporation method. The properties of the products were characterized by 1HNMR, FTIR and phase transition diagram. The microsphere/hydrogel was prepared for in vitro drug release research. The results showed microsphere/hydrogel hybrid system can alleviate initial burst release. After 650 hours, only 60 percent of the drugs were released. Kinetics research implied the drug release is controlled by diffusion/erosion mechanism.
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14

Lee, Ping I. "Kinetics of drug release from hydrogel matrices." Journal of Controlled Release 2 (November 1985): 277–88. http://dx.doi.org/10.1016/0168-3659(85)90051-3.

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15

Bichara, Ali, Jean-Pierre Montheard, and Jean-Louis Taverdet. "Kinetics of a drug release from a delayed release device." European Polymer Journal 34, no. 9 (September 1998): 1283–93. http://dx.doi.org/10.1016/s0014-3057(97)00264-4.

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16

Haidar, Ziyad S. "Mathematical Modeling for Pharmacokinetic Predictions from Controlled Drug Release Nano Systems: A Comparative Parametric Study." Biomedical and Pharmacology Journal 11, no. 4 (December 25, 2018): 1801–6. http://dx.doi.org/10.13005/bpj/1552.

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In the present work, several mathematical models well-known in the literature for simulating drug release kinetics are compared using available experimental data sets obtained in real systems with different drugs and nano-sized carriers. Herein, the χ2 minimization method, is employed concluding that the Korsmeyer-Peppas model provides the best-fit in all cases. Hence, (i) better understanding of the exact mass transport mechanism(s) involved in drug(s) release, and (ii) quantitative prediction of the drug release kinetics, can be computed.
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17

Manalan, B. Valli, Nadendla Swathi, Narra Nandini, N. Hari Sree, Nilla Tejaswi Sai Maha Lakshmi, Mohammed Afrin Roshanara, and Rama Rao Nadendla. "Formulate and evaluate once daily sustained release tablet of highly soluble drug of metformin HCL." International Journal of Research in Pharmaceutical Sciences and Technology 1, no. 4 (July 14, 2020): 138–45. http://dx.doi.org/10.33974/ijrpst.v1i4.206.

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The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.
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18

Sharma, Megha, Seema Kohli, and Abhisek Pal. "PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 3 (March 1, 2017): 103. http://dx.doi.org/10.22159/ajpcr.2017.v10i3.15310.

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ABSTRACTObjective: To develop and evaluate floating microspheres of repaglinide (RG).Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMCK4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirringspeed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infraredspectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. Theresults showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from themicrospheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailabilityand patient compliance.Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose.
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19

El-Ghannam, Ahmed. "Bioceramic Drug Delivery System for Cancer Treatment and Regenerative Medicine." Key Engineering Materials 696 (May 2016): 245–49. http://dx.doi.org/10.4028/www.scientific.net/kem.696.245.

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Silica-calcium-phosphate composite (SCPC) is a drug delivery platform that has successfully demonstrated the ability to bind and release several therapeutics including antibiotics, peptides, anticancer drugs, and growth factors. It has successfully demonstrated a unique capacity for bone regeneration. The present studies address the effect of the phosphate and silicate functional groups on drug binding and controlled release kinetics of Cisplatin (Cis). Moreover, the roles of ceramic composition and resorbability on rhBMP2 release kinetics and bone regeneration in a critical size calvarial defect in rabbit is presented.
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20

Suprianto, Suprianto. "ANALISIS KINETIKA PELEPASAN TEOFILIN DARI GRANUL MATRIKS KITOSAN." Jurnal Ilmiah Manuntung 2, no. 1 (January 26, 2017): 70. http://dx.doi.org/10.51352/jim.v2i1.50.

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Moment the drug dosage form development, it is important to study the drug release or dissolution that is recognized as an element in drug development. Mathematical models could help optimize the design of drugs to produce models of drug release information. Analysis of quantitative values obtained when depicting dissolution drug release profiles more easily when the mathematical concepts used to describe the drug release kinetics model. Model release of drugs known include zero order, first order, Higuchi models, models Hixon Crowell and Peppas Korsmeyer models. The purpose of this review apply mathematical concepts to study the phenomenon of drug release theophylline granules matrix made from chitosan
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21

Damiri, Fouad, Yahya Bachra, Chaimaa Bounacir, Asmae Laaraibi, and Mohammed Berrada. "Synthesis and Characterization of Lyophilized Chitosan-Based Hydrogels Cross-Linked with Benzaldehyde for Controlled Drug Release." Journal of Chemistry 2020 (May 18, 2020): 1–10. http://dx.doi.org/10.1155/2020/8747639.

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In this study, chitosan-based hydrogels were produced by incorporating three drugs with a different solubility into a polymer matrix. The lyophilized chitosan salt was prepared using an innovative and less-expensive synthetic process by the freeze-drying technique. Firstly, the three drugs (caffeine, ascorbic acid, and 5-fluorouracil (5-FU)) were selected as model drugs to test the in vitro release behavior of the hydrogel. The drugs were solubilized in chitosan salt, lyophilized, and cross-linked with benzaldehyde involving the formation of a Schiff base with (–C=N-) linkage to produce a physical hydrogel. Subsequently, the physicochemical properties of N-benzyl chitosan and lyophilized chitosan salt were evaluated by Fourier-transform infrared (FTIR) spectra, scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). The intrinsic viscosity of the conventional chitosan was determined by the Mark–Houwink–Sakurada equation. Moreover, the kinetics of hydrogel swelling and drug release were studied by the UV-visible method at physiological conditions (pH = 7.4 at 37°C). The results show that lyophilized N-benzyl chitosan had a maximum swelling ratio of 720 ± 2% by immersion in phosphate-buffered saline solutions (PBS) (pH = 7.4 at 37°C). In vitro drug releases were evaluated in PBS, and the obtained results show that the maximum drug release after 24 h was 42% for caffeine, 99% for 5-FU, and 94% for ascorbic acid. Then, to optimize the cumulative release of caffeine, Tween 20 was added and 98% as a release percentage was obtained. The drug-loading results were investigated with the Korsmeyer–Peppas kinetic model and applied to determine the drug release mechanism.
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Ebadi, Mona, Kalaivani Buskaran, Bullo Saifullah, Sharida Fakurazi, and Mohd Zobir Hussein. "The Impact of Magnesium–Aluminum-Layered Double Hydroxide-Based Polyvinyl Alcohol Coated on Magnetite on the Preparation of Core-Shell Nanoparticles as a Drug Delivery Agent." International Journal of Molecular Sciences 20, no. 15 (August 1, 2019): 3764. http://dx.doi.org/10.3390/ijms20153764.

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One of the current developments in drug research is the controlled release formulation of drugs, which can be released in a controlled manner at a specific target in the body. Due to the diverse physical and chemical properties of various drugs, a smart drug delivery system is highly sought after. The present study aimed to develop a novel drug delivery system using magnetite nanoparticles as the core and coated with polyvinyl alcohol (PVA), a drug 5-fluorouracil (5FU) and Mg–Al-layered double hydroxide (MLDH) for the formation of FPVA-FU-MLDH nanoparticles. The existence of the coated nanoparticles was supported by various physico-chemical analyses. In addition, the drug content, kinetics, and mechanism of drug release also were studied. 5-fluorouracil (5FU) was found to be released in a controlled manner from the nanoparticles at pH = 4.8 (representing the cancerous cellular environment) and pH = 7.4 (representing the blood environment), governed by pseudo-second-order kinetics. The cytotoxicity study revealed that the anticancer delivery system of FPVA-FU-MLDH nanoparticles showed much better anticancer activity than the free drug, 5FU, against liver cancer and HepG2 cells, and at the same time, it was found to be less toxic to the normal fibroblast 3T3 cells.
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23

Pattnaik, Satyanarayan, and Kamla Pathak. "Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research." Current Pharmaceutical Design 23, no. 3 (February 20, 2017): 467–80. http://dx.doi.org/10.2174/1381612822666161026162005.

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Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.
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24

Harada, S., S. Ehara, T. Segawa, K. Ishii, T. Sato, T. Kamiya, K. Sera, and S. Goto. "Innovation of hyaluronic acid-protamine microparticles and their kinetics in vivo." International Journal of PIXE 26, no. 01n02 (January 2016): 45–51. http://dx.doi.org/10.1142/s0129083516500054.

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The nanoparticles, which releases anticancer drug with response to radiation, were developed. Also, two categories were tested: (i) their ability to release anticancer drug in vitro; and (ii) their kinetics in the body, when they were injected through tail vein of BALB/c mice in vivo. To prepare the particles, hyaluronic acid and protamine were mixed into carboplatin solution, and reacted for 30 min in room temperature. Those particles were exposed to a single dose of 10 Gy of 140 KeV X-ray. Their ability to release carboplatin with response to radiation was expressed as the percentage of ruptured particles, basing on images of particles, using micro PIXE camera. The amount of released carboplatin was measured by quantitative PIXE method. The kinetics of particles in body was assessed by counting the number of particles, which were trapped in lungs, using micro PIXE camera. The mean diameter of particles was 743 ± 34 nm. By irradiation, 59.3 ± 7.23% of particles ruptured, and 95.9 ± 2.3% carboplatin was released from particles. The trapped particles in lungs were significantly reduced, when compared with previous alginate-hyaluronic particles.
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Iovanov, Rareș Iuliu, Ioan Tomuță, and Sorin Emilian Leucuța. "Development of a reservoir type prolonged release system with felodipine via simplex methodology." Medicine and Pharmacy Reports 89, no. 1 (September 28, 2015): 128–36. http://dx.doi.org/10.15386/cjmed-526.

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Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models.
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Torres-Luna, Cesar, Naiping Hu, Roman Domszy, Xin Fan, Jeff Yang, Robert M. Briber, Nam Sun Wang, and Arthur Yang. "Effect of Carbon Chain Length, Ionic Strength, and pH on the In Vitro Release Kinetics of Cationic Drugs from Fatty-Acid-Loaded Contact Lenses." Pharmaceutics 13, no. 7 (July 10, 2021): 1060. http://dx.doi.org/10.3390/pharmaceutics13071060.

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This paper explores the use of fatty acids in silicone hydrogel contact lenses for extending the release duration of cationic drugs. Drug release kinetics was dependent on the carbon chain length of the fatty acid loaded in the lens, with 12-, 14- and 18-carbon chain length fatty acids increasing the uptake and the release duration of ketotifen fumarate (KTF) and tetracaine hydrochloride (THCL). Drug release kinetics from oleic acid-loaded lenses was evaluated in phosphate buffer saline (PBS) at different ionic strengths (I = 167, 500, 1665 mM); the release duration of KTF and THCL was decreased with increasing ionic strength of the release medium. Furthermore, the release of KTF and THCL in deionized water did not show a burst and was significantly slower compared to that in PBS. The release kinetics of KTF and THCL was significantly faster when the pH of the release medium was decreased from 7.4 towards 5.5 because of the decrease in the relative amounts of oleate anions in the lens mostly populated at the polymer–pore interfaces. The use of boundary charges at the polymer–pore interfaces of a contact lens to enhance drug partition and extend its release is further confirmed by loading cationic phytosphingosine in contact lenses to attract an anionic drug.
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27

Kaur, Gagan, Milton T. W. Hearn, Toby D. M. Bell, and Kei Saito. "Release Kinetics of 6-Mercaptopurine and 6-Thioguanine from Bioinspired Core-Crosslinked Thymine Functionalised Polymeric Micelles." Australian Journal of Chemistry 66, no. 8 (2013): 952. http://dx.doi.org/10.1071/ch13125.

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A bioinspired core-bound polymeric micellar system based on hydrogen bonding and photo-crosslinking of thymine has been prepared from the amphiphilic block copolymers, poly(vinylbenzylthymine)-block-poly(vinylbenzyltriethylammonium chloride). The chemical loading and controlled release potential of these micelles was investigated using two drugs, 6-mercaptopurine and 6-thioguanine. The release kinetics of drug-loaded polymeric micelles was determined by pressure ultrafiltration and the effects of hydrogen bonding, core-crosslinking, and core size on the loading capacity and release kinetics were analysed. The results demonstrate that drug release rates are affected by hydrogen bonding in the micelle core. Furthermore, these studies indicate that drug release rates can be controlled by changing the size of the core and by photo-crosslinking thymine groups in the core.
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28

Lacoeuille, Franck, Emmanuel Garcion, Jean-Pierre Benoit, and Alf Lamprecht. "Lipid Nanocapsules for Intracellular Drug Delivery of Anticancer Drugs." Journal of Nanoscience and Nanotechnology 7, no. 12 (December 1, 2007): 4612–17. http://dx.doi.org/10.1166/jnn.2007.18114.

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As non-phagocytic eukaryotic cells can internalize particles <1 μm in size, small size (25 to 110 nm) lipid nanocapsules (LNC) are proposed for the intracellular drug delivery of anticancer drugs to cancer cells. LNC ofdifferent diameters were loaded with etoposide or paclitaxel and subsequently tested for drug release kinetics and their efficiency to reduce cancer cell growth in cell culture. Relative high drug loads could be achieved and sustained drug release can be provided over a period ofseveral days (etoposide) up to a few weeks (paclitaxel). While particle size exhibited only minor influences on the release kinetics, higher initial drug load led to a distinctly lower burst release. In a cancer cell culture model, etoposide or paclitaxel LNC showed a 4-fold or 40-fold higher efficiency, respectively than the drug solution while blank LNC were found to be less toxic than the pure drug at equivalent concentrations. The uptake and intracellular accumulation ofLNC was confirmed by confocal laser scanning microscopy after fluorescence labeling of the nanocarriers. This nanoparticulate system is able to achieve efficient intracellular drug concentrations and seems to be therefore a promising therapeutic approach in cancer treatment.
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29

Baeumer, Boris, Lipika Chatterjee, Peter Hinow, Thomas Rades, Ami Radunskaya, and Ian Tucker. "Predicting the drug release kinetics of matrix tablets." Discrete & Continuous Dynamical Systems - B 12, no. 2 (2009): 261–77. http://dx.doi.org/10.3934/dcdsb.2009.12.261.

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30

Liu, Chengsheng, Kashappa Goud H. Desai, Xuexi Tang, and Xiguang Chen. "Drug Release Kinetics of Spray-Dried Chitosan Microspheres." Drying Technology 24, no. 6 (July 2006): 769–76. http://dx.doi.org/10.1080/03602550600685325.

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31

Kelly, Sean M., Arun K. Upadhyay, Akash Mitra, and Balaji Narasimhan. "Analyzing Drug Release Kinetics from Water-Soluble Polymers." Industrial & Engineering Chemistry Research 58, no. 18 (February 7, 2019): 7428–37. http://dx.doi.org/10.1021/acs.iecr.8b05800.

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32

Tamayo, A., M. A. Mazo, M. D. Veiga, R. Ruiz-Caro, F. Notario-Pérez, and J. Rubio. "Drug kinetics release from Eudragit – Tenofovir@SiOC tablets." Materials Science and Engineering: C 75 (June 2017): 1097–105. http://dx.doi.org/10.1016/j.msec.2017.03.016.

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33

Durrani, Manzer J., Audrey Andrews, Roy Whitaker, and S. C. Benner. "Studies on Drug Release Kinetics from Carbomer Matrices." Drug Development and Industrial Pharmacy 20, no. 15 (January 1994): 2439–47. http://dx.doi.org/10.3109/03639049409042648.

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34

Zhang, Qiuhong, Xiang Li, Zhaohui Ren, Gaorong Han, and Chuanbin Mao. "Synthesis of CaTiO3Nanofibers with Controllable Drug-Release Kinetics." European Journal of Inorganic Chemistry 2015, no. 27 (August 18, 2015): 4532–38. http://dx.doi.org/10.1002/ejic.201500737.

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35

Ji, Yuanhui, Anna Katharina Lesniak, Anke Prudic, Raphael Paus, and Gabriele Sadowski. "Drug Release Kinetics and Mechanism from PLGA Formulations." AIChE Journal 62, no. 11 (May 19, 2016): 4055–65. http://dx.doi.org/10.1002/aic.15282.

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36

Jung, Hyun, Hyun-Mi Kim, Young Bin Choy, Seong-Ju Hwang, and Jin-Ho Choy. "Itraconazole–Laponite: Kinetics and mechanism of drug release." Applied Clay Science 40, no. 1-4 (June 2008): 99–107. http://dx.doi.org/10.1016/j.clay.2007.09.002.

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37

Li, Chun Yan, Cong Cong Hu, Zhi Guo Wen, and Sheng Xiong Dong. "The In Vitro Degradation Kinetics of Polyurethane Prodrug Materials." Advanced Materials Research 399-401 (November 2011): 1067–70. http://dx.doi.org/10.4028/www.scientific.net/amr.399-401.1067.

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The method of high performance liquid chromatography (HPLC) is established to determine the content of antibacterial agent — ciprofloxacin (CF) in the degradation solution of ciprofloxacin-polyurethane (CFPU) and investigate the in vitro degradation kinetics by plotting and fitting the cumulative release curves to inspect the effects of different medium and different concentrations on drug release. The results showed that the HPLC method is accurate, reliable and simple. The drug-release of CFPU was bioresponsive and could be accorded with first order kinetics. It was observed that CF was released from CFPU by a combination of diffusion and erosion mechanism, mainly in the manner of diffusion in the absence of infection while erosion mechanism in the presence of infection.
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38

Sutton, Damon, Shihu Wang, Norased Nasongkla, Jinming Gao, and Elena E. Dormidontova. "Doxorubicin and β-Lapachone Release and Interaction with Micellar Core Materials: Experiment and Modeling." Experimental Biology and Medicine 232, no. 8 (September 2007): 1090–99. http://dx.doi.org/10.3181/0702-rm-31.

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Polymer micelles with two different core-forming blocks, poly(d,l -lactide) (PLA) and poly(ε-caprolactone) (PCL), but the same coronal material, poly(ethylene glycol) (PEG), were investigated in this study as nanoscopic drug carriers. The release of two different drugs, doxorubicin (DOX) and β-lapachone (β-lap), from PEG(5k)-b-PCL(5k) and PEG(5k)-b-PLA(5k) micelles was studied at pH 5.0 and 7.4. Mathematical solutions of both Higuchi’s model and Fickian diffusion equations were utilized to elucidate the differences between the micelle core materials for the two drugs. The neutral and smaller of the two drugs tested, β-lap, demonstrated faster, pH-independent release, suggesting that no substantial changes occurred in either micelle core at lower pH. In contrast, the release rate of DOX was found to noticeably increase at lower pH with a larger cumulative amount of drug released. Different core materials were shown to have considerable influence on the release kinetics of both drugs: in both cases, the more hydrophobic PCL core showed slower drug release rates compared with the less hydrophobic PLA core.
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39

Kabir, Abul Kalam Lutful, Shimul Halder, and Abu Shara Shamsur Rouf. "In vitro Release Kinetic Study of Theophylline from Kollidon SR Polymer Based Matrix Tablet." Dhaka University Journal of Pharmaceutical Sciences 14, no. 1 (June 18, 2015): 43–48. http://dx.doi.org/10.3329/dujps.v14i1.23734.

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Controlled release tablet matrix of theophylline was prepared with kollidon SR, a spray dried powder grade polymer (polyvinyl acetate and povidone based matrix rate retarding hydrophobic materials) by utilizing direct compression technique. Different proportion of kollidon SR was used to develop the matrix builder in the five proposed formulations (F-1 to F-5) for the study of release rate retardant effect at 10, 12, 15, 18 and 21% of total weight of matrix tablet, respectively. The in vitro dissolution study of the matrices of those proposed tablet formulations were carried out in simulated gastric medium (pH 1.3) for first two hours and then in simulated intestinal medium (pH 6.8) for 6 hours using USP dissolution apparatus II (paddle method). The formulation F-3 (using 15% polymer) and F-4 (using 18 % polymer) met the optimum release profiles of active ingredient for 8 hr period of total study. The release kinetics for theophylline was plotted against zero order, first order and Higuchi release rate kinetics to evaluate the release mechanism of drug from the formulated tablet matrix. The release kinetics of formulation F-3 and F-4 was followed very closely by Higuchi release rate kinetic order than other kinetics such as zero order and first order kinetics which has been reflected the type of drug release from the tablet matrix by diffusion as well as erosion mechanism.Dhaka Univ. J. Pharm. Sci. 14(1): 43-48, 2015 (June)
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40

Bettini, Ruggero, Maria Cristina Bonferoni, Paolo Colombo, Laura Zanelotti, and Carla Caramella. "Drug Release Kinetics and Front Movement in Matrix Tablets Containing Diltiazem or Metoprolol/λ-Carrageenan Complexes." BioMed Research International 2014 (2014): 1–8. http://dx.doi.org/10.1155/2014/671532.

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In this work we investigated the moving boundaries and the associated drug release kinetics in matrix tablets prepared with two complexes betweenλ-carrageenan and two soluble model drugs, namely, diltiazem HCl and metoprolol tartrate aiming at clarifying the role played by drug/polymer interaction on the water uptake, swelling, drug dissolution, and drug release performance of the matrix. The two studied complexes released the drug with different mechanism indicating two different drug/polymer interaction strengths. The comparison between the drug release behaviour of the complexes and the relevant physical mixtures indicates that diltiazem gave rise to a less soluble and more stable complex with carrageenan than metoprolol. The less stable metoprolol complex afforded an erodible matrix, whereas the stronger interaction between diltiazem and carrageenan resulted in a poorly soluble, slowly dissolving matrix. It was concluded that the different stability of the studied complexes affords two distinct drug delivery systems: in the case of MTP, the dissociation of the complex, as a consequence of the interaction with water, affords a classical soluble matrix type delivery system; in the case of DTZ, the dissolving/diffusing species is the complex itself because of the very strong interaction between the drug and the polymer.
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41

Shang, Lei, Sam Zhang, Subbu S. Venkatraman, and Hejun Du. "Tailoring of Drug Release Kinetics by Partition Effect via Drug Immobilization." Nanoscience and Nanotechnology Letters 2, no. 1 (March 1, 2010): 16–20. http://dx.doi.org/10.1166/nnl.2010.1047.

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42

Toft, Egon. "Drug release kinetics from a drug-eluting stent with asymmetrical coat." Frontiers in Bioscience 22, no. 3 (2017): 407–15. http://dx.doi.org/10.2741/4491.

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43

Adibkia, Khosro, Sanaz Hamedeyazdan, and Yousef Javadzadeh. "Drug release kinetics and physicochemical characteristics of floating drug delivery systems." Expert Opinion on Drug Delivery 8, no. 7 (April 21, 2011): 891–903. http://dx.doi.org/10.1517/17425247.2011.574124.

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44

Balakrishnan, Brinda, John F. Dooley, Gregory Kopia, and Elazer R. Edelman. "Intravascular drug release kinetics dictate arterial drug deposition, retention, and distribution." Journal of Controlled Release 123, no. 2 (November 2007): 100–108. http://dx.doi.org/10.1016/j.jconrel.2007.06.025.

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45

Chowdhury, Sonia, Mandava Nithin Babu, K. Ankitha, B. Shirisha, Madhurika Sirigadi, and Esarapu Kavya. "A comparative study on effect of polymers on release kinetics glimepiride matrix tablet." Pharmaceutical and Biological Evaluations 4, no. 2 (April 2, 2017): 103. http://dx.doi.org/10.26510/2394-0859.pbe.2017.16.

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Objective: The Present investigation was performed to find out the effect of synthetic and natural polymers on the release properties of glimepiride matrix tablet. Glimepiride is a first third generation sulphonyl urea agent for the treatment of type- II diabetes mellitus. Methocel K15M, Olibanum Gum were used as key release modifying polymers.Methods: Nine formulations were prepared taking different concentration of natural and synthetic polymers, The drug excipient mixtures were subjected to pre-compression studies. The tablets were prepared by direct compression method; all formulations were subjected to physicochemical studies, in- vitro drug release, kinetic studies and stability studies. The physicochemical results were found within the limits.Results: FTIR study interpretation did not show any drug–excipient interaction The drug release from the optimized formulation F-7 was extended for a period of 12 hours. The release kinetics of F-7 formulation showed that the release of drug follows zero order models. The optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern.Conclusions: Results of the present study indicated the suitability of the above mentioned polymers in the preparation of sustained release formulation of Glimepiride for the management of type-II diabetes mellitus effectively.
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46

Karim, Samira, Mohiuddin Ahmed Bhuiyan, and Md Sohel Rana. "Formulation and in vitro Evaluation of Glimepiride Sustained Release Tablets: Comparison with Immediate Release Tablets." Bangladesh Pharmaceutical Journal 18, no. 2 (July 26, 2015): 157–62. http://dx.doi.org/10.3329/bpj.v18i2.24315.

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This work aims at the design of a sustained release formulation of glimepiride which is currently available in the treatment of type 2 diabetes mellitus and to investigate the effect of polymers on the release profile of glimepiride. Glimepiride sustained release tablets were prepared by direct compression method using different ratios of various release retarding polymers such as carbopol, ethyl cellulose, methocel K4 MCR, methocel K15 MCR, methocel K100 MCR and xanthum gum. These formulations were also compared with glimepiride immediate release tablets. The prepared tablets were subjected to various physical parameter tests including weight variation, friability, hardness, thickness, diameter, etc. In vitro dissolution studies of the formulations were done at pH 6.8 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. The percent releases of all the formulations (30) were 73.11%- 98.76% after 8 hours. The release pattern followed zero order kinetics and the release of the drug was hindered by the polymers used in the study. On the other hand, 100% drug was released within 1 hour from the immediate release tablet of glimepiride. The study reveals that the polymers used have the capacity to retard the release of the drug from the sustained release tablets and the more is the amount of the polymer in the formulation the less is the release of drug showing more retardation of drug release.Bangladesh Pharmaceutical Journal 18(2): 157-162, 2015
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47

Wójcik-Pastuszka, Dorota, Aleksandra Potempa, and Witold Musiał. "Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine." Molecules 25, no. 23 (December 3, 2020): 5711. http://dx.doi.org/10.3390/molecules25235711.

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Targeted drug delivery systems are a very convenient method of treating inflammatory bowel disease. The properties of pectin make this biopolymer a suitable drug carrier. These properties allow pectin to overcome the diverse environment of the digestive tract and deliver the drug to the large intestine. This investigation proposed bipolymeric formulations consisting of the natural polymer pectin and a synthetic polymer containing the drug 5-aminosalicylic acid. Pectin beads were prepared via ionotropic gelation involving the interaction between the hydrophilic gel and calcium ions. The obtained formulations consisted of natural polymer, 5-aminosalicylic acid (5-ASA) and one of the synthetic polymers, such as polyacrylic acid, polyvinylpyrrolidone, polyethylene glycol or aristoflex. The release of the drug was carried out employing a basket apparatus (USP 1). The acceptor fluid was pH = 7.4 buffer with added enzyme pectinase to reflect the colon environment. The amount of the released drug was determined using UV-Vis spectrophotometry at a wavelength of λ = 330 nm. The kinetics of the drug dissolution revealed that none of the employed models was appropriate to describe the release process. A kinetic analysis of the release profile during two release stages was carried out. The fastest drug release occurred during the first stage from a formulation containing pectin and polyethylene glycol. However, according to the applied kinetic models, the dissolution of 5-ASA was rather high in the formulation without the synthetic polymer during the second stage. Depending on the formulation, 68–77% of 5-ASA was released in an 8-hour time period. The FTIR and DSC results showed that there was no interaction between the drug and the polymers, but interactions between pectin and synthetic polymers were found.
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48

Rajeswari, Saripilli, Sravya Kudamala, and Kollapalli Venkata Ramana Murthy. "DEVELOPMENT, FORMULATION AND EVALUATION OF A BILAYER GASTRIC RETENTIVE FLOATING TABLETS OF RANITIDINE HCL AND CLARITHROMYCIN USING NATURAL POLYMERS." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 9 (July 22, 2017): 164. http://dx.doi.org/10.22159/ijpps.2017v9i9.20290.

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Objective: Bilayer gastric retentive floating tablets (BGRFT) with ranitidine HCl and clarithromycin using natural gums have been developed to prolong the gastric residence time and increase drug bioavailability. Literature review revealed no published studies on the present study.Methods: Immediate release (IR) layer prepared by using different diluents and super disintegrants like sodium starch glycolate, crosscarmellose sodium and crospovidone. Controlled released (CR) layer prepared by using neem gum, damar gum and copal gum. Prepared tablets were evaluated for in vivo and in vitro buoyancy, in vitro dissolution studies and fourier transformation-infrared spectroscopy (FTIR). Drug release was evaluated with zero and first order for release kinetics, Higuchi, Hixson-Crowell erosion models for release mechanism.Results: Prepared IR layer followed first order rate kinetics and CR layer followed zero order rate kinetics with non-Fickian diffusion mechanism. BGRFT also showed similar results as that of the individual layer. Optimized formulations were characterized by FTIR studies and found no interactions between drug and polymer.Conclusion: The results demonstrate the feasibility of the model in the development of BGRFT. BGRFT enhanced the drug release and finally the bioavailability of clarithromycin when compared with commercial tablet (Biomycin 250). The present study could establish the suitability of neem gum as CR polymer in the design of BGRFT.
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49

Albuquerque, J. S. V., I. W. L. Franca, G. F. Silva, A. L. O. Ferreira, and R. E. F. Q. Nogueira. "Macroporous Calcium Phosphate Bioceramics as Drug Release Agents: A Kinetics Study of Ampicillin Release." Key Engineering Materials 396-398 (October 2008): 675–78. http://dx.doi.org/10.4028/www.scientific.net/kem.396-398.675.

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Semi-synthetic beta-lactam antibiotics are the most important class of antibacterial agents. Their use in veterinary and human medicine is in continuous expansion. Calcium phosphate bioceramics have been used in medicine and dentistry for nearly 30 years. Calcium phosphate ceramics (CPC) are nowadays being widely used as drug delivery systems because of their desirable properties such as biocompatibility, bioresorbability, controlled release etc. In recent years In this work, kinetic models to describe ampicillin adsorption from CPC were investigated. Calcium phosphate bioceramic are analogous to the mineral component of bones, its properties make it suitable for implant materials and delivery agents of drugs
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50

Haroosh, Hazim J., Yu Dong, Shaimaa Jasim, and Seeram Ramakrishna. "Improvement of Drug Release and Compatibility between Hydrophilic Drugs and Hydrophobic Nanofibrous Composites." Materials 14, no. 18 (September 16, 2021): 5344. http://dx.doi.org/10.3390/ma14185344.

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Electrospinning is a flexible polymer processing method to produce nanofibres, which can be applied in the biomedical field. The current study aims to develop new electrospun hybrid nanocomposite systems to benefit the sustained release of hydrophilic drugs with hydrophobic polymers. In particular, electrospun hybrid materials consisting of polylactic acid (PLA):poly(ε-caprolactone) (PCL) blends, as well as PLA:PCL/halloysite nanotubes-3-aminopropyltriethoxysilane (HNT-ASP) nanocomposites were developed in order to achieve sustained release of hydrophilic drug tetracycline hydrochloride (TCH) using hydrophobic PLA:PCL nanocomposite membranes as a drug carrier. The impact of interaction between two commonly used drugs, namely TCH and indomethacin (IMC) and PLA:PCL blends on the drug release was examined. The drug release kinetics by fitting the experimental release data with five mathematical models for drug delivery were clearly demonstrated. The average nanofiber diameters were found to be significantly reduced when increasing the TCH concentration due to increasing solution electrical conductivity in contrast to the presence of IMC. The addition of both TCH and IMC drugs to PLA:PCL blends reduced the crystallinity level, glass transition temperature (Tg) and melting temperature (Tm) of PCL within the blends. The decrease in drug release and the impairment elimination for the interaction between polymer blends and drugs was accomplished by mobilising TCH into HNT-ASP for their embedding effect into PLA:PCL nanofibres. The typical characteristic was clearly identified with excellent agreement between our experimental data obtained and Ritger–Peppas model and Zeng model in drug release kinetics. The biodegradation behaviour of nanofibre membranes indicated the effective incorporation of TCH onto HNT-ASP.
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