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Journal articles on the topic 'Acrystal'
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Rusu, Iulian, Mihail-Liviu Craus, Daniel Sutiman, and Alice Rusu. "On the possible formation of Aurivillius phases in the oxide system Bi2O3-ZnO-Nb2O5." Journal of the Serbian Chemical Society 69, no. 1 (2004): 53–58. http://dx.doi.org/10.2298/jsc0401053r.
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This paper presents results concerning the possible synthesis of double perovskite and Aurivillius phases in the BZN system. Acrystal chemical criterion based on an elastic model for the structure was used in order to determine if the formation of layered bismuth compounds is favoured in the above system. The tempeature seems to be the decisive factor influencing Aurivillius phase formation.
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Leidermark, Daniel, Mikael Segersäll, Johan Moverare, and Kjell Simonsson. "Modelling of TMF Crack Initiation in Smooth Single-Crystal Superalloy Specimens." Advanced Materials Research 891-892 (March 2014): 1283–88. http://dx.doi.org/10.4028/www.scientific.net/amr.891-892.1283.
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In this paper the TMF crack initiation behaviour of the single-crystal nickel-base superalloyMD2 is investigated and modelled. TMF tests were performed in both IP and OP for varying mechanicalstrain ranges in the [001] crystallographic direction until TMF crack initiation was obtained. Acrystal plasticity-creep model was used in conjunction with a critical-plane approach, to evaluate thenumber of cycles to TMF crack initiation. The critical-plane model was evaluated and calibrated ata stable TMF cycle, where the effect of the stress relaxation had attenuated. This calibrated criticalplanemodel is able to describe the TMF crack initiation, taking tension/compression asymmetry aswell as stress relaxation anisotropy into account, with good correlation to the real fatigue behaviour.
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Somers, W. "1.9 Acrystal structure of interleukin 6: implications for a novel mode of receptor dimerization and signaling." EMBO Journal 16, no. 5 (March 1, 1997): 989–97. http://dx.doi.org/10.1093/emboj/16.5.989.
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Golovin, A. V., G. A. Khayrullina, B. Kraal, and А. М. Kopylov. "Identification of Novel RNA-Protein Contact in Complex of Ribosomal Protein S7 and 3’-Terminal Fragment of 16S rRNA in E. coli." Acta Naturae 4, no. 4 (December 15, 2012): 65–72. http://dx.doi.org/10.32607/20758251-2012-4-4-65-72.
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For prokaryotes in vitro, 16S rRNA and 20 ribosomal proteins are capable of hierarchical self- assembly yielding a 30S ribosomal subunit. The self-assembly is initiated by interactions between 16S rRNA and three key ribosomal proteins: S4, S8, and S7. These proteins also have a regulatory function in the translation of their polycistronic operons recognizing a specific region of mRNA. Therefore, studying the RNAprotein interactions within binary complexes is obligatory for understanding ribosome biogenesis. The non-conventional RNAprotein contact within the binary complex of recombinant ribosomal protein S7 and its 16S rRNA binding site (236 nucleotides) was identified. UVinduced RNAprotein cross-links revealed that S7 cross-links to nucleotide U1321 of 16S rRNA. The careful consideration of the published RNA protein cross-links for protein S7 within the 30S subunit and their correlation with the X-ray data for the 30S subunit have been performed. The RNA protein crosslink within the binary complex identified in this study is not the same as the previously found cross-links for a subunit both in a solution, and in acrystal. The structure of the binary RNAprotein complex formed at the initial steps of self-assembly of the small subunit appears to be rearranged during the formation of the final structure of the subunit.
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Tiu, C., G. Nicolae, and K. C. Tam. "Rheological properties of hydrophobically modified alkali-swellable acrysol emulsions." Journal of Polymer Research 3, no. 4 (October 1996): 201–9. http://dx.doi.org/10.1007/bf01493489.
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Hernández-Baltazar, E., G. A. Reyes-Sandoval, and J. Gracia-Fadrique. "Surface properties of an associative alkali soluble polymer (Acrysol TT-935)." Colloids and Surfaces A: Physicochemical and Engineering Aspects 238, no. 1-3 (May 2004): 113–22. http://dx.doi.org/10.1016/j.colsurfa.2004.02.025.
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Prajapati, Shailesh T., Hitesh H. Bulchandani, Dashrath M. Patel, Suresh K. Dumaniya, and Chhaganbhai N. Patel. "Formulation and Evaluation of Liquisolid Compacts for Olmesartan Medoxomil." Journal of Drug Delivery 2013 (October 21, 2013): 1–9. http://dx.doi.org/10.1155/2013/870579.
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Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly water-soluble drug with absolute bioavailability of 26%. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate. Liquisolid compacts were prepared using Acrysol El 135 as a solvent, Avicel PH 102, Fujicalin and Neusilin as carrier materials, and Aerosil as coating material in different ratios. The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial limits. The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets. Amongst carriers used Fujicalin and Neusilin were found to be more effective carrier materials for liquid adsorption.
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Prajapati, Shailesh T., Harsh A. Joshi, and Chhaganbhai N. Patel. "Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement." Journal of Pharmaceutics 2013 (September 24, 2013): 1–9. http://dx.doi.org/10.1155/2013/728425.
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Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.
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Ashara, Kalpesh C., Jalpa S. Paun, Moinuddin M. Soniwala, and Jayant R. Chavda. "Microemulgel of Voriconazole: an Unfathomable Protection to Counter Fungal Contagiousness." Folia Medica 59, no. 4 (December 20, 2017): 461–71. http://dx.doi.org/10.1515/folmed-2017-0051.
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AbstractBackground: Fluconazole and ketoconazole both have poor minimum inhibitory concentration than voriconazole. Voriconazole had serious side effects in oral and intravenous doses. It has poor water solubility. The objective of the study was to prepare and optimize microemulgel of voriconazole for topical delivery. Aim: Formulation, development, and evaluation of voriconazole microemulgel for topical delivery. Methods: Oil and emulsifi ers selected were on the basis of equilibrium solubility study and emulsification property respectively. The pseudo-ternary plot and constrained simplex lattice design were applied for preparation of microemulsions. Microemulsions were subjected to micelle size, zeta potential, polydispersity index, and in vitro study. They were optimized by Design-Expert®9.0.3.1 software. Formulation, development, evaluation and optimization of microemulgel were carried out. Microbial assay of an optimized batch of microemulgel was performed. Results: Solubility of voriconazole in Parker Neem®oil was 7.51±0.14 mg/g. Acrysol™K-150: PEG-400 in 4:1 ratio had the highest area for microemulsion. 59.2% Acrysol™K-150, 14.8% PEG-400, 11% Parker Neem®oil, 15% rose water, and 1% voriconazole as an optimized batch of microemulsion was selected for preparation of microemulgel. Carbomer 934P found a good gelling agent in 0-2% w/w concentration. An optimized batch of microemulgel had 0.974 desirability value. An optimized batch of microemulgel and Nizral®cream had 37.32±0.63% and 26.45±0.63% zones of inhibition. Conclusion: Topical antifungal treatment was successfully achieved with voriconazole microemulgel.
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K, Mahalaxmi, and Sailu Ch. "Design, Optimization and Evaluation of Repaglinide Self-Nanoemulsifying Drug Delivery for Enhanced Solubility." International Journal of Pharmaceutical Sciences and Nanotechnology 10, no. 6 (November 30, 2017): 3920–28. http://dx.doi.org/10.37285/ijpsn.2017.10.6.8.
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The aim of study was to develop self-nanoemulsifying systems of poorly water-soluble drug repaglinide, which is an antidiabetic drug in the class of medications known as meglitinides. Solubility of repaglinide in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). Surfactants and oil was selected based on solubility studies were further screened for their efficiency in formulation. Acrysol K 150, Kolliphor EL and Capmul MCM were selected as oil, surfactant and co-surfactant respectively. Formulation F8 was found to be optimized formulation on the basis of in vitro dissolution studies, particle size and zeta potential. The optimized formulation was then subjected to stability studies and was found to be stable after 6 months. Thus, SNEDDS were found to be influential in improving the release performance of repaglinide, indicating their potential to improve the solubility and oral bioavailability of repaglinide.
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Tiwari, Shradha, Shailesh Wadher, and Surendra Gattani. "NATEGLINIDE SILICA LIPIDHYBRID PARTICLES FOR IMPROVED SOLUBILITY." INDIAN DRUGS 57, no. 06 (August 21, 2020): 73–78. http://dx.doi.org/10.53879/id.57.06.12348.
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Porous silica-based drug delivery systems have shown substantial potential for improving the oral delivery of poorly water-soluble drugs.The major problem with nateglinide, a BCS Class II drug, is pHdependent solubility, limited aqueous solubility, poor dissolution and variable bioavailability. The aim of the present investigation was to develop a lipid-based solid formulation of nateglinide, as a strategy to improve both the solubility and the dissolution rate of the drug in a tablet dosage form. The silica lipid hybrid (SlH) particles were formulated using Miglyol812 and Acrysol el 135 as liquid lipid vehicles as well aslabrasol and Transcutol HP as surfactants.Nateglinide was dissolved in different lipids and later adsorbed on highly porous silica Sylloid PF244 to obtain free-flowing powders. The prepared nateglinide SlH was characterized by FT-IR, DSC, and XRD.Nateglinide SlH was evaluated for solubility and dissolution. SlH of NTG prepared with Miglyol 812 and Transcutol HP enhanced solubility of NTG 57.21 fold. From the study, it may be concluded that the oral solid lipid-based formulation, SlH has an improved potential for enhancing solubility and dissolution of BCS class II drugs like nateglinide.
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Barrón-Ortiz, Christina I., Matthew R. Sawchuk, Carmen Li, and Christopher N. Jass. "Conservation of Subfossil Bones from a Lacustrine Setting: Uncontrolled and Controlled Drying of Late Quaternary Vertebrate Remains from Cold Lake, Western Canada." Collection Forum 32, no. 1-2 (September 1, 2018): 1–13. http://dx.doi.org/10.14351/0831-4985-32.1.1.
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Abstract Water-saturated vertebrate remains (e.g., bone, antler, and ivory) are particularly challenging to stabilize for long-term storage, research, and analysis. These types of specimens are sensitive to damage caused by water loss, which frequently results in delamination, twisting, and cracking. The recovery of late Quaternary vertebrate remains from underwater areas of Cold Lake, western Canada, prompted us to conduct a series of analyses to better understand the preservation of the remains and their susceptibility to damage, and to test different conservation techniques to achieve successful drying. X-ray fluorescence analysis of a sample of specimens revealed that the remains have particularly high iron concentrations, a condition that might have contributed to weaken their structure, further compromising their integrity when drying. Additionally, we found that certain bone elements, such as long bones, are more susceptible to severe surface delamination than others, and as a result these specimens should be monitored more closely during their treatment. Of the four drying methods we tested, controlled air-drying produced the best results, followed by solvent-drying. In contrast, vacuum freeze-drying and vacuum freeze-drying with 20% v/v Acrysol WS-24 in water, an acrylic dispersion, while rapid, resulted in differing degrees of delamination and cracking.
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Sood, Jatin, Bharti Sapra, and Ashok K. Tiwary. "Drug in Adhesive Transdermal Formulation of Valsartan and Nifedipine: Pharmacokinetics and Pharmacodynamics in Rats." Current Drug Therapy 14, no. 2 (August 27, 2019): 153–67. http://dx.doi.org/10.2174/1574885514666181120114635.
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Background: The increasing complications associated with hypertension often require a combination of two or more drugs acting through different routes to counter the elevated blood pressure. Objective: The present investigation envisaged at preparing and evaluating a transdermal formulation containing gelled microemulsion drug in adhesive (DIA) patch for simultaneous systemic delivery of valsartan and nifedipine aimed at effective management of hypertension. Methods: An optimized microemulsion was prepared by using Captex® 500 (7.34% w/w), Capmul® MCM (4.24% w/w), Acrysol EL 135 (24.43% w/w), Transcutol P® (5% w/w) and water (58.9% w/w). Gelling was contributed by polyvinylpyrrolidone K 90F and polyethyleneimine where the latter also conferred skin adhesion properties to the patch. DIA patches were evaluated for in vitro drug release as well as in vivo pharmacokinetics and pharmacodynamics in rats. Results: In vitro permeation of nifedipine or valsartan from the selected DIA patch was 10.67-fold and 1.25-fold higher as compared to their aqueous dispersions. The relative bioavailability of nifedipine was 1.34 and that of valsartan was 2.18 from this DIA patch with respect to the oral administration of their aqueous suspension. Conclusion: Transdermal delivery of either drug alone was not effective in reducing methyl prednisolone acetate-induced hypertension, whereas, simultaneous transdermal delivery of both drugs from DIA patch effectively maintained systolic blood pressure at a normal level in these rats for 20 h.
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Bhagwat, Durgacharan Arun, and John Intru DSouza. "Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier." International Current Pharmaceutical Journal 1, no. 12 (November 1, 2012): 414–19. http://dx.doi.org/10.3329/icpj.v1i12.12451.
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Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419
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Fleming, Gwen F., F. William Simmons, Loyd M. Wax, Robert E. Wing, and Merle E. Carr. "Atrazine Movement in Soil Columns as Influenced by Starch-Encapsulation and Acrylic Polymer Additives." Weed Science 40, no. 3 (September 1992): 465–70. http://dx.doi.org/10.1017/s0043174500051924.
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Alternative herbicide formulations may have the potential to reduce atrazine leaching. This study was conducted to determine if starch-encapsulation produced using an extrusion process or several acrylic polymer additives reduced atrazine leaching in soil columns packed with Plainfield sand (98% sand and 0.7% organic matter). Three watering regimes were evaluated to determine the effects of water volume and rate of application on atrazine movement When 7.6 cm of water (0.44-pore volumes) was applied over 2 h, polymer treatments reduced atrazine movement from the soil surface by 9 to 21% compared to atrazine without the additives. With increased water volume and time, the effectiveness of several polymer treatments diminished. Acrysol ASE-108 and G110 polymers (mixed with atrazine at a 1:1 ratio) most effectively reduced atrazine leaching over all watering regimes. Starch encapsulation was more effective than any polymer additive in retarding atrazine movement Increasing the water volume from 7.6 to 15.2 cm (0.88-pore volumes) did not increase leaching of starch-encapsulated atrazine. Ninety-nine percent of the starch-encapsulated atrazine was retained in the top 5 cm of the column compared to only 18 and 13% of the dry flowable formulation (DF) when 0.44- and 0.88-pore volumes of water were applied over 2 and 4 h, respectively. When 0.88-pore volumes of water were applied over 12 d, 81% of the starch-encapsulated atrazine was retained in the upper 5 cm of the column compared to only 5% of the DF formulation of atrazine. This study indicates that starch encapsulation reduces atrazine movement to a greater extent than polymer additives and suggests that starch encapsulation may be an effective method of reducing atrazine leaching.
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Nagaraja, Sreeharsha, Girish Meravanige Basavarajappa, Ranjith Kumar Karnati, Esam Mohamed Bakir, and Swati Pund. "Ion-Triggered In Situ Gelling Nanoemulgel as a Platform for Nose-to-Brain Delivery of Small Lipophilic Molecules." Pharmaceutics 13, no. 8 (August 6, 2021): 1216. http://dx.doi.org/10.3390/pharmaceutics13081216.
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Background: Intranasal route offers a direct nose-to-brain delivery via olfactory and trigeminal nerves and minimizes the systemic exposure of the drug. Although reliable and non-invasive, intranasal administration of lipophilic neuroprotective agents for brain targeting is still challenging. Literature focuses on naturally-derived compounds as a promising therapeutics for chronic brain diseases. Naringin, a natural flavonoid obtained from citrus fruits possesses neuroprotective effects. By regulating multiple crucial cellular signaling pathways, naringin acts on several therapeutic targets that make it suitable for the treatment of neurodegenerative diseases like Alzheimer’s disease and making it a suitable candidate for nasal administration. However, the hydrophobicity of naringin is the primary challenge to formulate it in an aqueous system for nasal administration. Method: We designed a lipid-based nanoemulsifying drug delivery system of naringin using Acrysol K140 as an oil, Tween 80 as a surfactant and Transcutol HP as a cosolvent, to improve solubility and harness the benefits of nanosizing like improved cellular penetration. Intranasal instillations of therapeutic agents have limited efficacy due to drug washout and inadequate adherence to the nasal mucosa. Therefore, we reconstituted the naringin self-emulsifying system in a smart, biodegradable, ion-triggered in situ gelling hydrogel and optimized for desirable gel characteristics. The naringin-loaded composition was optimized and characterized for various physicochemical and rheological properties. Results: The formulation showed a mean droplet size 152.03 ± 4.6 nm with a polydispersity index <0.23. Ex vivo transmucosal permeation kinetics of the developed formulation through sheep nasal mucosa showed sustained diffusion and enhanced steady-state flux and permeability coefficient. Scanning and transmission electron microscopy revealed the spherical shape of emulsion droplets and entrapment of droplets in a gel structure. The formulation showed excellent biocompatibility as analyzed from the viability of L929 fibroblast cells and nasal mucosa histopathology after treatment. In vivo biodistribution studies revealed significantly higher drug transport and brain targeting efficiency. Conclusion: In situ gelling system with nanoemulsified naringin demonstrated a safe nasal delivery providing a new dimension to the treatment of chronic neurodegenerative diseases using small hydrophobic phytoconstituents with minimization of dose and related systemic adverse effects.
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Sandhya, Pamu, Pamu Poornima, and Darna V. R. N. Bhikshapathi. "Self Nanoemulsifying Drug Delivery System of Sorafenib Tosylate: Development and In Vivo Studies." Pharmaceutical Nanotechnology 8, no. 6 (December 28, 2020): 471–84. http://dx.doi.org/10.2174/2211738508666201016151406.
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Background: Sorafenib tosylate (SFN) belongs to the BCS class II drug with low solubility and undergoes first-pass metabolism, which leads to reduced bioavailability of 38%. Objective: The present study aimed at developing SFN SNEDDS to improve their solubility and bioavailability. Methods: Preliminary solubility studies were performed to identify oil, surfactant, and co-surfactant ratios. Pseudo tertiary phase diagram was constructed to select the areas of nanoemulsion based on the monophasic region. A total of 15 formulations of SFN SNEDDS were prepared and screened for phase separation and temperature variation using thermodynamic stability studies. These SNEDDS further characterized for % transmission, content of the drug, and in vitro dissolution analysis. The optimized formulation was analyzed for particle size, Z average, entrapment efficiency, and SEM analysis. Results: Based on the pseudo tertiary phase diagram, acrysol EL 135, kolliphor, and transcutol-P as oil, surfactant, and co-surfactant were selected, respectively. All the formulations were stable with no phase separation and maximum % transmittance of 98.92%. The formulation F15 was selected as an optimized one, based on maximum drug content of 99.89%, with 98.94% drug release within 1 hour and it will be stable for 6 months. From in vivo bioavailability studies, the Cmax of optimized SNEDDS (94.12±2.12ng/ml) is higher than pure SFN suspension (15.32±1.46 ng/ml) and the AUC0-∞ of optimized SNEDDS is also increased by 5 times (512.1±8.54 ng.h/ml) than pure drug (98.75±6.45ng.h/ml), which indicates improved bioavailability of the formulation. Conclusion: SFN loaded SNEDDS could potentially be exploited as a delivery system for improving oral bioavailability by minimizing first-pass metabolism and increased solubility. Lay Summary: Renal cell carcinoma accounts for 2% of global cancer diagnoses and deaths, it has more than doubled in incidence in the developed world over the past half-century, and today is the ninth most common neoplasm in the United States. Sorafenib is a protein kinase inhibitor indicated as a treatment for advanced renal cell carcinoma. The present study aimed at developing Sorafenib SNEDDS to improve their solubility and bioavailability. A total of 15 formulations of Sorafenib SNEDDS were prepared and screened for phase separation and temperature variation using thermodynamic stability studies. Sorafenib loaded SNEDDS could potentially be exploited as a delivery system for increased oral bioavailability by 5 times when comparing with pure drug by minimizing first-pass metabolism and increased solubility.
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Bhikshapathi, D. V. R. N., and Keerthi Priya. "Development and in vivo Evaluation Lovastatin by Self-Nanoemulsifying Drug Delivery System." International Journal of Pharmaceutical Sciences and Drug Research 10, no. 03 (March 25, 2018). http://dx.doi.org/10.25004/ijpsdr.2018.100310.
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In the present investigation, self-nanoemulsifying drug delivery system (SNEDDS), of Lovastatin is being formulated to increase the solubility and bioavailability. The optimized Lovastatin SNEDDS formulation (F8) has a composition of Acrysol EL 135 as oil phase, Lauro glycol 90 and Capmul MCM as surfactant and co-surfactant respectively. Formulation F8 was found to be best formulation based on evaluation parameters. No drug precipitation or phase separation was observed in the optimized formulation. The particle size of the optimized formulation was found to be 4.9 nm and Z-Average of 71.5 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -13.7 mV which comply with the requirement of the zeta potential for stability. Furthermore, pharmacokinetic studies in rats indicated that compared to the pure drug, the optimized SMEDDS formulation significantly improved the oral bioavailability of Lovastatin. Therefore, from our results the study suggests that the Lovastatin loaded self-nanoemulsifying formulation has a great potential for clinical application.
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JAYAPAL, NALLAPU, and YAMSANI VAMSHI VISHNU. "FORMULATION AND IN VIVO EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL IN WISTAR RATS." Asian Journal of Pharmaceutical and Clinical Research, June 5, 2021, 126–36. http://dx.doi.org/10.22159/ajpcr.2021.v14i7.42003.
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Objective: The aim was to formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of ramipril, an antihypertensive drug to improve the solubility and bioavailability.
Methods: Based on solubility studies oil phase (Sefsol 218), surfactant (Acrysol EL135), and cosurfactant (Transcutol P), respectively, were selected to prepare SNEDDS. Ramipril SNEDDS optimized employing box-Behnken design through the study of factors. All formulations were evaluated for particle size, zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), drug content, and in vitro drug release. The optimized formulation was characterized for Fourier transform infrared (FTIR), scanning electron microscopy (SEM), stability studies, and pharmacokinetic study.
Results: The mean particle size, PDI, ZP, EE, content uniformity, and in vitro drug release profile of optimized ramipril-loaded SNEDDS (RF14) were found to be 75.3±2.21nm, 0.126±0.05, −24.4±5.78mV, 98.74±1.97%, 99.52±1.67%, and 98.65±1.73%, respectively. FTIR studies revealed that there is no incompatibility between drug and excipients, SEM images exhibited nanoparticles to be more porous and in spherical shape. Stability studies indicated formulation was stable for 6 months. In vivo studies were conducted for optimized formulation RF14, the Tmax was found to be 0.5±0.62 and 0.5±0.95 h for the optimized and commercial formulations respectively, while Cmax was 25.16±1.73 ng/mL was significant (p<0.05) as compared to the ramipril pure drug 8.02±0.086 ng/mL. AUC0-t of the SNEDDS formulation was higher 355.49±1.76ng h/ml compared to pure drug 116.57±1.64 ng h/ml indicated higher amount of drug concentration in blood proving better systemic absorption of ramipril from SNEDDS formulation as compared to the pure drug.
Conclusion: It is concluded from the results that ramipril was successfully formulated into SNEDDS with higher concentration with fast action.