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Artykuły w czasopismach na temat „Bioavailability of W”

Autor: Grafiati

Data publikacji: 3 czerwca 2025

Data aktualizacji: 31 lipca 2025

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1

Karmańska, Aleksandra, Natalia Rękawiecka, and Bolesław Karwowski. "Coenzyme Q10- metabolism, supplementation, bioavailability." Farmacja Polska 80, no. 9 (2025): 645–56. https://doi.org/10.32383/farmpol/200800.

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Przedmiot badań Koenzym Q10 (CoQ10) 2,3-dimetoksy-5-metylo-6-dekaprenylobenzochinon, nazywany również ubichinonem lub ubidekarenonem odgrywa kluczową rolę w mitochondrialnej fosforylacji oksydacyjnej. W wysokich stężeniach występuje w tkankach wymagających zwiększonej ilości energii: serce, nerki, mięśnie. Efektywność biosyntezy koenzymu Q10 ulega obniżeniu u osób starszych stąd korzystny wpływ może mieć wprowadzenie jego suplementacji. Cel pracy W pracy omówiono zagadnienia dotyczące: • znaczenia koenzymu Q10 w organizmie człowieka jego udział w procesach fosforylacji oksydacyjnej, ferroptozi

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Liu, Chunxia, Li Lv, Wei Guo, et al. "Self-Nanoemulsifying Drug Delivery System of Tetrandrine for Improved Bioavailability: Physicochemical Characterization and Pharmacokinetic Study." BioMed Research International 2018 (September 27, 2018): 1–10. http://dx.doi.org/10.1155/2018/6763057.

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The main purpose of this study was to investigate the potential of self-nanoemulsified drug delivery system (SNEDDS) to improve the oral bioavailability of tetrandrine (Tet). SNEDDS was developed by using rational blends of excipients with good solubilizing ability for Tet which was selected based on solubility studies. Further ternary phase diagram was constructed to determine the self-emulsifying region. The optimal formulation with the best self-nanoemulsified and solubilization ability consisted of 40% (w/w) oleic acid as oil, 15% (w/w) SPC and 30% (w/w) Cremophor RH-40 as surfactant, and

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3

Singh, Sanjay Kumar, Parameswara Rao Vuddanda, Sanjay Singh, and Anand Kumar Srivastava. "A Comparison between Use of Spray and Freeze Drying Techniques for Preparation of Solid Self-Microemulsifying Formulation of Valsartan andIn VitroandIn VivoEvaluation." BioMed Research International 2013 (2013): 1–13. http://dx.doi.org/10.1155/2013/909045.

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The objective of the present study was to develop self micro emulsifying formulation (SMEF) of valsartan to improve its oral bioavailability. The formulations were screened on the basis of solubility, stability, emulsification efficiency, particle size and zeta potential. The optimized liquid SMEF contains valsartan (20% w/w), Capmul MCM C8 (16% w/w), Tween 80 (42.66% w/w) and PEG 400 (21.33% w/w) as drug, oil, surfactant and co-surfactant, respectively. Further, Liquid SMEF was adsorbed on Aerosol 200 by spray and freeze drying methods in the ratio of 2 : 1 and transformed into free flowing p

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Kushwaha, Anjali. "Cashew Nut Starch as Natural Excipient for Improved Bioavailability of Drugs." International Journal of Pharmaceutical Sciences and Nanotechnology 12, no. 4 (2019): 4616–22. http://dx.doi.org/10.37285/ijpsn.2019.12.4.8.

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The bioavailability of drug is affected by various excipients present in the formulation. In case of tablets, the role of binders is very important for release of drug and bioavailability. In the present study, starch was extracted from the cashew nuts and used as binding agentat a concentration of 2% w/v, 4% w/v, 6% w/v and 8% w/v. The tablets were formulated by using famotidine drug and they were further evaluated for various parameters like weight variation, hardness, friability, disintegration time, in vitro and in vivo drug release. The results show that all parameters were found within t

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5

Zhou, Huafeng, Guoqing Liu, Jing Zhang, et al. "Novel Lipid-Free Nanoformulation for Improving Oral Bioavailability of Coenzyme Q10." BioMed Research International 2014 (2014): 1–9. http://dx.doi.org/10.1155/2014/793879.

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To improve the bioavailability of orally administered lipophilic coenzyme Q10 (CoQ10), we formulated a novel lipid-free nano-CoQ10 system stabilized by various surfactants. Nano-CoQ10s, composed of 2.5% (w/w) CoQ10, 1.67% (w/w) surfactant, and 41.67% (w/w) glycerol, were prepared by hot high-pressure homogenization. The resulting formulations were characterized by particle size, zeta potential, differential scanning calorimetry, and cryogenic transmission electron microscopy. We found that the mean particle size of all nano-CoQ10s ranged from66.3±1.5 nm to92.7±1.5 nm and the zeta potential ran

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6

Jang, Ji-Hun, Seung-Hyun Jeong, and Yong-Bok Lee. "Enhanced Lymphatic Delivery of Methotrexate Using W/O/W Nanoemulsion: In Vitro Characterization and Pharmacokinetic Study." Pharmaceutics 12, no. 10 (2020): 978. http://dx.doi.org/10.3390/pharmaceutics12100978.

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Methotrexate, which is widely used in the treatment of cancer and immune-related diseases, has limitations in use because of its low bioavailability, short half-life, and tissue toxicity. Thus, in this study, a nano-sized water-in-oil-in-water (W/O/W) double emulsion containing methotrexate was prepared to enhance its lymphatic delivery and bioavailability. Based on the results from solubility testing and a pseudo-ternary diagram study, olive oil as the oil, Labrasol as a surfactant, and ethanol as a co-surfactant, were selected as the optimal components for the nanoemulsion. The prepared nano

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7

Wang, Chih-Yuan, Ching-Chi Yen, Mei-Chich Hsu, and Yu-Tse Wu. "Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility, Permeability, and Bioavailability of Sesamin." Molecules 25, no. 14 (2020): 3119. http://dx.doi.org/10.3390/molecules25143119.

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Sesamin (SSM) is a water-insoluble compound that is easily eliminated by liver metabolism. To improve the solubility and bioavailability of SSM, this study developed and characterized a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of SSM and conducted pharmacokinetic assessments. Oil and surfactant materials suitable for SNEDDS preparation were selected on the basis of their saturation solubility at 37 ± 0.5 °C. The mixing ratios of excipients were determined on the basis of their dispersibility, transmittance (%), droplet sizes, and polydispersity index. An SNEDDS

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8

Kushwaha, Anjali, and Pratap Manjul Singh. "Role of naturally isolated pear starch on the bioavailability of famotidine." Journal of Drug Delivery and Therapeutics 9, no. 3 (2019): 430–35. http://dx.doi.org/10.22270/jddt.v9i3.2704.

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Purpose- The bioavailability of any drug in the formulation is affected by various excipients presents in it. In case of tablets the role of binders is very important for dissolution of dosage form as well as bioavailability of drug. Thus in following study an attempt is made to improve the dissolution of drug by using pear starch as binding agents. The starch was extracted from the Pear fruits and used as a binder in different concentrations, in famotidine tablets and then evaluate them. Methods-The tablets were formulated by wet granulation method by using 2% w/v, 4% w/v, 6% w/v and 8% w/v o

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9

Madonna, Sandra, Agus Jatnika Effendi, Edwan Kardena, and Syarif Hidayat. "Bioavailability enhancement of petroleum-contaminated soil by electrokinetic remediation." E3S Web of Conferences 485 (2024): 02007. http://dx.doi.org/10.1051/e3sconf/202448502007.

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The Electro kinetic Remediation Technology (EKR) is recognized as the most potential remediation technology for soils with low permeability, like clay soil characteristics. Electrokinetic treatment could increase the bioavailability of contaminants in bioremediation petroleum-contaminated soil. The study, “Bioavailability enhancement of petroleum contaminated soil by electrokinetic remediation,” is experimental research in a laboratory to improve the bioavailability of petroleum hydrocarbons on clay during bioremediation with initial treatment using electrokinetic remediation techniques, findi

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10

Yang, Chen, Yixiang Wang, Yike Xie, et al. "Oat protein-shellac nanoparticles as a delivery vehicle for resveratrol to improve bioavailability in vitro and in vivo." Nanomedicine 14, no. 21 (2019): 2853–71. http://dx.doi.org/10.2217/nnm-2019-0244.

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Aim: Oat protein-shellac nanoparticles (NPs) were developed as a delivery system for resveratrol to improve bioavailability. Materials & methods: The NPs were prepared from w/w emulsion followed by cold-gelation. In vitro release and cell uptake mechanism of NPs were estimated by HPLC and confocal laser scanning microscopy. In vivo bioavailability and hepatoprotective activity of encapsulated resveratrol were studied using rat models. Results & conclusion: NPs (90–300 nm) protected resveratrol in gastric fluid, while allowing controlled release into small intestine in vitro. The optimi

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11

Verma, Hitesh, Surajpal Verma, Shyam Baboo Prasad, and Harmanpreet Singh. "Sublingual Delivery of Frovatriptan: An Indication of Potential Alternative Route." International Scholarly Research Notices 2014 (October 29, 2014): 1–9. http://dx.doi.org/10.1155/2014/675868.

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Frovatriptan, a 5-HT1B and 5-HT1D receptor agonist, is used for the treatment of acute migraine attack. This molecule is classified into second line therapy because of its slow onset of action (peak response obtained after 4 hours of administration) and low bioavailability (25%). Moreover, its therapy is the most costly among all triptans. Attempt has been made in present work to suggest a way out to fasten its onset of action and to enhance its bioavailability. Prepared tablets were evaluated by physicochemical tests, in vitro permeation studies, ex vivo permeation studies, and histopathologi

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12

Salem, Heba F., Amr Gamal, Haitham Saeed, Marwa Kamal, and Alaa S. Tulbah. "Enhancing the Bioavailability and Efficacy of Vismodegib for the Control of Skin Cancer: In Vitro and In Vivo Studies." Pharmaceuticals 15, no. 2 (2022): 126. http://dx.doi.org/10.3390/ph15020126.

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Skin cancer is the most frequent cancer throughout the world. Vismodegib (VSD) is a hedgehog blocker approved for the prevention and treatment of skin cancer. VSD, however, is poorly bioavailable and has been linked to side effects. This work focused on designing a nano-invasome gel as a vehicle for enhancing the permeation, bioavailability, and efficacy of VSD. Additionally, the combined effect of terpenes and ethanol was studied on the permeation of VSD compared with liposomes. The prepared VSD-loaded invasomes (VLI) formulation included cineole (1%v/v), cholesterol (0.15%w/w), phospholipid

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13

Tsekouras, Athanasios A., and Panos Macheras. "Re-examining digoxin bioavailability after half a century: Time for changes in the bioavailability concepts." Pharmaceutical Research 38, no. 10 (2021): 1635–38. http://dx.doi.org/10.1007/s11095-021-03121-w.

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Shirsand, S. B., G. V. Wadageri, S. A. Raju, and Gopikrishna Kolli. "Formulation and In Vivo Evaluation of Mucoadhesive Buccal Tablets of Carvedilol." International Journal of Pharmaceutical Sciences and Nanotechnology 6, no. 3 (2013): 2164–71. http://dx.doi.org/10.37285/ijpsn.2013.6.3.8.

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In present study we studied the feasibility of preparing mucoadhesive buccal delivery systems containing carvedilol to improve drug residence time on buccal mucosa and drug dissolution rate, to circumvent the first-pass metabolism and quick drug entry into the systemic circulation. Bilayer buccal tablets of carvedilol prepared using controlled release and mucoadhesive polymers (hydroxypropyl methylcellulose 15 cps, 50 cps, K4M and Carbopol 934p) along with impermeable backing layer (ethyl cellulose). 15 formulations were developed with varying concentrations of polymers. The designed tablets w

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15

Zaki, Randa Mohammed, Munerah M. Alfadhel, Manal A. Alossaimi, et al. "Central Composite Optimization of Glycerosomes for the Enhanced Oral Bioavailability and Brain Delivery of Quetiapine Fumarate." Pharmaceuticals 15, no. 8 (2022): 940. http://dx.doi.org/10.3390/ph15080940.

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This study aimed to formulate and statistically optimize glycerosomal formulations of Quetiapine fumarate (QTF) to increase its oral bioavailability and enhance its brain delivery. The study was designed using a Central composite rotatable design using Design-Expert® software. The independent variables in the study were glycerol % w/v and cholesterol % w/v, while the dependent variables were vesicle size (VS), zeta potential (ZP), and entrapment efficiency percent (EE%). The numerical optimization process resulted in an optimum formula composed of 29.645 (w/v%) glycerol, 0.8 (w/v%) cholesterol

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Rane, Devendra Revanand, Hemant Narhar Gulve, Vikas Vasant Patil, Vinod Madhaorao Thakare, and Vijay Raghunath Patil. "Formulation and evaluation of fast dissolving tablet of albendazole." International Current Pharmaceutical Journal 1, no. 10 (2012): 311–16. http://dx.doi.org/10.3329/icpj.v1i10.11848.

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Albendazole is broad spectrum anthelmintic use against many helminths. It is used for treatment of Threadworm, Hookworm, and Tapeworm. It has low bioavailability due to its first pass metabolism. In the present work, fast dissolving tablet of Albendazole was design with a view to and provide a quick onset of action. The main objective of the study was to formulate fast dissolving tablets of Albendazole to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablets prepared by direct compression and using super disintegrants in different conc

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Osei, Benjamin Appiah, and Mohammed Rufai Ahmed. "Edta, Water-Extractable Arsenic and Bioavailability of Arsenic in Soil/Tailings: the Effects of Zeolite and Beringite Amendments." Journal of Agricultural Studies 5, no. 4 (2018): 203. http://dx.doi.org/10.5296/jas.v6i1.12699.

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The effects of zeolite and beringite ( 0, 30 and 60 kg ha-1 w/w) on EDTA-extractable Arsenic (As), water soluble As, and bioavailability of arsenic (As) in non-mined agricultural soil and tailings of a mined site(capped and uncapped) were studied in a pot experiment. Un-amended non-mined agricultural soil was included as a control. EDTA-extractable and water extractable forms of As were monitored for 0-12-weeks after amendments and bioavailability of As was evaluated by growing lettuce (Lactuca sativa) on amended tailings/soil for 4-12 weeks after incubation. For EDTA-extractable As at week 12

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Bijle, Mohammed Nadeem, James Tsoi, Manikandan Ekambaram, Edward C. M. Lo, Clifton M. Carey, and Cynthia Kar Yung Yiu. "Enhanced Fluoride Bioavailability with Incorporation of Arginine in Child Dentifrices." Journal of Clinical Pediatric Dentistry 44, no. 5 (2020): 332–41. http://dx.doi.org/10.17796/1053-4625-44.5.7.

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Objective(s): To: 1) examine the fluoride concentrations in commercial child formula dentifrices (CFD)s; and 2) investigate the effect of arginine incorporation in CFDs on fluoride bioavailability. Study Design: Five commercial CFDs were examined for fluoride concentrations. Total, total soluble, and insoluble fluorides in CFDs were determined by the modified Taves acid-diffusion method (TAD). Ionic F and MFP were estimated by modified direct method with standard addition technique. L-arginine (L-Arg)/L-arginine monohydrochloride (L-Arg.HCl) were incorporated at 2% w/w in the commercial CFDs.

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Achile Akpa, Paul, Joseph Abuchi Ugwuoke, Anthony Amaechi Attama, et al. "Improved antimalarial activity of caprol-based nanostructured lipid carriers encapsulating artemether-lumefantrine for oral administration." African Health Sciences 20, no. 4 (2020): 1679–97. http://dx.doi.org/10.4314/ahs.v20i4.20.

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Background: Artemether and lumefantrine display low aqueous solubility leading to poor release profile; hence the need for the use of lipid-based systems to improve their oral bioavailability so as to improve their therapeutic efficacy. Aim and objective: The objective of this work was to utilize potentials of nanostructured lipid carriers (NLCs) for im- provement of the oral bioavailability of artemether and lumefantrine combination and to evaluate its efficacy in the treat- ment of malaria. This study reports a method of formulation, characterization and evaluation of the therapeutic e

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Lee, Jong-Hwa, and Gye-Won Lee. "Formulation Approaches for Improving the Dissolution Behavior and Bioavailability of Tolvaptan Using SMEDDS." Pharmaceutics 14, no. 2 (2022): 415. http://dx.doi.org/10.3390/pharmaceutics14020415.

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Tolvaptan, a selective vasopressin receptor antagonist, is a Class IV agent of Biopharmaceutical Classification System (BCS). To improve bioavailability after oral administration, the new tolvaptan-loaded self-microemulsifying drug delivery system (SMEDDS) was further optimized using a “design of the experiment (DoE)” including components of D-optional mixture design. Based on a solubility study of tolvaptan in various oils, surfactants, and cosurfactants, Capryol® 90, Tween 20, and Transcutol® HP [or polyethylene glycol 200 (PEG 200)] were finally selected for optimization of tolvaptan-loaded

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Chávez-Zamudio, Rubi, Angélica A. Ochoa-Flores, Ida Soto-Rodríguez, Rebeca Garcia-Varela, and Hugo Sergio García. "Preparation, characterization and bioavailability by oral administration of O/W curcumin nanoemulsions stabilized with lysophosphatidylcholine." Food & Function 8, no. 9 (2017): 3346–54. http://dx.doi.org/10.1039/c7fo00933j.

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Lee, Jaehyeok, Chul Haeng Lee, Jong-Geon Lee, So Yeon Jeon, Min-Koo Choi, and Im-Sook Song. "Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation." Pharmaceutics 14, no. 5 (2022): 1037. http://dx.doi.org/10.3390/pharmaceutics14051037.

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Ursodeoxycholate (UDCA) has low oral bioavailability and pH-dependent solubility and permeability. Thus, we developed a pH-modified extended-release formulation of UDCA using Na2CO3 as the alkalizing agent and hydroxypropyl methylcellulose (HPMC) as the release-modifying agent. The optimized pH-modified controlled-release UDCA formulation, with the UDCA:HPMC:Na2CO3 ratio of 200:600:150 (w/w/w), was prepared using a spray-drying method. Then, the formulation’s solubility, dissolution, and pharmacokinetic properties were characterized. In a pH-modified extended-release formulation of UDCA, the s

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Nair, Gupta, Al-Dhubiab, et al. "Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch." Pharmaceutics 11, no. 7 (2019): 359. http://dx.doi.org/10.3390/pharmaceutics11070359.

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The administration of pioglitazone as an oral therapy is restricted due to various challenges. The aim of the current investigation was to evaluate the suitability of pioglitazone in adhesive transdermal patch as an alternative delivery system, in order to improve therapeutic delivery. Drug in adhesive pioglitazone (2% w/w) transdermal patch were optimized for drug release, suitable adhesive, and skin permeation enhancer. The selected patch was examined for drug-loading capacity and the patch with greater pioglitazone (6% w/w) was evaluated in rat models. The release of pioglitazone was influe

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Song, Yanqing, Huan Gao, Sixi Zhang, Yue Zhang, Xiangqun Jin, and Jingmeng Sun. "Prescription Optimization and Oral Bioavailability Study of Salvianolic Acid Extracts W/O/W Multiple Emulsion." Biological & Pharmaceutical Bulletin 40, no. 12 (2017): 2081–87. http://dx.doi.org/10.1248/bpb.b17-00162.

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Dave, Pooja, and Chetan Detroja. "Thermosensitive Copolymeric PLGA-PEG-PLGA Nanomicelles of Raloxifene: Synthesis, Formulation, and In-vitro Characterization." International Journal of Pharmaceutical Sciences and Drug Research 15, no. 02 (2023): 189–95. http://dx.doi.org/10.25004/ijpsdr.2023.150210.

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The objective of the present research study has been to synthesize (PLGA-PEG-PLGA), a thermolabile and biodegradable triblock copolymer. The polymer was subjected to differential evaluation using NMR, XRD, and FTIR techniques for characterization. Raloxifene, a potential therapeutic for breast cancer, exerts poor water solubility and a low fraction of bioavailability owing to its pharmacokinetic properties. The synthesized polymer was used to load raloxifene-encapsulating polymeric micelles, which were then subjected to several evaluations with the aim of improving solubility and bioavailabili

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Dave, Pooja, and Chetan Detroja. "Formulation and Characterization of Raloxifene loaded Biodegradable Polymeric Nanomicelles." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 13, no. 01 (2023): 158–61. http://dx.doi.org/10.25258/ijddt.13.1.24.

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Raloxifene has been used to treat breast cancer; nevertheless, it has poor water solubility and a low bioavailability fraction because higher fi rst-pass metabolism hinders its application raloxifene nano micelles by using PLGA50:50 to enhance solubility and bioavailability. The solvent evaporation technique was used to prepare polymeric nano-micelles. Ral-loaded polymeric micelles had a zeta potential of - 0.71 mV, implying a practically neutral surface charge. Blank micelles and RAL-loaded micelles had similar average sizes of 84.29 nm and 95.41 nm, respectively. The drug encapsulating and d

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Navamanisubramanian, Raja, Raghunandan Nerella, and Shanmuganathan Seetharaman. "Pharmacokinetic Investigation to Study the In Vivo Bioavailability of Thiolated Chitosan Based Repaglinide Buccal Tablets." Pharmaceutical Sciences 26, no. 4 (2020): 414–22. http://dx.doi.org/10.34172/ps.2020.62.

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Background: Repaglinide (REP) is an antihyperglycemic drug having low bioavailability due to its extensive first-pass metabolism. The present study aimed to develop and pharmacokinetic investigte the thiolated chitosan (TC) based buccal tablets of REP for improved bioavailability. Methods: TC was prepared by conjugation of L-cysteine with chitosan. The amount of free thiol groups present in TC was determined by UV-spectrophotometry using Ellman’s reagent. TC based REP buccal tablets were prepared by two layers co-compression method and characterized for in vitro and ex vivo parameters. The in

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Ghalwash, Maha M., Amr Gamal Fouad, Nada H. Mohammed, et al. "Fabrication and In Vivo Evaluation of In Situ pH-Sensitive Hydrogel of Sonidegib–Invasomes via Intratumoral Delivery for Basal Cell Skin Cancer Management." Pharmaceuticals 18, no. 1 (2024): 31. https://doi.org/10.3390/ph18010031.

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Background/Objectives: Basal cell skin cancer (BCSC) develops when skin cells proliferate uncontrollably. Sonidegib (SDB) is a therapeutic option for the treatment of BCSC by inhibiting hedgehog signaling. The problems with SDB’s low solubility, poor bioavailability, resistance, poor targeting, and first-pass action make it less effective when taken orally. This investigation set out to design an intratumoral in situ pH-sensitive hydrogel of SDB-invasomes (IPHS-INV) that can effectively treat BCSC by improving SDB’s bioavailability, sustainability, targeting, and efficacy while also reducing i

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Kumar, Charit, and Arun Nanda. "Novel microwave-assisted solid dispersion technology enhances piroxicam dissolution and therapeutic efficacy: an in vitro and in vivo study." Journal of Applied Pharmaceutical Research 13, no. 1 (2025): 49–61. https://doi.org/10.69857/joapr.v13i1.921.

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Background: Piroxicam (PRX), a nonsteroidal anti-inflammatory drug, exhibits poor aqueous solubility, limiting its therapeutic efficacy. Enhancing solubility can directly improve bioavailability and therapeutic effectiveness. This study explores the development of a new solid dispersion (SD) system of PRX using polyvinylpyrrolidone (PVP K30) as a carrier by MW-assisted method. Methods: The involvement of microwave (MW) in the solvent evaporation method is a newer concept aimed at enhancing the solubility and in vivo bioavailability of PRX. Various ratios of PRX: PVPK30 (1:5, 1:7, 1:9, and 1:11

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Poudel, Surendra, and Dong Wuk Kim. "Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance." Pharmaceutics 13, no. 4 (2021): 497. http://dx.doi.org/10.3390/pharmaceutics13040497.

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Candesartan cilexetil (CC), a prodrug and highly effective antihypertensive agent, is a poorly soluble (BCS Class II) drug with limited bioavailability. Here, we attempted to improve CC’s bioavailability by formulating several CC-loaded amorphous solid dispersions with a hydrophilic carrier (PVPK30) and pH modifier (sodium carbonate) using the spray drying technique. Solubility, in vitro dissolution, and moisture content tests were used for screening the optimized formulation. We identified an optimized formulation of CC/PVPK30/SC, which at the ratio of 1:0.5:1 (w/w/w) exhibited a 30,000-fold

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Franceschinis, Erica, Marco Roverso, Daniela Gabbia, et al. "Self-Emulsifying Formulations to Increase the Oral Bioavailability of 4,6,4′-Trimethylangelicin as a Possible Treatment for Cystic Fibrosis." Pharmaceutics 14, no. 9 (2022): 1806. http://dx.doi.org/10.3390/pharmaceutics14091806.

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4,6,4′-trimethylangelicin (TMA) is a promising pharmacological option for the treatment of cystic fibrosis (CF) due to its triple-acting behavior toward the function of the CF transmembrane conductance regulator. It is a poorly water-soluble drug, and thus it is a candidate for developing a self-emulsifying formulation (SEDDS). This study aimed to develop a SEDDS to improve the oral bioavailability of TMA. Excipients were selected on the basis of solubility studies. Polyoxyl-35 castor oil (Cremophor® EL) was proposed as surfactant, diethylene glycol-monoethyl ether (Transcutol® HP) as cosolven

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Raval, Shilpa, Parva Jani, Pravin Patil, Parth Thakkar, and Krutika Sawant. "Enhancement of bioavailability through transdermal drug delivery of paliperidone palmitate-loaded nanostructured lipid carriers." Therapeutic Delivery 12, no. 8 (2021): 583–96. http://dx.doi.org/10.4155/tde-2021-0036.

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Aim: The work describes enhanced bioavailability of paliperidone palmitate through transdermal delivery using nanostructured lipid carriers (NLC). Materials & methods: NLCs were formulated by nanoprecipitation method followed by incorporation in transdermal patch and physicochemical characterization. Results: NLCs showed high percentage entrapment efficiency of 83.44 ± 0.8%, drug loading of 24.75 ± 1.10% (w/w), particle size of 173.8 ± 3.25 nm, polydispersity index of 0.143 ± 0.05 and zeta potential of -15.9 ± 0.75 mV. In vitro and ex vivo studies indicated zero-order controlled drug relea

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Kotharapu, Rama Koteswararao, and Srinivas Lankalapalli. "Development and Evaluation of Clopidogrel Bisulphate Multi-Unit Floating Mini-Tablets." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 173–80. http://dx.doi.org/10.22270/jddt.v9i4.3169.

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The objective of the present work was to formulate and characterize multi-unit floating drug delivery system of Clopidogrel bisulphate to increase the bioavailability and sustain the drug release properties up to 8 h with more predictable drug release kinetics that avoids all or nothing emptying effect wherefore to improve patient compliance. Clopidogrel bisulphate floating mini-tablets were prepared by effervescent approach with melt granulation and direct compression techniques alone and in combination using Hydroxypropyl methylcellulose (HPMC) K100M and Compritol 888 ATO at different concen

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Ahmed, Osama A. A., Hany M. El-Bassossy, Heba M. El-Sayed та Soad S. Abd El-Hay. "Rp-HPLC Determination of Quercetin in a Novel D-α-Tocopherol Polyethylene Glycol 1000 Succinate Based SNEDDS Formulation: Pharmacokinetics in Rat Plasma". Molecules 26, № 5 (2021): 1435. http://dx.doi.org/10.3390/molecules26051435.

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Despite its proven efficacy in diverse metabolic disorders, quercetin (QU) for clinical use is still limited because of its low bioavailability. D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) is approved as a safe pharmaceutical adjuvant with marked antioxidant and anti-inflammatory activities. In the current study, several QU-loaded self-nanoemulsifying drug delivery systems (SNEDDS) were investigated to improve QU bioavailability. A reversed phase high performance liquid chromatography (RP-HPLC) method was developed, for the first time, as a simple and sensitive technique for pharm

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Zhang, Siyu, Cuina Wang, Weigang Zhong, Alyssa H. Kemp, Mingruo Guo, and Adam Killpartrick. "Polymerized Whey Protein Concentrate-Based Glutathione Delivery System: Physicochemical Characterization, Bioavailability and Sub-Chronic Toxicity Evaluation." Molecules 26, no. 7 (2021): 1824. http://dx.doi.org/10.3390/molecules26071824.

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Glutathione (GSH) is a powerful antioxidant, but its application is limited due to poor storage stability and low bioavailability. A novel nutrient encapsulation and delivery system, consisting of polymerized whey protein concentrate and GSH, was prepared and in vivo bioavailability, antioxidant capacity and toxicity were evaluated. Polymerized whey protein concentrate encapsulated GSH (PWPC-GSH) showed a diameter of roughly 1115 ± 7.07 nm (D50) and zeta potential of 30.37 ± 0.75 mV. Differential scanning calorimetry (DSC) confirmed that GSH was successfully dispersed in PWPC particles. In viv

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Giri, Bhupendra Raj, Jung Suk Kim, Jong Hyuck Park, et al. "Improved Bioavailability and High Photostability of Methotrexate by Spray-Dried Surface-Attached Solid Dispersion with an Aqueous Medium." Pharmaceutics 13, no. 1 (2021): 111. http://dx.doi.org/10.3390/pharmaceutics13010111.

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Low aqueous solubility and poor bioavailability are major concerns in the development of oral solid-dosage drug forms. In this study, we fabricated surface-attached solid dispersion (SASD) to enhance the solubility, bioavailability, and photostability of methotrexate (MTX), a highly lipophilic and photo-unstable drug. Several MTX-loaded SASD formulations were developed for spray-drying using water as the solvent, and were investigated for their aqueous solubility and dissolution kinetics. An optimized ternary SASD formulation composed of MTX/ sodium carboxymethyl cellulose (Na-CMC)/sodium laur

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Giri, Bhupendra Raj, Jaewook Kwon, Anh Q. Vo, Ajinkya M. Bhagurkar, Suresh Bandari, and Dong Wuk Kim. "Hot-Melt Extruded Amorphous Solid Dispersion for Solubility, Stability, and Bioavailability Enhancement of Telmisartan." Pharmaceuticals 14, no. 1 (2021): 73. http://dx.doi.org/10.3390/ph14010073.

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Telmisartan (TEL, an antihypertensive drug) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its poor aqueous solubility. In this study, we enhanced the solubility, bioavailability, and stability of TEL through the fabrication of TEL-loaded pH-modulated solid dispersion (TEL pHM-SD) using hot-melt extrusion (HME) technology. We prepared different TEL pHM-SD formulations by varying the ratio of the drug (TEL, 10–60% w/w), the hydrophilic polymer (Soluplus®, 30–90% w/w), and pH-modifier (sodium carbonate, 0–10% w/w). More so, the tablets prepared from an optimi

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Kardogan, Beyza, Kadir Sekercioglu, and Yusuf Çagatay Erşan. "Compatibility and Biomineralization Oriented Optimization of Nutrient Content in Nitrate-Reducing-Biogranules-Based Microbial Self-Healing Concrete." Sustainability 13, no. 16 (2021): 8990. http://dx.doi.org/10.3390/su13168990.

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Microbially induced calcium carbonate precipitation (MICP) can be mentioned among the popular approaches to develop a self-healing concrete. The production of dissolved inorganic carbon through microbial activity is the main precursor for MICP in concrete and it is limited by the bioavailability of the nutrients. When nutrients are added to the mortar as admixtures, their bioavailability becomes more significant for crack repair because nutrients disperse in the mortar and considerable fraction stays far from a single crack. Therefore, the determination of bioavailability of nutrients and its

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Mishra, Rakesh, Shubham Paldewar, and Tanaji Nandgude. "Lipid based approach for bioavailability enhancement of boswellia serrata." Journal of medical pharmaceutical and allied sciences 11, no. 1 (2022): 4129–37. http://dx.doi.org/10.55522/jmpas.v11i1.1693.

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In past numerous studies reported the potential effect of Boswellia serrata in the treatment of various topical and systemic inflammatory diseases. Despite of potential pharmacological effects the oral delivery of BS is challenging due to poor bioavailability limiting its clinical applications. The objective of this study was to formulate and optimize lipid-based sustained release pellets of Boswellia serrata in order to improve solubility and oral bioavailability. Initially, solid dispersions were formulated by fusion method using hydrophilic grade lipids Gelucire 44/14 and 50/13 in different

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Zhang, Yongxiang, Minglang Ma, Jinyu Yang, et al. "Preparation, Characterization, and Oral Bioavailability of Solid Dispersions of Cryptosporidium parvum Alternative Oxidase Inhibitors." International Journal of Molecular Sciences 25, no. 13 (2024): 7025. http://dx.doi.org/10.3390/ijms25137025.

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The phenylpyrazole derivative 5-amino-3-[1-cyano-2-(3-phenyl-1H-pyrazol-4-yl) vinyl]-1-phenyl-1H-pyrazole-4-carbonitrile (LN002), which was screened out through high-throughput molecular docking for the AOX target, exhibits promising efficacy against Cryptosporidium. However, its poor water solubility limits its oral bioavailability and therapeutic utility. In this study, solid dispersion agents were prepared by using HP-β-CD and Soluplus® and characterized through differential scanning calorimetry, Fourier transform infrared, powder X-ray diffraction, and scanning electron microscopy. Physica

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Aisyah, Putri, and Suyatno Sutoyo. "Synthesis and Characterization of Ethanol Extract Nanoherb of Tapak Liman Leaves (Elephantopus scaber Linn.) by Ionic Gelation Method." International Journal of Progressive Sciences and Technologies 42, no. 1 (2023): 381. http://dx.doi.org/10.52155/ijpsat.v42.1.5855.

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Tapak Liman (Elephantopus scaber) is a plant that has been used by Indonesian people as a traditional medicine to treat diarrhea, fever, malaria, and coughs. Tapak Liman leaves contain compounds of flavonoids, phenols, and saponins. However, these phytochemical compounds exhibit low bioavailability properties. Therefore, a technology that can improve their bioavailability is needed. One approach is through the synthesis of Tapak Liman nanoparticles via the ionic gelation method using alginate and CaCl2. This study aims to determine the content of Tapak Liman leaves, synthesize nanoherb from it

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Zhou, Qiqian, Katie E. Lane, and Weili Li. "Evaluating the Stability and Digestibility of Long-Chain Omega-3 Algal Oil Nanoemulsions Prepared with Lecithin and Tween 40 Emulsifiers Using an In Vitro Digestion Model." Foods 13, no. 15 (2024): 2407. http://dx.doi.org/10.3390/foods13152407.

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The health benefits of long-chain omega-3 polyunsaturated fatty acid (LCn-3PUFA) intake have been well documented. However, currently, the consumption of oily fish (the richest dietary source of LCn-3PUFA) in the UK is far below the recommended level, and the low digestibility of LCn-3PUFA bulk oil-based supplements from triglyceride-based sources significantly impacts their bioavailability. LCn-3PUFA-rich microalgal oil offers a potential alternative for populations who do not consume oily fish, and nanoemulsions have the potential to increase LCn-3PUFA digestibility and bioavailability. The

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Mahdy, Ahmed M., Elsayed Elkhatib, Tiequan Zhang, Nieven O. Fathi, and Zhi-Qing Lin. "Nano-Scale Drinking Water Treatment Residuals Affect Arsenic Fractionation and Speciation in Biosolids-Amended Agricultural Soil." Applied Sciences 10, no. 16 (2020): 5633. http://dx.doi.org/10.3390/app10165633.

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An incubation experiment was conducted to determine the effects of nanoscale drinking water treatment residuals (nWTRs) on arsenic (As) fractionation and speciation in agricultural soil amended with biosolids. The soils were treated with biosolids of 3% (w/w), along with nWTR application rates of 0, 0.25, 0.50, or 1.00% (w/w). The results revealed that the As adsorption rate increased with increasing the As treatment level from 50 to 800 mg/L. The maximum efficiency of As adsorption was 95%–98% in the soil treated with nWTRs of 1%, while the least As adsorption was 53%–91% in the soil treated

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Salem, Heba F., Amr Gamal, Haitham Saeed, and Alaa S. Tulbah. "The Impact of Improving Dermal Permeation on the Efficacy and Targeting of Liposome Nanoparticles as a Potential Treatment for Breast Cancer." Pharmaceutics 13, no. 10 (2021): 1633. http://dx.doi.org/10.3390/pharmaceutics13101633.

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Breast cancer is the most frequent malignancy in women. This work focuses on developing deformable liposomes as a potential carrier for breast cancer treatment and studying the impact of improving dermal permeation on the efficacy and targeting of liposomes. Raloxifene (RXF), an oestrogen antagonist, was used as a model drug. Using Box–Behnken design, different formulations of RXF-loaded deformable liposome (RLDL) were prepared using different propylene glycol, phospholipid and cholesterol concentrations. The percentage of entrapment efficiency (Y1), particle size (Y2), zeta potential (Y3) and

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Arif, Sadia Tabassam, Shahiq uz Zaman, Muhammad Ayub Khan, et al. "Augmented Oral Bioavailability and Prokinetic Activity of Levosulpiride Delivered in Nanostructured Lipid Carriers." Pharmaceutics 14, no. 11 (2022): 2347. http://dx.doi.org/10.3390/pharmaceutics14112347.

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The present study is aimed to develop and optimize levosulpiride-loaded nanostructured lipid carriers (LSP-NLCs) for improving oral bioavailability and prokinetic activity of LSP. LSP-NLCs were optimized with D-optimal mixture design using solid lipid, liquid lipid and surfactant concentrations as independent variables. The prepared LSP-NLCs were evaluated for physicochemical properties and solid-state characterization. The in vivo oral pharmacokinetics and prokinetic activity of LSP-NLCs were evaluated in rats. LSP-NLCs formulation was optimized at Precirol® ATO 5/Labrasol (80.55/19.45%, w/w)

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Jabbar, Alhasan A., Israa Al-Ani, Ramadan I. Al-Shdefat, Nadia Ghazal, Anwar Jaffal та Mohamed H. Fayed. "Design of Experiment Approach for Enhancing the Dissolution Profile and Robustness of Loratadine Tablet Using D-α-Tocopheryl Polyethylene Glycol 1000 Succinate". Pharmaceutics 17, № 3 (2025): 380. https://doi.org/10.3390/pharmaceutics17030380.

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Background: Formulating poorly water-soluble drugs poses significant challenges due to their limited solubility and bioavailability. Loratadine (LTD), classified as a BCS II molecule, exhibits notably low solubility, leading to reduced bioavailability. Objective: This study aims to enhance the dissolution rate of LTD through the utilization of the wet granulation process using Tocopheryl polyethylene glycol 1000 succinate (TPGS). Methods: A Design-of-Experiment methodology was adopted to investigate and optimize the formulation variables for preparing an oral delivery system of LTD with improv

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Mahajan, Radhika Rajiv, Punna Rao Ravi, Riya Kamlesh Marathe, Ajay Gorakh Dongare, Apoorva Vinayak Prabhu, and Łukasz Szeleszczuk. "Design and Evaluation of Clove Oil-Based Self-Emulsifying Drug Delivery Systems for Improving the Oral Bioavailability of Neratinib Maleate." Pharmaceutics 16, no. 8 (2024): 1087. http://dx.doi.org/10.3390/pharmaceutics16081087.

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Neratinib maleate (NM), a tyrosine kinase inhibitor, is used in the treatment of breast cancer. NM is orally administered at a high dose of 290 mg due to its low solubility and poor dissolution rate at pH > 3, as well as gut-wall metabolism limiting its bioavailability. Self-emulsifying drug delivery systems (SEDDSs) of NM were developed in the current study to improve its oral bioavailability. The oily vehicle (clove oil) was selected based on the solubility of NM, while the surfactant and the cosurfactant were selected based on the turbidimetric analysis. Three different sets were screene

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Aldawsari, Hibah M., Usama A. Fahmy, Fathy Abd-Allah, and Osama A. A. Ahmed. "Formulation and Optimization of Avanafil Biodegradable Polymeric Nanoparticles: A Single-Dose Clinical Pharmacokinetic Evaluation." Pharmaceutics 12, no. 6 (2020): 596. http://dx.doi.org/10.3390/pharmaceutics12060596.

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Avanafil (AVA) is a second-generation phosphodiesterase-5 (PDE5) inhibitor. AVA shows high selectivity to penile tissues and fast absorption, but has a bioavailability of about 36%. The aim was to formulate and optimize AVA-biodegradable nanoparticles (NPs) to enhance AVA bioavailability. To assess the impact of variables, the Box–Behnken design was utilized to investigate and optimize the formulation process variables: the AVA:poly (lactic-co-glycolic acid) (PLGA) ratio (w/w, X1); sonication time (min, X2); and polyvinyl alcohol (PVA) concentration (%, X3). Particle size (nm, Y1) and EE% (%,

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Sy, Papa Mady, Sidy Mouhamed Dieng, Alphonse Rodrigue Djiboune, et al. "O/W Pickering emulsion stabilized by magnesium carbonate particles for drug delivery systems." Journal of Drug Delivery and Therapeutics 13, no. 2 (2023): 47–54. http://dx.doi.org/10.22270/jddt.v13i2.5925.

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This study investigates the formulation of surfactant-free Pickering emulsions that release a drug at a specific pH to improve its oral bioavailability. The stabilizing particles composed of magnesium carbonate particles. Pickering oil-in-water emulsions stabilized with magnesium carbonate particles and encapsulating a hydrophobic drug model (ibuprofen) were formulated using a high-energy process with rotor-stator turbo mixer (IKA® T25 digital ultra-Turrax). The experimental approach explored the impact of all formulation parameters, dispersed phase and amount of magnesium carbonate particles

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Chen, Ting, Junhui Yang, Lihua Chen, et al. "Use of ordered mesoporous silica-loaded phyto-phospholipid complex for BCS IV class plant drug to enhance oral bioavailability: a case report of tanshinone IIA." RSC Advances 6, no. 116 (2016): 115010–20. http://dx.doi.org/10.1039/c6ra22778c.

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A CDDS was composed of PC and SD, using TS as a model drug. The marked improvements in oral bioavailability by TSPC-SD may result from comprehensive effects, including improved lg P<sub>o/w</sub>andP<sub>app</sub>viaPC, and increased dissolution rates from SD.

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