scholarly journals Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats

2011 ◽  
pp. 521 ◽  
Author(s):  
Wei Wu ◽  
Wei He ◽  
Yanan Tan ◽  
Zhiqiang Tian ◽  
Lingyun Chen ◽  
...  
Keyword(s):  
Delivery Systems ◽  
Water Soluble ◽  
Food Protein ◽  
Poorly Water Soluble Drugs ◽  
In Vitro Characterization ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Pharmacokinetics In Rats

scholarly journals Solubility enhancement of carvedilol using drug–drug cocrystallization with hydrochlorothiazide

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shivarani Eesam ◽  
Jaswanth S. Bhandaru ◽  
Chandana Naliganti ◽  
Ravi Kumar Bobbala ◽  
Raghuram Rao Akkinepally
Keyword(s):  
Aqueous Solubility ◽  
Sem Analysis ◽  
Water Soluble ◽  
High Permeability ◽  
Poorly Water Soluble Drugs ◽  
Drug Discovery And Development ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dissolution In Vitro

Abstract Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

Clay-based Formulations for Bioavailability Enhancement of Poorly Water-soluble Drugs

2021 ◽  
Vol 22 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
High Surface ◽  
High Surface Area ◽  
Delivery Systems ◽  
Water Soluble ◽  
Limited Information ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Ideal System ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

: Clays have been used in various health care products, including drug delivery systems. Advanced formulations have been investigated to take full advantage of clays or clay-based materials. The remarkable properties of clays, such as high adsorption, high surface area, and high ion exchange capacities, provide an ideal system for the delivery of poorly water-soluble drugs. There is currently limited information on the classification and discussion of clay-based formulations for poorly water-soluble drugs. This review aims to describe efficient delivery systems that use clay as the main excipient in formulations. More details about the strategies of using clays in formulations as well as fabrication methods will be discussed. Moreover, combinations with other excipients in hybrid formulations will also be mentioned in evaluating the efficacy of these systems. The highlighted recent studies on clay-based formulations for poorly water-soluble drugs could provide fundamental approaches and prospects to apply them in drug development.

Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols

2004 ◽  
Vol 23 (3) ◽  
pp. 287-296 ◽  
Author(s):  
Janne Ørskov Christensen ◽  
Kirsten Schultz ◽  
Birgitte Mollgaard ◽  
Henning Gjelstrup Kristensen ◽  
Anette Mullertz
Keyword(s):  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
In Vitro Lipolysis ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Long Chain

scholarly journals Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

2013 ◽  
Vol 63 (4) ◽  
pp. 427-445 ◽  
Author(s):  
Katja Čerpnjak ◽  
Alenka Zvonar ◽  
Mirjana Gašperlin ◽  
Franc Vrečer
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Pharmaceutical Products ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Abstract Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

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