Literature DB >> 14727890

Solubilization of cyclosporin A.

Y Ran1, L Zhao, Q Xu, S H Yalkowsky.   

Abstract

This study investigated the solubilization of cyclosporin A (CsA), a neutral undecapeptide, by cosolvency, micellization, and complexation. Cosolvents (ethanol, propylene glycol, polyethylene glycol, tetrahydrofurfuryl alcohol polyethyleneglycol ether, and glycerin), surfactants (polyoxyethylene sorbitan monooleate [(Tween 80)], polyoxyethylene sorbitan monolaurate [(Tween 20)], and Cremophor EL), and cyclodextrins (alpha-cyclodextrin [(alphaCD)] and hydroxypropyl-beta-cyclodextrin[(HPbetaCD)] were used as solubilizing agents in this study. Surfactants had a noticeable effect in increasing CsA solubility. Twenty percent solutions of Tween 20, Tween 80, and Cremophor EL increased the solubility by 60 to 160 fold. Cyclodextrins can increase the CsA solubility, but alphaCD was more effective than HPbetaCD. Cosolvents on the other hand did not increase the solubility of CsA as much as expected from the LOGP (logarithm of water-octanol partition coefficient) value of CsA.

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Year:  2001        PMID： 14727890      PMCID： PMC2750256          DOI： 10.1208/pt020102

Source DB:  PubMed          Journal:  AAPS PharmSciTech        ISSN： 1530-9932            Impact factor:   3.246


  10 in total

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Review 3.  Pharmaceutical applications of cyclodextrins. 1. Drug solubilization and stabilization.

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Journal:  J Med Chem       Date:  1993-11-26       Impact factor: 7.446

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Journal:  J Pharm Sci       Date:  1985-04       Impact factor: 3.534

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Authors:  K A Connors; J A Mollica
Journal:  J Pharm Sci       Date:  1966-08       Impact factor: 3.534

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Journal:  Biochem Pharmacol       Date:  1990-07-01       Impact factor: 5.858

8.  Solubilization of fluasterone.

Authors:  L Zhao; P Li; S H Yalkowsky
Journal:  J Pharm Sci       Date:  1999-10       Impact factor: 3.534

9.  Characterization and administration of cyclosporine liposomes as a small-particle aerosol.

Authors:  B E Gilbert; S Z Wilson; N M Garcon; P R Wyde; V Knight
Journal:  Transplantation       Date:  1993-10       Impact factor: 4.939

Review 10.  Cyclosporin clinical pharmacokinetics.

Authors:  A Fahr
Journal:  Clin Pharmacokinet       Date:  1993-06       Impact factor: 6.447
  10 in total
  10 in total

1.  1H and 13C-NMR and molecular dynamics studies of cyclosporin a interacting with magnesium(II) or cerium(III) in acetonitrile. Conformational changes and cis-trans conversion of peptide bonds.

Authors:  Francesca Bernardi; Elena Gaggelli; Elena Molteni; Elena Porciatti; Daniela Valensin; Gianni Valensin
Journal:  Biophys J       Date:  2005-11-18       Impact factor: 4.033

2.  The BioGIT System: a Valuable In Vitro Tool to Assess the Impact of Dose and Formulation on Early Exposure to Low Solubility Drugs After Oral Administration.

Authors:  Alexandros Kourentas; Maria Vertzoni; Vicky Barmpatsalou; Patrick Augustijns; Stefania Beato; James Butler; Rene Holm; Neils Ouwerkerk; Joerg Rosenberg; Tomokazu Tajiri; Christer Tannergren; Mira Symillides; Christos Reppas
Journal:  AAPS J       Date:  2018-05-24       Impact factor: 4.009

3.  Improving cyclodextrin complexation of a new antihepatitis drug with glacial acetic acid.

Authors:  Jennifer L H Johnson; Yan He; Akash Jain; Samuel H Yalkowsky
Journal:  AAPS PharmSciTech       Date:  2017-03-08       Impact factor: 3.246

4.  Impact of Micellar Surfactant on Supersaturation and Insight into Solubilization Mechanisms in Supersaturated Solutions of Atazanavir.

Authors:  Anura S Indulkar; Huaping Mo; Yi Gao; Shweta A Raina; Geoff G Z Zhang; Lynne S Taylor
Journal:  Pharm Res       Date:  2017-03-28       Impact factor: 4.200

5.  Solubility enhancement of Cox-2 inhibitors using various solvent systems.

Authors:  N Seedher; S Bhatia
Journal:  AAPS PharmSciTech       Date:  2003       Impact factor: 3.246

6.  Comparison of 0.05% cyclosporine and 3% diquafosol solution for dry eye patients: a randomized, blinded, multicenter clinical trial.

Authors:  Chang Hyun Park; Hyung Keun Lee; Mee Kum Kim; Eun Chul Kim; Jae Yong Kim; Tae-Im Kim; Hong Kyun Kim; Jong Suk Song; Kyung Chul Yoon; Do Hyung Lee; Tae-Young Chung; Chul Young Choi; Hyun Seung Kim
Journal:  BMC Ophthalmol       Date:  2019-06-17       Impact factor: 2.209

7.  Nano-Delivery of a Novel Inhibitor of Polynucleotide Kinase/Phosphatase (PNKP) for Targeted Sensitization of Colorectal Cancer to Radiation-Induced DNA Damage.

Authors:  Sams M A Sadat; Melinda Wuest; Igor M Paiva; Sirazum Munira; Nasim Sarrami; Forughalsadat Sanaee; Xiaoyan Yang; Marco Paladino; Ziyad Binkhathlan; Feridoun Karimi-Busheri; Gary R Martin; Frank R Jirik; David Murray; Armin M Gamper; Dennis G Hall; Michael Weinfeld; Afsaneh Lavasanifar
Journal:  Front Oncol       Date:  2021-12-23       Impact factor: 6.244

8.  Novel poly(L-lactide-co-ε-caprolactone) matrices obtained with the use of Zr[Acac]₄ as nontoxic initiator for long-term release of immunosuppressive drugs.

Authors:  Katarzyna Jelonek; Janusz Kasperczyk; Suming Li; Piotr Dobrzynski; Henryk Janeczek; Bozena Jarzabek
Journal:  Biomed Res Int       Date:  2013-10-28       Impact factor: 3.411

Review 9.  Oral cyclosporine A--the current picture of its liposomal and other delivery systems.

Authors:  Aleksander Czogalla
Journal:  Cell Mol Biol Lett       Date:  2008-11-12       Impact factor: 5.787

10.  Efficacy of Topical Cyclosporine Nanoemulsion 0.05% Compared with Topical Cyclosporine Emulsion 0.05% and Diquafosol 3% in Dry Eye.

Authors:  Chang Hyun Park; Mee Kum Kim; Eun Chul Kim; Jae Yong Kim; Tae Im Kim; Hong Kyun Kim; Jong Suk Song; Kyung Chul Yoon; Do Hyung Lee; Hyung Keun Lee; Tae Young Chung; Chul Young Choi; Hyun Seung Kim
Journal:  Korean J Ophthalmol       Date:  2019-08
  10 in total

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