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Effect of nonionic surfactants in release media on accelerated in-vitro release profile of sirolimus eluting stents with biodegradable polymeric coating

摘要It is a well-known fact that sirolimus (SRL) undergoes degradation process via hydrolysis in aqueous media, leading to incorrect assessment of drug amount and thus release characteristics of formulations. The main objective of the present study was to evaluate the effect of nonionic surfactants in media on in-vitro release profiles for sirolimus eluting stents (SES) coated with biodegradable polymeric matrix. Phosphate buffer and acetate buffer incorporating nonionic surfactants with varying concentrations were examined for adequate solubility and stability (by RP-HPLC). Good sink condition was achieved in phosphate buffer (at pH 4.0) with 1.0%Tween 20, 1.0%Brij 35%and 0.5%Brij 58. Hydrodynamic size (by DLS) and the micelle-water partition coefficient (P) with standard free energy of solubilization (?Gs°) of drug were evaluated to get some understanding about the solubilization phenomena. About 80%of drug release during the period of 48 h was achieved in optimized drug release media which was 1.0%Tween 20 in phosphate buffer pH 4.0. The obtained accelerated SRL release profile in optimized medium cor-related well with the real time in-vitro release in phosphate buffer (pH 7.4). Surface morphology changes (by SEM), changes in gravimetric weights and molecular weight change (by GPC) were examined before and after drug release to understand the drug release mechanism which explains that the polymer did not undergo degradation during the drug release.

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作者单位 Department of Chemistry,Veer Narmad South Gujarat University,Surat 395007,India [1] Research and Development Department,Sahajanand Medical Technologies (SMT) Pvt. Ltd.,Surat 395007,India [2]
发布时间 2018-03-20(万方平台首次上网日期,不代表论文的发表时间)
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药物分析学报(英文)

药物分析学报(英文)

2018年8卷1期

45-54页

SCIMEDLINEISTICCSCDCA

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