溶解
胶束
肺表面活性物质
溶解度
化学
动态光散射
苄腈
色谱法
化学工程
有机化学
水溶液
生物化学
纳米颗粒
逆转录酶
核糖核酸
工程类
基因
作者
Ayşe Nur Oktay,James E. Polli
标识
DOI:10.1016/j.ijpharm.2022.122015
摘要
Etravirine is an antiviral whose oral absorption is limited by low solubility/dissolution. The objective was to predict and compare etravirine's surfactant-mediated dissolution into polyoxyethylene-10 lauryl ether (POE) and FeSSIF-V2, including the contribution of slow micelle diffusivity. Dynamic light scattering (DLS) was used to measure the size and diffusivity values of drug-loaded micelles. In vitro intrinsic dissolution into surfactant media were predicted using a model for surfactant-mediated dissolution. Compared to maleic buffer, POE and FeSSIF-V2 increased etravirine solubility 232-fold and 8.97-fold, respectively. From DLS, micelle diffusivity of drug-loaded POE micelle and FeSSIF-V2 mixed-micelle was 5.15x10-7 cm2/s and 5.76x10-8 cm2/s, respectively. Observed and predicted dissolution enhancement into POE were 50.7 and 31.3, and 1.26 and 1.24 into FeSSIF-V2, respectively. Hence, there was high dissolution enhancement into POE, although the observed enhancement was only 21.9% of the observed solubility enhancement, reflecting the attenuating impact of the large and slowly diffusing drug-loaded POE micelles. Meanwhile, there was minimal dissolution enhancement into FeSSIF-V2, and the observed enhancement was only 14.0% of the observed solubility enhancement, reflecting the even slower diffusing drug-loaded FeSSIF-V2 mixed-micelles compared to drug-loaded POE micelles. Results are considered in light of designing a single pharmaceutical surfactant system for dissolution that mimics a FeSSIF-V2 system.
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