1 Ocak 2022 Dergi makalesi Açık Erişim

Oktay, Ayse Nur; Polli, James E.

MARC21 XML

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    <subfield code="a">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) cm(2)/s and 5.76x10(-8) cm(2)/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.</subfield>
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    <subfield code="a">Oktay, Ayse Nur</subfield>
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    <subfield code="a">10.1016/j.ijpharm.2022.122015</subfield>
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    <subfield code="a">Comparison of a single pharmaceutical surfactant versus intestinal biorelevant media for etravirine dissolution: Role and impact of micelle diffusivity</subfield>
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    <subfield code="a">Polli, James E.</subfield>
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