Ondansetron HCl Microemulsions for Transdermal Delivery: Formulation and In Vitro Skin Permeation.

Jadupati Malakar, Amit Kumar Nayak, Aalok Basu
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引用次数: 21

Abstract

Ondansetron HCl delivery through oral route suffers due to its low bioavailability due to first-pass metabolism. Therefore, the microemulsion-based transdermal delivery may be a better substitute for it. The pseudoternary phase diagrams were constructed to determine compositions of microemulsions, and ondansetron HCl microemulsions for transdermal delivery were developed using isopropyl myristate or oleic acid as the oil phase, Tween 80 as the surfactant, and isopropyl alcohol as the cosurfactant evaluated for in vitro skin permeation through excised porcine skin. The in vitro skin permeation from these formulated microemulsions was sustained over 24 hours. The microemulsion F-8 (contained 10% of isopropyl myristate as oil phase, 8% of aqueous phase, and 82% of surfactant phase containing Tween 80 and isopropyl alcohol, 3 : 1) showed the highest permeation flux of 0.284 ± 0.003 μg/cm(2)/hour. All these microemulsions followed the Korsmeyer-Peppas model (R(2) = 0.971  to  0.998) with non-Fickian, "anomalous" mechanism over a period of 24 hours.

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盐酸昂丹司琼微乳经皮给药:配方和体外皮肤渗透。
盐酸昂丹司琼口服给药由于首过代谢导致生物利用度低而受到影响。因此,微乳化基透皮给药可能是其较好的替代品。以肉豆酸异丙酯或油酸为油相,吐温80为表面活性剂,异丙醇为助表面活性剂,制备了盐酸昂丹司琼透皮微乳,并对其体外透皮性进行了评价。这些配制的微乳液的体外皮肤渗透持续超过24小时。F-8微乳液(含10%肉豆酸异丙酯为油相,8%为水相,82%为表面活性剂,Tween 80与异丙醇为3∶1)的渗透通量最高,为0.284±0.003 μg/cm(2)/h。这些微乳在24小时内均符合Korsmeyer-Peppas模型(R(2) = 0.971 ~ 0.998),具有非菲克的“异常”机制。
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