Resveratrol-Loaded Dissolving Microneedles: Fabrication and in vitro Evaluation

Banghuai Xing, Kathy Qian Luo, Tiantian Gan, Yi Jin, Jianfang Feng, Meng Cheng, Liangxing Tu
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Abstract

Abstract Resveratrol (Res), an active ingredient derived from a multitude of plants, exhibits multiple pharmacological activities. However, its poor water solubility and low bioavailability present significant challenges to its clinical application. Our study aimed to improve the transdermal absorption of Res using dissolving microneedle (MN) technology, which could effectively overcome the stratum corneum barrier. Res-loaded dissolving microneedles (Res-MNs) were fabricated using polyvinyl pyrrolidone K90 (PVP K90) as the matrix material, and a two-step casting procedure was employed. The process was optimized using the Box–Behnken experimental design approach. The characteristics of Res-MNs in vitro, including morphology, solubility, safety evaluation, and skin permeation, were studied. The results showed that the optimum preparation conditions of Res-MNs were a centrifugation time of 10 minutes, a solvent concentration of 25%, and a prescription ratio (Res: matrix) of 0.375. The skin permeability of the Res-MNs was enhanced compared with Res suspension and Res gel. The cumulative release of Res-MNs in vitro was 75%, which was approximately 5 and 3 times that of the Res suspension group and Res gel group. These results suggest that dissolving MNs may represent a potential approach for enhancing the transdermal delivery of poorly absorbed drugs such as Res.
白藜芦醇微针的制备及体外评价
摘要白藜芦醇(Resveratrol, Res)是一种从多种植物中提取的活性成分,具有多种药理活性。然而,其水溶性差,生物利用度低,给其临床应用带来了重大挑战。我们的研究旨在利用溶解微针(MN)技术提高Res的透皮吸收,该技术可以有效地克服角质层屏障。以聚乙烯吡咯烷酮K90 (PVP K90)为基体材料,采用两步铸造工艺制备了负载稀土的溶解微针(Res-MNs)。采用Box-Behnken实验设计方法对工艺进行优化。研究了Res-MNs的体外形态、溶解度、安全性评价和透皮性等特性。结果表明,Res- mns的最佳制备条件为:离心时间10 min,溶剂浓度25%,处方比(Res: matrix) 0.375。与Res悬浮液和Res凝胶相比,Res- mns的皮肤渗透性增强。Res- mns体外累积释放量为75%,约为Res悬液组和Res凝胶组的5倍和3倍。这些结果表明,溶解MNs可能是一种潜在的方法,可以增强诸如Res等吸收不良药物的透皮递送。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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