Pluronic F127 表面穩定化 MOF 奈米粒結合可溶性微針以提升經皮治療系統應用潛力

Abstract

經皮治療系統能有效避免肝臟的首過效應並提升患者的方便性，具有極大的優勢。然而，皮膚角質層的屏障作用大幅限制了其實際應用。為了克服此瓶頸，本研究應用以 Pluronic F127 表面穩定處理的 MIL-100(Fe) 奈米粒子，嵌入聚乙烯吡咯烷酮與羧甲基纖維素（PVP/CMC）的混合高分子基質中，開發出一款複合性溶解型微針貼片。實驗結果顯示，Pluronic F127 的表面修飾成功抑制了奈米粒子的聚集現象，並顯著提升其分散穩定性。XRD、FTIR、XPS、BET 及 TGA 等分析進一步證實了Pluronic F127表面修飾的成功。在微針製備上，含有 10 wt% PVP 與 5 wt% CMC 的高分子基質搭配針長 1000 µm 的微針幾何形狀設計，可提供微針貼片足夠的機械強度與良好的加工適性。體外豬皮測試證實該微針能有效於皮膚建立微通道。同時，體外釋放試驗也顯示微針基質能迅速溶解，並在 30 分鐘內達到約 96% 的累積藥物釋放率。總結而言，本研究成功驗證了將 Pluronic F127 包覆之 MIL-100(Fe) 結合至溶解型微針中的可行性，為奈米粒子輔助經皮治療平台提供一項具發展潛力的設計方向。

Transdermal drug delivery systems can bypass hepatic first-pass metabolism and improve patient compliance, but their applications remain limited by the stratum corneum barrier. To overcome this challenge, this study developed a composite dissolving microneedle patch by incorporating Pluronic F127-stabilized MIL-100(Fe) nanoparticles into a polyvinylpyrrolidone/carboxymethylcellulose (PVP/CMC) matrix. Pluronic F127 surface modification effectively reduced nanoparticle aggregation and enhanced dispersion stability, and this successful surface modification was supported by XRD, FTIR, XPS, BET, and TGA analyses. Microneedles prepared from 10 wt% PVP + 5 wt% CMC with a 1000 µm microneedle geometry exhibited sufficient mechanical strength and suitable processability. Ex vivo porcine skin tests confirmed effective microchannel formation, and in vitro assays revealed that the cumulative release of the model payload reached approximately 96% within 30 min. In summary, this study validates the integration of PF127-MIL-100(Fe) nanoparticles into dissolving microneedles as a promising strategy for nanoparticle-mediated transdermal drug delivery.