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用于增强经毛囊递送的含L.提取物复合物的可溶微针的制备与表征

Fabrication and Characterization of Dissolving Microneedles Containing L. Extract Complex for Enhancement of Transfollicular Delivery.

作者信息

Chaiwarit Tanpong, Chanabodeechalermrung Baramee, Jantrawut Pensak, Ruksiriwanich Warintorn, Sainakham Mathukorn

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.

Center of Excellence in Materials Science and Technology, Chiang Mai University, Chiang Mai 50200, Thailand.

出版信息

Polymers (Basel). 2024 Aug 22;16(16):2377. doi: 10.3390/polym16162377.

Abstract

Dissolving microneedles are extensively applied in drug delivery systems to enhance penetration into the skin. In this study, dissolving microneedles fabricated from polyvinylpyrrolidone K90 (PVP-K90) and hydroxypropylmethyl cellulose (HPMC) E50 in different ratios were characterized. The selected formulations incorporated L. extract complex and its characteristics, transfollicular penetration, and safety were observed. The microneedles, fabricated from PVP K90: HPMC E50 in a ratio of 25:5 (P25H5) and 20:10 (P20H10), revealed excellent morphological structure, proper mechanical strength, and excellent skin insertion. P25H5 microneedles exhibited faster dissolution than P20H10 microneedles. Microneedles containing L. extract complex showed excellent morphological structure via scanning electron microscopy but decreased mechanical strength. P25H5-O, which exhibited an effective ability to enter skin, was selected for further investigation. This microneedle formulation had a high percentage of drug-loading content, enhanced skin penetration via the transfollicular route, and was safe for keratinocytes. As a result, the dissolving microneedle containing L. extract complex can be used to enhance transfollicular delivery through the skin with safety.

摘要

溶蚀性微针在药物递送系统中被广泛应用,以增强药物对皮肤的渗透。在本研究中,对由不同比例的聚乙烯吡咯烷酮K90(PVP-K90)和羟丙基甲基纤维素(HPMC)E50制备的溶蚀性微针进行了表征。观察了所选配方中掺入的L.提取物复合物及其特性、经毛囊渗透和安全性。由PVP K90与HPMC E50比例为25:5(P25H5)和20:10(P20H10)制成的微针,显示出优异的形态结构、适当的机械强度和良好的皮肤插入性能。P25H5微针的溶解速度比P20H10微针更快。含有L.提取物复合物的微针通过扫描电子显微镜显示出优异的形态结构,但机械强度有所下降。具有有效皮肤进入能力的P25H5-O被选用于进一步研究。这种微针制剂具有高载药量百分比,通过经毛囊途径增强了皮肤渗透,并且对角质形成细胞是安全的。因此,含有L.提取物复合物的溶蚀性微针可用于安全地增强经皮肤的经毛囊递送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c05e/11359393/9a4590d12e09/polymers-16-02377-g001.jpg

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