Preparation of tanshinone Ⅱ_(A) self-soluble microneedles and its inhibition on proliferation of human skin fibroblasts

作     者：Yanshan Zhan Xiaoqi Xu Xi Luo Ruiping Liu Yujian Lin Ping Zhao Jun Shi Yanshan Zhan;Xiaoqi Xu;Xi Luo;Ruiping Liu;Yujian Lin;Ping Zhao;Jun Shi

作者机构：School of Chinese Material MedicaGuangdong Pharmaceutical University of ChinaGuangzhou 510006China Department of Chemistry and Chemical EngineeringGuangdong Pharmaceutical University of ChinaZhongshan 528458China Engineering&Technology Research of Topical Precise Drug Delivery SystemGuangzhou Higher Education Mega CenterGuangzhou 510006China 

出 版 物：《Chinese Herbal Medicines》 (中草药（英文版）)

年 卷 期：2023年第15卷第2期

页      面：251-262页

学科分类：1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(No.82173982,2021) the Guangdong Natural Science Project(No.2018A0303130234) Excellent Young Teachers Training Project in Higher Education of Guangdong(No.YQ2015099) 

主　　题：human skin fibroblasts hypertrophic scar tanshinoneⅡ_(A) tanshinoneⅡ_(A)self-dissolving microneedles TGF-β1 

摘      要：Objective:Hypertrophic scars(HS)are a variety of skin tissue fibrosis disease that occurs in human skin,the effective therapeutic method of which is still inaccessible up to *** a bioactive constituent of a well-known medical plant,Salvia miltiorrhiza(Danshen in Chinese),tanshinone Ⅱ_(A)(TSA)is reported to inhibit cell proliferation in ***,the aim of this study was to prepare TSA self-soluble microneedles to strengthen its dermal retention and break through the difficulty of significantly thickening epidermal connective tissue and stratum corneum at the HS *** possible mechanism of action in suppressing HS was studied using human skin fibroblasts(HSF).Methods:Tanshinone Ⅱ_(A) self-dissolving microneedles(TSA-MN)was prepared using a negative mold casting *** prescription process of microneedle was optimized by Box-Behnken effect surface *** media were selected to investigate the ability of transdermal absorption and in vitro ***,according to Cell Counting Kit-8(CCK8)method as well as the Western blot method,the effect of TSA-MN on the biological characteristics of HSF was ***:With remarkable slow release effect and dermal retention,the release and transdermal properties of TSA-MN in vitro were better than both TSA and ordinary dosage *** effect of HSF confirmed the essential decrease in cell motility during cell proliferation and cell migration in vitro,which plays a significant role in down-regulating the secretion of transforming growth factor-β1(TGF-β1)in HSF and increasing the expression level of ***:The prepared TSA self-soluble microneedles is helpful in solving the problem of hypertrophic scars,with a stable dermal retention effect after process optimization.