聚乙丙交酯微球的制备及对曲安奈德的包载与释放研究  

Preparation of poly(lactic-co-glycolic acid)microsphere and its behaviors of encapsulation and release of triamcinolone acetonide

作　　者：袁文博 张华彤 乔从德[2] 王领[2] 栾明明 杨效登[2] Wenbo Yuan;Huatong Zhang;Congde Qiao;Ling Wang;Mingming Luan;Xiaodeng Yang(Engineering Technology Center,Shandong Guyuchun Biotechnology Co.,Ltd.,Jinan,Shandong 250098,China;Shandong Key Laboratory of Molecular Engineering,Qilu University of Technology,Shandong Academy of Sciences,Jinan,Shandong 250353,China)

机构地区：[1]山东谷雨春生物科技有限公司工程技术中心,山东济南250098 [2]齐鲁工业大学(山东省科学院)山东省轻工助剂重点实验室,山东济南250353

出　　处：《日用化学工业（中英文）》2023年第11期1266-1272,共7页China Surfactant Detergent & Cosmetics

基　　金：国家自然科学基金青年基金(21904074);山东省重点研发(2019JZZY011118);齐鲁工业大学(山东省科学院)重大创新专项(2022JBZ02-04)。

摘　　要：曲安奈德具有药性好、药效强、作用时间持久的优点,但是,油溶性使其应用不方便。聚乙丙交酯(Poly(lacticco-glycolic acid),PLGA)具有优良的生物相容性和生物降解性,可做成微球负载曲安奈德。本文以三氟甲磺酸为催化剂、葡萄糖为引发剂制备了聚乙丙交酯,并以核磁共振波谱和凝胶色谱法表征了聚乙丙交酯的分子结构、分子量和分子量分布。结果显示,所得聚乙丙交酯中乳酸和乙醇酸链段的质量比为50∶50,羧基封端,分子量介于36000~41000,分子量分布窄,分散性指数约为1.60。以高压静电喷雾法制得粒径小于20μm(d_(20)≥92%)的微球,该微球对曲安奈德亲脂性药物的载药量大于44%,能实现长达120 h的释放周期,而且在药物释放前期释放速率和时间呈现线性关系。文章为PLGA载药微球的制备和拓展曲安奈德在过敏性皮炎、神经性皮炎和慢性湿疹等皮肤疾病治疗提供基础数据,为功能性护肤品的开发提供参考。Triamcinolone acetonide has the advantages of strong medical efficacy and long duration,however,its oil solubility limits its application.Poly(lactic-co-glycolic acid)(PLGA)has excellent biocompatibility and biodegradability,which can be made into microspheres loaded with triamcinolone acetonide.In this work,the PLGA was prepared using trifluoromethanesulfonic acid as catalyst and glucose as initiator.The molecular structure,molecular weight and molecular weight distribution of PLGA were characterized by NMR and gel chromatography.The results showed that the mass ratio of lactic acid to glycolic acid segments in PLGA was 50∶50,and the molecules were terminated with carboxyl groups,and the molecular weight was between 36000 and 41000,exhibiting narrow molecular weight distribution(molecular weight distribution index was ca.1.60).The microspheres were made by electrostatic spraying method,whose particle size was less than 20μm(the content of microspheres of diameter being smaller than 20μm was more than 92%).The drug loading efficiency for triamcinolone acetonide was more than 44%,and the period of release was up to 120 h.In the initial stage of drug release,the relationship between drug release rate and time was linear.This work could provide basic data for the preparation of PLGA microspheres for drug-loading and expand the application of triamcinolone acetonide in the treatment of allergic dermatitis,neurodermatitis and chronic eczema.Moreover,this work could provide reference for the development of functional skin care products.

关 键 词：曲安奈德 聚乙丙交酯 微球 载药 

分 类 号：TQ658[化学工程—精细化工]