滨蒿内酯PLGA微球的制备、表征及体外释药研究  

Preparation, Characterization and in Vitro Release of Scoparone PLGA Microspheres

作　　者：孟梦 王浩 谢芹芹 刘家佳 徐维平 MENG Meng;WANG Hao;XIE Qinqin;LIU Jiajia;XU Weiping(School of Pharmacy,Anhui University of Traditional Chinese Medicine,Hefei 230012,China;Institute of Geriatrics,The First Affiliated Hospital of University of Science and Technology of China(Anhui Provincial Hospital),Hefei 230001,China;Ophthalmology Department,The First Affiliated Hospital of University of Science and Technology of China(Anhui Provincial Hospital),Hefei 230001,China;Key Laboratory of Tumor Immunology and Nutritional Therapy of Anhui Province,Hefei 230001,China)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]中国科学技术大学附属第一医院(安徽省立医院)老年病研究所,合肥230001 [3]中国科学技术大学附属第一医院(安徽省立医院)眼科,合肥230001 [4]肿瘤免疫与营养治疗安徽省重点实验室,合肥230001

出　　处：《中国药学杂志》2024年第20期1948-1955,共8页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金项目资助(52072360)。

摘　　要：目的 制备滨蒿内酯聚乳酸-羟基乙酸共聚物(PLGA)微球并优化其工艺,进行表征。方法 采用水包油(O/W)乳化溶剂挥发法制备滨蒿内酯PLGA微球,以微球表面形态、包封率、载药量为主要评价指标。在单因素试验基础上,通过星点设计优化处方,得到滨蒿内酯PLGA微球最佳制备条件,对所制备的微球进行表征分析。结果 滨蒿内酯PLGA微球呈淡黄色粉末状,球形表面光滑圆整,平均粒径为2.94μm。以无定形状态负载在PLGA微球中,载药量为4.28%,包封率为47.03%。结论 成功制得滨蒿内酯PLGA微球,粒径大小符合眼玻璃体腔注射要求,在模拟体外环境下,具有良好的缓释性能。该制备方法准确可靠,可为糖尿病视网膜病变的治疗提供新剂型。OBJECTIVE To prepare and characterize scoprone-loaded PLGA microspheres.METHODS Scoprone-loaded PLGA microspheres were constructed by a O/W emulsion-solvent evaporation method.Their surface morphology,encapsulation rate and drug loading of microspheres were the main evaluation indexes.Based on single factor experiment,the optimum preparation conditions of PLGA microspheres were obtained through central composite design.RESULTS Scoprone-loaded PLGA microspheres were light yellow powder and spherical in shape with smooth surface with size 2.94μm.Scoprone was loaded into PLGA microspheres with drug loading(4.28%)and encapsulation efficiency(47.03%).CONCLUSION Scoprone-loaded PLGA microspheres are constructed successfully.The particle size of microspheres meets the requirements of intraocular vitreous cavity injection,and has good slow-release performance under simulated in vitro environment.The preparation method is accurate and reliable,and can provide a new dosage form for the treatment of diabetic retinopathy.

关 键 词：滨蒿内酯 缓释微球 乳化溶剂挥发法 聚乳酸-羟基乙酸共聚物 星点设计-响应面优化法 

分 类 号：R944[医药卫生—药剂学]