具有主动靶向作用的纳米制剂的构建及体外药效学探讨  

Construction of a nanoformulation with active targeting and preliminary study on its in vitro pharmacodynamics

作　　者：刘淼[1] 彭颖 周星辰 LIU Miao;PENG Ying;ZHOU Xingchen(Department of Pharmacy,Hunan Cancer Hospital,Hunan Province,Changsha410011,China;Xiangya School of Pharmaceutical Sciences,Central South University,Hunan Province,Changsha410013,China;Department of Pharmacy,Xiangya Hospital,Central South University,Hunan Province,Changsha410008,China)

机构地区：[1]湖南省肿瘤医院药学部,湖南长沙410011 [2]中南大学湘雅药学院,湖南长沙410013 [3]中南大学湘雅医院药学部,湖南长沙410008

出　　处：《中国医药导报》2023年第1期4-8,共5页China Medical Herald

基　　金：湖南省自然科学基金科卫联合基金项目(2020JJ8091);国家自然科学基金资助项目(81903222)。

摘　　要：目的 构建一种载有多柔比星(DOX)并具有主动靶向性的纳米制剂。方法 用聚乳酸-羟基乙酸共聚物(PLGA)、DOX、多巴胺(DA)、氨基修饰聚乙二醇叶酸(NH2-PEG-FA)制备PLGA/DOX@PDA-PEG-FA纳米制剂,通过粒径、电位、载药量、包封率、药物释放特性对其表征,并使用荧光倒置显微镜及噻唑蓝(MTT)比色法对细胞摄取、生物相容性、细胞毒性等进行初步。结果 本研究成功制备了PLGA/DOX@PDA-PEG-FA纳米制剂,其具有明显的核壳结构,粒径约120 nm,壳层厚度约18 nm,ζ电位-18.1 m V,包封率和载药量分别为43.56%和1.86%,且具有明显缓释特性。MTT法表明载体材料生物相容性好,且细胞毒性呈剂量依赖性。结论 本研究所制备的纳米制剂具有较好的生物相容性、体外抗肿瘤作用,为PLGA广泛应用及有效降低化疗药物不良反应提供了新思路。Objective To construct an active targeting nanoformulation loaded with the chemotherapeutic Doxorubicin(DOX).Methods PLGA/DOX@PDA-PEG-FA nanoformulations were prepared by using polylactic acid-glycolic acid copolymer(PLGA),DOX,dopamine(DA),amino-modified polyethylene glycol folic acid(NH2-PEG-FA).Particle size,potential,drug loading,encapsulation efficiency,drug release characteristics were characterized,and cell uptake,biocompatibility,cytotoxicity were preliminarily discussed by fluorescence inverted microscope and thiazolyl blue(MTT)colorimetry.Results In this study,PLGA/DOX@PDA-PEG-FA nano-formulations were successfully prepared,which had an obvious core-shell structure with a particle size of about 120 nm,a shell thickness of about 18 nm,and ζ potential of-18.1 m V.The encapsulation efficiency and drug loading were 43.56% and 1.86%,respectively,and it had obvious sustained-release properties.MTT assay showed that the carrier material had good biocompatibility and the cytotoxicity was dose-dependent.Conclusion The nanocomposite prepared in this experiment has good biocompatibility and anti-tumor effect in vitro.The preparation provides a new idea for the wide application of PLGA and the effective reduction of adverse reactions of chemotherapy drugs.

关 键 词：纳米制剂 生物相容性 主动靶向性 体外抗肿瘤作用 

分 类 号：R96[医药卫生—药理学]