罗哌卡因乳酸羟基乙酸共聚物纳米粒的制备及体外释药研究  

Study on preparation and in vitro release of poly( lactide-co-glycolide) nanoparticle loaded with ropivacaine

作　　者：杨建藤 陈国忠[1] 黄爱文[2] 宋洪涛[2] 王丽萍[1] 

机构地区：[1]南京军区福州总医院麻醉科,福州医学硕士350025 [2]南京军区福州总医院药学科,福州350025

出　　处：《医学研究生学报》2015年第4期411-415,共5页Journal of Medical Postgraduates

基　　金：福建省科技计划项目(2012Y0054)

摘　　要：目的局部麻醉药体内生物半衰期短,且局部组织的高浓度极易造成药物经血管吸收入血产生中枢神经和心血管毒性反应。文中旨在制备罗哌卡因乳酸羟基乙酸共聚物纳米粒,优化工艺,并对其体外性质进行研究。方法以乳酸羟基乙酸共聚物(PLGA)为载体,采用O/W乳化溶剂挥发法制备包载罗哌卡因(RVC)的PLGA纳米粒,以纳米粒的粒径、包封率及载药量为考察指标,采用星点设计-效应面法优化制备工艺,进行体外释放研究。结果以优化处方制备的罗哌卡因乳酸羟基乙酸共聚物纳米粒(RVC-PLGA-NPS),外观光滑圆整,平均粒径为(331.21±2.11)nm,载药量、包封率分别为(13.81±1.35)%、(74.82±2.53)%。体外释药研究表示,96 h累积释药率达73%,释放曲线符合Higuchi方程。结论乳化溶剂挥发法适用于RVC-PLGA-NPS的制备,制得的纳米粒形态圆整,在体外具有明显的缓释行为。Objective The biological half-life in vivo of local anesthesia is short, high concentration in local tissue is in-clined to cause central nerve and cardiovascular toxicity due to the drug absorption into blood by blood vessels.The research was to pre-pare the poly （ lactide-co-glycolide） nanoparticle loaded with ropivacaine （ RVC-PLGA-NPS） , optimize its process, and determine its characteristics in vitro. Methods An oil-in-water emulsion solvent evaporation technique was adopted to prepare the RVC-PLGA-NPS.The formulation was optimized by central composite design/response surface method（CCD-RSM）, with the encapsulation effi-ciency（ EE） , drug loading（ DL） and particle size as the indexes.Research was also made on itsin vitro release by fitting different model equations. Results The acquired nanoparticals were smooth, with the mean particle size （331.21＆#177;2.11） nm, DL （13.81＆#177;1.35）%and EE （74.82＆#177;2.53）%.The accumulative release rate of the nanoparticals was about 73%in 96 h, which showed that Higuchi func-tion fitted the release curve. Conclusion The RVC-PLGA-NPS made by emulsion solvent evaporation technique have obvious drug-release behaviour in vitro.

关 键 词：罗哌卡因 纳米粒 乳酸羟基乙酸共聚物 星点设计-效应面法 体外释放 

分 类 号：R971.2[医药卫生—药品]