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

发布时间：2018-08-18 12:10

【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。
[Abstract]:Objective the biological half-life of local anesthetics in vivo is short and the high concentration of local tissue is easy to cause the central nervous and cardiovascular toxicity of drugs absorbed into blood by blood vessel. In this paper, the preparation of ropivacaine lactate glycolic acid copolymer nanoparticles, the optimization of the process, and the in vitro properties of ropivacaine were studied. Methods PLGA nanoparticles loaded with ropivacaine (RVC) were prepared by O / W emulsifying solvent volatilization method with (PLGA) as the carrier. The particle size, encapsulation efficiency and drug loading capacity of the nanoparticles were investigated. The preparation process was optimized by star design-effect surface method and the release in vitro was studied. Results the ropivacaine lactate glycolic acid copolymer nanoparticles (RVC-PLGA-NPS) prepared by optimized formulation were smooth and round in appearance. The average particle size was (331.21 卤2.11) nm, the drug loading capacity and the entrapment efficiency were (13.81 卤1.35) and (74.82 卤2.53), respectively. In vitro drug release studies showed that the cumulative drug release rate in 96 h was 73%, and the release curve was in accordance with Higuchi equation. Conclusion the emulsified solvent volatilization method is suitable for the preparation of RVC-PLGA-NPS.
【作者单位】：南京军区福州总医院麻醉科;南京军区福州总医院药学科;
【基金】：福建省科技计划项目(2012Y0054)
【分类号】：R943

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