去氢骆驼蓬碱聚乳酸纳米粒的制备及其药动学行为

目的制备去氢骆驼蓬碱聚乳酸纳米粒,并研究其药动学行为。方法制备纳米粒后,测定其粒径、PDI、Zeta电位、包封率、载药量、累积释放度。然后,绘制血药浓度-时间曲线,计算药动学参数。结果纳米粒平均粒径(195.38±2.02)nm,PDI 0.131±0.034,Zeta电位(-19.48±0.36)mV,包封率(76.37±1.08)%,载药量(8.81±0.25)%,24 h内累积释放度82.17%,释药过程符合Weibull模型(r=0.985 7)。与去氢骆驼蓬碱比较,纳米粒Tmax、Cmax、AUC0~t、AUC0~∞显著升高(P<0.05,P<0.01)。结论聚乳酸纳米粒可促进去氢骆驼蓬碱体内吸收,提高其口服生物利用度,并具有明显的缓释作用。

Preparation of harmine-loaded polylactic acid nanoparticles and their pharmacokinetic behaviors

AIM To prepare harmine-loaded polylactic acid nanoparticles and to study their pharmacokinetic behaviors.METHODS For the prepared nanoparticles, their particle size, PDI, Zeta potential, encapsulation efficiency, drug loading and accumulative release rate were determined. Subsequently, plasma concentration-time curve was drawn, followed by the calculation of pharmacokinetic parameters.RESULTS The nanoparticles shared average particle size of(195.38±2.02) nm, PDI of 0.131±0.034, Zeta potential of(-19.48±0.36) mV, encapsulation efficiency of(76.37±1.08)%, drug loading of(8.81±0.25)%, and accumulative release rate within 24 h of 82.17%, the drug release process accorded with Weibull model(r=0.985 7). the nanoparticles’ Tmax, Cmax, AUC0~t and AUC0~∞ were significantly increased(P<0.05,P<0.01).CONCLUSION Polylactic acid nanoparticles, with an obvious sustained-release effect, can promote the in vivo absorption of harmine and enhance the oral bioavailability.