姜黄色素聚电解质纳米粒大鼠体内药动学研究
Pharmacokinetics of Curcuminoids-loaded Polyelectrolyte Nanoparticles in Rats
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摘要: 目的 研究姜黄色素聚电解质纳米粒(CUR-PENPs)经大鼠尾静脉注射后的体内药代动力学。方法 通过静电吸附法制备CUR-PENPs并对其表征;以姜黄色素(CUR)溶液为对照,研究大鼠尾静脉注射CUR-PENPs的体内药动学。结果 透射电镜观察CUR-PENPs呈较规则类球体,平均粒径为(243.0±1.1)nm,Zeta电位为(-28.13±1.41)mV,载药量为5.5%。大鼠尾静脉注射CUR-PENPs的血药浓度-时间曲线下面积(AUC)为CUR溶液3.3倍,血浆清除率(CL)降为CUR溶液的27.8%。结论 CUR-PENPs能相对延长CUR体内滞留时间,提高药物AUC。Abstract: OBJECTIVE To investigate the pharmacokinetical process of curcuminoids-loaded polyelectrolyte nanoparticles (CUR-PENPs) by i.v. administration in rats. METHODS CUR-PENPs were prepared and characterized. The rats were administrated through tail vein with curcuminoids (CUR) solution and CUR-PENPs. RESULTS CUR-PENPs were quasi-spherical shapes observed by TEM. The mean particle size, Zeta potential and drug loading were (243.0 ± 1.1)nm, (-28.13 ± 1.41)mV and 5.5%, respectively. After i.v. administration the area under concentration-time curve (AUC) of CUR-PENPs were 3.30-fold higher than those of CUR solution, the clearance (CL) of CUR-PENPs were 27.8% that of CUR solution. CONCLUSION The results indicate that CUR-PENPs may extend the retention time of CUR and improve the AUC when compared with CUR solution.
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Key words:
- polyelectrolyte nanoparticles /
- curcuminoids /
- pharmacokinetics
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