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目的制备供口服给药的美洲大蠊提取物(CII-3)纳米粒,研究CII-3纳米粒的体外释放以及纳米粒对所包载的CII-3的体外保护作用。方法采用复乳/溶媒蒸发法制备CII-3纳米粒,以人工胃肠液及p H 7.4的磷酸盐缓冲液(PBS)为释放介质,采用福林酚法测定CII-3纳米粒的体外释药特征,并对纳米粒的体外释药行为进行方程拟合,找到最佳释放模型;采用茚三酮显色法分别测定CII-3和CII-3纳米粒在p H 1.2人工胃液中不同时间点的氨基酸释放量,并对二者的降解速率进行对比,观察将CII-3包载入纳米粒后是否对CII-3有保护作用。结果制得的CII-3纳米粒平均粒径为(109.9±0.6)nm,Zeta电位为(-37.5±3.5)m V。CII-3纳米粒前2 h在人工胃液中的累积释放率(Qt)为(22.63±1.17)%,此后在人工肠液中释放,60 h的Qt为(72.35±1.90)%,符合Higuchi释放模型,方程为Qt=8.287 2 t1/2+7.758 6。CII-3纳米粒在p H 7.4的PBS中10 d的Qt为(72.67±1.65)%,符合Weibull分布模型,方程为lnln[1/(1-Qt)]=0.403 7 ln(t-0.411 9)-1.713 3。CII-3在人工胃液中4 h基本全部降解,而包载入纳米粒后约70%CII-3在人工胃液中被降解。结论 CII-3纳米粒具有良好的缓释性,体外释放平稳。纳米粒中的CII-3在人工胃液中的稳定性提高。
OBJECTIVE To prepare CII-3 nanoparticles for oral administration and to study the in vitro release of CII-3 nanoparticles and the in vitro protective effect of nanoparticles on the encapsulated CII-3. Methods CII-3 nanoparticles were prepared by double emulsion / solvent evaporation method. The release of CII-3 nanoparticles by artificial intestinal medicine and p H 7.4 phosphate buffer (PBS) Drug characteristics and in vitro release behavior of nanoparticles were fitted to find the best release model; ninhydrin colorimetric determination of CII-3 and CII-3 nanoparticles in p H 1.2 artificial gastric juice in different time Point amino acid release, and the degradation rate of the two were compared to observe the CII-3 package into the nanoparticles whether CII-3 has a protective effect. Results The average diameter of CII-3 nanoparticles was (109.9 ± 0.6) nm and the Zeta potential was (-37.5 ± 3.5) mV. The cumulative release rate (Qt) of CII-3 nanoparticles in artificial gastric juice was (22.63 ± 1.17)% 2 h before releasing in artificial intestinal juice and the Qt was (72.35 ± 1.90)% at 60 h, which accorded with Higuchi release model , The equation is Qt = 8.287 2 t1 / 2 + 7.758 6. The Qt of CII-3 nanoparticles at 10 d in p H 7.4 was (72.67 ± 1.65)%, which was in accordance with the Weibull distribution model with the equation of lnln [1 / (1-Qt)] = 0.403 7 ln ) -1.713 3. CII-3 was almost completely degraded in artificial gastric juice for 4 h, while about 70% of CII-3 was degraded in artificial gastric juice after it was loaded into the nanoparticle. Conclusion CII-3 nanoparticles have a good sustained release, stable release in vitro. The stability of CII-3 in artificial gastric juice in the nanoparticle is improved.