番茄红素固体纳米胶束的质量评价及药动学研究

Preliminary quality evaluation and pharmacokinetics research of lycopene solid nano micelle

目的评价番茄红素固体纳米胶束(以下简称胶束)的质量,并研究其在大鼠体内的药动学行为。方法考察胶束的微观结构、粒径及分布、平均载药量、包封率、人工胃液或人工肠液中的释放特性。比较番茄红素油溶液(LPO)与胶束在大鼠体内的药动学特征。结果胶束遇水分散后形成的胶束粒径及分布都较均匀,平均载药量为1.401%±0.008%,包封率为90.26%±0.87%;在人工胃液中释放的程度较低,而在人工肠液中表现为持续释放。灌胃给予大鼠胶束和LPO后,以LPO为参比,胶束的相对生物利用度为183.48%。结论将番茄红素制成胶束后,其口服生物利用度得到了一定程度的提高,改善了番茄红素因溶解度低,生物利用度低下的问题,为胶束的开发提供了参考。

OBJECTIVE To investigate the quality of the lycopene solid nano micelle(LPSNM),and to study its pharmacokinetic profile in rats.METHODS The microstructure,particle size,distribution,the average drug load,encapsulation efficiency,and the release characteristics in simulated gastric fluid or simulated intestinal fluid of LPSNM were investigated.The pharmacokinetic profile of lycopene oil solution(LPO)and LPSNM in rats were compared.RESULTS The particle size and distribution of the micelle formed by dispersing the LPSNM in water were uniform.The average drug loading amount was 1.401%±0.008%,and the encapsulation efficiency was 90.26%±0.87%.In-vitro release test showed that the release rate of lycopene from LPSNM was low in the simulated gastric fluid but was relatively high and continuous release in simulated intestinal fluid.After oral administration of LPSNM and LPO,taking LPO as a reference,the relative bioavailability of LPSNM was 183.48%.CONCLUSION After the lycopene was prepared as LPSNM,the solubility of lycopene was effectively improved,and the oral bioavailability was also improved to a certain degree.This study provides a reference for further clinical development of LPSNM.