姜黄素HS15/Tween-80混合胶束口服给药生物利用度的研究

Enhancement of oral bioavailability of curcumin-loaded HS15/Tween-80 mixed micelles

目的制备一种HS15/Tween-80混合胶束,提高姜黄素的口服生物利用度。方法采用薄膜水化法制备姜黄素混合胶束;采用动态光散射法测定胶束粒径大小、Zeta电位、载药量和包封率;考察混合胶束中药物的体外稳定性及其释药行为;通过大鼠灌胃给药的方式考察姜黄素混悬液和姜黄素混合胶束的口服生物利用度。结果姜黄素混合胶束平均粒径大小为13nm,Zeta电位为–20mV;姜黄素混合胶束载药量为4.4%,其包封率大于95%,姜黄素混合胶束体外稳定性好,体外药物释放结果显示其具有一定的缓释效果;姜黄素混悬液和混合胶束100mg/kg,灌胃给药30min之后,姜黄素混合胶束给药组大鼠血药浓度水平显著高于姜黄素混悬液给药组(P<0.05),药物生物利用度提高至原来的1.7倍。结论姜黄素混合胶束可以有效地提高姜黄素的稳定性和生物利用度。

Objective To investigate tile enhancement of oral bioavailability of curcumin-loaded HS15/Tween-80 mixed micelles. Methods Curcumin-loaded mixed micelles were developed by a filming-rehydration method, and then characterized by a DLS for their particles size and Zeta potential. In vitro release study and stability test were also examined. The oral bioavailability study of curcumin and curcumin-loaded mixed micelles were performed after the oral administration. Results Curcumin-loaded mixed micelles had mean diameter of 13 nm and Zeta potential of-20 mV The stability of curcumin was improved after entrapped into mixed micelles and those micelles had highly drug encapsulation efficiency of above 95% and drug loading capacity of 4.4%. The results from in vitro release study showed that curcumin released from micelles slowly. Thirty minutes after oral administration of curcumin or curcumin-loaded mixed micelles （100 mg/kg）, the blood concentration of curcumin-loaded mixed micelles group was significantly higher than that of curcumin suspension group （P 〈 0.05）. The bioavailability of curcumin in mixed micelles was 1.7 times as much as that of curcumin suspension. Conclusion Curcumin-loaded mixed micelles could greatly improve the stability and oral bioavailability of curcumin.