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目的:研制辅酶Q10纳米结构脂质载体(Q10-NLC),并对其皮肤靶向性进行评价。方法:采用高压微射流技术制备Q10-NLC,运用响应面设计优化处方,并对其理化性能、稳定性及体外释放行为进行表征;采用Franze扩散池法评价Q10-NLC体外透皮性能。结果:通过响应面设计得到Q10-NLC优化处方,按照优化处方制备的Q10-NLC粒径为151.7 nm,多分散指数(PDI)0.144,Zeta电位-44.1 mV,载药量2.51%,包封率100%;24 h光照后,Q10-NLC中Q10含量下降5.59%,显著低于乳剂和乙醇溶液中Q10的光解量;体外药物释放表明,Q10-NLC具有明显的缓释行为;体外透皮吸收实验结果显示,Q10-NLC的药物皮肤滞留量为Q10乳剂的10.11倍。结论:Q10-NLC可有效提高Q10的稳定性,延长其作用时间,实现Q10皮肤靶向给药。
Objective: To develop a coenzyme Q10 nanostructured lipid carrier (Q10-NLC) and to evaluate its skin targeting. Methods: Q10-NLC was prepared by high-pressure micro-jet technique. Response surface design was used to optimize the formulation. The physical and chemical properties, stability and in vitro release behavior were characterized. Franco diffusion cell method was used to evaluate Q10-NLC in vitro. Results: Q10-NLC optimized formulation was obtained through response surface design. The particle size of Q10-NLC was 151.7 nm, the PDI was 0.144, the Zeta potential was -44.1 mV, the drug loading was 2.51% 100%. After 24 h light exposure, Q10 content in Q10-NLC decreased 5.59%, which was significantly lower than that of Q10 in emulsion and ethanol solution. In vitro drug release showed that Q10-NLC had a sustained release behavior. Absorption test results show that the drug Q10-NLC skin retention of 10.11 times the Q10 emulsion. Conclusion: Q10-NLC can effectively improve the stability of Q10, prolong its action time and achieve Q10 skin-targeted drug delivery.