摘要
目的设计制备皮肤外用花椒毒素纳米球,探讨花椒毒素纳米球对PUVA疗法光反应毒性的影响,以期优化外用PUVA疗法。方法采用溶剂置换-界面聚合物沉积法制备花椒毒素纳米球,筛选并优化花椒毒素纳米球的处方组成,优化后的纳米球在人工半透膜中考察其体外释放特性,并采用补骨脂素类化合物与DNA的反应模型考察其光反应效率。结果制备并优化后的花椒毒素纳米球其平均粒径为109nm,粒径分布度小于0.1,Zeta电位<-20mV,包封率为65.8%。在体外人工半透膜中的释放特性表明,相比Meladinine溶液,该花椒毒素纳米球具有良好的释放性能。花椒毒素制备成纳米球后,在与胸腺嘧啶的混合反应体系中的光反应速率明显有所降低,能起到控释的效应。结论花椒毒素纳米球有望能降低PUVA疗法的光反应毒性,从而成为改善PUVA疗法的新型制剂。
OBJECTIVE We developped xanthotoxin loaded PLGA nanospheres for topical formulation and to investigate its influences on PUVA photoreaction toxicity with the final goal of ameliorating the efficacy of PUVA therapy. METHODS Xanthotoxin loaded PLGA nanospheres were prepared by interfacial polymer deposition following solvent displacement and the formulation was optimized and we investigated its in vitro released profiles across artificial dialysis membrane, meanwhile its efficacy of photo-reaction using psoralen-DNA interaction model was determined. RESULTS The nanospheres optimized had a mean diameter （ 109 nm）, a narrow size distribution （ polydispersity index 〈 0.1 ）, and a negative surface charge （ zeta potential 〈 - 20 mV）. Its encapsulation efficiency was about 65. 8%. The release of xanthotoxin from nanospheres was significantly faster than from the correspondent Meladinine solution, xanthotoxin incorporated in the nanospheres can decrease the velocity of photoreaction with DNA. CONCLUSION Xanthotoxin loaded PLGA nanospheres for topical formulation could constitute a promising approach for controlling the xanthotoxin release in order to maintain its therapeutic activity with less side effects.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2009年第3期177-179,共3页
Chinese Journal of Modern Applied Pharmacy
基金
广东药学院科研启动基金(2006YKX08)
广东省医学科研基金(B2008080)
