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目的制备外用的载有补骨脂素的PLGA纳米粒,为临床上改进PUVA疗法降低其毒副作用奠定基础。方法采用溶剂置换-界面聚合物沉积法制备补骨脂素纳米粒。通过建立包封率测定方法,并结合其外观光学特征,优化出补骨脂素纳米粒的处方组成。并考查其物理化学特性以及在体外人工半透膜的释放特性和人体完整皮肤的渗透特性。结果优化条件下制备出的纳米粒平均粒径为(107.16±0.17)nm,粒径分布系数为(0.052±0.004),Zeta电位为(-8.82±0.28)mV,包封率为(83.62±1.98)%。在体外人工半透膜中的释放特性表明,该补骨脂素纳米粒具有良好的释放性能,24 h内释放率达75.84%。在人体皮肤中的渗透动力学特征表明,相比较于乙醇溶液制剂,该纳米粒在人体皮肤具有明显的缓控释特征,且能增加在人体皮肤中的贮存量。结论优化条件制备出的补骨脂素皮肤用纳米粒载药系统有可能成为临床上改进补骨素光化学疗法降低其毒副作用的一种新的经皮给药制剂。
Objective To prepare external psoralen loaded PLGA nanoparticles, which will lay the foundation for the clinical improvement of PUVA therapy to reduce its toxicity and side effects. Methods Psoralen nanoparticles were prepared by solvent displacement - interfacial polymer deposition. By establishing the method of determination of entrapment efficiency and combining with its appearance optical characteristics, the prescription composition of psoralen nanoparticles was optimized. And examining its physicochemical properties as well as the release characteristics of the artificial semipermeable membrane in vitro and the permeation characteristics of human intact skin. Results The average diameter of the prepared nanoparticles was (107.16 ± 0.17) nm, the size distribution coefficient was (0.052 ± 0.004) and the Zeta potential was (-8.82 ± 0.28) mV, the entrapment efficiency was (83.62 ± 1.98 )%. The in vitro release characteristics of artificial semi-permeable membrane showed that the psoralen nanoparticles had good release properties, and the release rate reached 75.84% in 24 h. The osmotic kinetics in human skin show that the nanoparticle has a markedly controlled release profile on human skin as compared to an ethanol solution formulation and increases the amount of storage in human skin. CONCLUSION: The psoralen skin-loaded nanoparticle drug delivery system prepared under optimal conditions may become a new transdermal drug delivery agent that can improve the side effects of puerarin photochemotherapy.