甲氧沙林脂质体凝胶的体外释药与稳定性研究

A Study of the In Vitro Drug Release and Stability of 8-methoxypsoralen Liposomal Gel

目的对甲氧沙林脂质体凝胶体外释药模式进行定量考察。方法以相同浓度甲氧沙林凝胶为对照,用透析法检测甲氧沙林脂质体凝胶的体外释药模式,并对其在4℃下贮存3周的释药稳定性进行研究。结果与甲氧沙林凝胶比较,甲氧沙林脂质体凝胶具有明显的缓释及长效作用,且前3 h释药符合H iguch i扩散模式(k=4.07%.-h1/2),3 h后遵循零级释药模式(k=0.66%.h-1)。而甲氧沙林凝胶在实验24 h内释药均符合H iguch i扩散模式(k=6.91%.h-1/2)。在贮存期内,甲氧沙林脂质体凝胶的释药模式及包封率均维持稳定。结论甲氧沙林脂质体凝胶体外释药具有明显的缓释特征,稳定性理想,值得进一步研究开发。

Objective To carry out a quantitative examination of the liposomal gel encapsulating 8-methoxypsoralen （LMOP-gel） with respect to its drug-release properties in vitro. Methods The in vitro drug-release properties of the LMOP gel was assayed with the dialysis method using 8-methoxypsoralen gel （8-MOP-gel） as the control. The stability of drug rele＆qe from the LMOP-gel within a period of 3 week storage at 4℃ was studied. Results In comparison with the 8-MOP-gel, the LMOP-gel was shown to have distinct sustained-release and long-acting properties. In the first 3 hours, the drug-release profile of the LMOP-gel followed the diffusion model of Higuchi（ rate constant k =4.07%· h^-1/2） . After the 3rd h, however, it obeyed the zero order-release model（ k = 0.66%·h^-l ）. In contrast, the drug release from the 8-MOP-gel followed the Higuchi （ k = 6.91%·h-1/2） diffusion model throughout the 24 hours of the experiment. Both the drug-release properties anti the drugentrapment percentage of the LMOP-gel were kept stable within the 3 week period of storage at 4℃. Conclusion The LMOPgel was shown to be provided with distinct sustained-release properties and ideal stability in the in vitro drug-release experiment. It is therefore worth further study and exploitation.