硝酸毛果芸香碱温敏型眼用脂质体凝胶的制备及体外释放

Preparation of pilocarpin nitrate thermosensitive ocular liposomal gel and its release in vitro

目的:制备硝酸毛果芸香碱(PN)温敏型眼用脂质体凝胶,并对其体外释放行为进行考察。方法:将PN脂质体分散于温敏基质泊洛沙姆407(P407)中制备PN脂质体凝胶,依据胶凝温度筛选处方中P407浓度,观察优化处方对兔眼的刺激性;双室法测定PN脂质体凝胶中药物的释放。结果:处方中P407最佳浓度为19%;PN脂质体凝胶对兔眼无明显刺激作用;脂质体凝胶中药物的释放明显慢于其他制剂,前2h释药符合Higuchi扩散模式,2h后较符合零级释药模式。结论:P407温敏型脂质体凝胶缓释作用明显且刺激性小,适合作为NP眼用给药载体。

Objective：To prepare pilocarpin nitrate （PN） thermosensitive liposomal gel for ophthalmic drug delivery, and study its release in vitro. Methods ： Poloxamer 407 （ P407 ） was used as thermosensitive material for PN liposomal gel. The concentration of P407 was optimized according to the temperature of gel. The irritation of selected formulation on rabbit eyes was observed. The two-compartment method was used to evaluate PN release from PN liposomal gel in vitro. Results：The optimum concentration of P407 in prescription was 19% without eye irritation. The release of PN from PN liposomal gel was slower than other preparations and followed Higuchi equation in the first 2 h and zero-order kinetics after 2 h. Conclusion：With a more sustained release and less irritation,P407 thermosensitive liposomal gel is a suitable vehicle for NP ophthahnic drug delivery.