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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 PN pilocarpine (PN) thermosensitive ophthalmic liposome gel and investigate its in vitro release behavior. Methods: PN liposomes were dispersed in poloxamer 407 (P407) to prepare PN liposome gel. The concentration of P407 in the prescription was screened according to the gelation temperature to observe the irritation of rabbit eyes. Determination of drug release from PN liposome gel by chamber method. Results: The optimum concentration of P407 in prescription was 19%. PN liposome gel had no obvious stimulating effect on rabbit eyes. The drug release in liposome gel was slower than other preparations. The release of the first 2h was consistent with Higuchi diffusion model, After 2h more in line with zero release mode. Conclusion: P407 temperature-sensitive liposome gel has obvious sustained release effect and small irritation, which is suitable as NP ophthalmic drug delivery carrier.