聚乙二醇化壳聚糖纳米粒的制备及局部滴眼给药性能评价

发布时间：2019-04-11 18:18

【摘要】：目的制备一种聚乙二醇修饰的壳聚糖纳米粒,评价其局部滴眼给药性能。方法以伏立康唑为模型药物,采用离子交联法制备载药的聚乙二醇化壳聚糖纳米粒,对其进行表征后,分别考察纳米粒的药物缓释能力、对眼表药物代谢动力学的影响及其角膜渗透性。结果聚乙二醇化壳聚糖纳米粒粒径为(235±23)nm,Zeta电位为(+23.1±0.6)mV,载药量为11.16%,包封率为61.35%。纳米粒体外释放药物非常缓慢,可持续释药48 h;相比于伏立康唑水溶液,纳米粒的药物浓度-时间曲线下面积明显增加,药物半衰期延长,清除率减少,眼表药物平均滞留时间延长(P0.05)。荧光标记的聚乙二醇化壳聚糖纳米粒可穿透角膜上皮逐渐向角膜基质渗透。结论与药物水溶液相比,聚乙二醇化壳聚糖纳米粒能够有效减少眼表药物的流失,改善药物的生物利用度。
[Abstract]:Objective to prepare a kind of chitosan nanoparticles modified by polyethylene glycol (PEG) and evaluate its local eyedrop performance. Methods the drug-loaded poly (ethylene glycol) chitosan nanoparticles were prepared by ion cross-linking method using Voliconazole as model drug. After characterization, the sustained-release ability of nanoparticles was investigated. Effects on pharmacokinetics of ocular surface and corneal permeability. Results the particle size of polyethylene glycol chitosan nanoparticles was (2335 卤23) nm,Zeta, the potential was (23.1 卤0.6) mV, the drug loading was 11.16%, and the entrapment efficiency was 61.35%. The drug release of nanoparticles in vitro was very slow and sustained for 48 hours. Compared with Voliconazole aqueous solution, the area under the concentration-time curve of nanoparticles was significantly increased, the half-life of the drug was prolonged, the clearance rate was decreased, and the average retention time of the drug on the surface of the eye was prolonged (P0.05). Fluorescence-labeled poly (ethylene glycol) chitosan nanoparticles can penetrate the corneal epithelium gradually into the corneal stroma. Conclusion compared with aqueous solution, polyethylene glycol chitosan nanoparticles can effectively reduce the loss of ocular surface drugs and improve the bioavailability of drugs.
【作者单位】：重庆医科大学附属永川医院眼科;重庆医科大学附属永川医院:中心实验室;
【分类号】：R943

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