[1]徐霁,周文君,蔡春华,等.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[J].第三军医大学学报,2017,39(13):1376-1380.
 XU Ji,ZHOU Wenjun,CAI Chunhua,et al.Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops[J].J Third Mil Med Univ,2017,39(13):1376-1380.
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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(/HTML )
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《第三军医大学学报》[ISSN:1000-5404/CN:51-1095/R]

卷:
39卷
期数:
2017年第13期
页码:
1376-1380
栏目:
基础医学
出版日期:
2017-07-15

文章信息/Info

Title:
Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops
作者:
徐霁周文君蔡春华刘世纯
重庆医科大学附属永川医院:眼科,中心实验室
Author(s):
XU Ji ZHOU Wenjun CAI Chunhua LIU Shichun

Department of Ophthalmology, Central Laboratory, Yongchuan Hospital of Chongqing Medical University, Chongqing, 402160, China

关键词:
壳聚糖聚乙二醇纳米粒
Keywords:
chitosan polyethylene glycol nanoparticles eyes
分类号:
R944.9; R969; R988.1
文献标志码:
A
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(P<0.05)。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 develop a polyethylene glycol modified (PEGylated) chitosan nanoparticle and evaluate its potential for ocular drug delivery by eye drops. Methods         Voriconazole was employed as model drug. The PEGylated chitosan nanoparticles were prepared by ionotropic gelification and characterized for the properties. In vitro drug release properties, ocular pharmacokinetics and corneal penetration of these nanoparticles were studied. Results        The PEGylated chitosan nanoparticle was 235±23 nm in particle size, 23.1±0.6 mV in zeta potential, 11.16% of drug loading capacity, and 61.35% of encapsulation efficiency. The sustained drug was released very slowly from the nanoparticles, for consecutive 48 h. Compared with voriconazole solution, the nanoparticles had significantly increased area under the concentration-time curve, prolonged halflife and decreased clearance rate of the loaded drug,  and prolonged residence time at the ocular surface (P<0.05). The corneal penetration study with the aid of fluorescent labeled nanoparticles showed that the nanoparticles could penetrate into the cornea. Conclusion         Compared with the aqueous solution, the PEGylated chitosan nanoparticle could prevent the drug loss on ocular surface and improve the drug bioavailability.

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更新日期/Last Update: 2017-07-14