Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops

Ji XU; Wenjun ZHOU; Chunhua CAI; Shichun LIU

doi:10.16016/j.1000-5404.201612057

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Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops

Basic Medicine | 更新时间：2026-01-09

- Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops
- Journal of Third Military Medical University Vol. 39, Issue 13, Pages: 1376-1380(2017)
- 作者机构：
  
  1.402160 重庆，重庆医科大学附属永川医院：眼科
  2.402160 重庆，重庆医科大学附属永川医院：中心实验室
- 作者简介：
- 基金信息：
- DOI：10.16016/j.1000-5404.201612057
  CLC： R944.9;R969;R988.1
- Received：08 December 2016，
  
  Revised：2017-03-13，
  
  Published：15 July 2017
- 稿件说明：
移动端阅览
Ji XU, Wenjun ZHOU, Chunhua CAI, et al. Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops[J]. Journal of Third Military Medical University, 2017, 39(13): 1376-1380.
DOI：

Ji XU, Wenjun ZHOU, Chunhua CAI, et al. Preparation and performance of PEGylated chitosan nanoparticles for ocular drug delivery by eye drops[J]. Journal of Third Military Medical University, 2017, 39(13): 1376-1380. DOI： 10.16016/j.1000-5404.201612057.

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(

＜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 chit

osan 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 (

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.

关键词

Keywords

references

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