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布林佐胺载壳聚糖-果胶黏膜黏附纳米囊用于青光眼的治疗:制剂、表征和药效学研究。

Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.

机构信息

Department of Pharmaceutics, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya, Koni, Bilaspur, Chhattisgarh 495009, India.

Department of Pharmaceutics, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya, Koni, Bilaspur, Chhattisgarh 495009, India.

出版信息

Int J Biol Macromol. 2020 Jun 1;152:1224-1232. doi: 10.1016/j.ijbiomac.2019.10.219. Epub 2019 Nov 18.

Abstract

AIM

Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. The aim of this study was to prepare BNZ loaded chitosan-pectin mucoadhesive nanocapsules (CPNCs) by polyelectrolyte complex coacervation method for ocular delivery and evaluated for its anti glaucoma efficacy.

METHODS

The prepared CPNCs were characterized for their particle size, polydispersity index, zeta-potential, surface morphology, entrapment efficiency, drug loading efficiency, mucoadhesive strength in-vitro and ex-vivo release. The pharmacodynamic studies were conducted for CPNCs on glaucoma induced rabbit eye model and compared with marketed product.

RESULT AND DISCUSSION

All the formulated CPNCs exhibited the size range from 217.01 ± 0.21 to 240.05 ± 0.08 nm and appropriate physico-chemical parameters, and depicted a couple of erosion- diffusion release of BNZ over a time of 8 h. Ex-vivo corneal permeation study concluded that BNZ loaded CPNCs crosses the cornea potentially higher rate as compared to the marketed product. In pharmacodynamic study, greater intraocular pressure lowering effect was achieved by CPNCs as compared to marketed drug product.

CONCLUSION

The result concluded that CPNCs are a feasible choice to conventional eye drops because of its ability to improve the bioavailability via its longer precorneal retention time and its ability to sustained release of the drug.

摘要

目的

布林佐胺(BNZ)是一种常用的碳酸酐酶抑制剂,用于治疗青光眼。本研究旨在通过聚电解质复合凝聚法制备 BNZ 载壳聚糖-果胶粘弹性纳米囊(CPNCs),用于眼部给药,并评价其抗青光眼疗效。

方法

对制备的 CPNCs 进行粒径、多分散指数、Zeta 电位、表面形态、包封率、载药量、体外和体外黏附强度以及体外释放度的评价。对 CPNCs 进行了青光眼诱导兔眼模型的药效学研究,并与市售产品进行了比较。

结果与讨论

所有配方 CPNCs 的粒径范围为 217.01 ± 0.21 至 240.05 ± 0.08nm,具有适当的物理化学参数,并在 8 小时内表现出 BNZ 的侵蚀-扩散释放。体外角膜渗透研究表明,与市售产品相比,BNZ 负载的 CPNCs 穿过角膜的潜在速度更高。在药效学研究中,CPNCs 比市售药物产品更能有效降低眼内压。

结论

研究结果表明,CPNCs 是一种可行的选择,因为它能够通过延长前房滞留时间来提高生物利用度,并能够持续释放药物。

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