Bioadhesive chitosan-loaded liposomes: A more efficient and higher permeable ocular delivery platform for timolol maleate

详细信息    查看全文

• 作者：Guoxin Tan^a ; Shihui Yu^a ; Hao Pan^b ; Jinyu Li^a ; Dandan Liu^c ; Kun Yuan^a ; Xinggang Yang^a ; ^{yangxg123@163.com} ; Weisan Pan^a ; ^{pppwwwsss@163.com}
• 关键词：Ocular drug delivery ; Liposomes ; Chitosan ; Bioadhesive ; Gamma scintigraphic ; Pharmacodynamics
• 刊名：International Journal of Biological Macromolecules
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：94
• 期：part_PA
• 页码：355-363
• 全文大小：2124 K
• 卷排序：94

文摘

The aim of this study was to develop and characterize a novel colloidal system, namely, timolol maleate chitosan coated liposomes (TM-CHL) to enhance the ocular permeation, precorneal residence time and bioavailability. The resulting TM-CHL was the most promising formulation with a mean particle size of 150.7 nm and an EE% of 75.83 ± 1.61%. In vitro release of the TM-CHL showed an extended drug release profile. The TM-CHL exhibited significant mucin adhesion and compared with commercial eye drops, TM-CHL produced a 3.18-fold increase in the apparent permeability coefficient (Papp), resulting in a significant enhancement of corneal permeation. In addition, the gamma scintigraphic study and the pharmacokinetic study showed that TM-CHL could be retained at the corneal surface for longer time compared with eye drops. The ocular irritation study indicated that the developed liposomes produced no significant irritant effects. Furthermore, pharmacodynamics results showed that the maximum intraocular pressure(IOP) produced by TM-CHL was (19.67 ± 1.14) mmHg compared with the (23.80 ± 1.49) mmHg for TM eye drops, revealing that TM-CHL was more effective in reducing the IOP. These results demonstrate that CHL is a potentially useful carrier for ocular drug delivery, which could improve the efficacy of TM.