Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 480, Issue 1-2, Pages 128-136Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2015.01.032
Keywords
Timolol maleate; Deacetylated gellan gum; Ocular drug delivery system; Liposomal-ion sensitivity in situ gel; Pharmacodynamics
Categories
Funding
- State Key Laboratory (Long-acting and Targeting Drug Delivery System)
- Foundation of Liaoning Educational Committee [L2014504]
- Doctoral Scientific Research Foundation of Liaoning Institute of Science and Technology [1406B04]
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This study was aimed to design a liposomal based ion-sensitive in situ ophthalmic delivery system of timolol maleate (TM). The TM liposome was produced by the reverse evaporation technique coupled with pH-gradients method (REVPR), and then was incorporated into deacetylated gellan gum gels. The TM liposome was demonstrated to be a round and uniform shape in TEM pictures. Compared with the TM eye drops, the TM liposome produced a 1.93 folds increase in apparent permeability coefficients (Papp), resulting in a significant increase of the corneal penetration. The TM-loaded liposome incorporated ion sensitive in situ gels (TM L-ISG) showed longer retention time on corneal surface compared with the eye drops using gamma scintigraphy technology. Draize testing showed that TM L-ISG was non-irritant for ocular tissues. The biggest efficacy of TM L-ISG occurred 30 min after eye drops administration, and efficacy disappeared after 240 min. Then, compared with the eye drops, the optimal TM L-ISG could quickly reduce the intraocular pressure and the effective time was significantly longer (P <= 0.05). These results indicate that liposome incorporated ion sensitive in situ gels have a potential ability for the opthalmic delivery. (C) 2015 Elsevier B.V. All rights reserved.
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