Sustained release timolol maleate loaded ocusert based on biopolymer composite

•Timolol maleate loaded ocuserts was prepared using natural polymer sodium alginate.•Significant reduction in IOP was observed within 3days.•Prepared ocuserts proved to be a viable alternative over conventional marketed formulations for the treatment of glaucoma. In the present investigation, the ef...

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Veröffentlicht in:International journal of biological macromolecules 2018-04, Vol.110, p.308-317
Hauptverfasser: Nair, Revathy V., S, Shefrin, Suresh, Akhil, K.R., Anoop, Nair, Sreeja C.
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Sprache:eng
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Zusammenfassung:•Timolol maleate loaded ocuserts was prepared using natural polymer sodium alginate.•Significant reduction in IOP was observed within 3days.•Prepared ocuserts proved to be a viable alternative over conventional marketed formulations for the treatment of glaucoma. In the present investigation, the effect of timolol maleate loaded ocuserts was studied as an alternative for conventional anti-glaucoma formulation. Ocuserts were prepared using natural polymer sodium alginate and ethyl cellulose. Physico-chemical properties along with drug entrapment efficiency (94–98%), content uniformity (93.1% ± 0.264–98.00% ± 0.321), in vitro drug release (83.42% ± 0.35 at end of 12 h), ex vivo permeation all showed satisfactory results, which was found to follow zero order kinetics. Ex vivo permeation studies showed better results, revealed that the permeability coefficient was dependent on polymer type. The sterility test accelerated stability studies and in vivo studies such as eye irritancy test, in vivo drug release of the optimized ocusert was determined. The anti-glaucoma activity was measured using Schiotz tonometer at different time interval. Significant reduction in Intra ocular pressure (IOP) within 3 days was observed in case of rabbits treated with ocusert in comparison to the rabbit treated with marketed eye drop formulation. Hence timolol maleate loaded ocuserts proved to be a promising and viable alternative over conventional eye formulation for the sustained and controlled ophthalmic drug delivery, targeting the drug within the ocular globe thus improving patient compliance for the treatment of glaucoma.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2018.01.029