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  • Title: In vivo evaluation and in-depth pharmaceutical characterization of a rapidly dissolving solid ocular matrix for the topical delivery of timolol maleate in the rabbit eye model.
    Author: Moosa RM, Choonara YE, du Toit LC, Tomar LK, Tyagi C, Kumar P, Carmichael TR, Pillay V.
    Journal: Int J Pharm; 2014 May 15; 466(1-2):296-306. PubMed ID: 24607446.
    Abstract:
    The purpose of this study was to investigate the in-depth pharmaceutical properties and in vivo behavior of a novel lyophilized rapidly dissolving solid ocular matrix (RD-SOM) as a 'solid eye drop' formulation comprising timolol maleate as the model drug. Thermal and molecular transition analysis displayed similar findings with no incompatibility between formulation components. Porositometric studies confirmed the presence of interconnecting pores across the matrix surface. The HETCAM test indicated an irritation score of 0 with the inference of good tolerability for the RD-SOM in the New Zealand White albino rabbit eye model. Ex vivo permeation across excised rabbit cornea showed an improved steady state drug flux (0.00052 mg cm(-2)min(-1)) and permeability co-efficient (1.7 × 10(-4)cmmin(-1)) for the RD-SOM compared to pure drug and a marketed eye drop preparation. UPLC analysis quantitatively separated timolol maleate and the internal standard (diclofenac sodium) and gamma irradiation was used as a terminal sterilization procedure. In vivo results revealed a peak concentration of timolol was reached at 104.9 min. In the case of a typical eye drop formulation a lower Cmax was obtained (1.97 ug/mL). Level A point-to-point IVIVC plots via the Wagner-Nelson method revealed a satisfactory R(2) value of 0.84. In addition, the biodegradability and ocular compatibility of the RD-SOM was confirmed by histopathological toxicity studies.
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