Chitosan/ β-glycerophosphate in situ forming thermo-sensitive hydrogel for improved ocular delivery of moxifloxacin hydrochloride

Eur J Pharm Sci. 2021 Oct 13:106041. doi: 10.1016/j.ejps.2021.106041. Online ahead of print.ABSTRACTThe aim of the current work is to develop a thermo-sensitive hydrogel system of moxifloxacin hydrochloride (MOX) for improved ocular delivery. Fifteen formulations were prepared at different concentrations of β-glycerophosphate disodium salt (β-GP) 12-20% (w/v) and chitosan (CS) 1.7-1.9% (w/v). MOX loaded optimized thermo-sensitive hydrogel system (F8), consisting of CS (1.8%, w/v) and β-GP (16%, w/v), showed optimum gelation temperature (35°C) and gelation time (2 min), thus selected for further investigations. It showed a significant decrease (p < 0.05) in the zeta potential value compared to CS solution with a favorable pH value (7.1) and confirmed thermoreversible behavior. MOX loaded F8 displayed a porous structure under scanning electron microscopy. Rheological investigation of MOX loaded F8 revealed the presence of a strong hydrogel network with high elasticity along with a small loss factor of 0.08 indicating a great ease of gel formation. The release of MOX from F8 was found to be governed by a combined mechanism of diffusion and relaxation. Biological assessment of two concentrations of MOX loaded F8 (0.25 and 0.5%) was conducted using healthy and infected male albino New Zealand rabbits, where an improved and prolonged antibacterial activity against Staphylococcus aureus compared to plain MOX (0.5%), marketed MOX eye drops (0.5%), was shown. Moreover, histopat...
Source: European Journal of Pharmaceutical Sciences - Category: Drugs & Pharmacology Authors: Source Type: research