Abstract

DESIGN, DEVELOPMENT AND EVALUATION OF LOMEFLOXACIN HYDROCHLORIDE NIOSOMAL GUM BASED IN SITU GELS FOR OTIC DRUG DELIVERY

Manal Yassien Hamza*

ABSTRACT

The aim of the present study was to design, formulate and evaluate lomefloxacin Hcl niosomal in situ gels to provide broad spectrum antibacterial activity for the treatment of ear infections aiming to increase drug concentration in the middle ear fluid, improve residence time and prolong drug release. LMN niosomes were prepared using different types of surfactants (Span20, Span 40, Span 60) with different molar ratios with respect to cholesterol (1:4, 1:6, 7:4, 7:6). Based upon the entrapment efficiency percentage (EE%) and acceptable release percentage of LMN after 8 hr and 24 hr formula F12 was chosen as the optimized formula as EE% found to be 90.3%, PS 537 nm and % drug released (Q8 64.8 %, Q24 87.9 %). Thus, niosomal in situ gels of the optimized formula F12 were prepared using Guar gum (GG) and Xanthan gum (XG) with the combination of Carbopol 940 as the gelling agent, Hydroxy propyl methyl cellulose (HPMCk100) and sodium alginate as viscosity imparting agents. The prepared formulations were evaluated for physical appearance, pH, gelling time, spreadability, drug content, rheological characteristic, in vitro drug release studies, accelerated stability and antimicrobial activity. The study revealed that physical appearance, pH, viscosity and drug content of all developed formulations were found to be satisfactory. The most effective combination of polymers were noted in F3 (0.2% GG, 0.4% CP, 0.5% SA) which gave satisfactory in situ gel forming formula, with a drug release 53.2% over7 hr and F8 (0.2% XG, 0.4% CP and 0.5% SA) showed release of 58.2% over7 hr and 100% for market product 0.3% at 5 hrs. The optimized formulations exhibited required viscosity with a remarkable increase in the viscosity after gelling. The optimized formulations were stable under accelerated temperature conditions. Therefore, the developed niosomal gum based in situ gel therapeutically efficacious and can acts as a suitable, valuable alternative to the conventional systems to reduce side effects and improve patient compliance.

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