Abstract
Purpose: Ofloxacin is a fluoroquinolone with broad-spectrum antibacterial action, used in treatment of systemic and local infections. Ofloxacin is BCS class II drug having low solubility, high permeability with short half-life. The present work was aimed to design, develop and optimize gellified emulsion of Ofloxacin to provide site targeted drug delivery. Transdermal drug delivery will enhance the bioavailability of the drug giving controlled drug release. Methods: Transdermal drug delivery system was designed with gelling agent (Carbopol 940 and HPMC K100M), oil phase (oleic acid) and emulsifying agent (Tween 80: Span 80). Effect of concentration of gelling agent on release of drug from transdermal delivery was studied by 32 factorial design. Emulgel was evaluated for physical appearance, pH, drug content, viscosity, spreadability, antimicrobial activity, in- vitro diffusion study and ex-vivo diffusion study. Results: FE-SEM study of the emulsion batch B5 has revealed formation of emulsion globules of approximately size 6-8 µm with -11.2 mV zeta potential showing good stability for the emulsion. Carbopol 940 had shown greater linear effect on drug release and viscosity of the formulations due to its high degree of gelling. In-vitro diffusion study through egg membrane had shown 88.58±1.82 % drug release for optimized batch F4. Ex-vivo diffusion study through goat skin indicated 76.68 ± 2.52% drug release. Conclusion: Controlled release Ofloxacin emulgel exhibiting good in-vitro and ex-vivo drug release proving good antimicrobial property was formulated.
Highlights
Formulations that are applied to the skin or to mucus membrane are referred as transdermal or topical
It belongs to BCS class II drug with low solubility and high permeability
After one month accelerated study, major peaks (Figure 1 A) of Ofloxacin were observed at 2936 cm-1 (CH2), 1714 cm-1(C=O), 1621 cm-1(NH3), 1550 cm-1(CF), 1459 cm-1(CH3) and 1086 cm-1(CH)
Summary
Formulations that are applied to the skin or to mucus membrane are referred as transdermal or topical. Drugs administered through the topical route may have both local and systemic effects, depending on where the application is made and on how the formulation is been constructed. Three different functions may be achieved via application of the formulations to human skin.[1] First function is the desirability to make the active remain on the surface of the skin, E.g. dermal insect repellents, skin infections, and cosmetics for skin decoration. The second function is for those topical formulations which are designed for dermal penetration of their actives into the deeper regions of the skin such as the viable epidermis and dermis. These are called as endodermal or diadermal formulations. The objective was to optimize controlled release emulgel delivery and to investigate the influence of concentration of gelling agents (HPMC K100M and Carbopol 940) on the drug delivery
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