The preparation and evaluation of some metronidazole formulations as gels and the study of their medicinal activities against pathogenetic microorganisms causing dermatitides

Abstract EN

In the present study, a labor has been made to develop gel type of transdermal therapeutic system comprising different concentrations of metronidazole with hydrophilic polymeric combinations using solid dispersion method.

Two main parts including chemical and biochemical were discussed in this study.

In the chemical part, In vitro drug release and kinetics of drug release were studied for all the prepared pharmaceutical formulations in this study.

The prepared formulations including GR3R and HR3R followed zero order, Korsmeyer-Peppas model and Fickian (n < 0.5) transport mechanism (diffusion controlled release).

In the biochemical part, the biochemical activities of all the prepared formulations (as antimicrobials) were studied (in vitro) in four types of microbes including 0TStaphylococcus aureus (Gram-positive), Staphylococcus epidermidis (Gram-positive), Candida albicans (yeast) and Trichophyton sp.0T (mold) by using agar diffusion method.

These formulations showed an increase in their biochemical activities against these isolates and these activities an associated with the increase in drug concentrations which were loaded with the selected polymers in this study and in addition to their possession of highest antimicrobial and biochemical activities to inhibit the growth of these microbial isolates as compared to pure drug and commercial gel at (p < 0.05).

Also, the prepared formulations including GR0R, GR3R, HR0R and HR3R were applied (in vivo) to the skin of male rabbits for studying subacute toxicity test (LDR50R), skin (back and rectal) irritation tests and the created skin irritation treatment test.

These formulations were not poisonous and non irritant, while HR3R formulation possessed of ability to treat the created skin irritation during (10-12) days.

. Key words :Metronidazole Gels, In Vitro & In Vivo Studies.