Metronidazole Loaded Novel Microemulsion Formulation for Topical Delivery and Characterization With Validated New UPLC Method

Abstract

The purpose of the study is to develop metronidazole (MET) containing microemulsion systems for topical application, to overcome limitations of local antibacterial treatments. For preparation of drug loaded microemulsions pseudo-phase diagram technique was applied; IPP as oil phase, Span 80 and Cremophor EL as surfactant, ethanol and propylene glycol as co-surfactant and distilled water was used as aqueous phase. Globule size ranging between 126.82.8 to 150.81.6 nm and PDI between 0.210.02 to 0.350.06 were obtained. Zeta potentials of the formulations measured as 0.480.08 – 0.680.14 mV and conductivity was between 0.50.0 and 0.60.0, implicating the formation of w/o emulsions. A UPLC method was developed and validated according to the ICH Q2 (R1) guideline, for quantification of MET, and drug content was calculated as 99.180.08 – 99.330.12%. MET release of 80.620.86% for S1MET and 62.061.08% for S2MET formulations at 24h, indicated the control over the MET release by the microemulsions. After 3. and 6. months, there were no difference in physicochemical properties of microemulsions and MET release showed similar profile; implicating the good stability of formulations.