Preparation and Evaluation of Transdermal Formulations of Ciprofloxacin hydrochloride

Abstract

Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic which exhibits its potent antibacterial activity through its inhibitory action on DNA gyrase and topoisomerase IV enzymes, essential for bacterial DNA replication. It has a short elimination half-life of approximately 4 hours and requires frequent dosing. It is similar to other antibiotics that upon oral administration the most frequently reported adverse reactions is gastrointestinal discomfort. The objective of the present work aimed to formulate and evaluate transdermal gel formulation of Ciprofloxacin HCl and to study the extent of its percutaneous absorption. Thus, maintaining a steady-state plasma level of the drug without passing through the liver. Transdermal gel formulations of Ciprofloxacin HCl were prepared, including gel bases of different concentrations, namely (Carboxymethylcellulose (CMC), Hydroxypropylmethylcellulose (HPMC) and Carbopol 940). Ciprofloxacin HCl was incorporated into the previous bases at 1% concentration, and the formulated gel bases were assessed for appearance, pH, rheological properties and in-vitro release. HPMC 3% hydrogel formula with peppermint oil as enhancer was chosen as it showed better release (98.9%) characteristics at pH 7.4 after three hours than other formulations, good homogeneity with pH of 6.12, and the gel exhibited first-order kinetics and pseudoplastic flow. The permeation study of this formula showed a sustained release profile within 24 hours, through rabbit membrane.