title: Formulation, characterization, and clinical evaluation of microemulsion containing clotrimazole for topical delivery.
abstract: The objective of the present study was to formulate and evaluate microemulsion systems for topical delivery of clotrimazole (CTM). The solubility of CTM in various oils was determined to select the oil phase of the microemulsion systems. Pseudoternary phase diagrams were constructed to identify the area of microemulsion existence. Five CTM microemulsion formulations (M1-M5) were prepared and evaluated for their thermodynamic stability, pH, refractive index, droplet size, viscosity, and in vitro release across cellulose membrane. Among the prepared microemulsion formulations, M3 (lemon oil/Tween 80/n-butanol/water) and M4 (isopropyl myristate/Tween 80/n-butanol/water) microemulsion systems were found to be promising according to their physical properties and CTM cumulative percentage release. Gel form of M3 and M4 were prepared using 1% Carbopol 940 as the hydrogel matrix. Both formulations were evaluated in the liquid and gel forms for drug retention in the skin in comparison to the marketed CTM topical cream and their stability examined after storage at 40°C for 6 months. Microemulsion formulations achieved significantly higher skin retention for CTM over the CTM cream. Stability studies showed that M4 preparations were more stable than M3. The in vitro anti-fungal activity of M4 against Candida albicans was higher than that of the conventional cream. Moreover, clinical evaluation proved the efficacy and tolerability of this preparation in the treatment of various topical fungal infections.
authors: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, Egypt.
authors: Fahima M
authors: FM
authors: Hashem
authors: Dalia S
authors: DS
authors: Shaker
authors: Mohamed Khalid
authors: MK
authors: Ghorab
authors: Mohamed
authors: M
authors: Nasr
authors: Aliaa
authors: A
authors: Ismail
mesh_terms: D000287:Administration, Topical; D000293:Adolescent; D000328:Adult; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry; D019905:Benzyl Alcohol / Q000737:chemistry; D003022:Clotrimazole / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use; D003881:Dermatomycoses / Q000188:drug therapy*; D004339:Drug Compounding; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry*; D005260:Female; D005990:Glycerol / Q000031:analogs & derivatives / Q000737:chemistry; D006801:Humans; D008297:Male; D051379:Mice; D008875:Middle Aged; D009226:Myristates / Q000737:chemistry; D009821:Oils / Q000737:chemistry; D019301:Oleic Acid / Q000737:chemistry; D010316:Particle Size; D010938:Plant Oils / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D012869:Skin Absorption; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D000935:Antifungal Agents; D004655:Emulsions; D009226:Myristates; D009821:Oils; D010938:Plant Oils; D011136:Polysorbates; D013501:Surface-Active Agents; C008205:isopropyl myristate; D019301:Oleic Acid; C000515:cremophor EL; D003022:Clotrimazole; C501365:lemon oil; D019905:Benzyl Alcohol; D005990:Glycerol