title: Preparation and evaluation of dermal delivery system of griseofulvin containing vitamin E-TPGS as penetration enhancer.
abstract: Griseofulvin, an antifungal agent, is a BCS class II drug slowly, erratically, and incompletely absorbed from the gastrointestinal tract in humans. The clinical failure of the conventional oral therapy of griseofulvin is most likely attributed to its poor solubility and appreciable inter- and intra-subject variation in bioavailability from different commercial products. Moreover, the conventional oral therapy is associated with numerous adverse effects and interactions with other drugs. The purpose of the study was to formulate a topical application of griseofulvin which would deliver the drug locally in a therapeutically effective concentration. Griseofulvin was solubilized in ethanol, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), and combinations of ethanol with varying amounts of TPGS; then, it was incorporated in the Carbopol (980 NF) base. The formulations were characterized and evaluated ex vivo using Laca mice skin, microbiologically against Microsporum gypseum and Microsporum canis and clinically in a small group of patients. The current study suggested that TPGS and ethanol synergistically enhanced the drug permeation and drug retention in the skin. The selected formulation F VII was found to be effective against M. gypseum and M. canis, non-sensitizing, histopathologically safe, stable at 4°C, 25°C, and 40°C with respect to percent drug content, permeation characteristics, pH, transparency, feel, viscosity, and clinically effective in a small group of subjects. The proposed topical formulation of griseofulvin may be an effective and convenient alternative to the currently available oral therapy for the treatment of superficial fungal infections.
authors: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
authors: Nidhi
authors: N
authors: Aggarwal
authors: Shishu
authors: S
authors: Goindi
authors: Swami Dass
authors: SD
authors: Mehta
mesh_terms: D000279:Administration, Cutaneous; D000328:Adult; D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005260:Female; D006118:Griseofulvin / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000378:metabolism; D006801:Humans; D008297:Male; D051379:Mice; D009181:Mycoses / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D010328:Patch Tests / Q000379:methods; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000138:chemical synthesis / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology; D014810:Vitamin E / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D055815:Young Adult
chemical_list: D014810:Vitamin E; D006118:Griseofulvin; D011092:Polyethylene Glycols; C014225:tocophersolan