title: Terbinafine hydrochloride nanovesicular gel: In vitro characterization, ex vivo permeation and clinical investigation.
abstract: In this work, nanovesicular chitosan gels were prepared for dermal delivery of terbinafine hydrochloride (TBN HCl). Ethosomes and vesicles containing different types of penetration enhancers (PEs) viz. Terpenes (cineole and limonene), labrasol and transcutol were developed. The prepared vesicles were evaluated for physical characteristics as well as skin interaction. The selected vesicles were incorporated into chitosan gel. An in vivo animal study was done on rat induced superficial Candida infection model. Moreover, randomized double blind clinical study was done on patients to compare the effect of the selected nanovesicular gel against the market product. Results showed the formation of nearly spherical, mostly deformable vesicular systems with size range of 95.5-530nm, zeta potential range of -0.1 to 15mV and entrapment efficiency range of 20-96.7%. Penetration enhancer vesicles (PEVs) prepared with 4% limonene (ELI4) showed the highest percent of drug deposition in the skin (53%) and the highest local accumulation efficiency value (35.3). In vivo animal study showed that the lowest fungal burden produced with ELI4 chitosan gel. Clinical studies showed cure rate of 86% within 7days treatment in case of limonene nanovesicular gel compared to 20% for market product (Lamisil® cream).
authors.affiliation: Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
authors.forename: Sara M
authors.initials: SM
authors.lastname: AbdelSamie
authors.affiliation: Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt. Electronic address: amany.kamel@yahoo.com.
authors.forename: Amany O
authors.initials: AO
authors.lastname: Kamel
authors.affiliation: Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
authors.forename: Omaima A
authors.initials: OA
authors.lastname: Sammour
authors.affiliation: Dermatology and Venereology Department, Faculty of Medicine, Al-Azhar University, Cairo, Egypt.
authors.forename: Shady M
authors.initials: SM
authors.lastname: Ibrahim
mesh_terms: D000818:Animals; D002176:Candida albicans; D002177:Candidiasis / Q000188:drug therapy*; D004304:Dosage Forms; D003875:Drug Eruptions; D005782:Gels / Q000008:administration & dosage / Q000737:chemistry; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry*; D009281:Naphthalenes / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D012869:Skin Absorption; D000077291:Terbinafine
chemical_list: D004304:Dosage Forms; D005782:Gels; D009281:Naphthalenes; D000077291:Terbinafine
keywords: Animal study; Clinical study; Dermal delivery; Penetration enhancer vesicles; Skin deposition; Terbinafine HCl