title: Novel carbopol-based transfersomal gel of 5-fluorouracil for skin cancer treatment: in vitro characterization and in vivo study.
abstract: 5-fluorouracil (5-Fu) is an antineoplastic drug, topically used for the treatment of actinic keratosis and nonmelanoma skin cancer. It shows poor percutaneous permeation through the conventionally applicable creams and thus inefficient for the treatment of deep-seated skin cancer. In the present article, transfersomal gel containing 5-Fu was investigated for the treatment of skin cancer. Different formulation of tranfersomes was prepared using Tween-80 and Span-80 as edge activators. The vesicles were characterized for particle size, shape, entrapment efficiency, deformability and in vitro skin permeation. Optimized formulation was incorporated into 1% carbopol 940 gel and evaluated for efficacy in the treatment of skin cancer. 5-Fu-loaded transfersomes (TT-2) has the size of 266.9 ± 2.04 nm with 69.2 ± 0.98% entrapment efficiency and highest deformability index of 27.8 ± 1.08. Formulation TT-2 showed maximum skin deposition (81.3%) and comparable transdermal flux of 21.46 µg/cm(2) h. The TT-2-loaded gel showed better skin penetration and skin deposition of the drug than the marketed formulation. Composition of the transfersomal gel has been proved nonirritant to the skin. We concluded that the developed 5-Fu-loaded transfersomal gel improves the skin absorption of 5-Fu and provide a better treatment for skin cancer.
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy .
authors.forename: Mohammed Ashif
authors.initials: MA
authors.lastname: Khan
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy .
authors.forename: Jayamanti
authors.initials: J
authors.lastname: Pandit
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy .
authors.forename: Yasmin
authors.initials: Y
authors.lastname: Sultana
authors.affiliation: b Department of Medical Elementology and Toxicology, Faculty of Science , Jamia Hamdard , and.
authors.forename: Sarwat
authors.initials: S
authors.lastname: Sultana
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy .
authors.forename: Asgar
authors.initials: A
authors.lastname: Ali
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy .
authors.forename: Mohammed
authors.initials: M
authors.lastname: Aqil
authors.affiliation: c Department of Pharmaceutics , Delhi Institute of Pharmaceutical Sciences and Research , New Delhi , India.
authors.forename: Meenakshi
authors.initials: M
authors.lastname: Chauhan
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D004548:Elasticity; D005472:Fluorouracil / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D005782:Gels / Q000737:chemistry*; D006601:Hexoses / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry*; D008297:Male; D051379:Mice; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D012869:Skin Absorption; D023422:Skin Irritancy Tests; D012878:Skin Neoplasms / Q000188:drug therapy; D014783:Viscosity
chemical_list: D000180:Acrylic Resins; D000970:Antineoplastic Agents; D005782:Gels; D006601:Hexoses; D008081:Liposomes; D011136:Polysorbates; C018665:sorbitan monooleate; C006903:carbopol 940; D005472:Fluorouracil
keywords: 5-fluorouracil; carbopol; skin cancer; topical delivery; transfersomal gel