title: Development of nanovesicular systems for dermal imiquimod delivery: physicochemical characterization and in vitro/in vivo evaluation.
abstract: The aim of the current investigation was to develop and statistically evaluate nanovesicular systems for dermal imiquimod delivery. To this purpose, transethosomes were prepared with phospholipid, ethanol and different permeation enhancers. Conventional ethosomes, with soy phospholipid and ethanol, were used as control. The prepared vesicles were characterized for size, zeta potential, stability and entrapment efficiency. The optimal transethosomal formulation with mean particle size of 82.3 ± 9.5 nm showed the higher entrapment efficiency (68.69 ± 1.7%). In vitro studies, permeation results of accumulated drug and local accumulation efficiency were significantly higher for transethosomes (24.64 µg/cm(2) and 6.70, respectively) than control (14.45 µg/cm(2) and 3.93, respectively). Confocal laser scanning microscopy of rhodamine 6G-loaded transethosomes revealed an enhanced retention into the deeper skin layers as compared to conventional ethosomes. Besides, Fourier-transform infra-red spectroscopy studies were also performed to understand the mechanism of interaction between skin and carriers. What's more, results of in vivo studies indicated the transethosomes of imiquimod providing the most effectiveness for dermal delivery among all of the formulations. These results suggested that transethosomes would be a promising dermal carrier for imiquimod in actinic keratose treatment.
authors.affiliation: Tianjin Key Laboratory of Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, 300072, People's Republic of China.
authors.forename: Man
authors.initials: M
authors.lastname: Ma
authors.forename: Jinping
authors.initials: J
authors.lastname: Wang
authors.forename: Fang
authors.initials: F
authors.lastname: Guo
authors.forename: Mingzhu
authors.initials: M
authors.lastname: Lei
authors.forename: Fengping
authors.initials: F
authors.lastname: Tan
authors.forename: Nan
authors.initials: N
authors.lastname: Li
mesh_terms: D000276:Adjuvants, Immunologic / Q000008:administration & dosage / Q000493:pharmacokinetics; D000279:Administration, Cutaneous; D000634:Aminoquinolines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems; D004355:Drug Stability; D006801:Humans; D000077271:Imiquimod; D066298:In Vitro Techniques; D055623:Keratosis, Actinic / Q000188:drug therapy; D008081:Liposomes / Q000737:chemistry; D008297:Male; D018613:Microscopy, Confocal; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry; D010316:Particle Size; D010539:Permeability; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D034421:Sus scrofa
chemical_list: D000276:Adjuvants, Immunologic; D000634:Aminoquinolines; D004337:Drug Carriers; D008081:Liposomes; D053769:Nanocapsules; D000077271:Imiquimod