title: [Microemulsion-based gel of fluorouracil for transdermal delivery].
abstract: This study is to prepare the microemulsion-based gel based on the W/O microemulsion and fluorouracil (5-Fu) as a model drug to study the transdermal characterization and observe its skin irritation of the microemulsion-based gel in vitro. IPM acted as oil phase, AOT as surfactant, Tween 85 as cosurfactant, water was added dropwise to the oil phase to prepare W/O microemulsion at room temperature using magnetic stirring, then 5-Fu powder was added. The gelatin was used as substrate to prepare 5-Fu microemulsion-based gel. The permeation flux of 5-Fu from 5-Fu microemulsion-based gel across excised mice skin was determined in vitro using Franz diffusion cell to study the influence of the amount of gelatin and the drug loading capacity. Refer to 5-Fu cream, the irritation of microemulsion and microemulsion-based gel on the rat skin was studied. Based on the water/AOT/Tween 85/IPM microemulsion, only the gelatin can form the microemulsion-based gel. At 25 degrees C, 32 degrees C and 40 degrees C, the amount of gelatin required for the formation of microemulsion-based gel were 7%, 14% and more than 17%, respectively. The 12 h transdermal cumulated permeation amount of 5-Fu from microemulsion-based gel containing 14% gelatin and 0.5% drug loading were (876.5 +/- 29.1) microg x cm(-2), 12.3 folds and 4.5 folds more than 0.5% 5-Fu aqueous solution and 2.5% (w/w) 5-Fu cream, respectively. Microemulsion-based gel exhibited some irritation, but could be subsided after drug withdrawal. Microemulsion-based gel may be a promising vehicle for transdermal delivery of 5-Fu and other hydrophilic drug.
authors.affiliation: Department ofPharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Yan-Yu
authors.initials: YY
authors.lastname: Xiao
authors.forename: Fang
authors.initials: F
authors.lastname: Liu
authors.forename: Zhi-Peng
authors.initials: ZP
authors.lastname: Chen
authors.forename: Qi-Neng
authors.initials: QN
authors.lastname: Ping
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D004143:Dioctyl Sulfosuccinic Acid; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004655:Emulsions; D005076:Exanthema / Q000139:chemically induced; D005472:Fluorouracil / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D005780:Gelatin / Q000737:chemistry; D008297:Male; D051379:Mice; D009226:Myristates / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D012867:Skin / Q000473:pathology; D012869:Skin Absorption; D013386:Succinates / Q000737:chemistry; D013501:Surface-Active Agents; D014783:Viscosity
chemical_list: D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D004655:Emulsions; D009226:Myristates; D011136:Polysorbates; D013386:Succinates; D013501:Surface-Active Agents; C008205:isopropyl myristate; D004143:Dioctyl Sulfosuccinic Acid; D005780:Gelatin; D005472:Fluorouracil