Microemulsion-based gel of fluorouracil for transdermal delivery.
- Author:
Yan-Yu XIAO
1
;
Fang LIU
;
Zhi-Peng CHEN
;
Qi-Neng PING
Author Information
1. Department ofPharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Administration, Cutaneous;
Animals;
Antimetabolites, Antineoplastic;
administration & dosage;
adverse effects;
pharmacokinetics;
Dioctyl Sulfosuccinic Acid;
Drug Carriers;
Drug Delivery Systems;
Emulsions;
Exanthema;
chemically induced;
Fluorouracil;
administration & dosage;
adverse effects;
pharmacokinetics;
Gelatin;
chemistry;
Male;
Mice;
Myristates;
chemistry;
Polysorbates;
chemistry;
Skin;
pathology;
Skin Absorption;
Succinates;
chemistry;
Surface-Active Agents;
Viscosity
- From:
Acta Pharmaceutica Sinica
2010;45(11):1440-1446
- CountryChina
- Language:Chinese
-
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.
