Development, Characterization and in vivo Localization Study of Topical 5-Fluorouracil Gels: A Comparative Study with Conventional Formulation
Subheet Kumar Jain and Richa Puri
Affiliation: Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, 143 005 India.
5-Fluorouracil (5-FU) is one of the most effective antineoplastic agents used for the treatment of skin cancers
and actinic keratosis (AK). Currently commercial formulation for topical 5-FU administration is available in the form of
solution or cream. Commercial topical formulations are associated with the limitation of very short retention time at the
administration site resulting in very poor skin permeation and deposition of drug. In the present study attempt was made
for the preparation, optimization and characterization of bioadhesive gel formulations for localized delivery of 5-FU. Four
bioadhesive gel formers, Carbopol 934, Carbopol 980, Methylcellulose (MC) and Poloxamer 188 were selected for the
preparation of 5-FU bioadhesive gel formulations. The formulations were characterized for characteristic parameters including
bioadhesive strength, skin deposition and interaction study. Carbopol 934 based bioadhesive gel formulation at
the concentration of 1.5% w/w showed the best physicochemical properties such as viscosity (2670±12.2 cP), which was
similar to the value obtained with the marketed cream (2870±14.4 cP), highest skin deposition (1290±56.4μg) and bioadhesive
strength (18.62 gf). Cutaneous irritation of optimized bioadhesive gel formulations was also tested using the Draize
test and only very slight erythema and no oedema was observed. In comparison, marketed formulation showed well defined
erythema along with oedema formation. The result of the present study demonstrated that formulation of Carbopol
934 based 5-FU bioadhesive gel is a better alternative to the traditional cream base for enhanced topical delivery of 5-FU.
The developed formulation will have the ease of application, better skin deposition and sustained release characteristic
with reduced skin toxicity.
Keywords: Bioadhesive strength, conventional cream, 5-FU, localization index, skin targeting.2
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