Microsponges enriched gel for enhanced topical delivery of 5-fluorouracil

Abstract

This study aimed to develop microsponges based topical gel formulation of 5-Fluorouracil (5-FU) for the treatment of skin cancer with enhanced skin deposition and reduced skin irritation potential. Microsponges were prepared by Quasi-emulsion solvent diffusion method using ethyl cellulose and Eudragit RL 30 D; and was optimised through detailed in vitro characterisation. Brunauer–Emmett–Teller (BET) analysis demonstrated higher surface area (2.4393 m²/g) and pore volume of developed microsponges formulation. Optimised formulation showed better thixotropic and texture properties compared to commercial cream formulation, used as control for comparison purpose. Further, the optimised formulation demonstrated 5.5-fold increase in skin deposition documented via in-vivo local bioavailability study, with significant reduction in skin irritation compared to the commercial formulation. Hence, the developed microsponges based formulation seems to be a viable alternative with enhanced topical delivery of 5-FU as compared to the commercial formulation.

Keywords:

• 5-Flurouracil
• microsponges
• skin targeting
• drug deposition
• anti-cancer activity
• skin irritation

Acknowledgements

Authors are also grateful to Department of Science and Technology, Fund for Improvement of S&T Infrastructure (DST-FIST) to Department of Pharmaceutical sciences. Authors are thankful to Shalaks pharmaceutical for providing 5-FU.

Disclosure statement

The authors declare that there are no conflict of interest in this work.

Additional information

Funding

The authors are thankful to UGC, New Delhi for granting (University with potential for excellence status) to Guru Nanak Dev University and providing the grant for establishment of centre of emerging life sciences. Authors are also grateful to Department of Science and Technology, New Delhi for providing the financial support under the project no. EMR/2007/0033648.