Formulation, Characterization and in vivo Evaluation of 5-Fluorouracil-Loaded Polymeric Micelles for Non-Melanoma Skin Cancer

Indian Journal of Pharmaceutical Education and Research

  • Navneet Mehan1M.M. College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Haryana, INDIA.
  • Vipin Saini1M.M. College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Haryana, INDIA.
  • Kumar Manish2Department of Pharmaceutics, ISF College of Pharmacy, Moga, Punjab, INDIA.
  • Manoj Goyal3Department of Anesthesia Technology, College of Applied Medical Sciences in Jubail, Imam Abdul Rahman Bin Faisal University, Jubail, SAUDI ARABIA.
  • Sheetal Devi1M.M. College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Haryana, INDIA.
  • Shinu Pottathil4Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, SAUDI ARABIA.
  • Shery Jacob5Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman, UNITED ARAB EMIRATES.
  • Anroop B Nair6Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, SAUDI ARABIA.

Volume 59 Issue 2 Pages 602-616

DOI: 10.5530/ijper.20251736

Abstract

Background: The goal of the study was to evaluate the prospective of fluorouracil-loaded polymeric micelles for topical delivery in non-melanoma skin cancer. Materials and Methods: Polymeric micelles were developed by thin film hydration technique and characterized for physico-chemical properties, in vitro drug release, ex vivo skin penetration as well as in vivo skin irritation and anticancer effect. Results: Preliminary studies were carried out in twelve Formulations (FM1-FM12) and the Formulation (FM4) with the highest entrapment efficiency (~95%) and greater drug release (~98%) was developed into gels (FG1-FG5). The selected gel Formulation (FG4) exhibited adequate viscosity (~5000 cP), ideal pH (~6.8), higher drug content (~79%), greater drug permeation (~70%) and good stability for three months. In vivo skin irritation results indicated the developed formulation is non-irritant. MTT assay indicates dose-dependent effect of FG4 with IC50 of 15.56 μg/mL. Anti-cancer activity assessed in rat models indicates the prominent reduction in tumor burden (volume) by 80% following application of fluorouracil-loaded micellar gel for 1 month. The histopathological study further confirms the activity of developed gel in melanoma skin cancer. Conclusion: The data observed suggests that the polymeric micelles could be a feasible option for delivering fluorouracil in the treatment of basal-cell carcinoma.

Keywords

  • Drug release
  • Fluorouracil
  • Polymeric micelles
  • Rats
  • Skin carcinoma.
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