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

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Article · Volume 59, Issue 2 · pp. 602–616

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

Navneet Mehan1, Vipin Saini1, Kumar Manish2, Manoj Goyal3, Sheetal Devi1, Shinu Pottathil4, Shery Jacob5, Anroop B Nair6

  1. 1M.M. College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Haryana, INDIA.
  2. 2Department of Pharmaceutics, ISF College of Pharmacy, Moga, Punjab, INDIA.
  3. 3Department of Anesthesia Technology, College of Applied Medical Sciences in Jubail, Imam Abdul Rahman Bin Faisal University, Jubail, SAUDI ARABIA.
  4. 4Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, SAUDI ARABIA.
  5. 5Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman, UNITED ARAB EMIRATES.
  6. 6Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, SAUDI ARABIA.

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 vitrodrug 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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