Design, Development, and Characterization of Imiquimod-Loaded Chitosan Films for Topical Delivery

AAPS PharmSciTech. 2019 Jan 8;20(2):58. doi: 10.1208/s12249-018-1288-5.

Abstract

Aldara™ (5% w/w imiquimod) topical cream is approved by the US FDA for the treatment of superficial basal cell carcinoma. However, the cream formulation suffers from dose variability, low drug availability due to the incomplete release, and poor patient compliance. To achieve sustained and complete release of imiquimod, chitosan films were prepared by casting using propylene glycol as a plasticizer. Chitosan films had appropriate physicochemical characteristics for wound dressing and excellent content uniformity and maintained the original physical form of imiquimod. Films were capable of releasing a defined dose of imiquimod over a period of 7 days. The bioactivity of imiquimod was not affected by its entrapment in chitosan matrix as indicated by the results of in vitro growth inhibition assay. In addition, the film formulation showed significantly (p ˂ 0.05) higher drug accumulation in the skin when compared to commercial cream formulation.

Keywords: basal cell carcinoma; chitosan; film formulation; imiquimod; topical drug delivery.

MeSH terms

  • Adjuvants, Immunologic / administration & dosage
  • Adjuvants, Immunologic / chemistry
  • Adjuvants, Immunologic / pharmacokinetics
  • Administration, Topical
  • Chitosan / administration & dosage
  • Chitosan / chemistry*
  • Chitosan / pharmacokinetics
  • Drug Delivery Systems / methods*
  • Drug Design*
  • Drug Liberation / drug effects
  • Drug Liberation / physiology
  • Humans
  • Imiquimod / administration & dosage
  • Imiquimod / chemistry*
  • Imiquimod / pharmacokinetics
  • Organ Culture Techniques
  • Skin Absorption / drug effects*
  • Skin Absorption / physiology

Substances

  • Adjuvants, Immunologic
  • Chitosan
  • Imiquimod