Encapsulation of Mentha Oil in Chitosan Polymer Matrix Alleviates Skin Irritation

AAPS PharmSciTech. 2016 Apr;17(2):482-92. doi: 10.1208/s12249-015-0378-x. Epub 2015 Aug 8.

Abstract

Mentha spicata L. var. viridis oil (MVO) is a potent antifungal agent, but its application in the topical treatment is limited due to its irritancy and volatility. It was aimed to develop more efficient, chitosan-incrusted MVO microspheres with reduced volatility and lesser irritancy and to dispense it in the form of ointment. Simple coacervation technique was employed to microencapsulate MVO in chitosan matrix. Morphological properties and polymer cross-linking were characterized by scanning electron microscopy and differential scanning calorimetry, respectively. Optimization was carried out on the basis of entrapment efficiency (EE) using response surface methodology. Well-designed microspheres having smooth surface and spherical shape were observed. EE (81.20%) of optimum batch (R21) was found at 1.62% w/v of cross-linker, 5.4:5 of MVO to chitosan ratio and at 1000 rpm. R21 showed 69.38 ± 1.29% in vitro MVO release in 12 h and 96.92% retention of MVO in microspheres even after 8 week. Ointments of PEG 4000 and PEG 400 comprising MVO (F1) and R21 (F2) were developed separately. F2 showed comparatively broader zone of growth inhibition (13.33 ± 1.76-18.67 ± 0.88 mm) and less irritancy (PII 0.5833, irritation barely perceptible) than that of F1. F2 was able to avoid the direct contact of mild irritant MVO with the skin and to reduce its rapid volatility. Controlled release of MVO helped in lengthening the duration of availability of MVO in agar media and hence improved its therapeutic efficacy. In conclusion, a stable and non-irritant formulation with improved therapeutic potential was developed.

Keywords: Candida; anti-fungal; essential oil; microspheres; primary irritation index.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Calorimetry, Differential Scanning / methods
  • Chemistry, Pharmaceutical / methods
  • Chitosan / chemistry*
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / chemistry
  • Drug Compounding / methods
  • Female
  • Male
  • Mentha / chemistry*
  • Microscopy, Electron, Scanning / methods
  • Microspheres
  • Ointments / administration & dosage
  • Ointments / chemistry
  • Particle Size
  • Plant Oils / administration & dosage*
  • Plant Oils / chemistry*
  • Polymers / chemistry*
  • Rabbits
  • Skin / drug effects*
  • Skin / microbiology

Substances

  • Delayed-Action Preparations
  • Ointments
  • Plant Oils
  • Polymers
  • Chitosan