In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine

Colloids Surf B Biointerfaces. 2020 Apr:188:110739. doi: 10.1016/j.colsurfb.2019.110739. Epub 2019 Dec 17.

Abstract

This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 μm, respectively, polydispersity index (PDI) < 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant.

Keywords: Eucalyptus oil; Microemulsion; Microemulsion-gel; Polymer; Transdermal film; Zidovudine.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Emulsions / administration & dosage
  • Emulsions / chemistry
  • Emulsions / metabolism
  • Eucalyptus Oil / administration & dosage
  • Eucalyptus Oil / chemistry
  • Eucalyptus Oil / metabolism
  • Gels / administration & dosage
  • Gels / chemistry
  • Gels / metabolism
  • Male
  • Methylcellulose / administration & dosage
  • Methylcellulose / chemistry*
  • Methylcellulose / metabolism
  • Particle Size
  • Prodrugs / administration & dosage
  • Prodrugs / chemistry*
  • Prodrugs / metabolism
  • Propylene Glycol / administration & dosage
  • Propylene Glycol / chemistry
  • Propylene Glycol / metabolism
  • Rats
  • Rats, Wistar
  • Skin / chemistry
  • Skin / metabolism
  • Skin Absorption
  • Surface Properties
  • Zidovudine / administration & dosage
  • Zidovudine / chemistry*
  • Zidovudine / metabolism

Substances

  • Emulsions
  • Gels
  • Prodrugs
  • Eucalyptus Oil
  • Zidovudine
  • Propylene Glycol
  • Methylcellulose