Thermosensitive hydrogel of hydrophobically-modified methylcellulose for intravaginal drug delivery

J Mater Sci Mater Med. 2012 Aug;23(8):1913-9. doi: 10.1007/s10856-012-4664-9. Epub 2012 May 9.

Abstract

Hydrogels with the advantages of prolonging drug release and administration convenience are necessary for intravaginal drug delivery to prevent sexual transmission of human immunodeficiency virus and other vaginal infections. In this study, the thermosensitive hydrogel of methylcellulose modified by stearic acid (MCS) were evaluated in the presence of NaCl and phosphates, which exhibited sol-to-gel transition performance at body temperature or even lower. The in vitro cytotoxicity and in vivo mucosal irritation were investigated and the results showed that MCS hydrogel possessed good biocompatibility similar with hydroxyethyl cellulose (HEC) gel. Significantly, the release studies revealed that MCS hydrogel could control tenofovir sustained release for 10 h without burst release, longer than that from HEC gel or poloxamer 407 hydrogel. Therefore, MCS thermosensitive hydrogel would be a promising carrier for intravaginal delivery of antiviral drugs for long time controlled release.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives*
  • Adenine / chemistry
  • Administration, Intravaginal
  • Animals
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / chemistry
  • Cells, Cultured
  • Delayed-Action Preparations / administration & dosage*
  • Delayed-Action Preparations / chemical synthesis*
  • Diffusion
  • Female
  • Hot Temperature
  • Hydrogels / chemical synthesis*
  • Hydrophobic and Hydrophilic Interactions
  • Materials Testing
  • Methylcellulose / chemical synthesis*
  • Organophosphonates / administration & dosage*
  • Organophosphonates / chemistry
  • Rabbits
  • Tenofovir
  • Vaginosis, Bacterial / drug therapy*
  • Vaginosis, Bacterial / pathology

Substances

  • Anti-HIV Agents
  • Delayed-Action Preparations
  • Hydrogels
  • Organophosphonates
  • Methylcellulose
  • Tenofovir
  • Adenine