Development of liposome gel based formulations for intravaginal delivery of the recombinant HIV-1 envelope protein CN54gp140

Eur J Pharm Sci. 2012 Aug 15;46(5):315-22. doi: 10.1016/j.ejps.2012.02.003. Epub 2012 Feb 15.

Abstract

Mucosally-administered vaccine strategies are widely investigated as a promising means of preventing HIV infection. This study describes the development of liposomal gel formulations, and novel lyophilised variants, comprising HIV-1 envelope glycoprotein, CN54gp140, encapsulated within neutral, positively charged or negatively charged liposomes. The CN54gp140 liposomes were evaluated for mean vesicle diameter, polydispersity, morphology, zeta potential and antigen encapsulation efficiency before being incorporated into hydroxyethyl cellulose (HEC) aqueous gel and subsequently lyophilised to produce a rod-shaped solid dosage form for practical vaginal application. The lyophilised liposome-HEC rods were evaluated for moisture content and redispersibility in simulated vaginal fluid. Since these rods are designed to revert to gel form following intravaginal application, mucoadhesive, mechanical (compressibility and hardness) and rheological properties of the reformed gels were evaluated. The liposomes exhibited good encapsulation efficiency and the gels demonstrated suitable mucoadhesive strength. The freeze-dried liposome-HEC formulations represent a novel formulation strategy that could offer potential as stable and practical dosage form.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • AIDS Vaccines / administration & dosage
  • AIDS Vaccines / chemistry*
  • AIDS Vaccines / immunology
  • Adhesiveness
  • Administration, Intravaginal
  • Animals
  • Cellulose / analogs & derivatives
  • Cellulose / chemistry
  • Chemistry, Pharmaceutical
  • Compressive Strength
  • Drug Compounding
  • Female
  • Freeze Drying
  • Gels
  • Hardness
  • Lipids / chemistry*
  • Liposomes
  • Mice
  • Mucins / metabolism
  • Recombinant Proteins / chemistry
  • Rheology
  • Surface Properties
  • Technology, Pharmaceutical / methods
  • Vaccines, Synthetic / chemistry
  • env Gene Products, Human Immunodeficiency Virus / administration & dosage
  • env Gene Products, Human Immunodeficiency Virus / chemistry*
  • env Gene Products, Human Immunodeficiency Virus / immunology

Substances

  • AIDS Vaccines
  • Gels
  • Lipids
  • Liposomes
  • Mucins
  • Recombinant Proteins
  • Vaccines, Synthetic
  • env Gene Products, Human Immunodeficiency Virus
  • gp140 envelope protein, Human immunodeficiency virus 1
  • Cellulose
  • hydroxyethylcellulose