Layer-by-layer vaginal films for acyclovir controlled release to prevent genital herpes

Int J Pharm. 2022 Nov 5:627:122239. doi: 10.1016/j.ijpharm.2022.122239. Epub 2022 Sep 27.

Abstract

Genital herpes is one of the most common sexually transmitted infections worldwide. It mainly affects women, as the rate of sexual transmission from male-to-female is higher than from female-to-male. The application of vaginal antivirals drugs could reduce the prevalence of genital herpes and prevent future infections. Layer-by-layer vaginal films were prepared by the solvent evaporation method using iota-carrageenan, hydroxypropyl methylcellulose and the polymethacrylates Eudragit® RS PO and Eudragit® S100, for the controlled release of acyclovir. The films were characterized by texture analysis and Raman spectroscopy. Swelling, mucoadhesion, and drug release studies were conducted in simulated vaginal fluid. The results show that Layer-by-Layer films exhibited adequate mechanical properties. The structuring of the layer-by-layer films allowed the controlled release of acyclovir and produced a prolonged mucoadhesion residence time of up to 192 h. The films formed in layer 2 by the combination of Eudragit® RS PO and S100 showed a controlled release of acyclovir for eight days, and adequate mechanical properties. These promising formulations for the prevention of genital herpes deserve further evaluation.

Keywords: Acyclovir controlled release; Genital herpes; Hydroxypropyl methylcellulose; Iota-carrageenan; Layer-by-layer film; Marine polymers.

MeSH terms

  • Acyclovir*
  • Antiviral Agents
  • Carrageenan
  • Delayed-Action Preparations / therapeutic use
  • Female
  • Herpes Genitalis* / drug therapy
  • Herpes Genitalis* / prevention & control
  • Humans
  • Hypromellose Derivatives / chemistry
  • Male
  • Solvents

Substances

  • Acyclovir
  • methylmethacrylate-methacrylic acid copolymer
  • Hypromellose Derivatives
  • Delayed-Action Preparations
  • Carrageenan
  • Antiviral Agents
  • Solvents