PEGylated liposomes for topical vaginal therapy improve delivery of interferon alpha

Eur J Pharm Biopharm. 2017 Apr:113:132-139. doi: 10.1016/j.ejpb.2016.12.029. Epub 2017 Jan 11.

Abstract

Recent studies regarding mucosal drug delivery indicate that nanosystems with surface-available polyethylene glycol (PEG) are able to penetrate mucus barrier, assure closer contact with the epithelium, and improve drug delivery to vagina. In the present work, we developed the mucus-penetrating PEGylated liposomes containing interferon alpha-2b (IFN α-2b), destined to provide localized therapy for human papilloma virus (HPV) vaginal infections. The PEGylated liposomes were of a mean size of 181±8nm, bearing a negative zeta potential of - 13mV and an entrapment efficiency of 81±10%. In vitro release experiments on model membrane showed a nearly non-existent IFN α-2b release from both the control and liposomally-associated IFN α-2b. However, the ex vivo penetration studies performed on the vaginal tissue obtained from pregnant sheep, showed the clear elevated IFN α-2b penetration from PEGylated liposomes as compared to the control. Furthermore, mucin studies confirmed the absence of interaction between the PEG-modified liposomes and mucin, confirming their ability to penetrate mucus and reach the deeper epithelium. The system holds a promise in improving topical delivery of IFN α-2b through enhanced efficacy of local anti-viral therapy.

Keywords: Human papilloma virus; Interferon; Mucus-penetrating liposomes; PEGylated liposomes; Vaginal therapy.

MeSH terms

  • Administration, Topical
  • Animals
  • Drug Administration Routes*
  • Female
  • Humans
  • Interferon alpha-2
  • Interferon-alpha / administration & dosage*
  • Liposomes*
  • Male
  • Polyethylene Glycols / chemistry*
  • Recombinant Proteins / administration & dosage
  • Sheep
  • Vagina*

Substances

  • Interferon alpha-2
  • Interferon-alpha
  • Liposomes
  • Recombinant Proteins
  • Polyethylene Glycols