Research paperPEGylated liposomes for topical vaginal therapy improve delivery of interferon alpha

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 ± 8 nm, bearing a negative zeta potential of - 13 mV 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.

Schematic drawing of PEGylated liposome and the IFN α-2b partitioning after 8 h ex vivo penetration experiment. *IFN α-2b in Intron A buffer.124