PEGylated liposomes for topical vaginal therapy improve delivery of interferon alpha

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.

Utilizing Liposomal Quercetin and Gallic Acid in Localized Treatment of Vaginal Candida Infections

“…The in vitro polyphenol release studies were performed by using Franz diffusion cells (1.77 cm 2 diffusion area, 12 mL acceptor volume; PermeGear, Bethlehem, PA, USA) [29] equipped with a V6A Stirrer (PermeGear, Bethlehem, PA, USA). The heating circulator (Julabo Laboratechnik, F12-ED, Seelbach, Germany) was set to maintain a temperature of 37 • C. To mimic the vaginal pH [30], the Pharmaceutics 2020, 12, 9 5 of 21 acceptor chambers were filled with phosphate buffer pH 4.5 and ethanol was added at the final concentration of 20% (v/v) [31][32][33] to ensure sink conditions during the study (the solubility of Q and GA in the releasing conditions was found to be 0.226 ± 0.042 mg/mL and 78.7 ± 3.4 mg/mL, respectively).…”

A Polymer Chemistry Point of View on Mucoadhesion and Mucopenetration

“…Recently, Jøraholmen et al prepared PEG‐coated liposomes intended for local delivery of interferon alpha‐2b (IFN α‐2b) to treat vaginal infections of human papilloma virus. Penetration studies performed on the vaginal tissue obtained from pregnant sheep showed elevated IFN α‐2b penetration from PEG‐coated liposomes (≈40% of the drug penetrated) as compared to the unencapsulated IFN α‐2b (≈10% of the drug penetrated).…”

Vaginal Delivery of Benzydamine Hydrochloride through Liposomes Dispersed in Mucoadhesive Gels

“…Considering optimal mucus-penetration, a nearly neutral vesicle surface charge is desirable to assure mucus-penetrating properties. 25) Liposomes were nanometer in size in the TEM image and appeared to be homogeneously dispersed. But when the particle size was measured, it was found in micrometer size.…”