Jøraholmen May Wenche, Basnet Purusotam, Acharya Ganesh, Škalko-Basnet Nataša
Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Universitetsveien 57, 9037 Tromsø, Norway.
Women's Health and Perinatology Research Group, Department of Clinical Medicine, University of Tromsø The Arctic University of Norway, Universitetsveien 57, 9037 Tromsø, Norway; Department of Obstetrics and Gynecology, University Hospital of North Norway, Sykehusveien 5738, 9038 Tromsø, Norway.
Eur J Pharm Biopharm. 2017 Apr;113:132-139. doi: 10.1016/j.ejpb.2016.12.029. Epub 2017 Jan 11.
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.
近期有关黏膜给药的研究表明，具有表面可利用聚乙二醇（PEG）的纳米系统能够穿透黏液屏障，确保与上皮细胞更紧密接触，并改善药物向阴道的递送。在本研究中，我们制备了含有干扰素α-2b（IFN α-2b）的可穿透黏液的聚乙二醇化脂质体，旨在为人乳头瘤病毒（HPV）阴道感染提供局部治疗。聚乙二醇化脂质体的平均粒径为181±8nm，ζ电位为 - 13mV，包封率为81±10%。在模型膜上进行的体外释放实验表明，对照品和脂质体结合的IFN α-2b几乎均无IFN α-2b释放。然而，对从怀孕绵羊获得的阴道组织进行的离体渗透研究表明，与对照相比，聚乙二醇化脂质体的IFN α-2b渗透明显增加。此外，黏蛋白研究证实聚乙二醇修饰的脂质体与黏蛋白之间不存在相互作用，证实了它们穿透黏液并到达更深层上皮细胞的能力。该系统有望通过增强局部抗病毒治疗的疗效来改善IFN α-2b的局部递送。
