Reimer K, Fleischer W, Brögmann B, Schreier H, Burkhard P, Lanzendörfer A, Gümbel H, Hoekstra H, Behrens-Baumann W
Mundipharma GmbH, Limburg, Germany.
Dermatology. 1997;195 Suppl 2:93-9. doi: 10.1159/000246039.
In recent years, liposomes have been increasingly explored as novel drug delivery systems, and several liposome-based drug products have been approved in Europe, the USA and Japan. Depending on size, composition and surface characteristics, liposomes interact specifically with biological structures. Liposomal drug products provide a topical activity at the desired locus of action and are deemed more effective and less toxic than conventional drug formulations. The combination of povidone-iodine (PVP-I) and liposomes unites the exceptional microbicidal activity of the antiseptic substance with the excellent tolerability and lack of immunogenicity of liposomes; in addition, liposomes provide a moist molecular film for the wound environment. The multilamellar vesicles act as microreservoirs hence prolonging the release of the active ingredient. Although no commercial product for repeated application on the eye is currently available, PVP-I has been used in ophthalmology not only for pre- and postoperative antisepsis, but also for the treatment of bacterial and viral conjunctivitis and for prophylaxis against ophthalmia neonatorum. For these indications, liposomal formulations with 2.5 and 5.0% PVP-I were developed. These eye drops are isotonic with tear fluid at pH 6. First in vitro tests demonstrated an excellent antimicrobial efficacy, and a placebo-controlled clinical study on volunteers showed a very good local tolerability. A study on rabbits demonstrated positive results of the PVP-I liposome eye drops compared to placebo and the broadspectrum antibiotic Polyspectran in a standardized model of Staphylococcus aureus deep eye infection. The other aim is a well-tolerated liposomal PVP-I hydrogel for improved antiseptic wound treatment with moisturizer. It has been reported that liposomes are enriched at the wound bottom for direct action against infection and support of wound healing. An animal study on the efficacy and tolerability of different formulations of a hydrogel with PVP-I liposomes in deep dermal burn wounds has indicated an outstanding quality of wound healing with smooth granulation tissue, less inflammation, less wound contraction and no hyperkeratotic reactivity, especially with the 3% PVP-I liposome formulation.
近年来,脂质体作为新型药物递送系统得到了越来越多的研究,并且几种基于脂质体的药物产品已在欧洲、美国和日本获得批准。根据大小、组成和表面特性,脂质体与生物结构发生特异性相互作用。脂质体药物产品在所需作用部位具有局部活性,并且被认为比传统药物制剂更有效且毒性更小。聚维酮碘(PVP-I)与脂质体的结合将防腐剂的卓越杀菌活性与脂质体的优异耐受性和无免疫原性结合在一起;此外,脂质体为伤口环境提供了一层湿润的分子膜。多层囊泡充当微储库,从而延长活性成分的释放。虽然目前尚无用于眼部重复给药的商业产品,但PVP-I已在眼科中使用,不仅用于术前和术后防腐,还用于治疗细菌性和病毒性结膜炎以及预防新生儿眼炎。针对这些适应症,开发了含2.5%和5.0% PVP-I的脂质体制剂。这些眼药水在pH 6时与泪液等渗。首次体外试验证明了其优异的抗菌效果,一项针对志愿者的安慰剂对照临床研究显示了非常好的局部耐受性。一项针对兔子的研究表明,在金黄色葡萄球菌深部眼部感染的标准化模型中,与安慰剂和广谱抗生素Polyspectran相比,PVP-I脂质体眼药水有阳性结果。另一个目标是开发一种耐受性良好的脂质体PVP-I水凝胶,用于改善防腐伤口治疗并带有保湿剂。据报道,脂质体在伤口底部富集,可直接对抗感染并支持伤口愈合。一项关于含PVP-I脂质体的水凝胶不同制剂在深度真皮烧伤伤口中的疗效和耐受性的动物研究表明,伤口愈合质量出色,有光滑的肉芽组织,炎症较少,伤口收缩较少且无角化过度反应,特别是3% PVP-I脂质体制剂。