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.
Research group for Host-Microbe Interaction, Department of Medical Biology, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Sykehusveien 44, 9037 Tromsø, Norway.
Mar Drugs. 2020 Jan 31;18(2):96. doi: 10.3390/md18020096.
Topical administration of drugs into the vagina can provide local therapy of vaginal infections, preventing the possible systemic side effects of the drugs. The natural polysaccharide chitosan is known for its excellent mucoadhesive properties, safety profile, and antibacterial effects, and thus it can be utilized in improving localized vaginal therapy by prolonging the residence time of a drug at the vaginal site while acting as an antimicrobial in synergy. Therefore, we aimed to explore the potential of chitosan, namely chitosan-coated liposomes and chitosan hydrogel, as an excipient with intrinsic antimicrobial properties. Liposomes were prepared by the thin-film hydration method followed by vesicle size reduction by sonication to the desired size, approximately 200 nm, and coated with chitosan (0.01, 0.03, 0.1, and 0.3%, w/v, respectively). The mucoadhesive properties of chitosan-coated liposomes were determined through their binding efficiency to mucin compared to non-coated liposomes. Non-coated liposomal suspensions were incorporated in chitosan hydrogels forming the liposomes-in-hydrogel formulations, which were further assessed for their texture properties in the presence of biological fluid simulants. The antibacterial effect of chitosan-coated liposomes (0.03%, 0.1% and 0.3%, w/v) and chitosan hydrogels (0.1% and 0.3%, w/w) on and was successfully confirmed.
将药物局部施用于阴道可以提供阴道感染的局部治疗,防止药物可能产生的全身副作用。天然多糖壳聚糖以其极好的粘膜粘附特性、安全性和抗菌作用而闻名,因此可以通过延长药物在阴道部位的停留时间,同时协同发挥抗菌作用,来改善局部阴道治疗。因此,我们旨在探索壳聚糖(即壳聚糖包被的脂质体和壳聚糖水凝胶)作为具有内在抗菌性能的赋形剂的潜力。脂质体通过薄膜水化法制备,然后通过超声处理将囊泡减小至所需的大小,约 200nm,并包被壳聚糖(分别为 0.01%、0.03%、0.1%和 0.3%,w/v)。通过比较与非包被脂质体的结合效率,确定壳聚糖包被脂质体的粘膜粘附特性。将非包被的脂质体混悬液掺入壳聚糖水凝胶中,形成脂质体-水凝胶制剂,并进一步在生物流体模拟物存在的情况下评估其质地特性。成功证实了壳聚糖包被脂质体(0.03%、0.1%和 0.3%,w/v)和壳聚糖水凝胶(0.1%和 0.3%,w/w)对 和 的抗菌作用。