title: Resveratrol-loaded liposomes for topical treatment of the vaginal inflammation and infections.
abstract: Resveratrol (RES), chemically known as 3,5,4'-trihydroxy-trans-stilbene, is a promising multi-targeted anti-oxidative and anti-inflammatory natural polyphenol. Preclinical studies showed its biological activities against the pathogens of sexually transmitted diseases causing vaginal inflammation and infections. Due to its low solubility and poor bioavailability, the optimal therapeutic uses are limited. Therefore, a clinically acceptable topical vaginal formulation of RES exhibiting optimal therapeutic effects is highly desirable. For this purpose, we prepared and optimized chitosan-coated liposomes with RES. The coated vesicles (mean diameter 200nm) entrapped up to 77% of RES, a sufficient load to assure required therapeutic outcome. In vitro drug release study showed the ability of liposomes to provide sustained release of RES. In vitro anti-oxidative activities of RES, namely DPPH and ABTS(•+) radicals scavenging assays, confirmed RES to be as potent as standard anti-oxidants, vitamins C and E. The anti-oxidative activities of RES and its corresponding liposomal formulation were also compared by measuring enhanced superoxide dismutase (SOD) activities in lipopolysaccharide (LPS)-induced J774A.1 cells. In vitro anti-inflammatory activities were compared by measuring nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-1β production in LPS-induced J774A.1 cells. Liposomal RES was found to exhibit stronger anti-oxidative and anti-inflammatory activities than RES solution.
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, Tromsø, Norway. Electronic address: may.w.joraholmen@uit.no.
authors.forename: May Wenche
authors.initials: MW
authors.lastname: Jøraholmen
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, Tromsø, Norway. Electronic address: natasa.skalko-basnet@uit.no.
authors.forename: Nataša
authors.initials: N
authors.lastname: Škalko-Basnet
authors.affiliation: Department of Obstetrics and Gynecology, University Hospital of North Norway, Tromsø, Norway; Women's Health and Perinatology Research Group, Department of Clinical Medicine, Tromsø, Norway. Electronic address: ganesh.acharya@uit.no.
authors.forename: Ganesh
authors.initials: G
authors.lastname: Acharya
authors.affiliation: Department of Obstetrics and Gynecology, University Hospital of North Norway, Tromsø, Norway; Women's Health and Perinatology Research Group, Department of Clinical Medicine, Tromsø, Norway. Electronic address: purusotam.basnet@uit.no.
authors.forename: Purusotam
authors.initials: P
authors.lastname: Basnet
mesh_terms: D000282:Administration, Intravaginal; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000627:therapeutic use; D000975:Antioxidants / Q000008:administration & dosage / Q000627:therapeutic use; D002460:Cell Line; D005260:Female; D053583:Interleukin-1beta / Q000378:metabolism; D008081:Liposomes / Q000008:administration & dosage*; D051379:Mice; D000077185:Resveratrol; D013267:Stilbenes / Q000008:administration & dosage* / Q000627:therapeutic use; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism; D014627:Vaginitis / Q000188:drug therapy*; D016585:Vaginosis, Bacterial / Q000188:drug therapy
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D053583:Interleukin-1beta; D008081:Liposomes; D013267:Stilbenes; D014409:Tumor Necrosis Factor-alpha; D000077185:Resveratrol
keywords: 1,1-Diphenyl-2-picrylhydrazyl (DPPH); 2,2′-Azino-bis(3-ethyl benzothiazoline)-6-sulfonic acid diammonium salt (ABTS); 3,5,4′-Trihydroxy-trans-stilbene; Anti-inflammatory; Anti-oxidant; Chitosan; L-nitro-arginine methyl ester (NAME); Liposomes; Mucoadhesive; Phosphatidylcholine; Resveratrol; Resveratrol (3,5,4′-trihydroxy-trans-stilbene); Vaginal infections; Vitamin C (ascorbic acid); Vitamin E (α-tocopherol)