Resveratrol-loaded liposomes for topical treatment of the vaginal inflammation and infections

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• 作者：May Wenche Jø ; raholmen^a ; ^{may.w.joraholmen@uit.no" class="auth_mail" title="E-mail the corresponding author} ; Nata&scaron ; a &Scaron ; kalko-Basnet^a ; ^{natasa.skalko-basnet@uit.no" class="auth_mail" title="E-mail the corresponding author} ; Ganesh Acharya^b ; ^c ; ^{ganesh.acharya@uit.no" class="auth_mail" title="E-mail the corresponding author} ; Purusotam Basnet^b ; ^c ; ^{purusotam.basnet@uit.no" class="auth_mail" title="E-mail the corresponding author}
• 关键词：ABTS ; 2 ; 2&prime ; -azino-bis(3-ethyl benzothiazoline)-6-sulfonic acid diammonium salt ; CAT ; catalase ; DPPH ; 1 ; 1-diphenyl-2-picrylhydrazyl ; DMSO ; dimethyl sulfoxide ; DMEM ; Dulbecco's modified eagle medium ; GPX ; glutathione peroxidase ; HIV-1 ; human immunodeficiency virus-1 ; HPV ; human papilloma virus ; HSV-2 ; human simplex virus type 2 ; IL-1尾 ; interleukin-1尾 ; iNOS ; inducible nitric oxide synthase ; LPS ; lipopolysaccharide ; L-NAME ; L-nitro-arginine methyl ester ; MDZ ; metronidazole ; NO ; nitric oxide ; PB
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2015
• 出版时间：15 November 2015
• 年：2015
• 卷：79
• 期：Complete
• 页码：112-121
• 全文大小：624 K

文摘

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 200 nm) 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)-伪 and interleukin (IL)-1尾 production in LPS-induced J774A.1 cells. Liposomal RES was found to exhibit stronger anti-oxidative and anti-inflammatory activities than RES solution.