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

Abstract

Resveratrol (RES), chemically known as 3,5,4'-trihydroxy-transstilbene, is a promising multi-targeted anti-oxidative and antiinflammatory 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 antiinflammatory activities were compared by measuring nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-1β production in LPSinduced J774A.1 cells. Liposomal RES was found to exhibit stronger antioxidative and anti-inflammatory activities than RES solution. Resveratrol (RES), chemically known as 3,5,4'-trihydroxy-trans-stilbene, is a 18 promising multi-targeted anti-oxidative and anti-inflammatory natural polyphenol. Preclinical 19 studies showed its biological activities against the pathogens of sexually transmitted diseases 20 causing vaginal inflammation and infections. Due to its low solubility and poor 21 bioavailability, the optimal therapeutic uses are limited. Therefore, a clinically acceptable 22 topical vaginal formulation of RES exhibiting optimal therapeutic effects is highly desirable. 7Corrections were made accordingly as mentioned on page 8, lines 210-217. 8 9Please discuss the possibility for using other polymers instead of chitosan. 11Some discussion was added on page 18, lines 551-555 12 13Spelling error -page 7, section 2.7., should be "Characterization…" instead of

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