Liposomal Delivery System Enhances Anti-Inflammatory Properties of Curcumin

Basnet, Purusotam; Hussain, Haider; Tho, Ingunn; Škalko‐Basnet, Nataša

doi:10.1002/jps.22785

Cited by 130 publications

(60 citation statements)

References 38 publications

(47 reference statements)

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“…The effects of RES and liposomal RES on SOD activity were measured in LPS-285 induced J774A.1 cells by the similar method as reported previously (Basnet et al, 2012). 286…”

Section: Measurement Of Sod Activity 284mentioning

confidence: 99%

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

Jøraholmen

Škalko‐Basnet

Acharya

et al. 2015

European Journal of Pharmaceutical Sciences

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106

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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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“…The effects of RES and liposomal RES on SOD activity were measured in LPS-285 induced J774A.1 cells by the similar method as reported previously (Basnet et al, 2012). 286…”

Section: Measurement Of Sod Activity 284mentioning

confidence: 99%

“…The effects of RES and liposomal-RES on the production of TNF-α and IL-1β in the 308 LPS-induced J774A.1 cells were measured as reported previously (Basnet et al, 2012). The 309 cell medium were replaced with the medium containing LPS (1 µg/ml) and/or samples (10 310 µg/mL).…”

Section: Effect On Il-1β and Tnf-α Production 307mentioning

confidence: 99%

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

Jøraholmen

Škalko‐Basnet

Acharya

et al. 2015

European Journal of Pharmaceutical Sciences

Self Cite

106

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“…The aim of this work was to determine the in vitro permeabilities of high and low permeable compounds and compare them to the permeabilities obtained with Transwell grown Caco-2 cell monolayers and rat jejunum in side-by-side diffusion chambers. Ultimately, our goal was to use this model as a prognostic tool enabling us the development of suitable liposomes for vaginal delivery of curcumin, which exerts numerous health-beneficial properties (27)(28)(29) but suffers from many pharmacokinetic shortcomings if applied orally (i.e., poor solubility and stability in gastrointestinal fluids, low permeability and extensive presystemic metabolism in the gut and liver; 30,31). Therefore, we prepared liposomes of different sizes containing curcumin, evaluated its permeability from liposomes and characterized potential rate-limiting steps in curcumin vaginal delivery (mechanism of absorption, metabolism, tissue binding, and affinity for mucus).…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of an In Vitro Vaginal Model for Assessment of Drug’s Biopharmaceutical Properties: Curcumin

et al. 2012

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Abstract. Vaginal administration is a promising alternative to the per-oral route in achieving systemic or local therapeutic effects, when intestinal drug absorption is hindered by problematic biopharmaceutical drug properties. The aim of this study was to establish an in vitro vaginal model and use it to characterize biopharmaceutical properties of liposomally associated curcumin destined for vaginal delivery. The in vitro permeability, metabolism, and tissue retention of high/low permeable compounds were assessed on cow vaginal mucosa and compared to the permeabilities determined through Caco-2 cells and rat jejunum in vitro. The results showed that the intestinal mucosa was superior to the vaginal one in categorizing drugs based on their permeabilities in high/low permeable classes. Passive diffusion was found to be the main mechanism of drug penetration through vaginal mucosa and it was not affected by transporterenzyme alliance, as their expression/activity was significantly reduced compared to the intestinal tract. Curcumin permeability from the solution form was the lowest of all tested substances due to its significant tissue retention and curcumin-mucus interactions. The permeability of liposomally associated curcumin was even lower but the binding of liposomally associated curcumin to the vaginal tissue was significantly higher. The permeability and tissue retention of liposomal curcumin were vesicle size dependent. Vaginal application of liposomally associated curcumin provides relatively high levels of curcumin in vaginal tissue, with limited systemic absorption.

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“…As shown in Figure 4A and B, compared with free Cur treatment, cells treated with both C 16 -SS-CSmPEG@Cur and C 16 -CC-CS-mPEG@Cur showed stronger fluorescence in the cytoplasm after 12 h. This may have been because of the drug delivery system enhancing the water solubility of Cur, which led to higher cellular uptake. 25 Meanwhile, there was a significant difference between C 16 -SS-CS-mPEG@Cur and C 16 -CC-CS-mPEG@Cur. Both micelles could be accumulated by Cur rapidly in the cells in 2 h and reached their maximum concentration in 12 h. However, when treated with C 16 -SS-CS-mPEG@Cur they still showed strong fluorescence while fluorescence showed visible decreases when treated with C 16 -CC-CS-mPEG@Cur after 24 h, even remaining obvious after 48 h. These results may have been due to unreleased Cur in C 16 -CC-CSmPEG@Cur being excreted with micelles, in contrast Cur released from C 16 -SS-CS-mPEG@Cur remained in the cells and played a pharmacodynamic role.…”

Section: Intracellular Drug Releasementioning

confidence: 91%

Curcumin-loaded redox response of self-assembled micelles for enhanced antitumor and anti-inflammation efficacy

Zhao

Cao

et al. 2017

IJN

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Liposomal Delivery System Enhances Anti-Inflammatory Properties of Curcumin

Cited by 130 publications

References 38 publications

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

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

Development and Evaluation of an In Vitro Vaginal Model for Assessment of Drug’s Biopharmaceutical Properties: Curcumin

Curcumin-loaded redox response of self-assembled micelles for enhanced antitumor and anti-inflammation efficacy

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