Evaluation of thein vivoacute antiinflammatory response of curcumin-loaded nanoparticles

Abstract

Curcumin is the main curcuminoid found in turmeric rhizomes and is a strong candidate to formulate foodstuff with specific properties. Among various bioactive properties of curcumin, its antiinflammatory activity is remarkable; on the other hand, its low water solubility leads to low absorption. Thus, new formulations need to be developed to improve its efficacy, and encapsulation is a promising alternative strategy in this regard. The objective of the present study was to obtain curcumin-loaded polyvinylpyrrolidone (PVP) nanoparticles and evaluate their acute in vivo antiinflammatory activity. Nanoparticles were obtained by complexation using the solid dispersion technique, and the characterization of nanoparticles showed that curcumin and PVP formed an amorphous solid solution. Encapsulated curcumin was colloidally stable in distilled water; this was attributed to the formation of hydrogen bonds between curcumin hydroxyl and PVP carbonyl groups. Rats were treated orally with single doses of curcumin and curcumin-loaded PVP nanoparticles, and antiinflammatory activity was evaluated by an experimental model of carrageenan-induced paw edema, myeloperoxidase (MPO) activity, and microcirculation in situ. Treatment with nanoparticles at 12.5 mg kg significantly reduced the intensity of edema and MPO activity, whereas pure curcumin only presented a significant effect at 400 mg kg. Curcumin inhibited cell migration since rolling and adherent leukocytes were significantly reduced using nanoparticles at 50 mg kg and curcumin at 400 mg kg. Compared to free curcumin, encapsulated curcumin was effective at lower doses; this might be due to the improved water affinity and colloidal stability of curcumin nanoparticles.

In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

“…Curcumin solid dispersion was obtained using the methodology described by Almeida et al (de Almeida et al, 2018) with minor modifications. Poloxamer 407 (3.600 g) and Tween 80 (0.360 g) were solubilized in acetone (36 mL) under gentle stirring at 25°C for 5 min.…”

“…Despite the proven efficacy of curcumin in relation to several biological activities, its low solubility decreases its bioavailability and therapeutic efficacy. However, nanoencapsulation have been used quite successfully to circumvent such low hydro solubility and/or bioavailability of curcumin (de Almeida et al, 2018;Rocha et al, 2014;Silva-Buzanello et al, 2016). Polyoxyethylene-polypropylene block copolymers surfactants (such as Poloxamer 407) are known to enhance dissolution rates and bioavailability of hydrophobic drugs (Vasconcelos et al, 2007).…”

Improved uptake and therapeutic intervention of curcumin via designing binary lipid nanoparticulate formulation for oral delivery in inflammatory bowel disorder

“…Despite curcumin's therapeutic benefits, translation of doses for clinical application is unfeasible due to its poor bioavailability contributed by poor solubility (<1 mg/ml), slow dissolution rate, extensive intestinal and hepatic metabolic transformation along with its rapid elimination [11,12]. So far, literature reports development of various drug delivery systems like liposomes [13,14], cyclodextrin complexes [15], self-emulsifying system [16,17], biodegradable polymeric nanoparticles [18,19], solid lipid nanoparticles (SLNs) [20,21], nano-emulsion [22,23] for topical and parenteral delivery of curcumin in variety of therapeutic applications. However, curcumin formulations have conferred confined success via oral route.…”

Nanodispersions of beta-carotene: effects on antioxidant enzymes and cytotoxic properties

“…16 Since beta-carotene presents remarkable bioactive properties and is also readily available in nature it is important to determine how the transformation in nanoparticles could influence beta-carotene bioactivity. Also, it is worth noting that nanoparticles usually present improved water affinity 17 which may be of interest to obtain pharmaceutical formulations and also to produce water-based food colorants.…”