Article

Curcumin nanoformulations: A future nanomedicine for cancer

Cancer Biology Research Center, Sanford Research/University of South Dakota, 2301 E. 60th Street North, Sioux Falls, SD 57104, USA.
Drug discovery today (Impact Factor: 5.96). 09/2011; 17(1-2):71-80. DOI: 10.1016/j.drudis.2011.09.009
Source: PubMed

ABSTRACT Curcumin, a natural diphenolic compound derived from turmeric Curcuma longa, has proven to be a modulator of intracellular signaling pathways that control cancer cell growth, inflammation, invasion and apoptosis, revealing its anticancer potential. In this review, we focus on the design and development of nanoparticles, self-assemblies, nanogels, liposomes and complex fabrication for sustained and efficient curcumin delivery. We also discuss the anticancer applications and clinical benefits of nanocurcumin formulations. Only a few novel multifunctional and composite nanosystem strategies offer simultaneous therapy as well as imaging characteristics. We also summarize the challenges to developing curcumin delivery platforms and up-to-date solutions for improving curcumin bioavailability and anticancer potential for therapy.

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    • "To overcome these delivery obstacles, different nanoscale delivery systems including liposomes (Narayanan et al., 2009; Tavano et al., 2014), nanostructured lipid carriers (Wu et al., 2010), nanoemulsions, polymeric micelles and polymeric nanoparticles (Coradini et al., 2014; Detoni et al., 2012; Yallapu et al., 2012) have been described as strategies to improve the bioavailability, the pharmacological efficacy as well as the limited photostability of these polyphenols. Among these nanocarriers, special interest has been aroused on developing polymeric nanoparticles, either as solid spheres or capsules, based on biodegradable and biocompatible materials (Mora-Huertas et al., 2010). "
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    ABSTRACT: Polyphenols, which are secondary plant metabolites, gain increasing research interest due to their therapeutic potential. Among them, resveratrol and curcumin are two agents showing antioxidant, anti-inflammatory, antimicrobial as well as anticarcinogenic effects. In addition to their individual therapeutic effect, increased activity was reported upon co-delivery of the two compounds. However, due to the poor water solubility of resveratrol and curcumin, their clinical application is currently limited. In this context, lipid-core nanocapsules (LNC) composed of an oily core surrounded by a polymeric shell were introduced as drug carrier systems with the potential to overcome this obstacle. Furthermore, the encapsulation of polyphenols into LNC can increase their photostability. As the attributes of the polyphenols make them excellent candidates for skin treatment, the aim of this study was to investigate the effect of co-delivery of resveratrol and curcumin by LNC upon topical application on excised human skin. In contrast to the formulation with one polyphenol, resveratrol penetrated into deeper skin layers when the co-formulation was applied. Based on vibrational spectroscopy analysis, these effects are most likely due to interactions of curcumin and the stratum corneum, facilitating the skin absorption of the co-administered resveratrol. Furthermore, the interaction of LNC with primary human skin cells was analyzed encountering a cellular uptake within 24h potentially leading to intracellular effects of the polyphenols. Thus, the simultaneous delivery of resveratrol and curcumin by LNC provides an intelligent way for immediate and sustained polyphenol delivery for skin disease treatment. Copyright © 2015. Published by Elsevier B.V.
    European journal of pharmaceutical sciences: official journal of the European Federation for Pharmaceutical Sciences 07/2015; DOI:10.1016/j.ejps.2015.07.018 · 3.01 Impact Factor
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    • "The main curcuminoids from Curcuma are curcumin, desmethoxycurcumin and bisdesmethoxycurcumin, three bioactive substances commonly used as spices and coloring agents in food. However, these molecules have poor bioactivity and instability in neutral and alkaline aqueous solutions (Tønnesen and Karlsen, 1985; Yallapu et al., 2012) and hydrophilic topical formulations. Besides, when curcuminoids were subjected to light exposure there was 30% degradation and 1.8% loss under oxygen action in 30 days. "
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    ABSTRACT: Solid lipid nanoparticles incorporating Curcuma longa L., Zingiberaceae, curcuminoids were produced by the hot melt emulsion method. A Box–Behnken factorial design was adopted to study the nanoparticles production at different levels of factors such as the percentage of curcuminoids, time of homogenization and surfactant ratio. The optimized nanoparticles were incorporated into hydrogels for stability, drug release and skin permeation tests. The average nanoparticle sizes were 210.4 nm; the zeta potential of −30.40 ± 4.16; the polydispersivity was 0.222 ± 0.125. The average encapsulation efficiency of curcumin and curcuminoids was 52.92 ± 5.41% and 48.39 ± 6.62%, respectively. Solid lipid nanocapsules were obtained with curcumin load varying from 14.2 to 33.6% and total curcuminoids load as high as 47.7%. The topical formulation showed good spreadability and stability when subjected to mechanical stress test remained with characteristic color, showed no phase separation and no significant change in pH. As a result of slow release, the nanoparticles were able to avoid permeation or penetration in the pig ear epidermis/dermis during 18 h. The topical formulation is stable and can be used in further in vivo studies for the treatment of inflammatory reactions, in special for radiodermitis.
    Revista Brasileira de Farmacognosia 02/2015; 1. DOI:10.1016/j.bjp.2014.11.010 · 0.80 Impact Factor
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    • "The intensity at 630 nm versus the concentration of the polymer (b). cancer therapy as a potent modulator of inflammatory cell signaling, which regulates cell proliferation, apoptosis, and invasion [22] [23]. Two major limits of CUR are its low solubility in water (0.4 ␮g/mL at pH 7.4) and degradation at physiological pH, resulting in a low bioavailability of CUR. "
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    ABSTRACT: One-step synthesis of amphiphilic polymers containing disulfide bond within the hydrophobic backbone was demonstrated via multi-component Passerini reaction. The obtained polymer was self-assembled into micelles in aqueous solution. Curcumin (CUR), an effective and safe anticancer agent, which was limited by its water insolubility and poor bioavailability, was loaded into the micelles as a model drug. The nanoscale polymeric micelles were confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM). Faster intracellular CUR release was observed by confocal laser scanning microscopy (CLSM) in the HeLa cells pretreated with GSH than in the unpretreated ones. Micelles also loaded with NH2-BODIPY which was almost non-fluorescent and gave strong enhanced fluorescence under acid conditions. The phenomenon of the stronger enhanced fluorescence in the pretreated HeLa cells showed further that the obtained polymer was reduction-sensitive. In vitro MTT assays showed that the micelles were biocompatible and CUR-loaded micelles had higher cellular proliferation inhibition in contrast to free CUR toward HeLa cells. These results highlight the potential of using multi-component Passerini reaction to make functional copolymers as smart nanocarriers for drug delivery.
    Colloids and surfaces B: Biointerfaces 01/2015; 126. DOI:10.1016/j.colsurfb.2014.12.030 · 4.15 Impact Factor
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