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: 6.69). 09/2011; 17(1-2):71-80. DOI: 10.1016/j.drudis.2011.09.009
Source: PubMed


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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    • "Doxorubicin (Dox) is a potent wide-spectrum cytotoxic agent, but it has been surffering from the notorious carditoxicity as well as the MDR problem. One popular strategy to address this issue is the co-encapsulation of Dox with a pleiotropic agent, curcumin (Cur) in nanocarriers (Sadzuka et al., 2012; Yallapu et al., 2012; Li et al., 2015). In such combination Cur played two roles and acted as both an anticancer agent and a chemosensitizer for MDR supression. "
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    ABSTRACT: The combinational delivery of doxorubicin and curcumin in a physically loaded nanocarrier offers the benefits of enhanced therapeutic efficacy and reduced adverse effects, but this strategy often suffers from the slow drug release followed by delayed onset of pharmacological action. This work reported the hydrazone-linked polymer-curcumin conjugate micelles containing physically loaded doxorubicin to address this problem; the ester-linked conjugate micelles were produced as the control. The pH-labile spherical micelles were less than 100 nm with a loading at 9.3 ± 0.5% (w/w, Curcumin) and 2.5 ± 0.1(w/w, Doxorubicin). Both agents were released at a faster rate in the pH-labile micelles compared to the control. The confocal laser scanning microscopy revealed a time-dependent co-localization of both agents in HepG2 cells. The IC50 of pH-labile conjugate micelles without doxorubicin in HepG2 cells was 27.7 ± 5.3 (μM), whereas the co-loaded micelles was lowered to 10.8 ± 3.4 (μM) (Cur-equivalent dose). The combination index calculation demonstrated a synergistic action of both agents in the co-loading nanocarrier. The current work provided an efficient nanocarrier system to achieve rapid on-demand drug release without onset delay of therapeutic action, which might add value to the clinical translation of the combinational delivery systems.
    International Journal of Pharmaceutics 09/2015; 495(1). DOI:10.1016/j.ijpharm.2015.09.022 · 3.65 Impact Factor
    • "The encapsulation of bioactive compounds represents an efficient strategy to improve their dispersibility in foods, to prevent their degradation under adverse environmental conditions , such as extreme pH and temperature, light exposure, presence of reactive oxygen species, to minimize the interaction with other food ingredients, as well as to promote their bioaccessibility and bioavailability (Ahmed et al., 2012; Yu et al., 2012; Yu and Huang, 2012; Yallapu et al., 2012). Moreover, the development of a better understanding of the correlation between particle structure and behavior in product and in body, is increasingly becoming an enabling tool for controlling the release of the encapsulated bioactives at target sites, for improving food compatibility, as well as for masking unpleasant tastes and flavors of food additives through tailored carrier Contents lists available at ScienceDirect "
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    ABSTRACT: Submicrometric lipid-based carriers were developed to encapsulate curcumin and deliver it to intestinal epithelial cells. A lipid matrix comprising monoolein, sunflower oil and water at weight ratio 1:1:1 was selected, upon screening of different combinations of amphiphilic molecules, vegetable oils and water, because of its high encapsulations efficiency of curcumin, retained over time and relatively lower content of amphiphilic molecules. Upon dispersion in aqueous phase, the carriers were stabilized by: (a) whey protein isolates (WPI), alone and (b) in combination with modified starch (WPI-MS), or by (c) polysorbate 20 (T20). Whereas T20-stabilized systems exhibited extremely fine particles (120nm), WPI and WPI-MS stabilized carriers were characterized by a significantly larger mean particle size (270nm). The thicker macromolecular layer of WPI and WPI-MS enabled better (a) physical stability, (b) controlled shell degradation during simulated digestion, and (c) curcumin bioaccessibility targeted at the intestinal digestion phase than T20-systems. However, uptake studies in HT29 cell lines, simulating intestinal epithelial cells, showed that WPI and WPI-MS carriers exhibited after 24h a lower relative uptake than T20-stabilized systems (about 60 % and 80 %, respectively), as a consequence of smaller size and higher cell adherence of T20 carriers to the cell membrane. Copyright © 2015. Published by Elsevier B.V.
    International Journal of Pharmaceutics 08/2015; 494(1). DOI:10.1016/j.ijpharm.2015.08.039 · 3.65 Impact Factor
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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; 78. DOI:10.1016/j.ejps.2015.07.018 · 3.35 Impact Factor
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