A Novel Solubility-Enhanced Curcumin Formulation Showing Stability and Maintenance of Anticancer Activity

Zhang, Fang; Koh, Gar Yee; Jeansonne, Duane; Hollingsworth, Javoris; Russo, Paul S.; Vicente, Graca; Stout, Rhett W.; Liu, Zhijun

doi:10.1002/jps.22512

Cited by 93 publications

(71 citation statements)

References 26 publications

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“…However, apart from the rigorous reaction conditions, the 93 modified curcumin tends to lose its functionalities, at least to some 94 degree. 95 Recently, solid dispersion method was also reported to over- 96 come the problems associated with curcumin [16,17]. Unlike nano 97 and chemical modification methods, solid dispersion is relatively 98 easy to prepare, with higher loading ability and stability.…”

Section: Introductionmentioning

confidence: 99%

Curcumin-Eudragit® E PO solid dispersion: A simple and potent method to solve the problems of curcumin

Lee

Shin

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

136

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Section: Introductionmentioning

confidence: 99%

Curcumin-Eudragit® E PO solid dispersion: A simple and potent method to solve the problems of curcumin

Lee

Shin

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

136

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“…Saturated solubility of CUR in water could not be detected because of spectrum shift from the wavelength of 420 nm to 280 nm due to its poor stability and decomposition under neutral-basic conditions (23). CUR solubility studies were carried out in diff erent aqueous and non-aqueous media and the results are shown in Fig.…”

Section: Curcumin Solubility Studymentioning

confidence: 99%

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Allam

Abdallah

2015

Acta Pharmaceutica

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Curcumin, a naturally occurring lipophilic molecule can exert multiple and diverse bioactivities. However, its limited aqueous solubility and extensive presystemic metabolism restrict its bioavailability. Curcumin phytosomes were prepared by a simple solvent evaporation method where free fl owing powder was obtained in addition to a newly developed semisolid formulation to increase curcumin content in soft gels. Phytosomal powder was characterized in terms of drug content and zeta potential. Thirteen diff erent soft gel formulations were developed using oils such as Miglyol 812, castor oil and oleic acid, a hydrophilic vehicle such as PEG 400 and bioactive surfactants such as Cremophor EL and KLS P 124. Selected formulations were characterized in terms of curcumin in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of curcumin phytosomes in complex formulations. Stability studies of chosen formulations prepared using the hydrophilic vehicle revealed a stable curcumin dissolution patt ern. In contrast, a dramatic decrease in curcumin dissolution was observed in case of phytosomes formulated in oily vehicles.Keywords: curcumin, phospholipid, phytosomes, bioavailability, lipids, soft gels INTRODUCTION Curcumin (CUR) found in the turmeric rhizomes can exert multiple and diverse bioactivities, including antioxidant, antitumor, anti-inflammatory, antidiabetic, antirheumatic, wound healing, antiviral, hepatoprotective, and anti-HIV activity (1). Despite the potential biological eff ects of CUR, poor bioavailability in both rodents and humans, as reported in several pharmacokinetic studies (2), demands high doses to reach therapeutic drug levels. Detectable serum levels were not achieved until doses of up to 3.6 g were used; consequently, a 3.6 g daily dose of oral CUR was used in the phase II clinical trial in patients with advanced colorectal cancer (3). Keeping in mind the promise of CUR as a therapeutically active agent and its poor oral absorption due to its limited aqueous solubility and extensive presystemic metabolism, it is necessary to develop a new formulation of CUR that could augment its oral absorption and enhance its therapeutic activity.To improve the bioavailability of CUR, numerous approaches and technologies have been investigated over the past decades, including the use of solid dispersion (4), copolymeric micelles (5), polymeric nanoparticles (6), lipid based nanoparticles (7), self microemulsion (8), liposomes (9) and complexation with phospholipids (10, 11). All these approaches are expected to provide bioavailability enhancement and improved absorption in the intestinal tract.Phytosomes are considered to be a safe and convenient delivery system, able to enhance oral bioavailability of poorly water soluble drugs. Their safety is related to the similarity between their structural components and the lipid content of mammalian cell membranes (12)(13)(14). Phytosomes show a bett er stability profi le than liposomes due to the unique chemical bond interact...

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“…Physicochemical properties of these sweeteners also differ from one another. Several studies have described the ability of SG to improve the solubility of other sweeteners or biomolecules (Lee, 2011;Goto & Clemente, 1998;Zhang et al, 2011;Uchiyama, Tozuka, Nishikawa, & Takeuchi, 2012). Other studies explore the capability of SGs to form different crystalline forms in addition to the amorphous form Copyright ©2016 ISEKI-Food Association (IFA) 10.7455/ijfs/5.2.2016.a4 (Carakostas et al, 2012;Lee, 2011;Prakash, DuBois, Cios, Wilkens, & Fosdick, 2008Upreti et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Solubility of Stevioside and Rebaudioside A in water, ethanol and their binary mixtures

2016

IJFS

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In order to investigate the solubility of Stevioside and Rebaudioside A in different solvents (ethanol, water, ethanol:water 30:70 and ethanol:water 70:30), supersaturated solutions of pre-crystalized steviol glycosides were maintained at different temperatures (from 5°C to 50°C) to reach equilibrium. Under these conditions significant differences were found in the extent of solubility. Rebaudioside A was poorly soluble in ethanol and water, and Stevioside was poorly soluble in water. Solvent mixtures more effectively promoted solubilisation, and a significant effect of temperature on solubility was observed. The two steviol glycosides showed higher solubilities and this behavior was promoted by the presence of the other sweetener. The polarity indices of the solvents were determined, and helped to explain the observed behavior. Several solute-solvent and solute-solute interactions can occur, along with the incidence of a strong affinity between solvents. The obtained results are in accordance with technological applications of ethanol, water and their binary mixtures for Stevioside and Rebaudioside A separations.

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A Novel Solubility-Enhanced Curcumin Formulation Showing Stability and Maintenance of Anticancer Activity

Cited by 93 publications

References 26 publications

Curcumin-Eudragit® E PO solid dispersion: A simple and potent method to solve the problems of curcumin

Curcumin-Eudragit® E PO solid dispersion: A simple and potent method to solve the problems of curcumin

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Solubility of Stevioside and Rebaudioside A in water, ethanol and their binary mixtures

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