Curcumin, solubility
89636445
Enhanced curcumin solubility by solid dispersion technique reduces fat accumulation in pigs
Lifestyle related diseases such as diabetes mellitus, arteriosclerosis and cardiac diseases are important illness for people around the world. Therefore, there is attempt to produce quality pork with high red meat and low fat content. In this study, the solid dispersion (SD) technique was used to enhance the solubility of curcumin from Turmeric Oleoresin (TO) for use in an animal diet. The SD technique was prepared by mixing TO with carrier (Polyethylene glycol, PEG400) and adsorbent (Magnesium oxide, MgO) at the ratio of 1:1:3 (TOPM) Curcumin was determined using high performance liquid chromatography (HPLC) The result showed that solubility rate of crude curcumin was increased with carrier and adsorbent (P<0.05) This mixed curcumin was used to reduce fat in pig. Twenty crossbred castrated male pigs (Large White x Landrace x Duroc) with an average weight of 30+ 3.2 kg were randomly allotted to receive basal diet with curcumin from TOPM at 0, 0.5, 1.0, and 1.5 g /kg of the diet. Blood samples were collected on days 0, 30, and 60. Each pig was raised to 100 kg and all pigs were slaughtered in the slaughter house. Longissimus dorsi (LD) muscles were collected from each pig. Lipid profiles in blood and muscle were determined. At 60 days of feeding, plasma lipid profile of pigs fed curcumin had higher high density lipoprotein cholesterol (HDL C) lower low density lipoprotein cholesterol (LDL C) and lower LDL C: HDL C ratio than those pigs fed no curcumin. Pigs fed curcumin at 0.5 g/kg diet reduced total cholesterol (TC) and triglycerides (TG) in LD muscles (P<0.05) It concluded that TO mixed with carrier and adsorbent by the SD technique can increase crude curcumin solubility. Top dressing TOPM in pig diets tend to reduce plasma TC, TG, LDL C, VLDL C, and LDL C: HDL C ratio.
Pitukpol Porn-anek Suthipong Uriyapongson Chaluntorn Vichasilp
101937880
Influence of Lipid Phase Composition of Excipient Emulsions on Curcumin Solubility, Stability, and Bioaccessibility
The influence of oil type on the ability of excipient emulsions to improve the solubility, stability, and bioaccessibility of curcumin was examined. Oil in water emulsions were prepared using coconut, sunflower, corn, flaxseed, or fish oils. These excipient emulsions were then mixed with powdered curcumin and incubated at 30 or 100 degC. For all oils, more curcumin was transferred from powder to excipient emulsion at 100 degC (190 200 mg/mL) than at 30 degC (30 36 mg/mL) which was attributed to increased curcumin solubility with temperature. Oil type influenced the stability and bioaccessibility of curcumin when excipient emulsions were exposed to simulated gastrointestinal tract conditions, which was attributed to differences in the molecular composition and physicochemical properties of the oils. Overall, the use of fish oil led to the highest effective curcumin bioavailability (38 This study provides valuable information for optimizing excipient emulsions to increase curcumin bioavailability in food, supplement, or pharmaceutical applications.
Food Biophysics
Li-qiang Zou Bingjing Zheng Ruojie Zhang Zipei Zhang Wei Liu Chengmei Liu Guodong Zhang Hang Xiao David Julian Mcclements
2917041
Enhancement of Curcumin Solubility by Phase Change from Crystalline to Amorphous in Cur TPGS Nanosuspension.
Nanosuspensions (NSs) were fabricated to enhance water solubility, dissolution rate, and oral adsorption of water insoluble curcumin using sonoprecipitation method. As a good stabilizer, d a Tocopherol polyethylene glycol 1000 succinate (TPGS) was used to improve the stability of curcumin TPGS NSs (Cur TPGS NSs) Ultrasonic homogenization (UH) could effectively enhance the solubility of curcumin and to produce homogeneous NSs with small particle sizes. Water solubility of curcumin was significantly improved from 0.6 mg/mL in pure water to 260 mg/mL in the mixture of curcumin and TPGS (1:10) with UH treatment. The mean particle size of Cur TPGS NSs was decreased significantly after UH and maintained between 208 and 246 nm. Lyophilized powder of Cur TPGS NSs was dissolved about 91.08% whereas the pristine curcumin powder was dissolved only 6.5% at pH 7.4. This study showed a great potential of Cur TPGS NSs as a good nano formulation of curcumin with enhanced solubility and improved oral adsorption.
Journal of food science
Gye Hwa Shin Jinglei Li Jin Hun Cho Jun Tae Kim Hyun Jin Park
21707392
Ovalbumin as a carrier to significantly enhance the aqueous solubility and photostability of curcumin: Interaction and binding mechanism study.
Egg ovalbumin (OVA) as a macromolecular carrier has the potential to improve the solubility and stability of insolubility bioactive molecules, however, their binding behavior and the mechanism is still ambiguous. In this work, the curcumin was selected as the target to study the interaction and binding mechanism between curcumin and OVA by thermodynamic titration technique in combination with molecular dynamic simulation. The results suggested that the binding included two steps: first, curcumin molecule entered into the hydrophobic pocket of OVA by hydrophobic interaction; and second the interaction was enhanced via hydrogen bonds, resulting in static fluorescence quenching and secondary structural change of OVA. This study provided further evidence in support of the proposed mechanism of the polyphenol protein binding by the "Hands gloves" model. Furthermore, when the OVA was as a carrier, the solubility of curcumin has been increased ~370 times to 32.73 mg/mL compared to that of free curcumin at pH 7.0. The photostability was enhanced significantly indicating that it is an efficient way to improve the stability of curcumin in contributing to its application in nutritional supplements or functional foods.
International journal of biological macromolecules
Yujia Liu Yanxue Cai Danyang Ying Yinlian Fu Yahong Xiong Xue-Yi Le
10927305
Hansen solubility parameters (HSP) for prescreening formulation of solid lipid nanoparticles (SLN) in vitro testing of curcumin loaded SLN in MCF 7 and BT 474 cell lines
Abstract Curcumin, a phenolic compound from turmeric rhizome (Curcuma longa) has many interesting pharmacological effects, but shows very low aqueous solubility. Consequently, several drug delivery systems based on polymeric and lipid raw materials have been proposed to increase its bioavailability. Solid lipid nanoparticles (SLN) consisting of solid lipid matrix and a surfactant layer can load poorly water soluble drugs, such as curcumin, deliver them at defined rates and enhance their intracellular uptake. In the present work, we demonstrate that, despite the drug's affinity to lipids frequently used in SLN production, the curcumin amount loaded in most SLN formulations may be too low to exhibit anticancer properties. The predictive curcumin solubility in solid lipids has been thoroughly analyzed by Hansen solubility parameters, in parallel with the lipid screening solubility tests for a range of selected lipids. We identified the most suitable lipid materials for curcumin loaded SLN, producing physicochemically stable particles with high encapsulation efficiency >90% Loading capacity of curcumin in SLN allowed preventing the cellular damage caused by cationic SLN on MCF 7 and BT 474 cells but was not sufficient to exhibit drug's anticancer properties. But curcumin loaded SLN exhibited antioxidant properties, substantiating the conclusions that curcumin's effect in cancer cells is highly dose dependent.
Pharmaceutical development and technology
Slavomira Doktorovova Eliana Barbosa Souto Amelia M Silva
220487861
Preparation and characterization of a solid dispersion containing curcumin and octenylsuccinate hydroxypropyl phytoglycogen for improved curcumin solubility.
Curcumin (CCM) is a natural and potent bioactive compound; however, its poor water solubility limits its performances and applications. In this study, octenylsuccinate hydroxypropyl phytoglycogen (OHPP) a dendrimer like, amphiphilic phytoglycogen derivative, was used to solubilize CCM and enable its inhibitory effect against pathogen Helicobacter pylori. The CCM OHPP solid dispersion (CCM OHPP SD) was prepared using spray drying and characterized for its molecular interaction (with FTIR) crystallinity (with X ray powder diffraction) solubility, and minimal bactericidal concentration (MBC) against three H. pylori strains. The results showed the presence of hydrogen bonds between CCM and OHPP in CCM OHPP SD and the transformation of CCM from crystalline to amorphous state due to its incorporation with OHPP. For CCM OHPP SD, the soluble amount of CCM was over 16,000 times that of CCM alone, and the dissolution rate reached 60 99% in 30 60 min. Against three strains of H. pylori, MBC values of CCM were 20 mg/mL for CCM OHPP SD, which were comparable with that of DMSO assisted CCM solutions. Overall, the results showed that OHPP was a highly effective solubilizer of CCM to enable its inhibitory efficacy against H. pylori.
European journal of pharmaceutical sciences official journal of the European Federation for Pharmaceutical Sciences
Ying Xie Y Yao
102791792
Curcumin: pharmaceutical solids as a platform to improve solubility and bioavailability
Curcumin (CUR) is the prime curcuminoid in the Indian dietary spice turmeric, Curcuma longa, a plant of the Zingiberaceae family. CUR has promising and diverse therapeutic benefits, such as antioxidant, anti inflammatory, antitumor, anti hyperglycemic, antimalarial, antibacterial, and antiviral activity, including anti Alzheimer's disease. However, CUR is yet to reach the status of a therapeutic drug candidate mainly because a standard solid dosage of curcumin suffers from poor oral bioavailability (0.05 mg mL 1, less than 1% The reasons behind its low bioavailability include poor solubility <8 mg mL 1 in water) low permeability and absorption, and rapid metabolism (short elimination half life of <2 h) A successful CUR therapy requires an appropriate formulation system that will enhance the bioavailability and offer greater therapeutic efficacy. This review covers a comprehensive description of the CUR pharmaceutical solids, such as polymorphs, cocrystals, eutectics, and coamorphous solid state forms with aim to determine ways to improve its physicochemical properties, including dissolution rate, solubility, physicochemical stability, mechanical strength, compressibility for tablet formation, and oral bioavailability. The cumulative publications in the past decade have forecast a bright future for development of an oral drug formulation of curcumin.
Kuthuru Suresh Ashwini K Nangia
4891461
Encapsulation of curcumin using supercritical antisolvent (SAS) technology to improve its stability and solubility in water.
This study aims to develop a formulation of a turmeric based dye extract using supercritical antisolvent (SAS) technology and different encapsulating polymers to improve the aqueous stability and solubility of curcumin. The dye formulation obtained by SAS consists of a mixture of Eudragit(r) L100 and Pluronic(r) 127 using tween 20 as a surfactant The characterization and quantification of curcumin extracts and the encapsulation product were conducted using high performance liquid chromatography (HPLC) The properties of the dye were determined using SEM, DSC, X ray diffraction, particle size, zeta potential, and oxygen radical absorbance capacity (ORAC) to measure antioxidant capacity. The dye formulation contained a curcumin content of 4.45 ug/mL. The average diameter of the amorphous particles was 5667.4 nm, and the zeta potential was 11.21 mV. The largest aqueous stability and solubility was observed at pH 4. From color comparison with a solution of tartrazine 200 ug/mL solution of dye formulation based on curcuminoids is equivalent to an approximated 30 ug/mL tartrazine solution.
Food chemistry
Alvaro Arango-Ruiz Angel Martin Maria Jose Cosero Claudio Jimenez Julian Londono Londono
19192555
Amorphous ternary nanoparticle complex of curcumin chitosan hypromellose exhibiting built in solubility enhancement and physical stability of curcumin.
The low aqueous solubility of curcumin (CUR) had greatly limited the clinical efficacy of CUR therapy despite its well known potent therapeutic activities. Previously, we developed amorphous nanoparticle complex (nanoplex) of CUR and chitosan (CHI) as a solubility enhancement strategy of CUR by electrostatically driven drug polyelectrolyte complexation. The CUR CHI nanoplex, however, (1) lacked a built in ability to produce prolonged high apparent solubility of CUR in the absence of crystallization inhibiting agents, and (2) exhibited poor physical stability during long term storage. For this reason, herein we developed amorphous ternary nanoplex of CUR, CHI, and hypromellose (HPMC) where HPMC functioned as the crystallization inhibitor. The effects of incorporating HPMC on the (1) physical characteristics and (2) preparation efficiency of the CUR CHI HPMC nanoplex produced were investigated. Compared to the CUR CHI nanoplex, the HPMC inclusion led to larger nanoplex (300 500 nm) having lower zeta potential (1 15 mV) and lower CUR payload (40 80% albeit with higher CUR utilization rates (100% attributed to the CUR interactions with both CHI and HPMC. The CUR CHI HPMC nanoplex's physical characteristics could be controlled by varying the HPMC to CHI ratio in the feed. Subsequently, the CUR CHI HPMC and CUR CHI nanoplexes were examined in terms of their (1) storage stability, (2) dissolution characteristics in simulated gastrointestinal fluids, and (3) in vitro solubility enhancement. The results showed that the CUR CHI HPMC nanoplex exhibited superior (i) amorphous state stability after twelve month storage, (ii) dissolution characteristics, and (iii) solubility enhancement in simulated gastrointestinal fluids, with minimal cytotoxicity towards human gastric epithelial cells.
Colloids and surfaces. B, Biointerfaces
Li Ming Lim The-Thien Tran Jerome Jie Long Wong Danping Wang Wean Sin Cheow Kunn Hadinoto
5026210
A curcumin diglutaric acid conjugated prodrug with improved water solubility and antinociceptive properties compared to curcumin
ABSTRACT In this work, a curcumin diglutaric acid (CurDG) prodrug was synthesized by conjugation of curcumin with glutaric acid via an ester linkage. The water solubility, partition coefficient, release characteristics, and antinociceptive activity of CurDG were compared to those of curcumin. The aqueous solubility of CurDG (7.48 mg/mL) is significantly greater than that of curcumin (0.068 mg/mL) A study in human plasma showed that the CurDG completely releases curcumin within 2 h, suggesting the ability of CurDG to serve as a prodrug of curcumin. A hot plate test in mice showed the highest antinociceptive effect dose of curcumin at 200 mg/kg p.o. whereas CurDG showed the same effect at an effective dose of 100 mg/kg p.o. indicating that CurDG significantly enhanced the antinociceptive effect compared to curcumin. The enhanced antinociceptive effect of CurDG may be due to improved water solubility and increased oral bioavailability compared to curcumin.
Bioscience, biotechnology, and biochemistry
Chawanphat Muangnoi Ponsiree Jithavech Pahweenvaj Ratnatilaka Na Bhuket Wiwat Supasena Wisut Wichitnithad Pasarapa Towiwat Nuansri Niwattisaiwong Ian S Haworth Pornchai Rojsitthisak