Pure Curcumin Research Articles

Antioxidant Potential of Curcumin-A Meta-Analysis of Randomized Clinical Trials.

Background: Antioxidant potential is defined as the ability to neutralize oxygen free radicals that are generated in excess due to environmental influences. The body’s defense mechanisms often require support in preventing the effects of oxidative stress. The literature data suggest that curcumin has antioxidant activity that can significantly reduce oxidative stress levels. The aim was to assess the impact of curcumin on oxidative stress markers. Methods: PubMed and Embase were searched from database inception until 27 September 2019 for randomized clinical trials in >20 patients treated with curcumin supplements and randomized to placebo/no intervention/physical activity to verify the antioxidant potential of curcumin. Results: Four studies were included in the meta-analysis, three of which were double-blind and one single-blind. A total of 308 participants took part in the research. A total of 40% of the respondents were men. The average age of participants was 27.60 ± 3.79 years. The average supplementation time was 67 days and the average dose of curcumin administered was 645 mg/24 h. Curcumin significantly increased total antioxidant capacity (TAC) (SMD = 2.696, Z = 2.003, CI = 95%, p = 0.045) and had a tendency to decrease malondialdehyde (MDA) concentration (SMD = −1.579, Z = −1.714, CI = 95%, p = 0.086). Conclusions: Pure curcumin has the potential to reduce MDA concentration and increase total antioxidant capacity.

Stoichiometrically Governed Curcumin Solid Dispersion and Its Cytotoxic Evaluation on Colorectal Adenocarcinoma Cells.

BackgroundColorectal cancer (CRC) is the third most commonly occurring cancer in men and the second most commonly occurring cancer in women. Curcumin (CMN) is obtained from a natural source and has no toxicity, even at high doses (8,000 mg/kg body weight in 24 hours) and was determined to have anticancer potency on several kinds of carcinoma. However, its medical applications were limited because of its low solubility and poor bioavailability.Materials and MethodsTo improve the medical applications of CMN, various hydrophilic carriers such as poloxamer 407 (PMX-407), poloxamer 188 (PMX-188), Gelucire 50/13 (Gel-50/13), and mannitol (MNL) were used to prepare a binary complex solid dispersion (SD). These binary SDs were characterized for aqueous solubility in various solvents. Physical stability, thermal behaviors, and morphology were determined by Fourier transform infrared spectrophotometric analysis, powder X-ray diffraction analysis, thermogravimetric analysis, differential scanning calorimetric analysis, scanning electron microscopy, dynamic light scattering study, and the novel dyeing test. In vitro drug release was determined by dissolution study. Based on the characterization, the better SD complex was optimized using Box-Behnken design (BBD). The cytotoxicity and apoptosis study of prepared CMN (C-SD) were used to test for colorectal adenocarcinoma cell lines.ResultsThese results showed that the solubility of CMN is greatly improved after complexation with PXM-407 in SD. CMN is practically insoluble in water at acidic and neutral pH; however, the SD of CMN with PXM-407 produced significant improvement in solubility (1.266±0.0242 mg/mL) and dissolution (91.36±0.431% at 30 minutes); similarly, these data fit with a phase solubility study and in silico molecular modeling. Moreover, the solid-state characterization revealed that the SD complex exhibits the intermolecular hydrogen bond with drug and carrier. Also, the complex does not undergo any chemical modification owing to the amorphous form, and the dye test showed better coloring impact indicating the solubility of CMN. The cell cycle arrest confirmed at G2/M phase from flow cytometry analysis, and Western blot investigation was recognized molecular level cell death and the complex induced more exploit DNA during apoptosis.ConclusionThis study confirmed that the ideal stoichiometric ratio of CMN with carrier to enhance its solubility was 1:1. This molecular complex of PXM-407 was found to be more effective against colorectal cancer (CRC) than pure CMN.

Application of the Box-Behnken design for the production of soluble curcumin: Skimmed milk powder inclusion complex for improving the treatment of colorectal cancer.

The main objective of this study was to develop a soluble product of the practically insoluble curcumin (CMN) to treat colorectal cancer more effectively than with pure CMN. To improve the solubility of CMN, various hydrophilic carriers of skimmed milk powder (SMP), polyvinylpyrrolidone (PVP), and mannitol (MNT) were utilized to prepare solid dispersion (SD) binary complexes. The prepared complexes were characterized in terms of their aqueous solubility and in vitro drug release and analyzed by Fourier transform infrared spectrophotometry, powder X‐ray diffractometry, scanning electron microscopy, dynamic light scattering, and the novel dyeing test. Based on this characterization, the best SD complex was optimized using the Box–Behnken design (RSM‐BBD). These results showed that the solubility of CMN was greatly improved in combination with SMP. The SD of CMN with SMP produced significantly improved solubility (0.646 ± 0.024 mg/ml) and dissolution (54.94 ± 3.21% at 5 min). Further, solid‐state characterization revealed that the complex exhibited intermolecular inclusion of the drug and carrier. Also, the complex did not undergo any chemical modification owing to its amorphous form, and the novel dye test showed better coloring impact, indicating the solubility of CMN. The in vitro cytotoxicity of the complex showed that 50% inhibition (IC50) of SW480 and Caco‐2 cells was achieved at a considerably lower concentration than that of pure CMN. Flow cytometry analysis confirmed that the cell cycle arrest was at G2/M phase (43.26% and 65.14%), and DNA fragmentation analysis investigation confirmed that the complex induced more DNA damage during apoptosis.

Curcumin Mitigates AFB1-Induced Hepatic Toxicity by Triggering Cattle Antioxidant and Anti-inflammatory Pathways: A Whole Transcriptomic In Vitro Study.

Aflatoxin B1 (AFB1) toxicity in livestock and human beings is a major economic and health concern. Natural polyphenolic substances with antioxidant properties have proven to be effective in ameliorating AFB1-induced toxicity. Here we assessed the potential anti-AFB1 activity of curcumin (pure curcumin, C, and curcumin from Curcuma longa, CL) in a bovine fetal hepatocyte-derived cell line (BFH12). First, we measured viability of cells exposed to AFB1 in presence or absence of curcumin treatment. Then, we explored all the transcriptional changes occurring in AFB1-exposed cells cotreated with curcumin. Results demonstrated that curcumin is effective in reducing AFB1-induced toxicity, decreasing cells mortality by approximately 30%. C and CL induced similar transcriptional changes in BFH12 exposed to AFB1, yet C treatment resulted in a larger number of significant genes compared to CL. The mitigating effects of curcuminoids towards AFB1 toxicity were mainly related to molecular pathways associated with antioxidant and anti-inflammatory response, cancer, and drug metabolism. Investigating mRNA changes induced by curcumin in cattle BFH12 cells exposed to AFB1 will help us to better characterize possible tools to reduce its consequences in this susceptible and economically important food-producing species.

Effects of Bacterial Nanocellulose Loaded with Curcumin and Its Degradation Products on Human Dermal Fibroblasts.

Bacterial nanocellulose has found applications in tissue engineering, in skin tissue repair, and in wound healing. Its large surface area enables the adsorption of various substances. Bacterial nanocellulose with adsorbed substances can serve as a substrate for drug-delivery of specific bioactive healing agents into wounds. In this study, we loaded a bacterial nanocellulose hydrogel with curcumin, i.e., an important anti-bacterial and healing agent, and its degradation products. These products were prepared by thermal decomposition of curcumin (DC) at a temperature of 180 °C (DC 180) or of 300 °C (DC 300). The main thermal decomposition products were tumerone, vanillin, and feruloylmethane. Curcumin and its degradation products were loaded into the bacterial nanocellulose by an autoclaving process. The increased temperature during autoclaving enhanced the solubility and the penetration of the agents into the nanocellulose. The aim of this study was to investigate the cytotoxicity and the antimicrobial activity of pure curcumin, its degradation products, and finally of bacterial nanocellulose loaded with these agents. In vitro tests performed on human dermal fibroblasts revealed that the degradation products of curcumin, i.e., DC 180 and DC 300, were more cytotoxic than pure curcumin. However, if DC 300 was loaded into nanocellulose, the cytotoxic effect was not as strong as in the case of DC 300 powder added into the culture medium. DC 300 was found to be the least soluble product in water, which probably resulted in the poor loading of this agent into the nanocellulose. Nanocellulose loaded with pure curcumin or DC 180 exhibited more antibacterial activity than pristine nanocellulose.

Preparation and characterization of curcumin solid dispersion using HPMC.

Curcumin solid dispersions were prepared using hydroxypropyl methylcellulose (HPMC) to enhance water solubility of curcumin. The particle size of curcumin solid dispersions was in range from 371 to 528nm and particles were shaped as spherical with wrinkles. The encapsulation efficiency was over 93% for all samples, and water solubility of curcumin was significantly improved to 238µg/mL when the ratio of curcumin to HPMC was 20:80. The results of X-ray diffraction, differential scanning calorimeter, and Fourier transform infrared spectroscopy showed that crystalline form of curcumin changed to amorphous form. Curcumin solid dispersions showed improved dissolution behavior compared to pure curcumin and the curcumin release kinetic studies were applied to find best-fitting model. This study showed a great potential of solid dispersion using HPMC as curcumin delivery system with improved water solubility and oral absorption. PRACTICAL APPLICATION: Curcumin has limited applications in the food industry because of low water solubility. Dongoh water-soluble curcumin (DW-CURs) were prepared by solid dispersion method with HPMC. Our results indicated that curcumin solid dispersions improved the water solubility of curcumin and showed a sustained release, demonstrating its possibility of body application. Therefore, DW-CURs are a promising formulation for application as a functional ingredient in the food industry.

A difunctional Pluronic®127-based in situ formed injectable thermogels as prolonged and controlled curcumin depot, fabrication, in vitro characterization and in vivo safety evaluation

Curcumin has been reported to be used widely against many types of pathological conditions in clinics. However, due to its limitations such as poor solubility, poor oral absorption and low stability have limited its applications. In the current study, a series of novel chemically cross-linkable depot gel formulations were developed based on thermoresponsive micellar polymer (Pluronic®127) with polyelectrolyte hydrophilic monomer, that is, 2-acrylamido-2-methylpropane sulfonic acid by cold and in situ grafting polymerization method. The formulations were aimed to deliver curcumin at controlled rate from in situ formed depot after administration through subcutaneous route in vivo. The sol-gel phase transitions of formulations were observed by rheological analysis, tube titling and optical transmittance measurements. Maximum swelling of gel formulations was observed at pH 7.4 and below CGT, that is, 25 °C. The in vitro release profile exhibits maximum drug release at pH 7.4 and 25 °C owing to relaxed gel state. In vitro degradation profile of gel formulations showed controlled degradation rate. Cell growth inhibition study confirmed the biocompatibility and safe nature of bare gel formulations against L929 cell lines. In vitro cytotoxic study showed that curcumin loaded in gel formulation has controlled pharmacological activity against HeLa and MCF-7 cancer cells as compared to free drug solution. The IC50 values calculated for pure curcumin solution (30 ± 0.77 µg/ml for HeLa and 27 ± 0.39 µg/ml for MCF-7) were found higher in comparison to curcumin-loaded thermogels against HeLa (19 ± 0.28 µg/ml and 23 ± 0.81 µg/ml) and MCF-7 (22 ± 0.54 µg/ml and 21 ± 0.49 µg/ml). Histopathological and hematological analysis showed the biocompatible nature of hydrogels. Structural confirmation was done by Fourier transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance spectroscopy (1H NMR). Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) confirmed the thermal stability of the gel formulation. The porous structure of gel formulations was assessed by scanning electron microscopic (SEM) analysis. Results concluded that newly developed gel formulations have thermoresponsive behavior with phase transition at body temperature and can be used as in situ controlled drug depot.

Composites of yeast glucan particles and curcumin lead to improvement of dextran sulfate sodium-induced acute bowel inflammation in rats

The goal of this work was to assess the usability of yeast glucan particles (GPs) as carriers for curcumin and determine the beneficial effect of a pharmacological composite of curcumin in GPs on dextran sulfate sodium induced colitis in rats. The assessment of the anti-inflammatory effect of particular substances was evaluated on the basis of the calculated disease activity index and by assessment of cytokines and enzymes from the gut tissue – tumor necrosis factor α (TNF-α), transforming growth factor β1, interleukin (IL)-1β, IL-6, IL-10, IL-17, catalase, superoxide dismutase 2, myeloperoxidase (MPO), and matrix metalloproteinase 9. Composites of GPs with incorporated curcumin showed promising results with the capability to lower symptoms of colitis and significantly decrease the production of pro-inflammatory cytokines TNF-α, IL-1β, IL-6, and the activity of MPO, as well. The anti-inflammatory effect of the composites was greater than those of pure GPs or curcumin.

Formulation of Curcumin-β-cyclodextrin-polyvinylpyrrolidone supramolecular inclusion complex: experimental, molecular docking, and preclinical anti-inflammatory assessment

This research planned to ameliorate an aqueous solubility and dissolution of Curcumin (CUR) by the formulation of inclusion complex with β-cyclodextrin (β-CD) and polyvinylpyrrolidone (PVP). The phase solubility study was performed to assess the solubility of CUR. The prepared CUR complex assessed for dissolution study, physicochemical evaluation, in-vitro antioxidant activity, molecular modeling, and anti-inflammatory assessment. The pivotal findings of phase-solubility studies demonstrate apparent stability constant (Kc) and complexation efficiency (CE) values for CUR-β-CD and CUR-β-CD-PVP complex was 175.4 M −1, 1.15% and 833.3.2 M −1 and 5.21%, respectively. The characterization results revealed amorphization of crystalline state (CUR) into amorphous state. The maximum drug release found with the ternary CUR complex (F7), i.e. 45.41 ± 3.78% in 6 h study. The chemical shift in the NMR supports that the aromatic ring of CUR is completely complexed inside the β-CD cavity. The antioxidant activity of pure CUR was found to be 58.02 ± 2.21% and CUR ternary complex (F7) showed significantly higher activity to 96.02 ± 2.46%. The in-vivo effect of CUR complex (F7) was also found significantly higher than that of pure CUR. The molecular modeling study depicted that PVP increased the stability of the ternary complex by forming the link between CUR and β-CD. Thus, the ternary inclusion complex of CUR-β-CD-PVP could contribute as an innovative outcome in the enhancement of solubility and in-vivo activity.

Self-microemulsifying drug delivery system (SMEDDS) of curcumin attenuates depression in olfactory bulbectomized rats

BackgroundCurrent therapies for depression remain limited and plagued by various side effects. Problems associated with curcumin administration include poor aqueous solubility and bioavailability issues. Hence to overcome these, curcumin self micro emulsifying drug delivery system (SMEDDS) which will result in a nanosize emulsion droplets when administered in vivo were formulated in the present study. MethodsDepression was induced by bilateral olfactory bulbectomy and the animals were randomized into 8 groups as normal, control [(vehicle 10 ml/kg, p.o., (per oral)], pure curcumin (10, 20, 40 mg/kg, p.o.), and curcumin SMEDDS (10, 20, 40 mg/kg, p.o). After 14 days of respective treatment, behavioral parameters such as open field test (OFT), ambulation counts and passive avoidance response (PAR) were evaluated. At the end of experiments, blood was withdrawn from r.o.p (retro orbital plexus) for serum cortisol estimation. ResultsIn OFT, increased central area frequency, peripheral area frequency, central area duration and decreased rearing and grooming were recorded with an increased ambulation counts. In PAR, significant reduction in number of trials and step down from platform was observed in the animals treated with test drug. Serum cortisol level was also found to be decreased in the test groups. ConclusionBehavioral and biochemical estimations in the present study revealed the improved brain permeability and further increase in biological activity of curcumin SMEDDS.

Green surfactant based synthesis of curcumin loaded poly lactic-co-glycolic acid nanoparticles with enhanced solubility, photo-stability and anti-biofilm activity

Curcumin, a polyphenol, has demonstrated bactericidal efficacy against a variety of infections in several clinical studies but unfortunately it has limited usage due to low water solubility and high degradability at neutral to basic pH conditions. In the present study, we optimised nanoprecipitation process using plant extracts (as green surfactants) for the synthesis of curcumin loaded poly lactic-co-glycolic acid nanoparticles. We optimised drug entrapment in curcumin loaded poly lactic-co-glycolic acid nanoparticles, attaining particles of ~90 ± 10 nm and drug loading of ~98 ± 2 μg curcumin/mg of nanoparticles. The in vitro release experiments have shown that these nanoparticles were able to release ~45% of their cargo in 8 h. Photo-stability experiments revealed ~22 ± 7.5% increase in photostability of curcumin loaded poly lactic-co-glycolic acid nanoparticles and solubility studies showed ~13 ± 2 fold increase in solubility. The developed nanoformulation displayed strong anti-bacterial efficacy against Escherichia coli and Staphylococcus aureus, compared to pure curcumin. These nanoparticles also disrupted the biofilm formed by these bacteria. The developed curcumin nanoformulation showed strong cytotoxicity towards HepG2 cells whereas these were found to be cytocompatible towards HEK293 cells. The present nanoformulation may be used for wound healing applications to prevent bacterial infection as well as an anticancer agent.

PERFORMANCE OF CURCUMIN IN NANOSIZED CARRIERS NIOSOMES AND ETHOSOMES AS POTENTIAL ANTI-INFLAMMATORY DELIVERY SYSTEM FOR TOPICAL APPLICATION

Curcumin (CUR) is one of the most commonly used herbal product; it shows effective anti-inflammatory and anti-oxidant effects. However, poor aqueous solubility and low permeability are the major challenges in therapeutic application of curcumin. One class of vesicular nanocarriers called “Niosome and ethosome” which have proved to possess distinct advantages were used to encapsulate curcumin and evaluated for their morphology, particle size, zeta potential, entrapment efficiency (EE%) and drug release. They were incorporated into hydroxy propyl methyl cellulose (HPMC15000) gel then, evaluated on the rat skin via inhibition of carrageenan induced rat paw edema. The results showed that the particle size of curcumin loaded niosomes and ethosomes were ranged (317.5±1.91 to 558.3±8.587 nm) and (182.1±5.3 to 354.5±30.03 nm), respectively. Skin permeation studies demonstrated that CUR permeability coefficient through rat kin for gel formulations of loaded vesicles was ~ four times higher as compared to free CUR. The in-vivo anti-inflammatory studies proved that gel formulations of CUR vesicles possessed higher significant inhibition of carrageenan induced rat paw edema when compared to pure curcumin. Accordingly, the results revealed that, curcumin loaded nanovesicels held great potential approaches as anti-inflammatory in topical application.

Effect of Various Nutraceuticals on Oncoprotein Heparan Sulfatase-2 Activity in Breast Cancer Cell Line

One in ten of all new cancers diagnosed worldwide are the cases of breast cancer and it is a most common form of cancer in women in both developing and developed countries. It is also the principal cause of death from cancer among women globally. Nutraceuticals, basically plant derived components are being used for the prevention and treatment of many diseases, including cancer. Heparan sulfatase-2 (hsulf-2) is a newly isolated oncoprotein, highly expressed in MCF-7 breast cancer cell line and inactivation of this protein possibly may prevent/impede the progression of the cancer. Many nutraceuticals viz. turmeric, ginger, soya and bael fruit extract as a whole and pure components curcumin and zerumbone have been studied in this report. Barring zerumbone, these nutraceuticals significantly inhibited the oncoprotein heparan sulfatase-2 (hsulf-2) activities isolated from MCF-7 breast cancer cell line, with an IC50 value at micro molar levels, indicating that these could be potential anticancer components. Curcumin inhibited cell proliferation with an IC50 value of 37.5 μM, subsequently induced apoptosis of breast cancer cell line. In conclusion, the findings of the present study may provide a basis for further study of these nutraceuticals in the treatment of breast cancer.

Synthesis and characterization of a composite organic semiconductor (curcumin-paracetamol/TiO2)

The aim of this work is to study some physical and chemical properties of an organic semiconductor (OSc)/ x%titanium dioxide (TiO2) heterosystem (with 0 ≤ x ≤ 20%) (OScs/ x%TiO2). The OSc is obtained from pure curcumin and paracetamol as starting molecules. The synthesis methodology of the mixtures of OScs/ x%TiO2 heterosystem involves a microwave-assisted multicomponent reaction using curcumin, paracetamol, and TiO2 as a heterogeneous solution. All mixtures were analyzed by Fourier-transform infrared spectroscopy, Raman spectroscopy, thermogravimetric analysis/differential thermal analysis, X-ray diffraction, ultraviolet–visible spectroscopy, and scanning electron microscopy. The results obtained show a new nanocomposite with interesting pharmaceutical, optical, electronic, and structural properties, which can be used in the fields of energy production, water purification, and air purification, as a biomaterial and for electronic applications.

The Study on Curcuminoids in Chromatography, Spectroscopy and Regioisomerism

The turmeric or Curcuma species was macerated with organic solvents. By executing both analytical and preparative thin-layer chromatographic analysis of the crude material, the chromatographic profile of the curcuminoids could be improved. The Nuclear Magnetic Resonance (NMR) spectra of the pure curcumin, demethoxycurcumin and bisdemethoxy-curcumin was acquired. Additional focus for discussion includes the keto–enol tautomerisation of the products. It is concluded that the understanding of this medicinal herb and its curcuminoidal content, is heightened with advanced technological aid.

Development and Evaluation of Curcumin Liquid Crystal Systems for Cervical Cancer

Curcumin is a hydrophobic compound with good anti-proliferative, anti-oxidative, and anti-cancer properties but has poor bioavailability. Liquid crystals (LC) can accommodate both hydrophilic and hydrophobic drugs. The aim of this study was to formulate and evaluate a novel vaginal drug delivery system for cervical cancer using a curcumin LC system. The curcumin LC system was formulated using surfactant, glycerol, and water together with curcumin. Three types of surfactants were used to optimize the formulation, i.e., Tween 80, Cremphor EL, and Labrasol. The optimized formulations were subjected to physicochemical analysis, and their efficacy was evaluated in HeLa cells. The pH of the formulations was in the range of 3.91–4.39. Environmental scanning electron microscopy (ESEM) observations revealed spherical as well as hexagonal micelles. In vitro release of LC curcumin from vaginal simulated fluid (VSF, pH 4.5) showed a release from 20.47% to 87.25%. The IC50 of curcumin in HeLa cells was 22.5 μg/mL, while the IC25 and IC75 were 6.5 μg/mL and 35μg/mL, respectively. The cytotoxicity of the formulations was determined in comparison with liquid crystals without curcumin and pure curcumin by performing a t-test based on a significance level of p less than or equal to 0.05 (p ≤ 0.05). The curcumin LC system was able to release the required amount of drug and was effective against the cervical cancer cell line examined.

Purification of Curcumin from Ternary Extract-Similar Mixtures of Curcuminoids in a Single Crystallization Step

Crystallization-based separation of curcumin from ternary mixtures of curcuminoids having compositions comparable to commercial extracts was studied experimentally. Based on solubility and supersolubility data of both, pure curcumin and curcumin in presence of the two major impurities demethoxycurcumin (DMC) and bis(demethoxy)curcumin (BDMC), seeded cooling crystallization procedures were derived using acetone, acetonitrile and 50/50 (wt/wt) mixtures of acetone/2-propanol and acetone/acetonitrile as solvents. Starting from initial curcumin contents of 67–75% in the curcuminoid mixtures single step crystallization processes provided crystalline curcumin free of BDMC at residual DMC contents of 0.6–9.9%. Curcumin at highest purity of 99.4% was obtained from a 50/50 (wt/wt) acetone/2-propanol solution in a single crystallization step. It is demonstrated that the total product yield can be significantly enhanced via addition of water, 2-propanol and acetonitrile as anti-solvents at the end of a cooling crystallization process.

Modulation of Pharmaceutical and Pharmacokinetic Attributes of Curcumin Encapsulated in Chitosan Using Spray Drying Technique

The present study is designed to formulate and characterize Curcumin (CUR) loaded Chitosan nanoparticles by ionic cross linking using TPP by employing spray drying technique to enhance the aqueous solubility, hence oral bio availability of Curcumin. Curcumin is very sparingly aqueous soluble, unstable in alkaline conditions and gets eliminated faster, resulting in poor bio availability. Curcumin in alcohol was used as drug loading solution. Tween 80 served as nano emulsifier and stabilizer. EE of optimized formulation F6 was found to be 98.5 ± 0.16 %. This formulation has an average particle size of 25 ± 0.1 nm. The Zeta potential of the formulation is -200 mV. FTIR results revealed the absence of characteristic CUR peak in Curcumin Chitosan nanoparticles implying the successful incorporation of CUR into the Chitosan matrix. DSC thermograms witnessed that the crystalline form of CUR is transformed into amorphous form, having better dissolution and stability profile. SEM imaging of the nanosuspension formulation showed the topological features of the prepared nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. % cumulative drug release studies exhibited very less drug release in Simulated Gastric Fluid (SGF- 3.97 %) and Simulated Intestinal Fluid (SIF - 4.2 %) exhibiting sustained release. Pure Curcumin showed burst release of approximately 95 % in 2 h in SGF with a decline in the concentration after 2 h in SIF due to significantly increased degradation in the alkaline conditions. The oral bioavailability (AUC) of Curcumin in female wistar rats increased 11-times following ingestion of Curcumin nanosuspension in comparison with conventional Curcumin suspension. The maximum concentration Cmax of 1034 ± 96 ng / ml for nanosuspension and 94 ± 9.4 ng / ml for Curcumin suspension and was observed at tmax of 2 h for both nanosuspension and suspension.

Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles.

BackgroundMost of the oral drugs have the properties of weak intestinal absorption and low bioavailability, which leads to little treatment to diseases. By nanotechnology, these drugs can be efficiently delivered to pass biological barriers and promote the cell uptake ability for the enhancement of the oral bioavailability.MethodsThe present work chose the prepared curcumin-loaded galactosylated albumin nanoparticles (Gal-BSA NPs) as the nano-drug samples to study the intestinal capacity and the oral bioavailability.ResultsThe cell uptake assay showed that the Gal-BSA NPs could promote the internalization of more curcumin into the Caco-2 cells. Moreover, the cell uptake mechanism of Gal-BSA-Cur NPs depended on the clathrin-mediated endocytosis transport. The intestinal permeation assay using one Ussing chamber exhibited that the absorptive amounts of curcumin in Gal-BSA-Cur NPs group were 1.5-fold of pure curcumin group. Meanwhile, the permeation mechanism of Gal-BSA-Cur NPs across the intestine mainly depended on the passive transport. The pharmacokinetics study in vivo suggested that the oral bioavailability of Gal-BSA-Cur NPs was improved by 1.4-fold compared with pure curcumin.ConclusionAll results demonstrated that Gal-BSA NPs could improve the intestinal absorption capacity and oral bioavailability of curcumin through the double absorption mechanisms of the clathrin-mediated endocytosis and the passive transport.

Study on condition of ultrasound-assisted thermo-alkali-modified peanut protein embedding curcumin for nanoparticles.

This study investigated the effects of ultrasound-assisted thermo-alkali modification on the molecular structure of peanut protein. Further, the preparation conditions involved in embedding curcumin by the modified pea protein were also studied. It was found that within the pH range of 7 < pH < 11, with an increase in pH, the content of free sulfhydryl group in peanut protein isolate gradually increased from 10.35 ± 0.63μmol/g (pH = 7) to 18.26 ± 0.93μmol/g (pH = 10); and the content of disulfide bonds decreased from 44.62 ± 0.48μmol/g (pH = 7) to 34.26 ± 2.03μmol/g (pH = 11). In the ultrasonic power range (P < 300W), with an increase in power, the content of free mercapto group in peanut protein isolate gradually increased from 12.44 ± 0.73μmol/g to 19.46 ± 0.24μmol/g (P = 250W); and the content of disulfide bonds decreased from 42.29 ± 1.24μmol/g to 33.28 ± 0.64μmol/g (P = 300W). Within the temperature range of 70°C < T < 90°C, with an increase in temperature, the content of free sulfhydryl group in peanut protein isolate gradually increased from 10.35 ± 0.94μmol/g (T = 70°C) to 19.67 ± 0.68μmol/g (T = 90°C), and the content of disulfide bonds decreased from 45.02 ± 2.84μmol/g (T = 70°C) to 34.26 ± 2.03μmol/g (T = 90°C). Response surface test was used to optimize the preparation conditions of nanoparticles from curcumin. The results showed that the optimum parameters of ultrasonic-assisted modification of peanut protein embedding curcumin were pH = 9.8, heating temperature T = 90°C, ultrasonic power Q = 225W, and heating time S = 21min. Under these conditions, the embedding rate of curcumin reached 83.27 + 1.06%, the ABTS+ scavenging activity generally decreases with time over the 2days period measured in PPI solution and PPI nanoparticles (PPN), the ABTS+ scavenging activity decreased from 40.8%, 52.2% and 67.3% to 27.1%, 39.0% and 60.5%, respectively. Compared with pure curcumin, the antioxidant activity was increased at presence of PPI.