Preparation Of Curcumin Research Articles

Highly bioavailable curcumin preparation with a co-grinding and solvent-free process.

Curcumin (Cur.) is a natural product isolated from the rhizome of Curcuma longa, with a variety of biological and pharmacological activities in food and pharmaceutical products. However, curcumin's poor solubility in water greatly limits its bioavailability and clinical applications. In this study, co‐grinding curcumin with food additives produced a mixture, which was evaluated for the solubility in water, dissolution, material morphology, in vivo bioavailability, cell uptake and entry mechanism. We tested 9 food additives in total and found that poloxamers performed the best. The 2 co‐grinding mixtures Cur./Kolliphor® P407 and Cur./Kolliphor® P188 with high drug loading at 65.5% significantly improved the curcumin aqueous solubility, subsequently increased its intestinal epithelial cell uptake and oral bioavailability. The relative bioavailabilities for the 2 co‐grinding mixtures were 309% and 163%, respectively, compared with curcumin API. Co‐grinding process has a broad application prospect and is suitable for industrial production.

Preparation and characterization of curcumin functionalized copper nanoparticles and their application enhances disease resistance in chickpea against wilt pathogen

Abstract For effective use of curcumin in plant disease management, it is imperative to increase its solubility. Decreasing the particle size can increase the surface area and enhance solubility. Therefore, the present study aims to prepare curcumin copper nanoparticles (Cur-CuNPs) to improve its aqueous solubility to use as an antifungal agent and to protect chickpea plants from the devastating pathogen, Fusarium oxysporum f. sp. ciceri (FOC). The Cur-CuNPs were analyzed by 1H NMR, 13C NMR spectroscopy. The structure, size, morphology was characterized through FTIR, SEM, TEM and XRD analyses. The Cur-CuNPs synthesized in this study was found to be freely dispersible in water and inhibits the growth of FOC under in vitro condition, protects the chickpea plant from wilt disease. Application of Cur-CuNPs to chickpea seed influenced the growth parameters such as root, shoot length, number of leaves and dry weight. These results indicate that Cur-CuNPs can be integrated in disease management strategies as fungicide and as nanofertilizer to enhance chickpea plant health.

Preparation, optimization and preliminary pharmacokinetic study of curcumin encapsulated turmeric oil microemulsion in zebra fish

The present investigation aimed to develop curcumin loaded turmeric oil microemulsion for brain targeting. An effort has been made to investigate the role of functional components in developing brain targeted formulation which could enhance the bioavailability and uptake of drug in the brain upon oral administration. Preliminary studies like solubility study, emulsification study and construction of the pseudo ternary phase diagram were performed for screening components. The formulation was optimized by using extreme vertices mixture design. The optimized formulation was characterized for appearance, stability to centrifugation, dilution potential, globule size, zeta potential and drug content. Furthermore, ex-vivo permeation in chicken gut sac non everted technique and pharmacokinetic study in adult zebra fishes were carried out. The optimized formulation was found to clear, yellow-colored with the absence of phase separation and precipitation denoted the stability of formulation to centrifugation and dilution. The mean globule size, polydispersity index, zeta potential and drug content was observed as 29.13± 0.12 nm, 0.23 ± 0.01,-12.33 ± 1.37 mV and 99.10±3.91 %, respectively. Ex vivo permeation study revealed 2.41 fold enhancement in the steady-state flux when compared to curcumin solution. Furthermore, optimized formulation showed shorter Tmax (5 min) and higher AUC(0-∞) (7.93 μg/brain*min) compared to the curcumin solution which showed similar Tmax and AUC(0-∞) of 2.78 μg/brain*min after oral administration to zebra fishes revealing 3.97 fold enhancement. The results revealed enhanced ex vivo oral absorption and enhanced in vivo brain pharmacokinetics of curcumin via functional microemulsion in the zebra fish model.

Preparation, characterization and cytotoxic applications of curcumin‐(±) α‐lipoic acid coloaded phosphorylated chitosan nanoparticles in MDA MB 231 breast cancer cell line

In the present work, curcumin in combination with (±) α‐Lipoic acid were used as the active agents for the preparation of phosphorylated chitosan nanoparticle. Ionic gelation method was used for the successful fabrication of the nanoparticles. Effective incorporation of the drugs in the polymeric system was revealed by Fourier‐transform infrared spectroscopy (FT‐IR) and X‐ray diffractometry (XRD). Scanning electron microscope, transmission electron microscope and dynamic light scattering method were used to analyze the morphology and dimensional characteristics of the nanoparticles. The swelling degree and drug release mechanism were studied at pH 5.0 and 7.4 for different time periods by UV‐visible spectrophotometer. Cytotoxicity study was performed by MTT assay analysis on normal human lymphocyte and MDA MB 231 breast cancer cell line. Trypan blue dye exclusion assay was performed to confirm the anticancer effect of the nanoparticles. The properties of the prepared nanoparticles recommended their possible application as anticancer agents.

Structural and therapeutic properties of curcumin solubilized pluronic F127 micellar solutions and hydrogels

Curcumin, the principle active constituent of turmeric, is known to have broad range of therapeutic properties. Its poor aqueous solubility and low bioavailability however, act as constraints for its biomedical applications. Recent studies have shown that incorporation of curcumin in nano-carriers like micelles, vesicles, polymeric nanoparticles etc. can help in overcoming these issues and improve its therapeutic abilities quite significantly. In this manuscript, we report preparation of curcumin solubilized pluronic F127 micellar solutions and hydrogels, along with their structural and therapeutic properties as obtained from SANS, rheological, anti-cancer and wound healing studies. Pluronic F127 being approved by FDA has been used quite extensively as excipient for drug delivery applications. Curcumin solubilization in the aqueous pluronic F127 system was carried out by briefly heating the copolymer solutions with curcumin at 90 °C. The concentrations of curcumin thus obtained were found to be comparable to those obtained by conventional methods of solubilization like thin film hydration or solvent evaporation method, and three orders of magnitude higher than that in pure water. SANS and rheological studies show that curcumin solubilization does not bring about any significant change in the structural and rheological properties of F127 micellar solutions and hydrogels. Curcumin solubilized F127 micellar solutions can be reconstituted after lyophilization, suggesting that curcumin remains nano-dispersed in lyophilized state. Micellar encapsulated curcumin exhibits very good stability in solution state in ambient condition but fails to show cytotoxicity against MCF7 cancer cells, presumably due to shielding of curcumin by large corona region of F127 micelles. Micellar curcumin containing F127 hydrogels on the other hand, exhibit wound healing abilities in mice model upon topical application. The results give an account of how some of the therapeutic properties of curcumin are manifested under micellar encapsulation and the role of pluronic F127 as excipient in those therapeutic applications.

Further Evidence of Benefits to Mood and Working Memory from Lipidated Curcumin in Healthy Older People: A 12-Week, Double-Blind, Placebo-Controlled, Partial Replication Study.

Curcumin (a flavonoid isolated from turmeric) affects several processes involved in neurocognitive aging. We have previously reported that short term (4-weeks) administration of a highly bioavailable curcumin preparation (Longvida©) improved working memory and reduced fatigue and stress reactivity in a healthy older cohort. The present trial (ACTRN12616000484448) was a partial replication study, evaluating similar effects at 4 and 12-weeks Longvida© supplementation. A double-blind, placebo-controlled, parallel-groups trial was conducted. Eighty participants aged 50–80 years (mean = 68.1, SD = 6.34) were randomised to receive Longvida© (400 mg daily containing 80 mg curcumin) or a matching placebo. Assessment took place at baseline then following 4 and 12 weeks treatment. Outcome measures included cognitive performance, mood and biomarkers. Compared with placebo, curcumin was associated with several significant effects. These included better working memory performance at 12-weeks (Serial Threes, Serial Sevens and performance on a virtual Morris Water Maze), and lower fatigue scores on the Profile of Mood States (POMS) at both 4 and 12-weeks, and of tension, anger, confusion and total mood disturbance at 4-weeks only. The curcumin group had significantly elevated blood glucose. These results confirm that Longvida© improves aspects of mood and working memory in a healthy older cohort. The pattern of results is consistent with improvements in hippocampal function and may hold promise for alleviating cognitive decline in some populations.

Preparation and antibiofilm studies of curcumin loaded chitosan nanoparticles against polymicrobial biofilms of Candida albicans and Staphylococcus aureus

Polymicrobial biofilms related infections are an important clinical problem with classical antibiotics being not sufficient in therapy. Here, curcumin (Cur) was loaded on positively charged chitosan nanoparticles (CSNP). The antibiofilm activities against mono- and polymicrobial biofilms of Candida albicans and Staphylococcus aureus were evaluated. The average diameter of CSNP-Cur was 134.37 ± 1.99 nm and its surface charge was +18.10 ± 0.82 mV. Cur released from NPs was slower at pH 7.4 than at pH 5.4. Scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM) were used to observe biofilm architecture and live/dead organisms within biofilm on medical silicone surface. CSNP-Cur exhibited excellent antibiofilm activity against planktonic bacteria or fungi, mono- and polymicrobial biofilm formations and preformed biofilms. SEM and CLSM showed that CSNP-Cur was able to reduce biofilm thickness as well as kill microbial cells embedded in biofilm on silicone surfaces.

The Effect of Modified Curcumin Compounds on the Numbers and Morphology of Microglia

Chronic neuroinflammation is a promising therapeutic target in many neurodegenerative and age‐related brain disorders. In this study, we investigated two highly bioavailable curcumin preparations, Longvida (LC) and Meriva (MC) for their anti‐inflammatory properties, using the GFAP‐IL6 mouse model. We hypothesized that the highly bioavailable curcumin, as a potent cytokine‐suppressive anti‐inflammatory drug, will decrease microglial and astroglial activation measured by cell number and morphology, and consequently improve motor and cognitive functions.MethodsGFAP‐IL6 and wild type mice were fed with LC and MC for 1 and 5 months, respectively. LC fed mice were tested on the elevated walking beam, Rotarod, Barnes maze and Novel object recognition tests before all the mice were sacrificed. Immunohistological staining for microglia and astrocytes were carried out and unbiased stereological analysis was completed for all groups on microglia(labelled by Iba‐1 and TSPO) and astrocytes numbers (GFAP) as well as the morphology of the cells were analyzed using the MBF Biosciences system (StereoInvestigator and Neurolucida 360).ResultsShort term MC oral administration lead to a dose‐dependent reduction in neuroinflammatory markers. Moreover, MC decreased the number of activated microglia and astroglia, as well as changed the microglial morphology from activated to resting state. Long term LC treatment led to a significant decrease in the number of microglia in the hippocampus and cerebellum and in turn, led to significant improvement of both motor and cognitive function. Both short‐ and long‐term consumption of modified curcumin preparations significantly downregulated microglial activation GFAP‐IL6 mice. Spatial memory and recognition memory improvements were also found in mice fed with LC in comparison to control counterparts. Our results promise potential therapeutic applications of both Longvida and Meriva curcumin against brain inflammation and associated cognitive and motor decline.Support or Funding InformationThe present study was supported by a project grant (#P00023016) by Indena S.P.A, Italy to GM and EG. F.U has been supported by a postgraduate scholarship by Western Sydney University.

Preparation and evaluation of curcumin grafted hyaluronic acid modified pullulan polymers as a functional wound dressing material

Curcumin grafted hyaluronic acid modified pullulan polymers (Cur-HA-SPu) by chemical conjugation was designed and prepared, and its film may be used to accelerate wound healing and help to fight infection. The synthesis of Cur-HA-SPu polymer was characterized by FT-IR, 1H NMR and DSC. Cur-HA-SPu film has a higher swelling ratio than that of HA-SPu film. Moreover, the good biocompatibility of Cur-HA-SPu polymer was confirmed by skin irritation, cytotoxicity and hemolysis tests. Compared to Cur, the MTT and proliferation test carried out in L929 cells revealed that Cur-HA-SPu polymer showed no cytotoxicity and enhanced cell proliferation. Cur-HA-SPu polymer exhibited a certain bactericidal activity against E. coli and S. aureus. Furthermore, the materials showed antioxidant activity when DPPH method determined. Wound healing study using wistar rat model demonstrated that Cur-HA-SPu film obtained better wound healing result than that of HA-SPu film or natural healing. The above results suggest that Cur-HA-SPu film is a promising and safety formulation for accelerating skin wound healing.

The effect of molecular weight and content of PEG on in vitro drug release of electrospun curcumin loaded PLA/PEG nanofibers

This study focused on preparation of curcumin (CUR) loaded poly (lactic acid) (PLA) nanofibers by electrospinning technique. The hydrophilicity of nanofibers was modified by the addition of poly (ethylene glycol) (PEG) with molecular weight of 1500 in different weight (0, 5, 10, 15, and 20 wt% related to the PLA content) and also by the addition of PEG with different molecular weights (6000, 3350, 1500, 600, 400) in the same content of 10 wt% related to the PLA content. The electrospun PLA/CUR/PEG nanofibers are characterized by scanning electron microscopy, differential scanning calorimetry, Fourier-transform infrared spectroscopy, contact angle measurements and weight loss investigation in the phosphate buffered saline. Vertical diffusion cell was used to perform in vitro drug release from the prepared nanofiber mats through recording curcuminoids content by high performance liquid chromatography. The results showed that the drug release was intensified with decrease in the molecular weight of PEG and increase in the PEG content. As well, the adhesion assay of the PLA/CUR/PEG nanofiber mats were examined and the related SEM images revealed that the MG-63 cells could growth well and spread out over the surface of the PLA/CUR/PEG nanofiber mats with 20 wt% of PEG1500 in comparison with the nanofibers containing 0 wt% of PEG1500. Eventually, the prepared electrospun CUR-loaded nanofibers with capable of providing a susceptible medium for accelerating the drug release can be good candidate for wound dressing applications.

Fabrication of nanopatterned PLGA films of curcumin and TPGS for skin cancer.

Squamous cell carcinoma treatment has limited therapeutic options and the incidence rate is increasing recently. In the present investigation, we developed poly(lactic-co-glycolic acid) (PLGA) nanopatterned films (NPFs) through poly dimethyl siloxane (PDMS) cast molding technique and explored its therapeutic efficacy in combination with curcumin and tocopherol poly (ethylene glycol) 1000 succinate (TPGS). Herein, we demonstrate the preparation and characterization of curcumin loaded tocopherol polyethylene glycol 1000 succinate stabilized poly (lactic-co-glycolic) acid nanopatterned films (CTP-NPFs). CTP-NPFs showed good in vitro cytotoxicity towards human skin cancer cell line (A431) when compared to that of unpattern films. CTP-NPFs effectively inhibited the progression of 7, 12-Dimethylbenz[a]anthracene (DMBA)/croton oil induced skin cancer in Swiss albino mice. The nanopatterned films could be used as an alternate treatment for skin cancer.

Effects of Highly Absorbable Curcumin in Patients with Impaired Glucose Tolerance and Non-Insulin-Dependent Diabetes Mellitus

Oxidative stress is enhanced by various mechanisms. Serum oxidized low-density lipoprotein (LDL) is a useful prognostic marker in diabetic patients with coronary artery disease. To examine the effects of Theracurmin®, a highly absorbable curcumin preparation, on glucose tolerance, adipocytokines, and oxidized LDL, we conducted a double-blind placebo-controlled parallel group randomized trial in patients with impaired glucose tolerance or non-insulin-dependent diabetes mellitus. We randomly divided the patients with impaired glucose tolerance or non-insulin-dependent diabetes mellitus and stable individuals into the placebo group and the Theracurmin® (180 mg daily for 6 months) group. Of the 33 patients analyzed, 18 (14 males and 4 females) were administered placebo and 15 (9 males and 6 females) were administered Theracurmin®. The patient characteristics did not differ between the two groups. The primary endpoint, HbA1c, did not differ significantly between the two groups. However, the level of α1-antitrypsin-low-density lipoprotein (AT-LDL), the oxidized LDL, significantly increased (p = 0.024) in the placebo group from the beginning of the trial up to 6 months, although there was no such change in the Theracurmin® group. The percentage change in BMI from the beginning of the trial up to 6 months tended to be higher in the Theracurmin® group than in the placebo group. Patients in the Theracurmin® group tended to have a larger percentage change in adiponectin and LDL-C than those in the placebo group. Patients in the Theracurmin® group showed a smaller percentage change in AT-LDL than those in the placebo group. This study suggests that the highly absorbable curcumin could potentially inhibit a rise in oxidized LDL in patients with impaired glucose tolerance or non-insulin-dependent diabetes mellitus. This trial is registered with UMIN000007361.

Изучение пребиотических свойств кисломолочного продукта, обогащенного препаратами инулина, куркумина и хрома

В статье представлены результаты изучения пребиотических свойств кисломолочного продукта, обогащенного препаратами инулина, куркумина и хрома.
 Исследования проводились на лабораторных мышах, больных сахарным диабетом 2 типа, у которых искусственным путем было спровоцировано заболевание, при котором возникает дисбактериоз кишечника. Исследовался характер изменений количества и состава кишечной микрофлоры, на фоне которого изучался эффект коррекции кишечной микрофлоры при использовании кисломолочного продукта обогащенного препаратами инулина и хрома. Полученные данные после окончания коррекции продуктом свидетельствуют о стабилизации состава кишечной микрофлоры у лабораторных мышей.

Impregnation of Curcumin into a Biodegradable (Poly-lactic-co-glycolic acid, PLGA) Support, to Transfer Its Well Known In Vitro Effect to an In Vivo Prostate Cancer Model.

Prostate cancer (PCa) is one of the most common cancers in older men and is associated with high mortality. Despite advances in screening for early detection of PCa, a large proportion of patients continue to be diagnosed with metastatic disease, with ~20% of men showing a high tumor grade and stage. Medicinal plant extracts have a great potential to prevent/treat PCa, as well as to reduce its incidence/prevalence and improve survival rates. One of the most promising extracts is curcumin, which is a major, nontoxic, bioactive compound of Curcuma longa. Curcumin has strong antitumor activity in vitro. However, its potential beneficial in vivo affects are limited by its low intestinal absorption and rapid metabolism. In this study, curcumin was impregnated into a biodegradable poly(lactic-co-glycolic) acid (PLGA) support and characterized by FTIR and DSC, and its release by UV spectrophotometry. PLGA-curcumin was tested in different subcutaneous PCa xenograft models (PC3, 22rv1, and DU145 PCa cell-lines), and its effects evaluated by tumor progression an immuno-histochemical analysis (Trichromic, Ki67 and TUNEL stainings), were compared with those of a commercial curcumin preparation. Our results indicate that curcumin-impregnated PLGA is significantly more active (~2-fold increase) with respect to oral curcumin, which supports its use for subcutaneous administration.

Preparation and Characterization of Curcumin Loaded Dextrin Sulfate- Chitosan Nanoparticles for Promoting Curcumin Anticancer Activity

Curcumin as a natural medicinal agent has been proved to kill cancer cells effectively. However, its biomedical applications have been hindered owing to its poor bioavailability. Many nanoparticulate systems have been introduced to overcome this problem. Among this types polymeric-based nanoparticles which exhibit unique properties allowing their use as a efficient drug carrier. Developing a polymeric- blend nanoparticles will offer a promising nanocarrier with excellent biocompatibility, biodegradability and low immunogencity.
 In this study, curcumin nano-vehicle has been made up by combining dextren sulfate and chitosan (DSCSNPs). DSCSNPs have been characterized using different techniques. Transmission electron microscopy (TEM) which revealed the spherical, smooth surface of the nano-formulation. Dynamic light scattering (DLS) for measuring DSCSNPs hydrodynamic- diameter. Zeta potential measurements showed nanoparticles high stability. Fourier transform infrared spectroscopy (FTIR) confirmed successful combination between the two polymers and curcumin loading on naoparticles surface. Curcumin release profile out of DSCSNPs showed high drug release in tumor acidic microenvironment. In vitro cytotoxicity measurements demonstrated that curcumin loaded polymeric nanoparticles (DSCSNPs-Cur) have high therapeutic efficacy against colon (HCT-116) and breast (MCF-7) cancer cells compared with free curcumin. DSCSNPs as a combined biopolymers is an excellent candidate for improving curcumin bioavailability allowing its use as anticancer agent.

Evaluation of Antipsoriatic Activity of Topical Curcumin by using Mouse Tail Model

Background; Psoriasis is a one of the common dermatological diseases with no curative topical or systemic treatment, Curcumin is a naturally occurring phytochemical present in turmeric; it was traditionally used for the treatment of many skin diseases. This study was designed to evaluate the anti-psoriatic effect of curcumin preparations. Objectives; this study aimed to examine the probability of anti-psoriatic activity of topical curcumin by using mouse tail model. Methods; The extracted curcumin was assessed for antipsoriatic activity using a mouse tail model of psoriasis. 18 animals were divided into three groups (6 animals each). Group A: control group (cream base treated group) Group B: (treated with curcumin cream 1%) Group C: (treated with curcumin cream 2 %) Granular layer formation, epidermal thickness and drug activity were taken as an evaluating parameter to detect the efficacy of the new preparation. Results; The local application of curcumin 1%, 2% on the mouse tail skin produced a significant differentiation in the epidermis, as seen from its degree of orthokeratosis ( 43.4± 0.75) and ( 44.4 ±0.98 ) respectively when compared with the negative control (17.06±2.5 ). Conclusion;                   Topical curcumin have anti-psoriatic activity  and  seems to be well tolerated on skin since the incidence of side effects was limited except staining of  skin by an orange color.

Effects of phytosomal curcumin on anthropometric parameters, insulin resistance, cortisolemia and non-alcoholic fatty liver disease indices: a double-blind, placebo-controlled clinical trial

PurposeCurcumin has shown to exert a positive impact on human glucose metabolism, even if its bioavailability is usually very low. The present study aimed to explore the effect of phosphatidylserine- and piperine-containing curcumin phytosomes on a large number of metabolic parameters related to insulin resistance, in the context of a randomized double-blind placebo-controlled trial involving 80 overweight subjects with suboptimal fasting plasma glucose.MethodsSubjects were randomized to be treated with indistinguishable tablets (2 per day, to be taken after dinner) containing 800 mg phytosomal curcumin (Curserin®: 200 mg curcumin, 120 mg phosphatidylserine, 480 mg phosphatidylcholine and 8 mg piperine from Piper nigrum L. dry extract) for 8 weeks.ResultsAfter 56-day treatment, the curcumin-treated group experienced a significant improvement in fasting plasma insulin (FPI), HOMA index, waist circumference, blood pressure, triglycerides (TG), HDL-C, liver transaminases, gamma-GT, index of liver steatosis and serum cortisol compared to the baseline. FPI, TG, liver transaminases, fatty liver index and serum cortisol level also significantly improved compared with the placebo-treated group. Compared to the baseline, at the end of the study placebo group experienced an improvement only in FPG and TG.ConclusionIn conclusion, the present trial shows that supplementation with a phytosomal preparation of curcumin containing phosphatidylserine and piperine could improve glycemic factors, hepatic function and serum cortisol levels in subjects with overweight and impaired fasting glucose.

Preparation and characterization of curcumin loaded caseinate/zein nanocomposite film using pH-driven method

Functional edible films manufactured from crop by-products is promising for food industry. In this study, antioxidant films prepared from self-assembled curcumin-loaded sodium caseinate (NaCas)-zein composite nanoparticles was investigated. Nanocomposite film-forming dispersions were obtained by dissolving curcumin into polymer mixtures with NaCas/zein ratios of 100:0, 75:25 and 50:50 at pH 12.0, and then neutralized back to pH 7.0. The colloidal particles showed an average particle size and ζ-potential around 131–184 nm and -40 mv, respectively. Regardless of the NaCas/zein ratio in film-forming dispersions, the curcumin presence enabled NaCas/zein film to exhibit red-yellow color and antioxidant properties as evaluated by DPPH radical scavenging activity. Surface properties of films were further characterized by contact-angle measurement and scanning electron microscopy. An increasing proportion of zein could significantly improve the tensile strength (from 3.12 to 7.85 MPa) and constrain moisture transfer as indicated by decreased water vapor permeability from 0.87 to 3.56 × 10−10 g·Pa·m-1·s-1. However, the elongation resistance of NaCas-based films was compromised from 50.5% to 30.8%. When the zein proportion in the formulation reached 50:50, curcumin showed the best stability under elevated temperatures and long-time storage. The underlying mechanism of this alcohol-free process to prepare zein-based nanocomposite film is also proposed and discussed.

Comparison of Two Commercial Preparations of Curcumin using the Caco-2 in vitro Assay of Human Intestinal Permeability

Objectives: The transport of curcuminoids in Caco-2 cell monolayers, which are widely used as an in vitro model of drug permeability in the human small intestine, was investigated. The formulations tested demonstrated two distinct methods for enhancing the intestinal absorption and bioavailability of curcumin: a curcumin– phospholipid complex and a turmerone/piperine-enhanced curcumin product. Design and outcome measures: Two unique formulations representing distinct approaches to maximizing curcumin bioavailability were compared with each other and with standard control compounds. Outcomes evaluated included apparent permeability, which reflects the ability of drug molecules to penetrate the intestinal tract; percentage recovery of compound through the Caco-2 monolayer; and efflux ratio, which is generally considered to reflect the role of efflux proteins in expelling compounds from the intestinal lumen. Results: In our widely used Caco-2 cell model experiments, the absorption of curcumin from each unique commercial formulation was equivalent at the single concentration tested. Furthermore, curcumin efflux was substantially reduced in the turmerone/piperine formula, though the difference between formulations was not significant. This reduction of curcumin efflux was expected on the basis of reports of piperine’s P-glycoprotein-inhibitory activity. Conclusion: The results of the present experiment strongly suggest that the incorporation of turmerones and piperine into curcumin preparations may be a simple way to improve the poor bioavailability of curcumin, which has previously been shown to be improved by the formulation of curcumin into curcumin–phospholipid complexes.

A W/O emulsion mediated film dispersion method for curcumin encapsulated pH-sensitive liposomes in the colon tumor treatment

The CaCO3 encapsulated liposome with pH sensitivity is an efficient carrier for the delivery of chemotherapeutic drugs. Herein, we provided an innovative method that take advantage of a W/O emulsion to prepare CaCO3 encapsulated liposomes for the delivery of curcumin. The liposomes with both CaCO3 and curcumin encapsulated (LCC) showed high sensitivity to reduced pH (the environment of lysosomes). Due to the inherent pH sensitivity of CaCO3, LCC swelled and released the encapsulated curcumin rapidly in acidic medium. The lysosome escape capability and promoted accumulation of curcumin in the cytosol from LCC was verified with respect to that of curcumin loaded liposomes (CLIPO). Despite the similar cytotoxicity within curcumin preparations in vitro at high concentration, LCC exhibited optimal antitumor effect in an azoxymethane (AOM)/dextran sodium sulfate (DSS)-induced colorectal cancer model, which was attributed to the long circulation time and efficient intracellular delivery of curcumin from LCC. It is suggested that the solubility and cytosolic delivery of curcumin are greatly improved by LCC, which accounts for the increased pharmacodynamic effect of curcumin. Thus, the CaCO3 encapsulated liposomes developed in this study is an ideal carrier for the hydrophobic drugs in potential clinical application.