Baek JS , Cho CW Eur J Pharm Biopharm , 117:132-140, 12 Apr 2017 The purpose of this study was the comparative measurement of the increases in levels of curcuminoids (curcumin, demethoxycurcumin, bisdemethoxycurcumin) and the metabolite tetrahydrocurcumin after oral administration of three different . 2019 Aug;44(4):459-480. doi: 10.1007/s13318-019-00545-z. Enhanced oral bioavailability and improved pharmacokinetics afforded to drugs through nanoformulation potentially allows for modified, more patient acceptable regimens. The low water solubility of curcumin which leads to poor bioavailability, however, has been highlighted as a major limiting factor. The intended route of delivery of the studied nanomedicine nanostructured polymer (such as nanoparticles, dendrimers, micelles and drug conjugates) was oral. 145 Combinations of curcumin with piperine and quercetin have been successfully used for the. Enhancing Curcumin Oral Bioavailability Through Nanoformulations. We're encouraged by curcumin's promising role in treating cancer and reducing risk. (2012) The oral absorption rates of all the drug candidates of statin group exhibits different. Indian . We report here that the water solubility of curcumin could be increased from 0.6 μ g/ml to 7.4 μ g/ml (12-fold increase) by the use of heat. This study, for the first time, provides a comprehensive overview of the application of natural-products-based nanoformulations in the management of metabolic syndrome. Comparative bioavailability of curcumin, tumeric, and Biocurcumax TM in traditional vehicles using non-everted rat intestinal sac model. (2012) ^ Hu L1, et al. Enhancing Curcumin Oral Bioavailability Through Nanoformulations. to Curcumin Catechin is a phytochemical largely present in Acacia catechu which is known for its biological potential, but its utilization is greatly limited by its low bioavailability. Curcumin is the active ingredient in the spice turmeric. Enhancing Curcumin Oral Bioavailability Through Nanoformulations. Curcumin is a well-known compound that possesses pleiotropic activity, including anticancer activity. In this scenario, Gao et al. (iv) Chewable 5000ug - 27% - A dissolvabletablet of B 12 that is absorbed through the sublingual mucosa (v) Liposome 1000ug - 14% - A liposome oral spray of B 12 with particle sizes of approximately 100 nm. Ipar VS, Dsouza A, Devarajan PV. The use of polyphenols and specifically quercetin, for improving memory and mental endurance has shown significant effects among rats. (CUR), named CUR-PLGA-NPs, and to study the effect and mechanisms enhancing the oral bioavailability of CUR. The majority of oral curcumin is excreted in the feces (≤90%), . The AUC of THERACURMIN was 27-fold higher than that of curcumin powder. Over the years, natural compounds have been explored as an alternative to conventional cancer therapies such as surgery, radiotherapy, and chemotherapy. . In addition, curcumin was proven to be anti-diabetic, hepatoprotective . European Journal of Drug Metabolism and . Food Research International, 2016. 260 Application of curcumin-loaded nanocarriers for food, drug and cosmetic purposes Enhancing the performance of PEG-b-PCL-based nanocarriers for curcumin through its conjugation with lipophilic biomolecules Show all authors. In a study conducted by Cruz-Correa et al., oral curcumin was prescribed to the patients with adenomatous polyposis. Thus, the incorporation of curcumin in drugs depends on increasing the water solubility of the compound and enhancing its stability and bioavailability. The maximum oral dose of 8 gm/day of curcumin does not produce any toxic effects [7]. Strategies . Jamwal R. Bioavailable curcumin formulations: A review of pharmacokinetic studies in healthy volunteers. Clinically validated dosages were used for both products, and plasma levels of all three major curcuminoids [curcumin (1a), demethoxycurcumin (1b), and bisdemethoxycurcumin (1c)] were evaluated. Atorvastatin oral absorption is reported by 30% and of which 12% would be the bioavailability [6]. The area under the blood concentration-time curve ( AUC) after the oral administration of THERACURMIN was found to be more than 40-fold higher than that of curcumin powder in rats. • Prolonged lipolysis of SLNs was due to interfacial hindrance by long-PEGylation. J Agric Food Chem. Ganesh NS, Hanumanthachar Joshi GB, Jayanthi C, Singh DP (2013) Buoyant multiparticulate drug delivery-A focus on hydrogel beads. Due to the cause for the poor bioavailability atorvastatin is absorbed primarily from the It enhances its aqueous solubility and targeted delivery to the tissue of interest that prompts to enhance the bioavailability, better drug conveyance, and more expeditious treatment. Introduction. Anti-inflammatory and anti-hepatitis C virus (HCV) activities have been associated with CUR. recent advances in the development of strategies to improve oral bioavailability. The low oral bioavailability of curcumin may be speculated as a plausible factor that limits its effects in humans. by Taylor & Francis. A pilot cross-over study to evaluate human oral bioavailability of BCM-95CG (Biocurcumax), a novel bioenhanced preparation of curcumin. It is readily metabolized in the body, but many active metabolites of curcumin have been identified that could also be exploited for therapy. CUR-PLGA-NPs were prepared according to a solid-in-oil-in-water (s/o/w) solvent evaporation method and exhibited a smooth and . However, due to unsatisfactory aqueous solubility and hence low bioavailability, clinical application of curcumin has been greatly restrained. Curcumin, another bioactive natural product and a promising candidate against many diseases including cancer has limitations due to its poor bioavailability. This study reviews the recent efforts in the application of nanotechnology in formulation of natural drugs to improve NDs treatment. After overnight incubation, different concentrations of Cur/M, DTX/M or DTX-Cur/M were added and treated cells for 24 hrs or 48 hrs. The results showed a significant increment of 3.95 times in Cmax, and 194.2% in bioavailability, compared to the curcumin suspension. Enhancing the bioaccessibility of hydrophobic bioactive agents using mixed colloidal dispersions: Curcumin-loaded zein nanoparticles plus digestible lipid nanoparticles. The drug release of atorvastatin and curcumin from ACCNS 1 to ACCNS 6 chitosan nanoparticles exhibited burst release of atorvastatin (12.52 ± 1.2% to 15.39 ± 1.3%) and curcumin (14.47 ± 1.3% to 14.66 ± 1.4%) at first 30 min and later on showed a kind of biphasic release pattern with a gradual increase in releasing drug until 48 h period of . Methods: Solid dispersions have been utilized in the last few decades to improve the bioavailability and stability of curcumin. Curcumin possesses a plethora of interesting pharmacological effects. Several curcumin nanoformulations have been developed, and others are still under clinical trials assessment . This study, for the first time, provides a comprehensive overview of the application of natural-products-based nanoformulations in the management of metabolic syndrome. Enhancing Curcumin Oral Bioavailability Through Nanoformulations. In the present research work catechin rich extract has ique with minimized dosing employing Eudragit L 100 as a polymer for enhancing its bioavailability. ^ Yu H1, Huang Q. It has been shown to induce cell death in a variety of cancer cells, however, its effect on CAL27‑cisplatin-resistant human oral cancer cells (CAR cells) has not been elucidated to date. etc, [] have multiple pharmacological properties such as antioxidant, antitumor, and anti-inflammatory effects and so on. Formulated monoclonal antibody which conjugates with curcumin . Curcumin is a promising therapeutic agent that exhibits manifold therapeutic activities. Applicable Strategies of Curcumin in Drug Delivery Systems Primary attempts to increase bioavailability of curcumin by using piperine promoted over 100% and 2000% curcumin bioavailability in rats and humans respectively, but they could Combined with piperine, curcumin can synergistically improve anti-inflammatory and antioxidant activity. This research was implemented to determine the safety and efficacy of curcumin in patients with adenomatous polyposis. Nanoformulations of these natural substrates are effective tactics to overcome such problems and can enhance their bioavailability (Ratheesh et al., 2017). • Enhanced bioavailability was due to prolonged lipolysis and good mucus permeability. Cells at logarithmic phase were seeded in a 96-well plate at the density of 3.5×10 3 cells per well. Abstract Oral administration is an appealing route of delivering cancer treatments. iii. Enhancing absorption and bioavailability of curcumin and turmeric. With the ongoing development of nanotechnology, the nanoparticles have its own importance in novel drug delivery system. There is now growing scientific evidence to support the effectiveness of the use of herbal supplements in the prevention and control of diabetes. Integrating curcumin into nanocarriers through various methods is an appropriate and fruitful choice to upsurge the biological activity of curcumin, which increases its bioavailability and solubility, long time circulation, and However, it is challenging to study curcumin as it exhibits poor aqueous solubility and low permeability and it is a substrate for P-glycoprotein (P-gp). Eur J Drug Metab Pharmacokinet, 44(4):459-480, 01 Aug 2019 Cited by: 7 articles | PMID: 30771095. Review Furthermore, the use of nanotechnology and a targeted drug delivery system may improve the bioavailability of curcumin. Preparation and enhancement of oral bioavailability of curcumin using microemulsions vehicle. The relative absorption of a standardized curcuminoid mixture and its corresponding lecithin formulation (Meriva) was investigated in a randomized, double-blind, crossover human study. Eur J Drug Metab Pharmacokinet. Recently, nanoformulations with co-delivery of multiple chemotherapeutic agents with synergistic action like doxorubicin in combination with curcumin, anticancer drugs, quinine or siRNA, enable to overcome cancer cell drug resistance [151-154]. Therefore, utilization of several approaches for the enhancement of bioavailability may improve clinical outcomes. Thus, there is a growing research interest in developing more effective and less toxic . A process for preparation of the water soluble nanoformulation is described. Curcumin is characterized with extremely low solubility in water (11ng/ml) and significant presystemic biotransformation, mainly via glucuronide and sulfate conjugation. Few natural products have demonstrated the range of protective and therapeutic promise as have turmeric and . Singh DP, Joshi H, Roopa G (2012) Enhancement of oral bioavailability of Curcumin by solid dispersion technology. Insolubility in water at acidic or neutral pH and its incomplete absorption leads to poor bioavailability. Being multi-functional, curcumin has been proposed in the prevention and treatment of a broad spectrum of diseases. Poor absorption, fast metabolism, and rapid systemic clearance are the most important factors contributing to low curcumin levels in plasma and tissues. However, curcumin has not yet been approved as a therapeutic agent due to its low solubility, bioavailability, and rapid metabolism [72,73]. PLGA Nanoparticles Improve the Oral Bioavailability of Curcumin in Rats: Characterizations and Mechanisms . Through the bypassing of the gut, intravenous curcumin is the only answer that can deliver the full healing, anti-cancer potential of curcumin. For solid dispersion preparation, Kollidon VA . Even . Recent studies in the design and development of oral delivery systems for curcumin to enhance the solubility and oral bioavailability, including liposomes, nanoparticles and polymeric micelles, phospholipid complexes, and microemulsions are summarized. The emergence of nanoscience, which is the creation and utilization of materials and tools on nanometer scale, has exerted a deep influence . Ipar VS, Dsouza A, Devarajan PV. Different phytochemicals including curcumin, berberine . However, the gastrointestinal tract is characterized by specific and efficient physical, chemical, and biological barriers that decrease the bioavailability of medications, including chemotherapeutics. Curcumin is natural occurring, highly lipophilic, main pharmacological active phytochemical compound of turmeric. 2019 Aug;44(4):459-480. doi: 10.1007/s13318-019-00545-z. nanoformulations [30]. Download Download PDF. curcuminoids were exhibited very poor solubility in water and therefore the systemic bioavailability were also very low, which attributed very poor absorption, faster metabolism and systemic elimination after oral administration. Improving the oral bioavailability of curcumin using novel organogel-based nanoemulsions. [] Owing to low water solubility (only 11 ng/mL) [] and poor permeability, CUR belongs to the biopharmaceutics classification system (BCS . Vinod S. Ipar, Anisha Dsouza, Padma V. Devarajan, Enhancing Curcumin Oral Bioavailability Through Nanoformulations, European Journal of Drug Metabolism and Pharmacokinetics, 10.1007/s13318-019-00545-z, (2019). This helps explain the encouraging medicinal and physiologic benefits of curcumin, despite its poor bioavailability and systemic tissue distribution . Different types of the Curcumin-based Nanoformulations[9] 2. Nanosizing these compounds may help to increase their solubility, bioavailability, and promisingly enhance their efficacy. Nanosizing these compounds may help to increase their solubility, bioavailability, and promisingly enhance their efficacy. The maximum oral dose of 8 gm/day of curcumin does not produce any toxic effects [7]. One area of nanomedicine research that could help resolve problems associated with poor adherence, is the use of long-acting preparations for monthly to quarterly dosing [42-47] . PMID: 30771095. Abstract The delivery of drugs through the oral route is regarded as most optimal to achieve desired therapeutic effects and patient compliance. Curcumin's full pharmacological potential is limited owing to its extremely limited water solubility. it is argued that curcumin's health-enhancing benefits may at least be partly derived via its positive gastrointestinal effect. A single oral dose of 5 mg PLGA-curcumin containing 350 μg of curcumin resulted in 3-4 fold higher concentration and prolonged presence of curcumin in the brain than that obtained with 5 mg of . In recent decades, the fields of material science and nanomedicine have generated several delivery platforms . J Agric Food Chem. Jamwal R. Bioavailable curcumin formulations: A review of pharmacokinetic studies in healthy volunteers. Curcumin-self-nanophospholipid dispersions were reported to enhance oral bioavailability of curcumin over conventional formulations in rats . Nanotechnology was used as enhancement of oral bioavailability of drugs and/or solubility and permeability of drug. metabolism, which results in poor bioavailability. It also is effective in managing side effects and improving the quality of life for people with cancer. Oral bioavailability of curcumin was enhanced >12-fold using long-PEGylated SLNs. Unfortunately, it is also characterized by problematic drug delivery and scarce bioavailability, representing the main problem related to the use of this compound. However, it is challenging to study curcumin as it exhibits poor aqueous solubility and low permeability and it is a substrate for P-glycoprotein (P-gp). Then, healthy human volunteers were administered orally 30 mg of THERACURMIN or curcumin powder. • in 64th Indian Pharmaceutical Congress (IPC). The result clearly indicates that the solubility and dissolution of CUR-NS were significantly higher than those of native curcumin [94].Pharmacokinetics and biodistribution results of CUR-NS after intravenous administration in rabbits and mice showed that CUR . Curcumin, an active constituent of turmeric has been associated with various health benefits. Different phytochemicals including curcumin, berberine . Furthermore, free curcumin is unstable; it is susceptible to fragmentation with time, especially in neutral medium. However, its nanoformulations are reported to have greater effects in cancer therapeutics by targeting tumors and reducing the dose required [31]. 16%, through anti-inflammatory and other mechanisms. Ipar, V. S., Dsouza, A., & Devarajan, P. V. (2019). Oral Bioavailability: Issues and Solutions via Nanoformulations Kamla Pathak • Smita Raghuvanshi. Curcumin nanoformulations and their implications in PC. Curcumin is well established as an anti-inflammatory and anti-oxidant. Like EGCG, several possibilities for overcoming drawbacks related to the insufficient absorption of . documented a novel nanosuspension of curcumin (CUR-NS) and studied its bioactivity and pharma-cokinetics. • Good mucus permeability was due to the neutral surface charge of the mixed micelles. It is a natural anti-oxidant and has shown many pharmaceutical activities in the preclinical and clinical studies such as antioxidant, anti-microbial, anti-cancer and anti-alzheimer disease effects. Curcumin (diferuloymethane) is a natural compound, possessing a potent antioxidant activity, and other biologically interesting effects (Perrone et al., 2015), but whose therapeutic use is strongly limited by the very low solubility and oral bioavailability (it belongs to class IV of the Biopharmaceutical Classification System, BCS), along with . The oral route is not and should not be considered a lost cause in this effort. Curcumin-containing nanocarriers increase bioavailability, cell uptake, and curcumin antitumor activity [87, 88]. Curcumin is efficacious against colon cancer, cystic fibrosis, and a variety of other disorders. Curcumin loaded silica-coated flexible This paper envisages discussing the various types of oral liposomes were prepared to enhance the bioavailability of lipid delivery systems available, so that an insight is gained curcumin and it was found that bioavailability is 7.76 fold into all these carriers, and the formulation scientist can make . 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