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Studies on Dissolution Behaviour of Nanoparticulate Curcumin Formulation  [PDF]
R. Ravichandran
Advances in Nanoparticles (ANP) , 2013, DOI: 10.4236/anp.2013.21010
Abstract:

Curcumin is the main biologically active phytochemical compound of turmeric that has been widely used by ancient cultures throughout Asia. However the dissolution rate limited absorption and pre-absorption degradation limits its use as a potential therapeutic. In this study an attempt has been made to overcome the above limitations by curcumin delivery through nanotechnology. Nanocurcumin solid dosage formulations were prepared and studied for its dissolution behaviour. Considerable improvement in the dissolution behavior was observed in the drug nanocrystal-loaded solid dosage forms. This is expected to enhance the bioavailability of poorly soluble medicinal herbs such as turmeric in the body.

Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers  [PDF]
Yogesh B. Pawar,Bhushan Munjal,Saurabh Arora,Manoj Karwa,Gunjan Kohli,Jyoti K. Paliwal,Arvind K. Bansal
Pharmaceutics , 2012, DOI: 10.3390/pharmaceutics4040517
Abstract: Numerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic formulation of CRM (CRM-LF) in human subjects. C max, T max and AUC 0– ¥ were found to be 183.35 ± 37.54 ng/mL, 0.60 ± 0.05 h and 321.12 ± 25.55 ng/mL respectively, at a dose of 750 mg. The plasma profile clearly showed three distinct phases, viz., absorption, distribution and elimination. A close evaluation of the primary pharmacokinetic parameters provided valuable insight into the behavior of the CRM after absorption by CRM-LF. CRM-LF showed a lag time ( T lag) of 0.18 h (around 12 min). Pharmacokinetic modeling revealed that CRM-LF followed a two-compartment model with first order absorption, lag time and first order elimination. A high absorption rate constant ( K 01, 4.51/h) signifies that CRM-LF ensured rapid absorption of the CRM into the central compartment. This was followed by the distribution of CRM from the central to peripheral compartment ( K 12, 2.69/h). The rate of CRM transfer from the peripheral to central compartment ( K 21, 0.15/h) was slow. This encourages higher tissue levels of CRM as compared with plasma levels. The study provides an explanation of the therapeutic efficacy of CRM, despite very low/undetectable levels in the plasma.
Enhanced bioavailability and efficiency of curcumin for the treatment of asthma by its formulation in solid lipid nanoparticles
Wang W, Zhu R, Xie Q, Li A, Xiao Y, Liu H, Cui D, Chen Y, Wang S
International Journal of Nanomedicine , 2012, DOI: http://dx.doi.org/10.2147/IJN.S30428
Abstract: hanced bioavailability and efficiency of curcumin for the treatment of asthma by its formulation in solid lipid nanoparticles Original Research (3128) Total Article Views Authors: Wang W, Zhu R, Xie Q, Li A, Xiao Y, Liu H, Cui D, Chen Y, Wang S Published Date July 2012 Volume 2012:7 Pages 3667 - 3677 DOI: http://dx.doi.org/10.2147/IJN.S30428 Received: 31 January 2012 Accepted: 09 March 2012 Published: 17 July 2012 Wenrui Wang,1,* Rongrong Zhu,1,* Qian Xie,1 Ang Li,1 Yu Xiao,1 Kun Li,1 Hui Liu,2 Daxiang Cui,3 Yihan Chen,1 Shilong Wang1 1East Hospital, School of Life Science and Technology, Tongji University, Shanghai, People’s Republic of China; 2Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, Shanghai, People’s Republic of China; 3National Key Laboratory of Nano/Micro Fabrication Technology, Shanghai Jiao Tong University, Shanghai, People’s Republic of China *These authors contributed equally to this study Abstract: Curcumin has shown considerable pharmacological activity, including anti-inflammatory, but its poor bioavailability and rapid metabolization have limited its application. The purpose of the present study was to formulate curcumin-solid lipid nanoparticles (curcumin-SLNs) to improve its therapeutic efficacy in an ovalbumin (OVA)-induced allergic rat model of asthma. A solvent injection method was used to prepare the curcumin-SLNs. Physiochemical properties of curcumin-SLNs were characterized, and release experiments were performed in vitro. The pharmacokinetics in tissue distribution was studied in mice, and the therapeutic effect of the formulation was evaluated in the model. The prepared formulation showed an average size of 190 nm with a zeta potential value of -20.7 mV and 75% drug entrapment efficiency. X-ray diffraction analysis revealed the amorphous nature of the encapsulated curcumin. The release profile of curcumin-SLNs was an initial burst followed by sustained release. The curcumin concentrations in plasma suspension were significantly higher than those obtained with curcumin alone. Following administration of the curcumin-SLNs, all the tissue concentrations of curcumin increased, especially in lung and liver. In the animal model of asthma, curcumin-SLNs effectively suppressed airway hyperresponsiveness and inflammatory cell infiltration and also significantly inhibited the expression of T-helper-2-type cytokines, such as interleukin-4 and interleukin-13, in bronchoalveolar lavage fluid compared to the asthma group and curcumin-treated group. These observations implied that curcumin-SLNs could be a promising candidate for asthma therapy.
Novel micelle formulation of curcumin for enhancing antitumor activity and inhibiting colorectal cancer stem cells
Wang K, Zhang T, Liu L, Wang XL, Wu P, Chen ZG, Ni C, Zhang JS, Hu FQ, Huang J
International Journal of Nanomedicine , 2012, DOI: http://dx.doi.org/10.2147/IJN.S34702
Abstract: vel micelle formulation of curcumin for enhancing antitumor activity and inhibiting colorectal cancer stem cells Original Research (2629) Total Article Views Authors: Wang K, Zhang T, Liu L, Wang XL, Wu P, Chen ZG, Ni C, Zhang JS, Hu FQ, Huang J Published Date August 2012 Volume 2012:7 Pages 4487 - 4497 DOI: http://dx.doi.org/10.2147/IJN.S34702 Received: 06 June 2012 Accepted: 27 June 2012 Published: 13 August 2012 Ke Wang,1 Tao Zhang,1 Lina Liu,2 Xiaolei Wang,1 Ping Wu,1 Zhigang Chen,1 Chao Ni,1 Junshu Zhang,1 Fuqiang Hu,4 Jian Huang1,3 1Cancer Institute, 2Department of Pharmacy, Second Affiliated Hospital (Binjiang Branch), 3Department of Oncology, Second Affiliated Hospital, Zhejiang University School of Medicine, 4College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China Background and methods: Curcumin has extraordinary anticancer properties but has limited use due to its insolubility in water and instability, which leads to low systemic bioavailability. We have developed a novel nanoparticulate formulation of curcumin encapsulated in stearic acid-g-chitosan oligosaccharide (CSO-SA) polymeric micelles to overcome these hurdles. Results: The synthesized CSO-SA copolymer was able to self-assemble to form nanoscale micelles in aqueous medium. The mean diameter of the curcumin-loaded CSO-SA micelles was 114.7 nm and their mean surface potential was 18.5 mV. Curcumin-loaded CSO-SA micelles showed excellent internalization ability that increased curcumin accumulation in cancer cells. Curcumin-loaded CSO-SA micelles also had potent antiproliferative effects on primary colorectal cancer cells in vitro, resulting in about 6-fold greater inhibition compared with cells treated with a solution containing an equivalent concentration of free curcumin. Intravenous administration of curcumin-loaded CSO-SA micelles marginally suppressed tumor growth but did not increase cytotoxicity to mice, as confirmed by no change in body weight. Most importantly, curcumin-loaded CSO-SA micelles were effective for inhibiting subpopulations of CD44+/CD24+ cells (putative colorectal cancer stem cell markers) both in vitro and in vivo. Conclusion: The present study identifies an effective and safe means of using curcumin-loaded CSO-SA micelles for cancer therapy.
Curcumin: An Anti-Inflammatory Molecule from a Curry Spice on the Path to Cancer Treatment  [PDF]
Purusotam Basnet,Natasa Skalko-Basnet
Molecules , 2011, DOI: 10.3390/molecules16064567
Abstract: Oxidative damage and inflammation have been pointed out in preclinical studies as the root cause of cancer and other chronic diseases such as diabetes, hypertension, Alzheimer’s disease, etc. Epidemiological and clinical studies have suggested that cancer could be prevented or significantly reduced by treatment with anti-oxidant and anti-inflammatory drugs, therefore, curcumin, a principal component of turmeric (a curry spice) showing strong anti-oxidant and anti-inflammatory activities, might be a potential candidate for the prevention and/or treatment of cancer and other chronic diseases. However, curcumin, a highly pleiotropic molecule with an excellent safety profile targeting multiple diseases with strong evidence on the molecular level, could not achieve its optimum therapeutic outcome in past clinical trials, largely due to its low solubility and poor bioavailability. Curcumin can be developed as a therapeutic drug through improvement in formulation properties or delivery systems, enabling its enhanced absorption and cellular uptake. This review mainly focuses on the anti-inflammatory potential of curcumin and recent developments in dosage form and nanoparticulate delivery systems with the possibilities of therapeutic application of curcumin for the prevention and/or treatment of cancer.
Effects of polymer molecular weight on relative oral bioavailability of curcumin
Tsai YM, Chang-Liao WL, Chien CF, Lin LC, Tsai TH
International Journal of Nanomedicine , 2012, DOI: http://dx.doi.org/10.2147/IJN.S32630
Abstract: ts of polymer molecular weight on relative oral bioavailability of curcumin Original Research (3166) Total Article Views Authors: Tsai YM, Chang-Liao WL, Chien CF, Lin LC, Tsai TH Published Date June 2012 Volume 2012:7 Pages 2957 - 2966 DOI: http://dx.doi.org/10.2147/IJN.S32630 Received: 04 April 2012 Accepted: 03 May 2012 Published: 15 June 2012 Yin-Meng Tsai,1 Wan-Ling Chang-Liao,1 Chao-Feng Chien,1 Lie-Chwen Lin,1,2 Tung-Hu Tsai,1,3 1Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, 2National Research Institute of Chinese Medicine, 3Department of Education and Research, Taipei City Hospital, Taipei, Taiwan Background: Polylactic-co-glycolic acid (PLGA) nanoparticles have been used to increase the relative oral bioavailability of hydrophobic compounds and polyphenols in recent years, but the effects of the molecular weight of PLGA on bioavailability are still unknown. This study investigated the influence of polymer molecular weight on the relative oral bioavailability of curcumin, and explored the possible mechanism accounting for the outcome. Methods: Curcumin encapsulated in low (5000–15,000) and high (40,000–75,000) molecular weight PLGA (LMw-NPC and HMw-NPC, respectively) were prepared using an emulsification-solvent evaporation method. Curcumin alone and in the nanoformulations was administered orally to freely mobile rats, and blood samples were collected to evaluate the bioavailability of curcumin, LMw-NPC, and HMw-NPC. An ex vivo experimental gut absorption model was used to investigate the effects of different molecular weights of PLGA formulation on absorption of curcumin. High-performance liquid chromatography with diode array detection was used for quantification of curcumin in biosamples. Results: There were no significant differences in particle properties between LMw-NPC and HMw-NPC, but the relative bioavailability of HMw-NPC was 1.67-fold and 40-fold higher than that of LMw-NPC and conventional curcumin, respectively. In addition, the mean peak concentration (Cmax) of conventional curcumin, LMw-NPC, and HMw-NPC was 0.028, 0.042, and 0.057 μg/mL, respectively. The gut absorption study further revealed that the HMw-PLGA formulation markedly increased the absorption rate of curcumin in the duodenum and resulted in excellent bioavailability compared with conventional curcumin and LMw-NPC. Conclusion: Our findings demonstrate that different molecular weights of PLGA have varying bioavailability, contributing to changes in the absorption rate at the duodenum. The results of this study provide the rationale for design of a nanomedicine delivery system to enhance the bioavailability of water-insoluble pharmaceutical compounds and functional foods.
Gastro-retentive floating beads of curcumin β-cyclodextrin complex to treat stomach tumors  [cached]
Shishu Goindi,Kamalpreet Mann,Nidhi Aggarwal
Alternative Medicine Studies , 2011, DOI: 10.4081/ams.2011.e12
Abstract: The aim of present study was to develop a multi-unit gastro-retentive floating dosage form of curcumin with targeted and sustained release characteristics. Although, protective effect of curcumin against inflammation and cancer is well documented, the clinical potential is underutilized owing to the physicochemical properties of the molecule which lead to poor oral bioavailability. Aqueous solubility of curcumin was enhanced by complex formation with β-cyclodextrin (β-CD). This complex with enhanced solubility profile was further used to prepare multiple unit floating beads. Floating beads of curcumin β-cyclodextrin complex (FBCC) were prepared by dripping a mixture of sodium alginate and hydroxypropyl methylcellulose solution into calcium chloride solution acidified with acetic acid. FBCC were evaluated for percent drug entrapment, diameter, surface topography, buoyancy, in vitro release and pharmacodynamic activity against Benzo(a) pyrene [B(a)P] induced forestomach papillomas in albino female mice (Balb/C strain). The investigation revealed that floating beads possessed optimum formulation characteristics. The drug release from FBCC was fickian and sufficiently sustained for 12 h. Results of antitumor studies against B(a)P induced neoplasia of forestomach suggests that the tumor incidence significantly reduced (50%) using FBCC where as pure curcumin resulted in only 25% reduction. A multi-unit floating dosage form of curcumin β-CD complex possessing sustained release characteristics was developed for targeting gastric tumors. Results of in vitro studies and anti-tumor studies in animals suggest that FBCC can be safely and effectively used to treat neoplasia of stomach. However, these preliminary investigations warrant further pharmacokinetic studies and clinical evaluation in humans
Oral Bioavailability of Simvastatin Novel Formulation in Albino Rats  [PDF]
Singla.N,Gupta.G.D,Kohli.K,Jain
Journal of Pharmaceutical Science and Technology , 2009,
Abstract: The aim of this study was to compare the single dose oral bioavailability of two formulations of Simvastatin in albino rats. Plasma was analyzed for simvastatin using a sensitive, reproducible, accurate and validated LC-MS/MS method. Pharmacokinetic parameters including AUC0-t, AUC0-∞, Cmax, Tmax, and t1/2 were determined from plasma concentration for both formulations. Self-emulsifying Formulation of simvastatin showed a significant improvement in bioavailability (1.5 fold) as compared with the conventional tablets.
A pilot cross-over study to evaluate human oral bioavailability of BCM-95 CG (BiocurcumaxTM), a novel bioenhanced preparation of curcumin  [cached]
Antony B,Merina B,Iyer V,Judy N
Indian Journal of Pharmaceutical Sciences , 2008,
Abstract: Curcumin, the bioactive component of turmeric, Curcuma longa has an exceptionally wide spectrum of activities including antioxidant, anti-inflammatory and anti-cancer properties, and is currently under different phases of clinical trials for various types of soft tissue cancers. However, although in vitro and animal studies have shown anticancer activities of curcumin for virtually all types of human cancers, its poor bioavailability in the human body has severely limited its application to these diseases. Methods to increase its oral bioavailability are a subject of intense current research. Reconstituting curcumin with the non-curcuminoid components of turmeric has been found to increase the bioavailability substantially. In the present clinical study to determine the bioavailability of curcuminoids, a patented formulation, BCM-95 CG was tested on human volunteer group. Normal curcumin was used in the control group. Curcumin content in blood was estimated at periodical intervals. After a washout period of two weeks the control group and drug group were crossed over BCM-95 CG and curcumin, respectively. It was also compared with a combination of curcumin-lecithin-piperine which was earlier shown to provide enhanced bioavailability. The results of the study indicate that the relative bioavailability of BCM-95 CG (Biocurcumax TM ) was about 6.93-fold compared to normal curcumin and about 6.3-fold compared to curcumin-lecithin-piperine formula. BCM-95 CG thus, has potential for widespread application for various chronic diseases.
Scale up, optimization and stability analysis of Curcumin C3 complex-loaded nanoparticles for cancer therapy  [cached]
Ranjan Amalendu P,Mukerjee Anindita,Helson Lawrence,Vishwanatha Jamboor K
Journal of Nanobiotechnology , 2012, DOI: 10.1186/1477-3155-10-38
Abstract: Background Nanoparticle based delivery of anticancer drugs have been widely investigated. However, a very important process for Research & Development in any pharmaceutical industry is scaling nanoparticle formulation techniques so as to produce large batches for preclinical and clinical trials. This process is not only critical but also difficult as it involves various formulation parameters to be modulated all in the same process. Methods In our present study, we formulated curcumin loaded poly (lactic acid-co-glycolic acid) nanoparticles (PLGA-CURC). This improved the bioavailability of curcumin, a potent natural anticancer drug, making it suitable for cancer therapy. Post formulation, we optimized our process by Reponse Surface Methodology (RSM) using Central Composite Design (CCD) and scaled up the formulation process in four stages with final scale-up process yielding 5 g of curcumin loaded nanoparticles within the laboratory setup. The nanoparticles formed after scale-up process were characterized for particle size, drug loading and encapsulation efficiency, surface morphology, in vitro release kinetics and pharmacokinetics. Stability analysis and gamma sterilization were also carried out. Results Results revealed that that process scale-up is being mastered for elaboration to 5 g level. The mean nanoparticle size of the scaled up batch was found to be 158.5 ± 9.8 nm and the drug loading was determined to be 10.32 ± 1.4%. The in vitro release study illustrated a slow sustained release corresponding to 75% drug over a period of 10 days. The pharmacokinetic profile of PLGA-CURC in rats following i.v. administration showed two compartmental model with the area under the curve (AUC0-∞) being 6.139 mg/L h. Gamma sterilization showed no significant change in the particle size or drug loading of the nanoparticles. Stability analysis revealed long term physiochemical stability of the PLGA-CURC formulation. Conclusions A successful effort towards formulating, optimizing and scaling up PLGA-CURC by using Solid-Oil/Water emulsion technique was demonstrated. The process used CCD-RSM for optimization and further scaled up to produce 5 g of PLGA-CURC with almost similar physicochemical characteristics as that of the primary formulated batch.
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