Preparation, characterization, pharmacokinetics, and tissue distribution of curcumin nanosuspension with TPGS as stabilizer

Gao, Yan; Li, Zhonggang; Sun, Min; Li, Houli; Guo, Chenyu; Cui, Jing; Li, Aiguo; Cao, Fuyang; Xi, Yang; Lou, Hongxiang; Zhai, Guangxi

doi:10.3109/03639041003695139

Cited by 102 publications

(56 citation statements)

References 47 publications

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“…[42][43][44][45] With the encapsulation of MPEG-PLA micelles, Cur was more easily taken up by glioma cells and reached a higher concentration in C6 and U251 cell lines compared with free Cur, which was demonstrated in Figures 5 and 6. In this study, since the results of MTT assay showed that the cell viability of C6 and U251 cell lines in the Cur/MPEG-PLA micelle group decreased more significantly, we speculate that the high drug uptake of Cur/MPEG-PLA micelles in glioma cells may contribute much to the enhanced antiglioma activity in vitro.…”

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confidence: 85%

Biodegradable micelles enhance the antiglioma activity of curcumin in vitro and in vivo

Zheng

Gao

Liu

et al. 2016

IJN

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Curcumin (Cur), a natural polyphenol of Curcuma longa , has been recently reported to possess antitumor activities. However, due to its poor aqueous solubility and low biological availability, the clinical application of Cur is quite limited. The encapsulation of hydrophobic drugs into nanoparticles is an effective way to improve their pharmaceutical activities. In this research, nanomicelles loaded with Cur were formulated by a self-assembly method with biodegradable monomethoxy poly(ethylene glycol)-poly(lactide) copolymers (MPEG-PLAs). After encapsulation, the cellular uptake was increased and Cur could be released from MPEG-PLA micelles in a sustained manner. The Cur-loaded MPEG-PLA micelles (Cur/MPEG-PLA micelles) exhibited an enhanced toxicity on C6 and U251 glioma cells and induced more apoptosis on C6 glioma cells compared with free Cur. Moreover, the therapy efficiency of Cur/MPEG-PLA micelles was evaluated at length on a nude mouse model bearing glioma. The Cur/MPEG-PLA micelles were more effective on suppressing tumor growth compared with free Cur, which indicated that Cur/MPEG-PLA micelles improved the antiglioma activity of Cur in vivo. The results of immunohistochemical and immunofluorescent analysis indicated that the induction of apoptosis, antiangiogenesis, and inhibition of cell proliferation may contribute to the improvement in antiglioma effects. Our data suggested that Cur/MPEG-PLA may have potential clinic applications in glioma therapy.

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confidence: 85%

Biodegradable micelles enhance the antiglioma activity of curcumin in vitro and in vivo

Zheng

Gao

Liu

et al. 2016

IJN

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“…[19][20][21] Gao et al showed that the area under curve (AUC) of the plasma concentration curve in the formation of curcumin nanosuspension was 3.8-fold greater than that of native curcumin in rabbits. 22) In the present study, we generated a highly absorptive curcumin dispersed with colloidal nanoparticles which is dissolved in gum ghatti solution.…”

Section: Discussionmentioning

confidence: 99%

A Novel Drug Delivery System of Oral Curcumin Markedly Improves Efficacy of Treatment for Heart Failure after Myocardial Infarction in Rats

Sunagawa

Wada

Suzuki

et al. 2012

Biological & Pharmaceutical Bulletin

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Curcumin is an inhibitor of p300 histone acetyltransferase activity, which is associated with the deterioration of heart failure. We reported that native curcumin, at a dosage of 50 mg/kg, prevented deterioration of the systolic function in rat models of heart failure. To achieve more efficient oral pharmacological therapy against heart failure by curcumin, we have developed a novel drug delivery system (DDS) which markedly increases plasma curcumin levels. At the dosage of 0.5 mg/kg, DDS curcumin but not native curcumin restored left ventricular fractional shortening in post-myocardial infarction rats. Thus, our DDS strategy will be applicable to the clinical setting in humans.Key words curcumin; drug delivery system; heart failure Signals through hemodynamic overload finally reach the nuclei of cardiac myocytes and activate hypertrophy-responsive transcriptional factors such as GATA-binding protein 4, myocyte enhancer factor 2 and serum response factor. 1,2) Activities of these factors are regulated by histone deacetylases and an intrinsic histone acetyltransferase (HAT), p300.3-5) Curcumin is an inhibitor of p300 HAT activity and widely employed as a healthy food diet. Recently, we have reported that native curcumin, at the dosage of 50 mg/kg, prevents the deterioration of systolic function in rat models of hypertension-or myocardial infarction (MI)-induced heart failure.6,7) However, native curcumin powder is insoluble in water, and the absorption of orally administered curcumin is limited. While curcumin, at 50 mg/kg/d, may be safe in humans, 8) the intestinal absorption efficiency at this dosage is inadequate in this form. Since the amount of daily water intake is limited in patients with congestive heart failure, a large volume of water to take medicine is a burden for these patients. Therefore, a more efficient system for heart failure therapy will be desirable in actual clinical practice. We have developed a curcumin drug delivery system (DDS), by which the absorption efficiency is much more favorable than that of native curcumin powder.9)The present study examined a hypothesis that this system is useful for heart failure therapy in post-MI rats. MATERIALS AND METHODS Preparation of DDS CurcuminCurcumin powder was extracted from Indian turmeric by using alcohol. DDS of curcumin preparation was previously described. 9) Shortly, gum ghatti, mainly consists of polysaccharides, obtained from the exudation of ghatti trees, was dissolved in water to make gum ghatti solution. Curcumin powder was mixed into this solution, and water and glycerin were added to adjust the weight. This mixture was ground by a wet grinding mill (DYNO-MILL ® KDL, Willy A Bachofen AG, Switzerland), and then, dispersed by a high-pressure homogenizer (Homogenizer 15MR-8TA, APV Gaulin). DDS curcumin consisted of 10 w/w% curcumin, 2% other curcuminoids such as demethoxycurcumin and isdemethoxycurcumin, 46% glycerin, 4% gum ghatti, and 38% water.Chemicals Curcumin powder, mepronil, β-glucuronidase (from Helix pomatia), distilled water (H 2...

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“…Curcumin nanosuspension (CUR-NS) was stabilized by d--tocopheryl polyethylene glycol 1000 succinate (TPGS), which has been examined for its pharmacokinetics after intravenous administration to rabbits and mice [27]. It was interesting to observe that these formulations increased the plasma concentration of curcumin by 3.8 times, thus increasing its bioavailability.…”

Section: Novel Drug Delivery Systemsmentioning

confidence: 99%

Perspectives on New Synthetic Curcumin Analogs and their Potential Anticancer Properties

Vyas¹,

Dandawate²,

Padhyé³

et al. 2013

Current Pharmaceutical Design

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Curcumin is the active component of dried rhizome of Curcuma longa, a perennial herb belonging to ginger family, cultivated extensively in south and southeastern tropical Asia. It is widely consumed in the Indian subcontinent, south Asia and Japan in traditional food recipes. Extensive research over last few decades has shown that curcumin is a potent anti-inflammatory agent with powerful therapeutic potential against a variety of cancers. It suppresses proliferation and metastasis of human tumors through regulation of various transcription factors, growth factors, inflammatory cytokines, protein kinases and other enzymes. It induces apoptotic cell death and also inhibits proliferation of cancer cells by cell cycle arrest. Pharmacokinetic data has shown that curcumin undergoes rapid metabolism leading to glucuronidation and sulfation in the liver and excretion in the feces, which accounts for its poor systemic bioavailability. The compound has, therefore, been formulated and administered using different drug delivery systems such as liposomes, micelles, polysaccharides, phospholipid complexes and nanoparticles that can overcome the limitation of bioavailability to some extent. Attempts to avoid rapid metabolism of curcumin until now have been met with limited success. This has prompted researchers to look for new synthetic curcumin analogs in order to overcome the drawbacks of limited bioavailability and rapid metabolism, and gain efficacy with reduced toxicity. In this review we provide a summarized account of novel synthetic curcumin formulations and analogs, and the recent progress in the field of cancer prevention and treatment.

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Preparation, characterization, pharmacokinetics, and tissue distribution of curcumin nanosuspension with TPGS as stabilizer

Abstract: Nanosuspension could serve as a promising intravenous drug-delivery system for curcumin.

Cited by 102 publications

References 47 publications

Biodegradable micelles enhance the antiglioma activity of curcumin in vitro and in vivo

Biodegradable micelles enhance the antiglioma activity of curcumin in vitro and in vivo

A Novel Drug Delivery System of Oral Curcumin Markedly Improves Efficacy of Treatment for Heart Failure after Myocardial Infarction in Rats

Perspectives on New Synthetic Curcumin Analogs and their Potential Anticancer Properties

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