The in vitro stability and in vivo pharmacokinetics of curcumin prepared as an aqueous nanoparticulate formulation

Mohanty, Chandana; Sahoo, Sanjeeb K.

doi:10.1016/j.biomaterials.2010.04.062

Cited by 449 publications

(333 citation statements)

References 47 publications

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“…Therefore, particularly innovative nanoformulations have been developed to overcome these problems. Interestingly, it has been reported that encapsulation of curcumin in the form of curcuminoid mixture in micelles or nanoparticles retards the degradation of curcumin (18)(19)(20)(21)(22)(23). In this present study, we focused on the curcuminoid mixture because the anticancer and antiinflammatory activities of this mixture were stronger than that of pure curcumin alone and because the curcuminoid mixture has been used in most clinical trials (5,24).…”

Section: Introductionmentioning

confidence: 92%

A Kinetic Degradation Study of Curcumin in Its Free Form and Loaded in Polymeric Micelles

Naksuriya

Steenbergen

Toraño

et al. 2016

AAPS J

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Abstract. Curcumin, a phenolic compound, possesses many pharmacological activities and is under clinical evaluation to treat different diseases. However, conflicting data about its stability have been reported. In this study, the kinetic degradation of curcumin from a natural curcuminoid mixture under various conditions (pH, temperature, and dielectric constant of the medium) was investigated. Moreover, the degradation of pure curcumin at some selected conditions was also determined. To fully solubilize curcumin and to prevent precipitation of curcumin that occurs when low concentrations of co-solvent are present, a 50:50 (v/v) aqueous buffer/methanol mixture was used as standard medium to study its degradation kinetics. The results showed that degradation of curcumin both as pure compound and present in the curcuminoid mixture followed first order kinetic reaction. It was further shown that an increasing pH, temperature, and dielectric constant of the medium resulted in an increase in the degradation rate. Curcumin showed rapid degradation due to autoxidation in aqueous buffer pH=8.0 with a rate constant of 280×10 -3 h -1, corresponding with a half-life (t 1/2 ) of 2.5 h. Dioxygenated bicyclopentadione was identified as the final degradation product. Importantly, curcumin loaded as curcuminoid mixture in ω-methoxy poly (ethylene glycol)-b-(N-(2-benzoyloxypropyl) methacrylamide) (mPEG-HPMA-Bz) polymeric micelles and in Triton X-100 micelles was about 300-500 times more stable than in aqueous buffer. Therefore, loading of curcumin into polymeric micelles is a promising approach to stabilize this compound and develop formulations suitable for further pharmaceutical and clinical studies.

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Section: Introductionmentioning

confidence: 92%

A Kinetic Degradation Study of Curcumin in Its Free Form and Loaded in Polymeric Micelles

Naksuriya

Steenbergen

Toraño

et al. 2016

AAPS J

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“…Cancer is the most dreaded disease and it involves abnormal cell growth with capability to spread to other parts of the body (Mohanty and Sahu 2010). Chemotherapy, surgery and radiotherapy strategies are being used for the treatment of cancers in current times but these measures of treatment are not effective against advanced stages of cancers (Feng and Chien 2003).…”

Section: Introductionmentioning

confidence: 99%

Flavonoids from Heliotropium subulatum exudate and their evaluation for antioxidant, antineoplastic and cytotoxic activities II

2016

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The flavonoids are the largest group of phenolic compounds isolated from a wide range of higher plants. These compounds work as antimicrobials, anti-insect agents and protect plants from other types of biotic and abiotic stresses. Various researchers have suggested that flavonoids possessed antioxidant, antineoplastic and cytotoxic activities. The main objective of this study was to test dichloromethane fraction of resinous exudate of Heliotropium subulatum for their antioxidant, antineoplastic and cytotoxic activities, as well as to search new antioxidant and antineoplastic agents for pharmaceutical formulations. Five flavonoids were isolated from resinous exudate of this plant species and screened for their in vitro and in vivo antioxidant models (DPPH radical scavenging, reducing power, superoxide anion scavenging, metal chelating scavenging systems, catalase and lipid peroxidation), antineoplastic (Sarcoma 180), and cytotoxic (Chinese hamster V79 cells) activities. Tricetin demonstrated maximum antioxidant activity against both in vitro and in vivo experimental systems while galangin exhibited maximum inhibition (78.35%) at a dose of 10 lg/kg/day against Sarcoma 180. Similarly, it was found that galangin also showed highest activity (21.1 ± 0.15%) at a concentration of 70 lg/ml to Chinese hamster V79 cells. The observed results suggest that tricetin has a potential to scavenge free radicals in both in vitro and in vivo models while the galangin could be considered as antitumor and cytotoxic agent.

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“…[52][53][54] These strategies include implantable curcumin carrier, 55 curcumin microparticles 56 and nanoparticles. 57 Pharmacokinetic studies reported that curcumin nano-formulation displayed a larger area under curve (AUC)-time curve as compared with free curcumin. [57][58][59] For example, encapsulation of curcumin by poly(lactic-co-glycolide) (PLGA) nanoparticles provided a significant higher maximal concentration (1000-fold increase) as compared with free curcumin following 60 min of i.v.…”

Section: Pathological Bone Environmentmentioning

confidence: 99%

“…administration in mice. 57 Curcumin nano-formulation has been explored especially for cancer therapy. [60][61][62] In this attempt, modulation of key properties of nanoparticles such as their size, surface charge and chemistry has been reported to favor their accumulation into the tumor tissue and optimize biological interactions with tumor cells.…”

Section: Pathological Bone Environmentmentioning

confidence: 99%

Therapeutic actions of curcumin in bone disorders

2016

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Curcumin is the active component of turmeric extract derived from the Curcuma longa plant. In the last decade, curcumin has raised a considerable interest in medicine owing to its negligible toxicity and multiple therapeutic actions including anti-cancer, anti-inflammatory and anti-microbial activities. Among the various molecular targets of curcumin, some are involved in bone remodeling, which strongly suggests that curcumin can affect the skeletal system. The review sheds light on the current and potential applications of curcumin to treat bone disorders characterized by an excessive resorption activity. Within the scope of this review, the novel formulations of curcumin to overcome its physico-chemical and pharmacokinetic constraints are also discussed.

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The in vitro stability and in vivo pharmacokinetics of curcumin prepared as an aqueous nanoparticulate formulation

Cited by 449 publications

References 47 publications

A Kinetic Degradation Study of Curcumin in Its Free Form and Loaded in Polymeric Micelles

A Kinetic Degradation Study of Curcumin in Its Free Form and Loaded in Polymeric Micelles

Flavonoids from Heliotropium subulatum exudate and their evaluation for antioxidant, antineoplastic and cytotoxic activities II

Therapeutic actions of curcumin in bone disorders

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