Curcumin Enhances Oral Bioavailability and Anti-Tumor Therapeutic Efficacy of Paclitaxel upon Administration in Nanoemulsion Formulation

Ganta, Srinivas; Devalapally, Harikrishna; Amiji, Mansoor M.

doi:10.1002/jps.22157

Cited by 112 publications

(65 citation statements)

References 39 publications

(57 reference statements)

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“…Over the last decade, nanoemulsion-based delivery systems have been gained interest in the pharmaceuticals [1][2][3][4] , food and beverage [5][6][7][8] , cosmetics [9][10][11] , agrochemicals [12][13][14] and other 15 industries. The main purposes are to encapsulate, protect, and deliver lipophilic components such as drugs, vitamins, food supplements, antioxidants, antimicrobials, pesticides.…”

Section: Introductionmentioning

confidence: 99%

Preparation of nanoemulsions by phase inversion temperature (PIT)

Jintapattanakit¹

2018

Pharm Sci Asia

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Section: Introductionmentioning

confidence: 99%

Preparation of nanoemulsions by phase inversion temperature (PIT)

Jintapattanakit¹

2018

Pharm Sci Asia

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“…11,12 In the present study, pharmacokinetics profile of paclitaxel was explored specially emphasizing in the pre-treatment with curcumin which causes inhibition of CYP3A4 and P-gp activities. 3 On the other hand, systemic elimination of paclitaxel occurs by hepatic metabolism involving CYP3A4. 13 Paclitaxel is also a substrate for P-gp, encoded by the ABCB1 (mdr-1) gene, that functions as a transporter and is believed to be an important factor in the resistance to absorption and biliary elimination of many drugs, including paclitaxel.…”

Section: Resultsmentioning

confidence: 99%

“…1,2 It has a significant clinical application for which it is in the World Health Organization's List of Essential Medicines but oral bioavailability of this drug is disgustingly limited by poor water solubility, P-gp efflux and CYP3A metabolism. [3][4][5] Currently, it is administered through intravenous route that is also related to some clinical compromises due to the side effect of used formulation excipients. Several research activities are going on to counteract these situations through different formulation approaches.…”

Section: Introductionmentioning

confidence: 99%

“…6 Curcumin, a diarylheptanoid from Curcuma longa (turmeric) is one of the most extensively investigated and well-defined phytochemical having chemo preventive properties. 3 Curcumin suppresses drug metabolizing enzymes like CYP3A4 in liver and is also capable of inducing change in drug transporter for P-gp and thus increased the bioavailability of certain drugs like sulfasalazine and midazolam. It also modifies the physiological activity in the gastrointestinal tract leading to better absorption of drugs.…”

Section: Introductionmentioning

confidence: 99%

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Enhancement of Paclitaxel Oral Bioavailability in Swiss Mice by Four Consecutive Days of Pre-Treatment with Curcumin

Sharma¹,

Magotra²,

Nandi³

et al. 2017

IJPER

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Objective: Poor water solubility, P-glycoprotein (P-gp) efflux property and substrate of CYP3A lead to low oral bioavailability that limit the oral use of paclitaxel, a key anticancer drug. Though several formulation approaches were tried to combat this low absorption profile but effect of pre-treatment with curcumin, a naturally occurring CYP3A and P-gp inhibitor on augmentation of paclitaxel plasma level is not reported till now. Therefore, the objective of the present study is to asses any change in oral pharmacokinetics of paclitaxel. Materials and Methods: curcumin was administered orally to the Swiss mice at a dose of 100 mg/kg for four days and on the fifth day, pharmacokinetics of paclitaxel was carried out at dose of 35 mg/kg orally alone and curcumin pre-treated animals. Results: There is enhancement of Cmax and AUC by 1.4 to 1.5 fold when compared with oral paclitaxel alone treatment that leads to improve in oral bioavailability of paclitaxel. Conclusion: Curcumin can be an ideal candidate for regular use to improve the bioavailability of paclitaxel followed by decrease in dose related side effects. Furthermore, anticancer effect of Curcumin itself as well as with paclitaxel could clinically manage cancer promisingly.

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“…Another strategy of increasing bioavailability was to prepare micro-emulsions of curcumin which are isotropic nanostructures and stable solutions comprising of surfactant, oil and water. In another study, Ganta and co-workers [30] have reported that curcumin nanoemulsion increases the bioavailability of paclitaxel up to 5.2-fold, and there was a 3.2-fold increase in its accumulation at the tumor site in an oral administration to SKOV-3 tumor-bearing xenografts mice models. This was possible due to down-regulation of intestinal cytochrome P450 3A2 (CYP3A2) protein levels.…”

Section: Novel Drug Delivery Systemsmentioning

confidence: 94%

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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Curcumin Enhances Oral Bioavailability and Anti-Tumor Therapeutic Efficacy of Paclitaxel upon Administration in Nanoemulsion Formulation

Cited by 112 publications

References 39 publications

Preparation of nanoemulsions by phase inversion temperature (PIT)

Preparation of nanoemulsions by phase inversion temperature (PIT)

Enhancement of Paclitaxel Oral Bioavailability in Swiss Mice by Four Consecutive Days of Pre-Treatment with Curcumin

Perspectives on New Synthetic Curcumin Analogs and their Potential Anticancer Properties

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