Emerging role of nanocarriers to increase the solubility and bioavailability of curcumin

Mohanty, Chandana; Das, Manasi; Sahoo, Sanjeeb K.

doi:10.1517/17425247.2012.724676

Cited by 155 publications

(92 citation statements)

References 121 publications

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“…7,8 We hypothesized that encapsulating CUR with poly-(lactic-co-glycolic acid) (PLGA)-based nanoparticles would enhance the bioavailability of CUR administered orally because of PLGA's ability to disperse in water, pass through the gut, bypass first-pass metabolism, and endure the harsh external conditions of the gastrointestinal tract (chemical and enzymatic degradation). 4,[9][10][11][12][13] Our hypothesis is supported by previous studies that reported that encapsulated CUR with PLGA-based nanoparticles administrated orally to rats increased CUR levels in the plasma. [14][15][16][17][18] However, to the best of our knowledge, there are no data about CURG, despite the fact that it is the main metabolite of CUR found in the plasma.…”

supporting

confidence: 86%

“…[4][5][6] CUR's low bioavailability in vivo was confirmed by our previous work in which CUR absorbed through the intestinal cells of rats was predominantly conjugated as curcumin glucuronide (CURG) and low levels of unmetabolized CUR were found in the blood. 7,8 We hypothesized that encapsulating CUR with poly-(lactic-co-glycolic acid) (PLGA)-based nanoparticles would enhance the bioavailability of CUR administered orally because of PLGA's ability to disperse in water, pass through the gut, bypass first-pass metabolism, and endure the harsh external conditions of the gastrointestinal tract (chemical and enzymatic degradation).…”

mentioning

confidence: 62%

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Metabolic fate of poly-(lactic-co-glycolic acid)-based curcumin nanoparticles following oral administration

Harigae¹,

Nakagawa²,

Miyazawa³

et al. 2016

IJN

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Purpose Curcumin (CUR), the main polyphenol in turmeric, is poorly absorbed and rapidly metabolized following oral administration, which severely curtails its bioavailability. Poly-(lactic-co-glycolic acid)-based CUR nanoparticles (CUR-NP) have recently been suggested to improve CUR bioavailability, but this has not been fully verified. Specifically, no data are available about curcumin glucuronide (CURG), the major metabolite of CUR found in the plasma following oral administration of CUR-NP. Herein, we investigated the absorption and metabolism of CUR-NP and evaluated whether CUR-NP improves CUR bioavailability. Methods Following oral administration of CUR-NP in rats, we analyzed the plasma and organ distribution of CUR and its metabolites using high-performance liquid chromatography-tandem mass spectrometry. To elucidate the mechanism of increased intestinal absorption of CUR-NP, we prepared mixed micelles comprised of phosphatidylcholine and bile salts and examined the micellar solubility of CUR-NP. Additionally, we investigated the cellular incorporation of the resultant micelles into differentiated Caco-2 human intestinal cells. Results Following in vivo administration of CUR-NP, CUR was effectively absorbed and present mainly as CURG in the plasma which contained significant amounts of the metabolite compared with other organs. Thus, CUR-NP increased intestinal absorption of CUR rather than decreasing metabolic degradation and conversion to other metabolites. In vitro, CUR encapsulated in CUR-NP was solubilized in mixed micelles; however, whether the micelles contained CUR or CUR-NP had little influence on cellular uptake efficiency. Therefore, we suggest that the high solubilization capacity of CUR-NP in mixed micelles, rather than cellular uptake efficiency, explains the high intestinal absorption of CUR-NP in vivo. Conclusion These findings provide a better understanding of the bioavailability of CUR and CUR-NP following oral administration. To improve the bioavailability of CUR, future studies should focus on enhancing the resistance to metabolic degradation and conversion of CUR to other metabolites, which may lead to novel discoveries regarding food function and disease prevention.

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supporting

confidence: 86%

mentioning

confidence: 62%

Metabolic fate of poly-(lactic-co-glycolic acid)-based curcumin nanoparticles following oral administration

Harigae¹,

Nakagawa²,

Miyazawa³

et al. 2016

IJN

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“…It has been mainly reported for its anticancer properties and found to be beneficial as antibacterial, antifungal, antiamoebic, antioxidant, antidiabetic, anti-HIV and in neuro-generative and respiratory diseases [2][3][4][5][6][7][8][9]. Despite having an array of medicinal properties, there are certain challenges with its physicochemical properties such as low aqueous solubility (3.12 g/L, 25°C), degradation at intestinal pH, fast hepatic metabolism and elimination, which reduces its bioavailability [10][11][12].…”

Section: Introductionmentioning

confidence: 99%

“…Conjugation of bioavailability enhancers such as piperine, Bio-curcumin-95 (BCM-95) has been used as alternative strategies to enhance its bioavailability [16][17][18][19]. In the past decade, nanotechnology has emerged as a unique approach that has found enormous applications in delivering lipophilic drugs with better bioavailability [10,20]. In this approach, submicron particles are formed which get stabilized by use of steric and electrostatic stabilizers [21].…”

Section: Introductionmentioning

confidence: 99%

“…There have seen many reports which support spray drying technique due to its various advantages that are hard to be achieved by other techniques [26]. Spray drying process directly atomizes the drug in a hot gas current to obtain powder [10,20]. The spherical particles obtained have better flow property than conventional methods used for drying [27].…”

Section: Introductionmentioning

confidence: 99%

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Formulation of Curcumin Nanosuspension Using Box-Behnken Design and Study of Impact of Drying Techniques on Its Powder Characteristics

Kaur

Bawa

Rajesh

et al. 2017

Asian J Pharm Clin Res

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Objective: The objective of this study was to formulate curcumin nanosuspension (NS) using Box-Behnken design (BBD) and solvent-antisolvent technique to overcome the challenges related to its poor dissolution rate.Methods: Sodium lauryl sulfate (SLS) and poly vinyl pyrrolidone K-60 (PVPK-60) have been used as a surfactant and polymer, respectively, to stabilize the NS. Ethanol was used as solvent to dissolve curcumin and water was used as antisolvent. The study revealed that SLS to curcumin ratio, PVPK-60 to curcumin ratio, solvent to antisolvent ratio and speed of mixing were the critical parameters that affected particle size and zeta potential of the formulation. Hence, based on Box-BBD, 25 formulations were prepared by varying these critical parameters. The optimized batch of CRM NS was further solidified using spray drying as well as rotary evaporation techniques to have a better insight for selection of solidification process in terms of retention of particle size, charge, flow, dissolution, and stability.Results: About 39.47 folds decrease in particle size of raw CRM was observed after conversion into NS. Further, about 53.57 and 45.45 folds decrease in particle size was observed after spray drying and rotary evaporation. Both the dried nanoparticles have shown comparatively higher solubility, powder flow, and dissolution rate as that of raw CRM. Powder X-ray diffraction study revealed the formation of amorphous nanoparticles. Accelerated stability study revealed that nanoparticles dried by spray drying were able to retain the properties such as particle size, flow, and dissolution rate as compared to rotary evaporated powders. Conclusion:It can be concluded that spray drying technique could offer many advantages while loading CRM nanoparticles into tablets for their oral administration.

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Phytopharmaceuticals for Treating Sexually Transmitted Diseases

Ugoeze¹

2022

Herbal Drugs for the Management of Infectious Diseases

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Emerging role of nanocarriers to increase the solubility and bioavailability of curcumin

Cited by 155 publications

References 121 publications

Metabolic fate of poly-(lactic-co-glycolic acid)-based curcumin nanoparticles following oral administration

Metabolic fate of poly-(lactic-co-glycolic acid)-based curcumin nanoparticles following oral administration

Formulation of Curcumin Nanosuspension Using Box-Behnken Design and Study of Impact of Drying Techniques on Its Powder Characteristics

Phytopharmaceuticals for Treating Sexually Transmitted Diseases

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