Enhanced solubility and dissolution of curcumin by a hydrophilic polymer solid dispersion and its insilico molecular modeling studies

Gangurde, Avinash B.; Kundaikar, Harish; Javeer, Sharadchandra Dagadu; Jaiswar, Divakar R.; Degani, Mariam S.; Amin, Purnima D.

doi:10.1016/j.jddst.2015.08.005

Cited by 47 publications

(24 citation statements)

References 24 publications

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“…The latter is a major problem for the industrial use of lutein since most foods are waterbased and also because bioavailability is greatly decreased when pure lutein is orally consumed (Sant'Anna, V., Gurak, Marczak, & Tessaro, 2013;Ye, Lei, Wang, & Zhao, 2017). Solid dispersions have demonstrated the ability to improve the bioavailability and water affinity of food-related bioactive substances such as curcumin and betacarotene (Frizon, Oliveira, Maria, Lina, & Maldonado, 2013;Gangurde et al, 2015;Gul et al, 2015). It has been successfully applied to non-food drugs like felodipine (Karavas, Ktistis, Xenakis, & Georgarakis, 2006), loratadine (Frizon et al, 2013), and carbamazepine (Sethia & Squillante, 2004) demonstrating the versatility of this approach.…”

Section: Introductionmentioning

confidence: 99%

Influence of nanoencapsulated lutein on acetylcholinesterase activity: In vitro determination, kinetic parameters, and in silico docking simulations

et al. 2020

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A B S T R A C TLutein is a bioactive found in dark leafy vegetables that may be used as a nutraceutical agent in foodstuff and an inhibitor of key enzymes of the human body such as those involved in the cholinergic system. However, its high hydrophobicity leads to low bioavailability and must be overcome if lutein is to be added in foods. The objective of this study was to evaluate the influence of nanoencapsulated lutein in the activity of the acetylcholinesterase enzyme. The in vitro study was carried out using water in order to evaluate the impact of encapsulation on the hydrophilicity of lutein. In vitro assays showed that lutein, both free and nanoencapsulated, presented a mixedtype inhibition behavior, and encapsulated lutein was able to inhibit acetylcholinesterase activity even in an aqueous medium. Inhibition was also showed by the in silico docking results which show that lutein interacted with the pocket region of the enzyme. that the damage to the cholinergic system is closely related to brain dysfunctions such as affective disorders, depression, schizophrenia and https://doi.

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Section: Introductionmentioning

confidence: 99%

Influence of nanoencapsulated lutein on acetylcholinesterase activity: In vitro determination, kinetic parameters, and in silico docking simulations

et al. 2020

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“…The supernatant solutions were then passed through whatman filter paper and analyzed by UV spectrophotometry at 419 nm. All solubility measurements were performed in triplicate [25].…”

Section: Saturation Solubilitymentioning

confidence: 99%

Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Deshkar

Satpute

2019

Int J App Pharm

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Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility. Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution. Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets. Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

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“…Despite being noticeable for the physical mixture of PVP and curcumin, these bands could not be visualized in the obtained nanoparticles spectra, as exemplified with the 3510 cm -1 band in Figure 1B4, indicating that curcumin should be located inside the PVP matrix. In fact, this type of attenuation effect is often considered as an evidence of an efficient encapsulation (Gangurde, Kundaikar, Javeer, Jaiswar, Degani, & Amin, 2015;Silva-Buzanello et al, 2016;Yallapu et al, 2010).…”

Section: Characterization Of Solid Dispersion Nanoencapsulated Curcuminmentioning

confidence: 99%

Bioactive evaluation and application of different formulations of the natural colorant curcumin (E100) in a hydrophilic matrix (yogurt)

et al. 2018

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2Curcumin (E100) is a natural colorant that, besides conferring color, has bioactivity, serving as an alternative to some artificial colorants. As a hydrophobic colorant, its modification/compatibilization with the aqueous medium is required to improve stability and enable its application in hydrophilic food matrices. Herein, different formulations of curcumin (curcumin powder: PC, water-dispersible curcumin: DC: and nanoencapsulated curcumin: NC) were evaluated as yogurt colorants. PC showed the strongest bioactivity in all assays (EC50 values: 63±2 to 7.9±0.1 µg.mL -1 ; GI50 values: 48±1 to 17±1 µg.mL -1 and MIC values: 0.0625 to 0.5 mg.mL -1 ), which might indicate that DC and NC reduce the short-term accessibility to curcumin. The tested curcumin formulations produced yogurts with different appearance, specifically associated with their color parameters, besides presenting slight changes in nutritional composition and free sugars and fatty acids profiles. The water compatible formulations (DC and NC) showed advantages over hydrophobic (PC) having a wider industrial utilization.

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Enhanced solubility and dissolution of curcumin by a hydrophilic polymer solid dispersion and its insilico molecular modeling studies

Cited by 47 publications

References 24 publications

Influence of nanoencapsulated lutein on acetylcholinesterase activity: In vitro determination, kinetic parameters, and in silico docking simulations

Influence of nanoencapsulated lutein on acetylcholinesterase activity: In vitro determination, kinetic parameters, and in silico docking simulations

Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Bioactive evaluation and application of different formulations of the natural colorant curcumin (E100) in a hydrophilic matrix (yogurt)

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