α-Glucosyl hesperidin induced an improvement in the bioavailability of pranlukast hemihydrate using high-pressure homogenization

Uchiyama, Hiromasa; Tozuka, Yuichi; Asamoto, Fusatoshi; Takeuchi, Hirofumi

doi:10.1016/j.ijpharm.2011.03.017

Cited by 20 publications

(7 citation statements)

References 16 publications

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“…According to the biopharmaceutical classification system (BCS) [19,20], PRS was classified as a low solubility/low permeability drug (BCS class IV). There were several formulation studies to improve the dissolution profile of PRS HH by applying formulation technologies [21][22][23]. However, it has been challenging to increase the bioavailability of PRS.…”

Section: Dissolution Testsmentioning

confidence: 99%

Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs II: Solvate and cocrystal

Furuta

Mori

Yoshihashi

et al. 2015

Journal of Pharmaceutical and Biomedical Analysis

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Section: Dissolution Testsmentioning

confidence: 99%

Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs II: Solvate and cocrystal

Furuta

Mori

Yoshihashi

et al. 2015

Journal of Pharmaceutical and Biomedical Analysis

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“…Furthermore, nanocomposite formation with these functional food additives using a wet milling process can create nanoparticles from poorly soluble compounds as effectively as high-pressure homogenization. 50 Therefore, Rutin-G may help to create highly dispersed FA nanoparticles <100 nm, thus forming nanocomposites with FA. Nanoparticles usually exhibit strong aggregation due to their high surface energy and a large specific surface area, resulting in low solubility and absorption.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

Inhibition of Photodegradation of Highly Dispersed Folic Acid Nanoparticles by the Antioxidant Effect of Transglycosylated Rutin

Kadota

Semba

Shakudo

et al. 2016

J. Agric. Food Chem.

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We developed highly dispersible and photostable nanoparticles of vitamin, folic acid (FA). FA was wet bead milled with milling and dispersing adjuvants and transglycosylated compounds such as α-glucosyl hesperidin (Hesperidin-G) and rutin (Rutin-G), which solubilized FA. The milled slurries of FA particles with transglycosylated compounds consisted of nanosized particles with a median diameter of <100 nm. The lyophilized formulations of these slurries retained their nanometer size after resuspension in water with no aggregation. The apparent solubility of FA in these formulations was 100-fold higher than that of untreated FA. The solubilizing effect of Rutin-G may affect the particle size reduction and dispersibility of FA. The photostability results showed that the strong antioxidant activity of Rutin-G substantially increased the photostability of FA solution. On the basis of these results, bead milling of FA with Rutin-G is a promising technique for developing highly dispersible, photostable nanoparticle FA formulations.

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“…noted that hesperidin inhibits fructose's absorption for Caco-2 cells [55]. Regarding to nanotechnology applied to cancer treatment, some studies have demonstrated the higher permeability of hesperidin nanoparticles to Caco-2 cells [10,53].…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

“…Thus, the improvement of the physicochemical properties of hesperidin through the design of innovative drug delivery carriers to overcome such limitations appears as an important tool. Along these lines, since hesperidin have demonstrated cytotoxicity activity both in vitro and in vivo methodologies [6][7][8][9][10][11][12], nanoencapsulation emerge as a tool for the secure, sustained, and efficient release of hesperidin as cancer treatment via oral administration. Nanoparticles have been successfully used to improve the oral bioavailability of natural compounds [13].…”

Section: Introductionmentioning

confidence: 99%

Optimized Chitosan-Coated Gliadin Nanoparticles Improved the Hesperidin Cytotoxicity over Tumor Cells

Filho

Machado

Diedrich

et al. 2021

Braz. arch. biol. technol.

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Hesperidin is a natural compound which is found in citric fruits and presents antitumor and antimicrobial activities. However, the in vivo efficacy of Hesperidin is reduced due to its low oral bioavailability. Protein-based nanoparticles have been applied to improve biological parameters of drugs and natural compounds. Gliadin is a monomeric protein present in wheat. In this study, gliadin-based nanoparticles containing hesperidin were obtained by desolvation technique and a Taguchi orthogonal array design was employed to optimize the formulation. The independent variables were set as concentration of CaCl2 (0.5; 1 or 2%) and stabilizing agent (Pluronic F68, Tween 80 or sodium caseinate). The dependent variables consisted of mean diameter, polydispersity index, zeta potential, and encapsulation efficiency. The results showed significant effects on the dependent variables when 1% CaCl2 and Pluronic F68 were used. The optimized formulation was coated with chitosan to increase the physical stability of the nanoparticles. The final nanoparticles presented a mean diameter of 321 nm and polydispersity index of 0.217, and spherical shape. After coating, the Zeta potential was +21 mV, and the encapsulation efficiency was 73 %. The in vitro release assay showed that about 98% of the drug was released from the nanoparticles after 48 h. Moreover, HIGHLIGHTS A Taguchi design optimized the development of hesperidin-loaded gliadin nanoparticles. A chitosan-coating was added to improve the physical stability of nanoparticles. Nanoparticles reduced the hesperidin cytotoxicity over healthy Vero cells. Nanoparticles improved the hesperidin cytotoxicity over tumor cells.

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α-Glucosyl hesperidin induced an improvement in the bioavailability of pranlukast hemihydrate using high-pressure homogenization

Cited by 20 publications

References 16 publications

Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs II: Solvate and cocrystal

Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs II: Solvate and cocrystal

Inhibition of Photodegradation of Highly Dispersed Folic Acid Nanoparticles by the Antioxidant Effect of Transglycosylated Rutin

Optimized Chitosan-Coated Gliadin Nanoparticles Improved the Hesperidin Cytotoxicity over Tumor Cells

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