Mixed Micelle System Produced by Interaction Between Transglycosylated Stevia and an Ionic Surfactant Improves Dissolution Profile of Mefenamic Acid

Fujimori, Miki; Kadota, Kazunori; Tozuka, Yuichi

doi:10.1016/j.xphs.2016.12.024

Cited by 15 publications

(12 citation statements)

References 44 publications

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“…As shown in Figure 1, the dispersed powder of CF-rutin-G in water was in a suspended form. We previously demonstrated that further supplementation (with an additive agent) of the binary system compound-transglycosylated compound solution may be a promising method to significantly enhance dissolution and stabilize the supersaturated state (Fujimori et al, 2017;Kadota et al, 2016b). Nonetheless, these extra additives are not approved in the food industry.…”

Section: Selection Of the Optimal Sucrose Fatty Acid Esters To Developmentioning

confidence: 99%

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Preparation of a Highly Water-dispersible Powder Containing Hydrophobic Polyphenols Derived from Chrysanthemum Flower with Xanthine Oxidase-inhibitory Activity

Kadota

Hashimoto

Yamaguchi

et al. 2018

FSTR

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We aimed to develop a highly water-dispersible dry powder of hydrophobic polyphenols derived from chrysanthemum flower. A dry powder resulting from the mixture of an ethanolic extract of chrysanthemum flower (CF) with transglycosylated rutin (rutin-G) and sucrose fatty acid esters (SEs) was successfully formulated. This powder dispersed easily in water, and the mean particle size in water remained at ~150 nm without apparent changes even after one-week storage. Furthermore, the particle size of the dispersed powder prepared by heat-and-acid treatment shifted below 100 nm after one-week storage. The xanthine oxidase-inhibitory activity of the resulting CF-rutin-G-SEs powder was almost equivalent to that of chrysanthemum flower oil according to in vitro analysis. This technique for preparing a highly water-dispersible dry powder from natural products containing hydrophobic polyphenols should be applicable to the development of functional food products.

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Section: Selection Of the Optimal Sucrose Fatty Acid Esters To Developmentioning

confidence: 99%

“…To implement the practical use of this technology in the food industry, a further reduction in the amount of the excipient is desired. (Fujimori et al, 2017;Kadota et al, 2016aKadota et al, , 2016bUchiyama et al, 2012). Nonetheless, these extra additives were not approved as food additives.…”

Section: Introductionmentioning

confidence: 99%

Preparation of a Highly Water-dispersible Powder Containing Hydrophobic Polyphenols Derived from Chrysanthemum Flower with Xanthine Oxidase-inhibitory Activity

Kadota

Hashimoto

Yamaguchi

et al. 2018

FSTR

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“…41 The comparison indicates a promising enhancement of the solubility in water under the specific conditions of the equilibrium solubility study. Several investigations suggested that in ternary system, the synergistic effect of polymers is a result of both headhead and electrostatic interactions 42 . In addition, the hydrophobic blocks of the copolymer form the core of the micelle that serves as a microenvironment for incorporation and accommodation of the lipophilic molecules.…”

Section: Resultsmentioning

confidence: 99%

Improved Dissolution of Albendazole from High Drug Loaded Ternary Solid Dispersion: Formulation and Characterization

Halder¹,

Azad²,

Iqbal³

et al. 2021

Dhaka Univ. J. Pharm. Sci

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Bioavailability of a poorly water-soluble drug, e.g., widely used anthelmintic drug Albendazole (ABZ), is very low and thus, to obtain an optimized therapeutic efficacy, the aqueous solubility of such drugs needs to be enhanced. The objective of this study was to develop an effective high drug-loaded solid dispersion (SD) of ABZ with two biocompatible drug carriers, namely Soluplus® and Ludiflash® to improve its physicochemical characteristics. Equilibrium solubility study was performed to choose the optimum polymer ratio among the formulations and it showed up to 50-fold enhanced solubility compared to crystalline ABZ in water. X-Ray Powder Diffraction (XRPD) and Differential Scanning Calorimetry (DSC) studies of SD-ABZ showed reduced crystallinity of ABZ in the SD. The polymeric carriers, notably Soluplus®, are thought to play a key role in the reduction of crystallinity and molecular polydispersity of ABZ. The dissolution studies in water showed improved dissolution of SD-ABZ compared to crystalline ABZ, with a quick onset of drug release followed by gradual dissolution. However, due to high drug-loading and retention of crystalline ABZ in the sample, the dissolution behavior was not as expected, and may require further studies to optimize the SD-ABZ formulation. Dhaka Univ. J. Pharm. Sci. 20(2): 149-158, 2021 (December)

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“…The mixed surfactant system made it possible to decrease the amount of Stevia-G needed to enhance the apparent solubility of insoluble drugs compared to using Stevia-G alone. The mixed micellization of Stevia-G and the cationic surfactant lauryl trimethylammonium chloride (LTAC) enhanced the solubility of mefenamic acid in water . Stevia-G has strong interactions with LTAC, and it formed a stable mixed micelle that has a lower cmc compared to that of Stevia-G. Further studies into the mixed micelle properties of Stevia-G with ionic surfactants are required for their use in pharmaceutical applications.…”

Section: Introductionmentioning

confidence: 99%

“…We have reported the mixed micelle system using Stevia-G, transglycosylated stevia derived from Stevia rebaudiana. 14 Stevia-G is recognized as safe by the US Food and Drug Administration and has been shown to have no cytotoxicity to a Caco-2 cell. 15 Interestingly, Stevia-G has a surface-active property and could form micelles in an aqueous medium.…”

Section: ■ Introductionmentioning

confidence: 99%

Investigation of Physiological Properties of Transglycosylated Stevia with Cationic Surfactant and Its Application To Enhance the Solubility of Rebamipide

et al. 2018

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The poor water solubility of rebamipide was enhanced by the mixed micelles of transglycosylated stevia (Stevia-G) and trimethylammonium chloride with varying carbon chain length (C n TAC, n = 14, 16, and 18). Fluorometry, isothermal titration calorimetry (ITC) and dynamic light scattering techniques examined the aggregation properties of Stevia-G and C n TAC. Synergism was found between Stevia-G and C n TAC using the approaches of Clint and Rubingh. The negative interaction parameter (average β m = −4.17, −5.47, and −7.07) and excess free energy (average ΔG° ex = −2.47, −3.06, and −3.88 kJ mol–1) increased with increasing chain length of C n TAC. The negative B 1 values by the Maeda approach suggested that chain–chain interactions contribute to the formation of a mixed micelle. The solubilization of rebamipide in the mixed micelle was evaluated in the term of the molar solubilization ratio (MSR) and partition coefficient (K m). The K m from the Stevia-G/C16TAC system was highest at a low mole fraction of C n TAC (0.2–0.6). In conclusion, the solubilization of rebamipide was more favorable between Stevia-G and C16TAC, although the stability of the mixed micelle was enhanced by an increase in hydrophobicity of the longer chain lengths used in C n TAC.

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Mixed Micelle System Produced by Interaction Between Transglycosylated Stevia and an Ionic Surfactant Improves Dissolution Profile of Mefenamic Acid

Cited by 15 publications

References 44 publications

Preparation of a Highly Water-dispersible Powder Containing Hydrophobic Polyphenols Derived from Chrysanthemum Flower with Xanthine Oxidase-inhibitory Activity

Preparation of a Highly Water-dispersible Powder Containing Hydrophobic Polyphenols Derived from Chrysanthemum Flower with Xanthine Oxidase-inhibitory Activity

Improved Dissolution of Albendazole from High Drug Loaded Ternary Solid Dispersion: Formulation and Characterization

Investigation of Physiological Properties of Transglycosylated Stevia with Cationic Surfactant and Its Application To Enhance the Solubility of Rebamipide

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