4.5 Article

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

Journal

JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 106, Issue 4, Pages 1117-1123

Publisher

WILEY
DOI: 10.1016/j.xphs.2016.12.024

Keywords

mixed micelles; transglycosylated stevia; Rubingh model; ionic surfactants; mefenamic acid

Funding

  1. Hosokawa Powder Technology Foundation

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Transglycosylated stevia (stevia-G) can effectively improve the dissolution and bioavailability of poorly water-soluble drugs. Furthermore, addition of an ionic surfactant to stevia-G solution has been shown to enhance the dissolution effect of stevia-G on flurbiprofen. Herein, 4 surfactants, namely sodium dodecyl sulfate, sodiumN-dodecanoylsarcosinate, sodiummonododecyl phosphate, and lauryltrimethylammonium chloride (LTAC) were screened to investigate their synergistic effect with stevia-G in enhancing the solubility of mefenamic acid (MFA). The ternary formulation containing LTAC produced the highest increase in solubility, whereas the binary MFA/LTAC formulation did not increase the solubility of MFA. Surface tensionwas evaluated to analyze the interaction between stevia-G and each ionic surfactant, wherein the Rubingh model was applied to predict mixed micelle formation between stevia-G and LTAC. Interaction parameters calculated by theRubinghmodel reflected mixed micelleformationbetween stevia-G andLTAC relative tothe self-interactions of the 2 individual surfactants. All interactionparameters in this system showed negative values, indicating a favorable interaction (e.g., hydrogen bond or electrostatic and dipole) between binary components in the mixed micelles. Spray-dried particles of ternary formulations (MFA/stevia-G/LTAC) were prepared to evaluate the dissolution profile and physicochemical properties. Dissolution profiling showed that the concentration of MFA released from spray-dried particles was significantly higher than untreated MFA. (C) 2017 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.

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