<p>Solutol^®HS15+pluronicF127 and Solutol^®HS15+pluronicL61 mixed micelle systems for oral delivery of genistein</p>

Abstract

Purpose: We aimed to prepare two oral drug delivery systems consisting of polyoxyl 15 hydroxystearate (HS15) with pluronicF127 (F127) and HS15 with pluronicL61 (L61) to overcome the challenges of genistein’s poor oral bioavailability. This provides a good strategy for enhancing the potential value of genistein. Methods: We designed two binary mixed micelle systems employing the organic solvent evaporation method using surfactants (HS15, L61, and F127). Formulations (GEN-F and GEN-L) were characterized by transmission electron microscopy. Drug content analysis, including entrapment efficiency (EE%), drug loading (DL%), and the cumulative amount of genistein released from the micelles, was performed using HPLC. The permeability of optimum formulation was measured in Caco-2 cell monolayers, and the oral bioavailability was evaluated in SD rats. Results: The solutions of GEN-F and GEN-L were observed to be transparent and colorless. GEN-F had a lower EE% of 80.79±0.55% and a DL% of 1.69±0.24% compared to GEN-L, which had an EE% 83.40±1.36% and a DL% 2.26±0.18%. TEM results showed that the morphology of GEN-F and GEN-L was homogeneous and resembled a spherical shape. The dilution and storage conditions had no significant effect on particle size and EE%. Genistein demonstrated a sustained release behavior when encapsulated in micelles. Pharmacokinetics study showed that the relative oral bioavailability of GEN-F and GEN-L increased by 2.23 and 3.46 fold while also enhancing the permeability of genistein across a Caco-2 cell monolayer compared to that of raw genistein. Conclusion: GEN-F and GEN-L as a drug delivery system provide an effective strategy for enhancing and further realizing the potential value of GEN.

Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

“…The EE and DLE of GMs prepared with Soluplus® and vitamin E D-α-tocopheryl PEG 1000 succinate were 97:12 ± 2:11% and 3:87 ± 1:26%, respectively [41]. These results indicate that the method adopted in the present study produces GMs with higher DLE and EE.…”

“…Higher concentrations of Tween 80 produced smaller micelles and higher DLE and EE. GMs were previously synthesized using polyoxyl 15-hydroxystearate combined with Pluronic F127 or Pluronic L61, yielding an EE of 80:79 ± 0:55% and DLE of 1:69 ± 0:24% or an EE of 83:40 ± 1:36% and DLE of 2:26 ± 0:18%, respectively [41].…”

Fluorinated Polymeric Surfactant with a Pluronic-like Structure and Its Application as a Drug Carrier

“…A micelle system conjugated by stearic acid and Pluronic F68 was prepared by Ashok Kumar Jangid to improve the therapeutic efficacy of baicalin . In addition, the challenge of genistein’s poor oral bioavailability was overcome by a mixed micelle system of polyoxyl-15hydroxystearate (HS15) + Pluronic-F127 (F127) designed by Ding’s group . Many reports have shown that approximately 40% or more of active pharmaceutical ingredients are derived from incompletely water-soluble ingredients, which illustrates the significance of developing a novel surfactant to meet the requirements of new drugs.…”