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Pluronic F127/Pluronic P123/vitamin E TPGS mixed micelles for oral delivery of mangiferin and quercetin: Mixture-design optimization, micellization, and solubilization behavior
Journal of Molecular Liquids ( IF 5.3 ) Pub Date : 2018-10-28 , DOI: 10.1016/j.molliq.2018.10.089
Santi Thanitwatthanasak , Leonard M.C. Sagis , Pakamon Chitprasert

Mixed micelles (MMs) of Pluronic F127 (F127), Pluronic P123 (P123), and Vitamin E TPGS (TPGS) copolymers were prepared by the thin-film sonication method to encapsulate two phenolics with different polarities: magniferin (MGF) and quercetin (QCT). Mixture design was applied for the multi-response optimization of formulations of MGF-loaded MMs (MGF-MMs) and QCT-loaded MMs (QCT-MMs) with high encapsulation efficiency (EE) and drug loading (DL), but low critical micelle concentration (CMC). The optimal mass fractions of F127/P123/TPGS were 0.120/0.328/0.552 for MFG-MMs and 0.131/0.869/0.000 for QCT-MMs, providing EE (>95% (w/w)) and DL (>4.5% (w/w)) higher than those obtained by their individual copolymer components. The CMCs of MFG/QCT-MMs, detected by dynamic light scattering (DLS), were 0.009 ± 0.001 and 0.011 ± 0.001% (w/v), respectively, slightly lower than those obtained by profile analysis tensiometry (PAT). The results revealed that the PAT-CMC represented complete MM formation, while the DLS-CMC detected mono-molecular micelles. The MGF/QCT-MMs showed spherical morphology with diameters of 14.26 ± 0.52 and 21.50 ± 0.37 nm, and their zeta-potentials were −2.89 ± 1.70 and −3.22 ± 1.92 mV, respectively. Nuclear overhauser effect spectroscopy showed that MGF located in both hydrophilic and hydrophobic parts of MMs by orienting its xanthone backbone towards the core, but its glucoside close to the corona. QCT was preferentially located in the PPO core. Both MGF/QCT-MMs had excellent dissolution ability and sustained release in the simulated gastrointestinal environment. This study demonstrated that mixture design was successfully applied for multi-response optimization MM formulations of MGF and QCT, and the developed MMs had potential application as nanoparticle-based drug delivery systems.



中文翻译:

用于口服芒果苷和槲皮素的Pluronic F127 / Pluronic P123 /维生素E TPGS混合胶束:混合物设计优化,胶束化和增溶行为

通过薄膜超声处理方法制备了Pluronic F127(F127),Pluronic P123(P123)和维生素E TPGS(TPGS)共聚物的混合胶束(MMs),以包封两种极性不同的酚类化合物:氧化镁(MGF)和槲皮素( QCT)。混合物设计用于多反应优化载有MGF的MM(MGF-MM)和QCT的MM(QCT-MM)的配方,具有高封装效率(EE)和载药量(DL),但临界胶束低浓度(CMC)。对于MFG-MM,F127 / P123 / TPGS的最佳质量分数为0.120 / 0.328 / 0.552,对于QCT-MM,F127 / P123 / TPGS的最佳质量分数为0.131 / 0.869 / 0.000,可提供EE(> 95%(w / w))和DL(> 4.5%( w / w))高于其各自的共聚物组分所获得的那些。通过动态光散射(DLS)检测到的MFG / QCT-MMs的CMC分别为0.009±0.001和0.011±0.001%(w / v),略低于通过轮廓分析张力测定法(PAT)获得的结果。结果表明,PAT-CMC代表完整的MM形成,而DLS-CMC检测到单分子胶束。MGF / QCT-MMs呈球形,直径为14.26±0.52和21.50±0.37 nm,它们的Zeta电位分别为-2.89±1.70和-3.22±1.92 mV。核过载效应谱表明,MGF通过将其x吨酮主链朝向核心定向而定位在MM的亲水和疏水部分中,而其糖苷则靠近日冕。QCT优先位于PPO核心。两种MGF / QCT-MM在模拟胃肠道环境中均具有出色的溶解能力和持续释放。

更新日期:2018-10-28
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