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基于二元泊洛尼克的混合胶束系统:改善生物活性成分A增溶效果的有效解决方案。

Binary Pluronics based mixed micellar systems: Effective solution for improved solubilization of Biochanin A.

作者信息

Kaur Jaspreet, Singla Pankaj, Kaur Inderpreet

机构信息

Department of Chemistry, UGC-Center for Advanced Studies, Guru Nanak Dev University, Amritsar 143005, India.

School of Engineering, Merz Court, Claremont Road, Newcastle University, Newcastle UponTyne NE17RU, United Kingdom.

出版信息

Spectrochim Acta A Mol Biomol Spectrosc. 2024 Jan 5;304:123279. doi: 10.1016/j.saa.2023.123279. Epub 2023 Aug 18.

DOI:10.1016/j.saa.2023.123279
PMID:37633096
Abstract

The present work was carried out to appraise the solubilization of Biochanin (BCA), a natural hydrophobic drug in pure Pluronics (P84, P123 and F127) as well as binary mixed micelles (P84-P123 and F127-P123) followed by an interactional study using various state of art techniques. The critical micelle concentration (CMC) of binary mixtures P84-P123 and F127-P123 was found to be significantly lower than pure Pluronics justifying the candidature of mixed micelles (MMs) as a better solubilizer for BCA. UV-visible studies revealed the enhanced solubility of BCA in P84-P123 (1:2) MMs (3.51 ± 0.087 mg/mL) and F127-P123 (1:2) MMs (2.94 ± 0.046 mg/mL) as compared to micelles of pure Pluronics (10% w/v), P84 (2.25 ± 0.039 mg/mL) and F127 (1.12 ± 0.036 mg/mL). Differential pulse voltammetry (DPV) results demonstrated significantly superior binding of BCA with P84-P123 (1:2) MM (K = 2.60 × 10 M) as compared to pure P84 (K = 1.415 × 10 M). Mixed micellization (P84-P123 (1:2)) leads to increase in micellar hydrodynamic diameter (D = 16.09 nm) as compared to pure Pluronic P84 micelles (D = 15.71 nm) which was further amplified (D = 17.69 nm) after BCA loading. Different formulations of pure and MMs were subjected to in vitro drug release and MMs were found to slow down BCA release as compared to pure Pluronics (P84, P123). The results obtained in this study proved that P84-P123 (1:2) MMs are superior and more effective for the solubilization of BCA than pure and other MMs. Thus, the examined MMs hold the potential for advancing the development of solubilization techniques for other hydrophobic drugs with significant pharmacological value.

摘要

开展本研究是为了评估天然疏水性药物大豆苷元(BCA)在纯泊洛沙姆(P84、P123和F127)以及二元混合胶束(P84 - P123和F127 - P123)中的增溶作用,随后使用各种先进技术进行相互作用研究。发现二元混合物P84 - P123和F127 - P123的临界胶束浓度(CMC)显著低于纯泊洛沙姆,这证明混合胶束(MMs)作为BCA的更好增溶剂是合适的。紫外 - 可见光谱研究表明,与纯泊洛沙姆(10% w/v)、P84(2.25±0.039 mg/mL)和F127(1.12±0.036 mg/mL)的胶束相比,BCA在P84 - P123(1:2)MMs(3.51±0.087 mg/mL)和F127 - P123(1:2)MMs(2.94±0.046 mg/mL)中的溶解度有所提高。差分脉冲伏安法(DPV)结果表明,与纯P84(K = 1.415×10 M)相比,BCA与P84 - P123(1:2)MM(K = 2.60×10 M)的结合明显更优。与纯泊洛沙姆P84胶束(D = 15.71 nm)相比,混合胶束化(P84 - P123(1:2))导致胶束流体动力学直径增加(D = 16.09 nm),在负载BCA后进一步增大(D = 17.69 nm)。对纯胶束和MMs的不同制剂进行了体外药物释放研究,发现与纯泊洛沙姆(P84、P123)相比,MMs减缓了BCA的释放。本研究获得的结果证明,P84 - P123(1:2)MMs在增溶BCA方面比纯胶束和其他MMs更优越、更有效。因此,所研究的MMs具有推进其他具有重要药理价值的疏水性药物增溶技术发展的潜力。

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