Nano micelle mediated In-Vitro release kinetics of two Biopharmaceutical Classification System (BCS) class II drugs with varying hydrophobicity

IF 2.3 4区 化学 Q3 CHEMISTRY, PHYSICAL
Neelam Mishra-Kadam, Ashwini M. Savle, Mihar S. Shaikh, Kinjal D. Solanki, Ankit B. Shah, Nilesh S. Pandya, Yogesh K. Kadam
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Abstract

This study investigates the in-vitro release kinetics of two BCS Class-II hydrophobic drugs, Irbesartan (IRB) and Lamotrigine (LAM), from nano micellar systems composed of Pluronic® (P84, F108) and Tetronic® (T1307) copolymers. Prior to release studies, drug solubilization efficiency and micelle size were evaluated using UV–Visible spectroscopy and Dynamic Light Scattering, both in the presence and absence of NaCl. Among the tested formulations, Pluronic® P84 demonstrated superior solubilization for both drugs, enhancing IRB and LAM solubility by ~ 3.6/2.3 times compared to F108 and ~ 1.6/1.9 times compared to T1307 in 1 M NaCl. Additionally, P84 formed smaller (~ 15 to 16.5 nm), more stable micelles, indicating its potential for effective drug delivery. Drug release profiles were assessed over 24 h and fitted to various kinetic models-zero-order, first-order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas-to elucidate the dominant release mechanisms. For IRB, release from aqueous and 1% P84 micellar systems followed the Hixson-Crowell model (99.8% and 96.7%), indicating surface area-dependent dissolution. Formulations with 1% P84 + 1 M NaCl (87.8%) and 1% T1307 (90.1%) adhered to the Higuchi model, suggesting diffusion-controlled release. The Korsmeyer-Peppas model best described IRB release from 1% T1307 + 1 M NaCl (82.0%), indicating combined diffusion and erosion mechanisms. In contrast, LAM release from all systems followed the Korsmeyer-Peppas model, reflecting a consistent anomalous transport behaviour. Overall, these results demonstrate the significant influence of micellar composition and ionic conditions on solubilization and drug release, providing guidance for the rational design of micellar drug delivery systems.

Graphical Abstract

纳米胶束介导两种不同疏水性生物制药分类系统(BCS)ⅱ类药物的体外释放动力学
本研究研究了由Pluronic®(P84, F108)和Tetronic®(T1307)共聚物组成的纳米胶束体系中两种BCS ii类疏水药物Irbesartan (IRB)和Lamotrigine (LAM)的体外释放动力学。在释放研究之前,在存在和不存在NaCl的情况下,使用紫外可见光谱和动态光散射来评估药物的增溶效率和胶束大小。在测试的配方中,Pluronic®P84对这两种药物都有较好的增溶性,在1 M NaCl中,IRB和LAM的溶解度比F108提高了~ 3.6/2.3倍,比T1307提高了~ 1.6/1.9倍。此外,P84形成了更小(~ 15 ~ 16.5 nm)、更稳定的胶束,表明其具有有效药物递送的潜力。在24 h内评估药物释放谱,并拟合各种动力学模型(零级、一级、Higuchi、Hixson-Crowell和korsmeyer - peppas),以阐明主要释放机制。对于IRB,水溶液和1% P84胶束体系的释放符合Hixson-Crowell模型(99.8%和96.7%),表明溶解依赖于表面积。1% P84 + 1 M NaCl(87.8%)和1% T1307(90.1%)的配方符合Higuchi模型,呈扩散控制释放。Korsmeyer-Peppas模型最好地描述了1% T1307 + 1m NaCl(82.0%)中IRB的释放,表明了扩散和侵蚀的联合机制。相反,所有系统的LAM释放都遵循Korsmeyer-Peppas模式,反映了一致的异常输运行为。综上所述,这些结果表明胶束组成和离子条件对药物的增溶和释放有显著影响,为胶束给药系统的合理设计提供了指导。图形抽象
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来源期刊
Colloid and Polymer Science
Colloid and Polymer Science 化学-高分子科学
CiteScore
4.60
自引率
4.20%
发文量
111
审稿时长
2.2 months
期刊介绍: Colloid and Polymer Science - a leading international journal of longstanding tradition - is devoted to colloid and polymer science and its interdisciplinary interactions. As such, it responds to a demand which has lost none of its actuality as revealed in the trends of contemporary materials science.
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