Sikander Mehwish, Tulain Ume Ruqia, Malik Nadia Shamshad, Mahmood Arshad, Alqahtani Mohammed S, Erum Alia, Khan Muhammad Tariq
Faculty of Pharmacy, University of Sargodha, Sargodha, Pakistan.
Faculty of Pharmacy, Capital University of Science and Technology, Islamabad, Pakistan.
Nanotechnol Sci Appl. 2025 Feb 27;18:115-137. doi: 10.2147/NSA.S502002. eCollection 2025.
Natural polymers have emerged as versatile and sustainable alternatives to synthetic polymers in pharmaceutical and biomedical applications. This study focuses on the extraction of arabinoxylan (AX) from maize husk and its potential as a promising excipient to enhance the solubility and oral bioavailability of Aripiprazole (APZ), a poorly water-soluble antipsychotic drug, offering a robust strategy for overcoming challenges associated with hydrophobic drugs.
APZ-loaded AX nanoparticles were synthesized using the ionotropic gelation technique. The formulation with the highest encapsulation efficiency designated as FN4 was selected for detailed characterization. Various analytical techniques, including Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD), and Differential Scanning Calorimetry (DSC), were employed to assess the morphological, crystalline, and thermal properties of the nanoparticles. In vitro release studies were conducted on both simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8) to evaluate drug dissolution behaviour. The everted sac method was utilized to assess the permeation and transport of APZ from the AX-based nanoparticles.
The FN4 formulation exhibited an encapsulation efficiency of 88.9% ± 1.77%, with a particle size of 284.4 nm, a polydispersity index (PDI) of 0.346, and a zeta potential of 20.7 mV. SEM analysis revealed a uniform distribution of polyhedral-shaped nanoparticles. XRD and DSC analyses indicated that APZ was in an amorphous state within the nanoparticles. Drug release was more pronounced at pH 6.8, with the AX nanoparticles showing sustained release. The everted sac method demonstrated enhanced permeation of APZ across intestinal membranes, supporting the potential of AX nanoparticles in improving drug absorption.
The AX-based nanoparticle formulation significantly improved the solubility, pH-dependent release profile, and sustained release of APZ, offering a promising strategy to enhance the oral bioavailability of poorly soluble drugs. These findings suggest that AX nanoparticles could serve as an effective delivery system for enhancing the therapeutic potential of hydrophobic drugs like APZ.
在制药和生物医学应用中，天然聚合物已成为合成聚合物的通用且可持续的替代品。本研究聚焦于从玉米皮中提取阿拉伯木聚糖（AX）及其作为一种有前景的辅料来提高阿立哌唑（APZ）溶解度和口服生物利用度的潜力，APZ是一种水溶性差的抗精神病药物，为克服与疏水性药物相关的挑战提供了强有力的策略。
采用离子凝胶法合成负载APZ的AX纳米颗粒。选择包封率最高的制剂（命名为FN4）进行详细表征。采用多种分析技术，包括扫描电子显微镜（SEM）、X射线衍射（XRD）和差示扫描量热法（DSC），来评估纳米颗粒的形态、结晶和热性能。在模拟胃液（pH 1.2）和模拟肠液（pH 6.8）中进行体外释放研究，以评估药物溶解行为。采用外翻肠囊法评估基于AX的纳米颗粒中APZ的渗透和转运。
FN4制剂的包封率为88.9%±1.77%，粒径为284.4 nm，多分散指数（PDI）为0.346，zeta电位为20.7 mV。SEM分析显示多面体形状的纳米颗粒分布均匀。XRD和DSC分析表明，纳米颗粒内的APZ呈无定形状态。在pH 6.8时药物释放更为显著，AX纳米颗粒呈现出缓释特性。外翻肠囊法表明APZ跨肠膜的渗透增强，支持了AX纳米颗粒在改善药物吸收方面的潜力。
基于AX的纳米颗粒制剂显著提高了APZ的溶解度、pH依赖性释放曲线和缓释性能，为提高难溶性药物的口服生物利用度提供了一种有前景的策略。这些发现表明，AX纳米颗粒可作为一种有效的递送系统，以增强像APZ这样的疏水性药物的治疗潜力。
