Unraveling the Impact of Stabilizers on Nanocrystal Preparation and Oral Absorption: A Case Study of Poorly Soluble Andrographolide

IF 9.6 1区材料科学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Nano Letters Pub Date : 2024-12-23 DOI:10.1021/acs.nanolett.4c05230

Bingwen Ding, Zhenting Zheng, Jianjia Su, Jieying Zhou, Shihao Xu, Wei Luo, Houlin Su, Ying Li, Wei Xiong

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引用次数: 0

Abstract

Drug nanocrystal engineering is an attractive pharmaceutical approach to enhancing the oral bioavailability of poorly soluble drugs. The mechanism of drug nanocrystal stabilization, however, is unclear. Here we developed andrographolide nanocrystals (AG-NCs) with various nonionic surfactants (Pluronic-F127, TPGS, or Brij-S20). We detected AG micelles (AG-MCs) at an andrographolide to nonionic surfactant ratio of 10:10 (w/w) and poor AG-NC size stability. We thus quantified the unbound Pluronic-F127 in AG-NCs and found that the proposed instantaneous binding rate sharply declined with increasing Pluronic-F127 input. We determined that the saturation dose of TPGS on AG-NCs was approximately 10:10 (w/w) and recommend it as a key criterion for nanocrystal formulation. Although AG-NCs exhibited a marginally faster dissolution rate, they possessed better mucus-penetrating and transmembrane transport capacities and significantly enhanced oral absorption compared to AG-MCs. These findings give insights into the impact of a stabilizer during the preparation process and the oral absorption of drug nanocrystals.

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来源期刊

Nano Letters 工程技术-材料科学：综合

CiteScore

16.80

自引率

2.80%

发文量

1182

审稿时长

1.4 months

期刊介绍： Nano Letters serves as a dynamic platform for promptly disseminating original results in fundamental, applied, and emerging research across all facets of nanoscience and nanotechnology. A pivotal criterion for inclusion within Nano Letters is the convergence of at least two different areas or disciplines, ensuring a rich interdisciplinary scope. The journal is dedicated to fostering exploration in diverse areas, including: - Experimental and theoretical findings on physical, chemical, and biological phenomena at the nanoscale - Synthesis, characterization, and processing of organic, inorganic, polymer, and hybrid nanomaterials through physical, chemical, and biological methodologies - Modeling and simulation of synthetic, assembly, and interaction processes - Realization of integrated nanostructures and nano-engineered devices exhibiting advanced performance - Applications of nanoscale materials in living and environmental systems Nano Letters is committed to advancing and showcasing groundbreaking research that intersects various domains, fostering innovation and collaboration in the ever-evolving field of nanoscience and nanotechnology.