用于口服药物输送的Zwitterionic交联脂酸纳米载体
Hongcen Hou1, Cheng Yang1, Shiyong Zhang1,2
1College of Chemistry, Sichuan University, Chengdu 610064, China. yangchengyc@scu.edu.cn.
Nanoscale
|March 11, 2026
概括
对交联的脂酸纳米粒子 (cLAS) 的Zwitterionic sulfobetaine修饰增强了口服纳米输送. 这改善了跨越生物障碍的药物运输,使生物可用性增加了1.49倍.
科学领域:
- 材料科学 材料科学 材料科学
- 纳米技术纳米技术
- 生物医学工程 生物医学工程
背景情况:
- 交联的脂酸纳米粒子 (cLA) 为口服纳米输送提供了高稳定性.
- 它们强大的负面电荷 (-68 mV) 阻碍了粘液和上皮细胞的相互作用,限制了运输.
- 聚硫化的骨干提供了固有的透障碍能力.
研究的目的:
- 为了提高交叉链接的脂酸纳米颗粒的口服纳米递送效率.
- 为了克服强大的负面电荷所带来的局限性.
- 改善跨界运输和药物的生物可用性.
主要方法:
- 修改cLA纳米颗粒与zwitterionic sulfobetaine,以创建cLAS. 这是一个非常简单的方法.
- 对cLA和cLAS的表面潜力的表征.
- 在使用马林-6作为模型药物的斯普拉格-道利大鼠中进行的药理动力学研究.
主要成果:
- 硫贝修饰降低了纳米粒子表面潜力至-11mV.
- 减少静电排斥促进了与生物障碍物的更好的相互作用.
- 形成了一层水化层,屏蔽与粘膜的相互作用.
- 与cLA相比,cLAS组的库马林-6的相对生物利用率增加了1.49倍.
结论:
- 修改了硫贝的cLAS纳米颗粒显著提高了口服药物递送的效率.
- 修改后的纳米粒子通过减少表面电荷排斥来克服以前的运输限制.
- cLAS为口服纳米输送提供了一个有前途的平台,具有临床转化潜力.
相关概念视频
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
76
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
76
01:23Oral Drug Delivery Systems: Introduction
147
Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.
147
01:11Oral Drug Delivery Systems: Delayed-Release Systems
91
Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...
91
01:24Modified-Release Drug Delivery Systems: Site-Targeted
70
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
70
01:26Oral Drug Delivery Systems: Continuous-Release Systems
130
Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...
130
01:27Bioavailability Enhancement: Drug Permeability Enhancement
288
After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
288