相关实验视频

Updated: Jun 28, 2025

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

基于协同效应的多功能奇托桑聚合微粒用于改善口服帕克利塔塞尔的生物可用性

Wei Zhang^1,2,3, Qian Zhang^3,4, Yuhan Yang^3,5

¹Guangxi Institute of Botany, Chinese Academy of Sciences, No. 85 Yanshan Town, Yanshan District, Guilin, 541006, People's Republic of China.

Drug delivery and translational research

|April 20, 2024

概括

这项研究开发了一种新的小系统,以改善口服帕克利塔塞尔 (PTX) 的吸收. 增强的输送系统显著增加了生物可用性和细胞吸收,提供了一个有前途的口服药物输送解决方案.

科学领域:

生物材料科学生物材料科学
药物输送系统药物输送系统
纳米技术纳米技术

背景情况:

帕克利塔塞尔 (PTX) 的口服受限于其生物可用性较差.
基托-胆固醇酸 (CS-SA) 菌根为药物输送提供了潜力.
增强细胞的功能对于改善口服吸收至关重要.

研究的目的:

开发一种多功能细胞系统,以增强口服帕克利塔塞尔 (PTX) 的吸收.
研究L-carnitine (LC) 修饰和Quercetin (Que) 联合封装对小胞表现的协同效应.
为了评估口服生物可用性和PTX载菌体的细胞吸收.

主要方法:

用薄膜-超音波分散技术制备用LC修饰的CS-SA小粒,并与Que一起加载.
微粒性质的表征,包括颗粒大小,药物负载和微粒临界度 (CMC).
实验室持续释放研究,Caco-2细胞吸收测定和CYP3A4酶抑制试验.

主要成果:

准备好的小粒呈现出均的球形 (148.3 nm),高药物负载 (7.05%),低CMC (16.89 μg/ml).
与传统配方相比,带有PTX的菌体表现出持续释放的特性和168.08%的口服相对生物可用性.
LC修饰和Que共载显著促进了细胞吸收,Que抑制了CYP3A4代谢酶活性.

结论:

开发的多功能酸盐聚合基显示出作为PTX有效的口服输送系统的潜力.
LC和Que的协同作用有助于增强药物吸收和降低新陈代谢.
这种新型的菌根系统为改善吸收不良药物的口服生物可用性提供了一个有希望的策略.

关键词:

基托桑米塞尔 (Chitosan micelles) 是一种植物.对于L-卡尼丁来说,它是一种口服生物可用性口服生物可用性帕克利塔克塞尔 (Paclitaxel) 是一种药物.奎尔丁 (Quercetin) 是一种青素.

更多相关视频

A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

Published on: December 23, 2016

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

相关概念视频

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...

Drugs that Stabilize Microtubules

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...