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Development of High-Drug-Loading Nanoparticles.
ChemPlusChem ( IF 3.0 ) Pub Date : 2020-08-10 , DOI: 10.1002/cplu.202000496
Yun Liu 1 , Guangze Yang 1 , Song Jin 1 , Letao Xu 1 , Chun-Xia Zhao 1
Affiliation  

Formulating drugs into nanoparticles offers many attractive advantages over free drugs including improved bioavailability, minimized toxic side effects, enhanced drug delivery, feasibility of incorporating other functions such as controlled release, imaging agents for imaging, targeting delivery, and loading more than one drug for combination therapies. One of the key parameters is drug loading, which is defined as the mass ratio of drug to drug‐loaded nanoparticles. Currently, most nanoparticle systems have relatively low drug loading (<10 wt%), and developing methods to increase drug loading remains a challenge. This Minireview presents an overview of recent research on developing nanoparticles with high drug loading (>10 wt%) from the perspective of synthesis strategies, including post‐loading, co‐loading, and pre‐loading. Based on these three different strategies, various nanoparticle systems with different materials and drugs are summarized and discussed in terms of their synthesis methods, drug loadings, encapsulation efficiencies, release profiles, stabilities, and their applications in drug delivery. The advantages and disadvantages of these strategies are presented with an objective of providing useful design rules for future development of high‐drug‐loading nanoparticles.

中文翻译:

高载药纳米颗粒的开发。

与游离药物相比,将药物配制成纳米颗粒具有许多诱人的优势,包括改善的生物利用度,最小的毒副作用,增强的药物递送,并入其他功能(如控释,成像剂,成像,靶向递送以及装载多种药物以进行组合)的可行性。疗法。关键参数之一是载药量,载药量定义为载药与载药纳米颗粒的质量比。当前,大多数纳米颗粒系统具有相对较低的药物载量(<10wt%),并且增加药物载量的开发方法仍然是挑战。这份Minireview概述了从合成策略(包括后加载,共同加载和预加载)的角度研究开发具有高药物负载(> 10 wt%)的纳米颗粒的最新研究。基于这三种不同的策略,就具有不同材料和药物的各种纳米颗粒系统进行了总结和讨论,涉及其合成方法,载药量,包封效率,释放曲线,稳定性及其在药物递送中的应用。提出了这些策略的优缺点,目的是为高载药纳米颗粒的未来开发提供有用的设计规则。
更新日期:2020-09-21
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