本文選題：納米醫(yī)學　切入點：物理藥劑學　出處：《第二軍醫(yī)大學學報》2017年06期 　論文類型：期刊論文

【摘要】：納米醫(yī)藥在腫瘤治療方面顯示出巨大的潛力,它不僅能克服一些小分子藥物水溶性差、代謝快、靶向性差的缺點,還能包載多種分子進行多模態(tài)診療。盡管優(yōu)點眾多,也有不少新型納米體系被不斷報道,但真正能轉(zhuǎn)化進入臨床應用的很少,納米藥物仍存在著體內(nèi)穩(wěn)定性差、循環(huán)代謝快等問題,從而限制了納米藥物的功效,導致納米醫(yī)藥進入"體外性能優(yōu)異-體內(nèi)表現(xiàn)差"發(fā)展瓶頸期。我們認為,從根本上解決納米醫(yī)藥發(fā)展瓶頸問題依賴于其基本的物理化學特性,也就是納米制劑的物理藥劑學理論方法的研究和創(chuàng)新。因此,本文從腫瘤微環(huán)境特點出發(fā),圍繞臨床應用中的實際問題,結(jié)合大分子弗洛里赫金斯參數(shù)和標度理論等相關理論,以物理化學為手段,建立系列納米醫(yī)藥的物理藥劑學相關原理,并以遞送疏水化療藥物的納米膠束為例,系統(tǒng)地闡述載體組成、自組裝、藥物裝載和釋放以及穩(wěn)定性等相關理化特性與體內(nèi)外性能的相關關系及體內(nèi)相互作用的基本機制。
[Abstract]:Nanopharmaceuticals show great potential in tumor therapy, not only to overcome the shortcomings of some small molecular drugs, such as poor water solubility, fast metabolism, poor targeting, but also to carry a variety of molecules for multimodal diagnosis and treatment. Many new nanosystems have been reported, but few of them can really be transformed into clinical applications. Nanopharmaceuticals still have some problems such as poor internal stability, fast circulation and metabolism, which limits the efficacy of nanopharmaceuticals. As a result, nanopharmaceuticals have entered the bottleneck period of "excellent performance in vitro-poor performance in vivo". We believe that the fundamental solution to the bottleneck problem in the development of nanopharmaceuticals depends on their basic physical and chemical properties. That is, the research and innovation of the physical pharmacology theory of nanopharmaceuticals. Therefore, based on the characteristics of tumor microenvironment and the practical problems in clinical application, this paper combines the related theories such as macromolecular Floriheggins parameter and scaling theory. The physical pharmacological principles of a series of nanopharmaceuticals were established by means of physical chemistry. Taking the nano-micelles delivering hydrophobic chemotherapeutic drugs as an example, the composition and self-assembly of the carriers were systematically described. The relationship between the physical and chemical properties of drug loading, release and stability and the relationship between in vivo and in vitro properties, and the basic mechanism of in vivo interaction.
【作者單位】： 第二軍醫(yī)大學國際合作腫瘤研究所;
【基金】：國家自然科學基金(31470964,81171450)~~
【分類號】：R943
，

本文編號：1592342