Drug distribution in nanostructured lipid particles
Drug distribution in nanostructured lipid particles
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纳米结构脂质颗粒中的药物分布
DOI：
10.1016/j.ejpb.2016.10.008
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发表时间：
2017
影响因子：
4.9
通讯作者：
C. Teutloff
中科院分区：
文献类型：
--
作者：
Siavash Saeidpour;S. B. Lohan;A. Solik;Victoria Paul;R. Bodmeier;Gaith Zoubari;M. Unbehauen;R. Haag;R. Bittl;M. Meinke;C. Teutloff
即使在对脂基纳米粒进行了25年的研究后，仍然没有常规的程序，但针对有效的药物装载和定义的释放曲线的纳米粒的靶向设计仍然是如此。它需要关于药物与脂类化合物的相互作用以及它在纳米颗粒中的定位和分布的详细知识。本文介绍了一种用于局部治疗炎症性皮肤疾病的糖皮质激素--地塞米松的纳米级脂质微粒(NLP)的研究，该微粒由格列菲尔和维特索尔组成固体脂质，卡普利诺为液体脂质。用94 GHz的EPR光谱监测了3-(Carboxy)-2，2，5，5-tetramethyl-1-pyrrolidinyloxy(DxPCA)自旋标记的地塞米松与其微环境的相互作用。在室温下，用X-波段EPR研究了自旋标记药物的迁移率。为了将从EPR得到的磁参数和动力学参数与NLP中自旋探针的局部环境联系起来，对单个脂类化合物中的DxPCA进行了研究。反映DxPCA环境极性的磁性参数以及描述药物流动性的参数表明，在脂类胶体分散的情况下，NLP DxPCA附着在纳米颗粒的表面。虽然亲脂性药物几乎只与水溶液中的NLP有关，但稀释实验表明，它可以很容易地从纳米颗粒中释放出来。
The targeted design of nanoparticles for efficient drug loading and defined release profiles is even after 25 years of research on lipid-based nanoparticles still no routine procedure. It requires detailed knowledge about the interaction of the drug with the lipid compounds and about its localisation and distribution in the nanoparticle. We present here an investigation on nano-sized lipid particles (NLP) composed of Gelucire and Witepsol as solid lipids, and Capryol as liquid lipid, loaded with Dexamethasone, a glucocorticoid used in topical treatment of inflammatory dermal diseases. The interactions of Dexamethasone, which was spin-labelled by 3-(Carboxy)-2,2,5,5-tetramethyl-1-pyrrolidinyloxy (DxPCA), with its microenvironment are monitored by EPR spectroscopy at 94 GHz at low temperatures. The mobility of the spin-labelled drug was probed by X-band EPR at room temperature. In order to relate the magnetic and dynamic parameters deduced from EPR to the local environment of the spin probe in the NLP, investigations of DxPCA in the individual lipid compounds were carried out. The magnetic parameters reflecting the polarity of DxPCA’s environment as well as the parameters describing the mobility of the drug reveal that in the case of colloidal dispersions of the lipids and also the NLP DxPCA is attached to the surface of the nanoparticles. Although the lipophilic drug is almost exclusively associated with the NLP in aqueous solution, dilution experiments show, that it can be easily released from the nanoparticle.
体内 EPR 将封装在多层脂质体中的亲水物质局部递送至无毛小鼠和正常小鼠的皮肤。
DOI：
10.1016/s0168-3659(99)00272-2
发表时间：
2000
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Honzak,L;Sentjurc,M;Swartz,HM
通讯作者：
Swartz,HM