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用于关节腔内给药的EtoGel:关节疾病治疗的新挑战。

EtoGel for Intra-Articular Drug Delivery: A New Challenge for Joint Diseases Treatment.

作者信息

Cristiano Maria Chiara, Mancuso Antonia, Giuliano Elena, Cosco Donato, Paolino Donatella, Fresta Massimo

机构信息

Department of Experimental and Clinical Medicine, Campus Universitario-Germaneto, "Magna Græcia" University of Catanzaro, Viale Europa, I-88100 Catanzaro, Italy.

Department of Health Science, Campus Universitario-Germaneto, "Magna Græcia" University of Catanzaro, Viale Europa, I-88100 Catanzaro, Italy.

出版信息

J Funct Biomater. 2021 May 16;12(2):34. doi: 10.3390/jfb12020034.

Abstract

Ethosomes have been proposed as potential intra-articular drug delivery devices, in order to obtain a longer residence time of the delivered drug in the knee joint. To this aim, the conventional composition and preparation method were modified. Ethosomes were prepared by using a low ethanol concentration and carrying out a vesicle extrusion during the preparation. The modified composition did not affect the deformability of ethosomes, a typical feature of this colloidal vesicular topical carrier. The maintenance of sufficient deformability bodes well for an effective ethosome application in the treatment of joint pathologies because they should be able to go beyond the pores of the dense collagen II network. The investigated ethosomes were inserted in a three-dimensional network of thermo-sensitive poloxamer gel (EtoGel) to improve the residence time in the joint. Rheological experiments evidenced that EtoGel could allow an easy intra-articular injection at room temperature and hence transform itself in gel form at body temperature into the joint. Furthermore, EtoGel seemed to be able to support the knee joint during walking and running. In vitro studies demonstrated that the amount of used ethanol did not affect the viability of human chondrocytes and nanocarriers were also able to suitably interact with cells.

摘要

有人提出将乙醇脂质体作为潜在的关节内给药装置,以便使所递送的药物在膝关节中具有更长的停留时间。为此,对传统的组成和制备方法进行了改进。乙醇脂质体是通过使用低乙醇浓度并在制备过程中进行囊泡挤压来制备的。改进后的组成并未影响乙醇脂质体的可变形性,这是这种胶体囊泡局部载体的一个典型特征。保持足够的可变形性对于乙醇脂质体在关节疾病治疗中的有效应用是个好兆头,因为它们应该能够穿过致密的II型胶原网络的孔隙。将所研究的乙醇脂质体插入热敏泊洛沙姆凝胶(EtoGel)的三维网络中,以延长其在关节中的停留时间。流变学实验证明,EtoGel在室温下可轻松进行关节内注射,并因此在体温下在关节内转变为凝胶形式。此外,EtoGel似乎能够在行走和跑步过程中支撑膝关节。体外研究表明,所用乙醇的量不会影响人软骨细胞的活力,并且纳米载体也能够与细胞进行适当的相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/391d/8162362/57d497b2ccb4/jfb-12-00034-g001.jpg

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