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磁性羧甲基化β-环糊精作为金刚烷胺递送的pH敏感载体系统的设计、表征及评价:一种靶向药物递送的新方法

Design, characterization, and evaluation of magnetic carboxymethylated β-cyclodextrin as a pH-sensitive carrier system for amantadine delivery: a novel approach for targeted drug delivery.

作者信息

Hadadian Mehrdad, Allahyari Reza, Mahdavi Behnam, Rezaei-Seresht Esmail

机构信息

Department of Chemistry, Faculty of Science, Hakim Sabzevari University Sabzevar Iran

出版信息

RSC Adv. 2025 Jan 3;15(1):446-459. doi: 10.1039/d4ra06269h. eCollection 2025 Jan 2.

Abstract

In this study, a magnetic carboxymethylated β-cyclodextrin (Mag/CM-β-CD) was developed as a carrier system to assess its capability on drug delivery application by forming an inclusion complex with amantadine (Amn) as a drug model. The synthesized inclusion complex (Mag/CM-β-CD/Amn) was analyzed using various techniques, including FT-IR, XRD, BET, TGA, TEM, VSM, and DLS. The encapsulation efficiency and drug release study of Mag/CM-β-CD/Amn were adopted using the spectroscopic method. Furthermore, the kinetics of drug release by different mathematical models was studied. The cytotoxicity evaluation of Mag/CM-β-CD and Mag/CM-β-CD/Amn was studied using MTT assay against the HUVEC cell line. The TEM imaging showed a spherical morphology and average size of less than 25 nm for the drug complex. Mag/CM-β-CD showed high EE% by absorbing 81.51% of amantadine. Mag/CM-β-CD/Amn showed a pH-sensitive manner with a higher release rate at acidic pH. In addition, a kinetic study reveals that the release process followed the Fickian mechanism and was governed by diffusion. The MTT assay demonstrated low toxicity for the Mag/CM-β-CD/Amn complex in HUVEC cells, showing a cell viability of 57.13% at a concentration of 1000 μg mL. The results indicate that the developed system is an effective vehicle for transporting drugs in targeted drug delivery applications.

摘要

在本研究中,开发了一种磁性羧甲基化β-环糊精(Mag/CM-β-CD)作为载体系统,通过与作为药物模型的金刚烷(Amn)形成包合物来评估其在药物递送应用中的能力。使用包括傅里叶变换红外光谱(FT-IR)、X射线衍射(XRD)、比表面积分析(BET)、热重分析(TGA)、透射电子显微镜(TEM)、振动样品磁强计(VSM)和动态光散射(DLS)等各种技术对合成的包合物(Mag/CM-β-CD/Amn)进行了分析。采用光谱法对Mag/CM-β-CD/Amn进行包封率和药物释放研究。此外,还研究了不同数学模型下药物释放的动力学。使用MTT法针对人脐静脉内皮细胞(HUVEC)细胞系研究了Mag/CM-β-CD和Mag/CM-β-CD/Amn的细胞毒性评估。TEM成像显示药物复合物呈球形形态,平均尺寸小于25 nm。Mag/CM-β-CD通过吸收81.51%的金刚烷显示出高包封率。Mag/CM-β-CD/Amn在酸性pH下表现出pH敏感性,释放速率更高。此外,动力学研究表明,释放过程遵循菲克扩散机制,受扩散控制。MTT分析表明,Mag/CM-β-CD/Amn复合物在HUVEC细胞中具有低毒性,在浓度为1000 μg/mL时细胞活力为57.13%。结果表明,所开发的系统是靶向药物递送应用中运输药物的有效载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38ce/11698272/69231d9550f9/d4ra06269h-s1.jpg

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