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用于改善药物递送的载喹硫平微针透皮贴剂的研发与表征

Development and characterization of quetiapine-loaded microneedles-based transdermal patches for improved drug delivery.

作者信息

Itbar Maryam, Imran Khan Muhammad, Akhtar Muhammad Furqan, Ahmad Zulcaif, Farhan Sohail Muhammad, Madni Asadullah, Erum Alia, Khan Aslam, Ali Ahsan, Naeem Qaisar Muhammad

机构信息

Riphah Institute of Pharmaceutical Sciences, Riphah International University, 54000, Lahore, Pakistan.

Department of Chemistry, Lahore University of Management Sciences (LUMS), Lahore, Pakistan.

出版信息

J Pharm Pharmacol. 2025 Aug 4;77(8):1042-1058. doi: 10.1093/jpp/rgaf013.

Abstract

OBJECTIVES

This study was executed to prepare and characterize quetiapine (antipsychotic drug)-loaded microneedles-based transdermal patch for improved drug delivery.

METHODS

This study was executed to develop microneedles-based transdermal patches (MNS) for quetiapine delivery. Eight MNS patches loaded with quetiapine (MNS1-MNS8) were fabricated using varying concentrations of sodium alginate and carboxymethyl cellulose. First four MNS patches (MNS1, MNS2, MNS3, and MNS4) were prepared by keeping sodium alginate concentration constant (6%) and increasing CMC concentration from 3% to 6%, whereas MNS5, MNS6, MNS7, and MNS8 were developed using sodium alginate to CMC concentrations 7:3, 7:4, 8:3, and 8:4, respectively. Solvent casting technique was opted for preparation of MNS patches. MNS were characterized for thickness, folding endurance, insertion capacity, drug content, morphology, and ex-vivo permeation profile using Wistar rat skin.

KEY FINDINGS

FTIR studies revealed the compatibility of quetiapine with formulation composites. Thickness and folding endurance was ranged in between 0.53-0.55 mm and 25-264, respectively. SEM of optimized patch showed sharp pointed needles. Ex-vivo permeation studies showed percent drug release of 84.34% from MNS1 after 48 h.

CONCLUSIONS

The overall findings of study proposed that the quetiapine-loaded MNS patches hold promise for the improved transdermal delivery of quetiapine.

摘要

目的

本研究旨在制备并表征载有喹硫平(抗精神病药物)的微针透皮贴剂,以改善药物递送。

方法

本研究旨在开发用于递送喹硫平的微针透皮贴剂(MNS)。使用不同浓度的海藻酸钠和羧甲基纤维素制备了8个载有喹硫平的MNS贴剂(MNS1 - MNS8)。前四个MNS贴剂(MNS1、MNS2、MNS3和MNS4)通过保持海藻酸钠浓度恒定(6%)并将CMC浓度从3%增加到6%来制备,而MNS5、MNS6、MNS7和MNS8分别使用海藻酸钠与CMC浓度比为7:3、7:4、8:3和8:4来制备。选择溶剂浇铸技术制备MNS贴剂。使用Wistar大鼠皮肤对MNS进行厚度、折叠耐久性、插入能力、药物含量、形态和体外渗透曲线的表征。

主要发现

傅里叶变换红外光谱(FTIR)研究揭示了喹硫平与制剂复合材料的相容性。厚度和折叠耐久性分别在0.53 - 0.55毫米和25 - 264之间。优化贴剂的扫描电子显微镜(SEM)显示针尖尖锐。体外渗透研究表明,48小时后MNS1的药物释放百分比为84.34%。

结论

该研究的总体结果表明,载有喹硫平的MNS贴剂有望改善喹硫平的透皮递送。

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