田口设计优化依托度酸和槲皮素负载的微孔微球:一种提高载药效率的方法。

IF 3.7 3区 医学 Q2 CHEMISTRY, MEDICINAL
Sourav Chougule, Hafiz Ahmed, Snigdha Singh, Mukta Agrawal, Ravish J Patel, Amit Alexander
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引用次数: 0

摘要

介孔二氧化硅纳米颗粒(MSN)由于其优异的载药效率,近年来在药物载体体系中的应用受到了广泛的关注。然而,与其他基于脂质的药物递送系统相比,药物装载过程具有相当大的挑战性。在此基础上,合成了不同催化剂的微孔微球,并利用BET分析仪对其进行了IV型吸附-脱附等温线表征。借助Taguchi DOE,考察了溶剂选择和其他工艺参数(药物与msn比、装载周期、搅拌速度)对BCSⅱ类和ⅳ类模型药物依托度酸(ETD)和槲皮素(QUR)装载的影响。最高载药量%预测值与实验值接近(ETD和QUR分别为19.04±0.50%和11.40±0.18%)。有趣的是,溶剂选择对ETD的载药量影响最大,而对QUR的影响不显著。因此,反映了药物装载到msn的一般程序不能遵循,必须进行批判性研究。此外,ETD和QUR的加入提高了微孔微球的水溶性(分别为3.08倍和2.5倍)。利用体外药物释放动力学模型,评价微细粒微球在不同药物释放介质中的ETD和QUR的体外释放特性,探讨微细粒微球的体外释放机制。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Optimizing etodolac and quercetin loaded MSNs using taguchi design: an approach for enhancing drug loading efficiency.

The application of mesoporous silica nanoparticles (MSN) as a drug carrier system got immense attention in the past few years due to their exceptional high drug loading efficiency. However, the process of drug loading is quite challenging compared to other lipid-based drug delivery systems. Hence, the MSNs using different catalysts were synthesized, and their mesoporous material characteristic was confirmed by the type IV adsorption-desorption isotherm using BET analyzer. The effect of solvent selection and other process parameters (drug to MSNs ratio, period of loading, and stirring speed) on the loading of BCS class II and IV model drugs etodolac(ETD) and quercetin(QUR) respectively were investigated with the help of Taguchi DOE. The predicted value for the highest % drug loading was close to the experimental value(19.04 ± 0.50 % and 11.40 ± 0.18 % for ETD and QUR respectively). It was interesting to note, that the solvent selection had the highest impact on the drug loading of ETD into the MSNs, whereas for QUR this parameter was insignificant. Hence reflecting that a generalized procedure for the drug loading into the MSNs cannot be followed and had to be critically studied. Also, the loading of ETD and QUR into the MSNs improved the aqueous solubility (3.08 and 2.5 folds respectively). Further the in-vitro drug release properties were evaluated for ETD and QUR from MSNs in various drug release mediums to explore their release mechanism from MSNs using in vitro drug release kinetic modelling.

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来源期刊
CiteScore
7.30
自引率
13.20%
发文量
367
审稿时长
33 days
期刊介绍: The Journal of Pharmaceutical Sciences will publish original research papers, original research notes, invited topical reviews (including Minireviews), and editorial commentary and news. The area of focus shall be concepts in basic pharmaceutical science and such topics as chemical processing of pharmaceuticals, including crystallization, lyophilization, chemical stability of drugs, pharmacokinetics, biopharmaceutics, pharmacodynamics, pro-drug developments, metabolic disposition of bioactive agents, dosage form design, protein-peptide chemistry and biotechnology specifically as these relate to pharmaceutical technology, and targeted drug delivery.
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