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研究埃洛石纳米管作为一种潜在的口服改良递药平台用于不同 BCS 分类药物：药物释放动力学的特性、优化和评价。

Investigating Halloysite Nanotubes as a Potential Platform for Oral Modified Delivery of Different BCS Class Drugs: Characterization, Optimization, and Evaluation of Drug Release Kinetics.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.

出版信息

Int J Nanomedicine. 2021 Mar 1;16:1725-1741. doi: 10.2147/IJN.S299261. eCollection 2021.

DOI:10.2147/IJN.S299261
PMID:33688188
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7935346/
Abstract

PURPOSE: This study systematically investigated the potential of four model drugs (verapamil HCl, flurbiprofen, atenolol, and furosemide), each belonging to a different class of Biopharmaceutics Classification Systems (BCS) to be developed into oral modified release dosage forms after loading with halloysite nanotubes (HNTs). METHODS: The drugs were studied for their loading (mass gain %) by varying solvent system, method, pH, and ratios of loading into the nanotubes using D-optimal split-plot design with the help of Design Expert software. Drug-loaded halloysites were characterized by XRD, DTA, FTIR, SEM, and HPLC-UV-based assay procedures. Dissolution studies were also performed in dissolution media with pH 1.2, 4.5, and 6.8. Moreover, the optimized samples were evaluated under stress stability conditions for determining prospects for the development of oral dosage forms. RESULTS: As confirmed with the results of XRD and DTA, the drugs were found to be converted into amorphous form after loading with halloysite (HNTs). The drugs were loaded in the range of ~7-9% for the four drugs, with agitation providing satisfactory and equivalent loading as compared to vacuum plus agitation based reported methods. FTIR results revealed either only weak electrostatic (verapamil HCl and flurbiprofen) or no interaction with the surface structure of the HNTs. The dissolution profiling depicted significantly retarded release of drugs with Fickian diffusion from a polydisperse system as a model that suits well for the development of oral dosage forms. HPLC-UV-based assay indicated that except furosemide (BCS class IV), the other three drugs are quite suitable for development for oral dosage forms. CONCLUSION: The four drugs investigated undergo phase transformation with HNTs. While agitation is an optimum method for loading drugs with various physicochemical attributes into HNTs; solvent system, loading ratios and pH play an important role in the loading efficiency respective to the drug properties. The study supports the capability of developing HNT-based modified release oral dosage forms for drugs with high solubility.

摘要

目的：本研究系统地考察了 4 种模型药物（盐酸维拉帕米、氟比洛芬、阿替洛尔和呋塞米）的潜力，这 4 种药物分别属于生物药剂学分类系统（BCS）的不同类别，在负载纳米管后可开发为口服缓释剂型。

方法：采用 D-最优分割实验设计，借助 Design Expert 软件，考察了不同溶剂体系、方法、pH 值以及载药量比对药物载入纳米管的影响，对药物的载药量（质量增益%）进行了研究。采用 XRD、DTA、FTIR、SEM 和 HPLC-UV 分析方法对负载羟硅钠石的药物进行了表征。在 pH 值为 1.2、4.5 和 6.8 的溶解介质中进行了溶解研究。此外，还在稳定性条件下对优化后的样品进行了评估，以确定开发口服剂型的前景。

结果：XRD 和 DTA 结果证实，药物在负载羟硅钠石（HNTs）后被转化为无定形形式。四种药物的载药量在 7-9%之间，与真空搅拌法相比，搅拌法提供了令人满意的等效载药量。FTIR 结果表明，只有弱静电相互作用（盐酸维拉帕米和氟比洛芬）或与 HNTs 的表面结构无相互作用。溶出曲线表明，药物以菲克扩散形式从多分散体系中释放缓慢，这是一种适合开发口服剂型的模型。HPLC-UV 分析表明，除了呋塞米（BCS 分类 IV）外，其他三种药物都非常适合开发口服剂型。

结论：本研究中考察的四种药物与 HNTs 发生了相变。虽然搅拌是一种优化的方法，适用于将具有各种物理化学特性的药物载入 HNTs；但溶剂系统、载药量比和 pH 值对药物性质的载药效率起着重要作用。该研究支持开发基于 HNT 的缓释口服剂型的能力，适用于高溶解度的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/99f2435f95ed/IJN-16-1725-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/3a302b73f42f/IJN-16-1725-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/0db9f4474064/IJN-16-1725-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/a671d2d7777f/IJN-16-1725-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/c26c77146df9/IJN-16-1725-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/99f2435f95ed/IJN-16-1725-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/3a302b73f42f/IJN-16-1725-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/0db9f4474064/IJN-16-1725-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/a671d2d7777f/IJN-16-1725-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/c26c77146df9/IJN-16-1725-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ada9/7935346/99f2435f95ed/IJN-16-1725-g0005.jpg

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本文引用的文献

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