Initial doxycycline hyclate diffusion and solvent exchange from borneol-based in situ forming matrices using UV–Vis imaging

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Nutdanai Lertsuphotvanit , Jesper Østergaard , Pornsit Chaiya , Warakon Thammasut , Thawatchai Phaechamud
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Abstract

UV–Visible (UV–Vis) imaging provides real-time and spatially resolved insights into drug transport, solvent diffusion, and matrix formation, making it a useful tool for evaluating in situ forming matrices (ISMs). ISMs are injectable liquids that solidify upon contact with aqueous environments to sustain drug release. Borneol, a poorly water-soluble and biocompatible monoterpene alcohol, was selected as the matrix former, with triacetin as a hydrophobic co-solvent to modulate drug release in a concentration-dependent manner. This study investigated the effects of borneol matrix and triacetin concentration on solvent exchange, matrix structure, and drug transport in borneol-based ISMs. Formulations containing borneol (40 % w/w), doxycycline hyclate (0.5 % w/w), and triacetin (0–25 % w/w) in N-methyl-2-pyrrolidone (NMP) were characterized by microscopy and UV–Vis imaging to evaluate morphology, solvent diffusion, and drug release. The results showed that borneol matrices effectively restricted solvent and drug transport. Incorporation of 5 % w/w triacetin had a negligible effect on initial solvent exchange and drug release, whereas 25 % w/w triacetin disrupted matrix integrity, resulting in accelerated solvent exchange and unrestricted Dox diffusion. A strong linear correlation between drug and solvent diffusion was observed, with the borneol matrix promoting more efficient drug transport under equivalent solvent diffusion conditions compared to the non-matrix system. Overall, UV–Vis imaging provided real-time insights into solvent exchange mechanisms, matrix formation, and drug release behavior in ISM, confirming that borneol matrices with 5 % w/w triacetin loading can prolong drug release.

Abstract Image

用紫外-可见成像技术研究冰片基原位成形基质中初始多西环素水合扩散和溶剂交换
紫外-可见(UV-Vis)成像提供了实时和空间分辨的药物运输,溶剂扩散和基质形成的见解,使其成为评估原位形成基质(ISMs)的有用工具。ISMs是可注射液体,与水环境接触后固化以维持药物释放。选择难水溶性、生物相容性较差的单萜醇——冰片作为基质前体,以三乙酸乙酯为疏水共溶剂,以浓度依赖性方式调节药物释放。本研究考察了冰片基质和三乙酸乙酯浓度对冰片基质中溶剂交换、基质结构和药物转运的影响。在n -甲基-2-吡咯烷酮(NMP)中加入冰片(40% w/w)、水合强力霉素(0.5% w/w)和三乙酰素(0 - 25% w/w),通过显微镜和紫外可见成像对其进行表征,以评估其形貌、溶剂扩散和药物释放。结果表明,冰片基质有效地限制了溶剂和药物的运输。加入5% w/w的三乙酸酯对初始溶剂交换和药物释放的影响可以忽略不计,而25% w/w的三乙酸酯破坏了基质的完整性,导致溶剂交换加速和Dox扩散不受限制。药物与溶剂扩散之间存在很强的线性关系,在同等溶剂扩散条件下,与非基质系统相比,冰片基质促进了更有效的药物运输。总体而言,UV-Vis成像提供了ISM中溶剂交换机制、基质形成和药物释放行为的实时洞察,证实了5% w/w三乙酸苷负载的冰片基质可以延长药物释放。
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来源期刊
CiteScore
8.00
自引率
8.00%
发文量
879
审稿时长
94 days
期刊介绍: The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.
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