用于口服给药的 Eudragit® RS 100 负载氟比洛芬纳米颗粒的开发、基于 QbD 的优化、体内药代动力学和体外评估。

IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Journal of microencapsulation Pub Date : 2024-11-16 DOI:10.1080/02652048.2024.2427294
Shilpa Mandpe, Eknath Kole, Vishal Parate, Aniruddha Chatterjee, Arun Mujumdar, Jitendra Naik
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引用次数: 0

摘要

本研究旨在开发和评估负载氟比洛芬的聚合物纳米粒子,以实现药物的持续释放,提高疗效并减少给药次数,从而改善患者的治疗效果。采用管式微反应器和喷雾干燥法制备了氟比洛芬负载聚合物纳米粒子,并通过盒式贝肯设计进行了优化。表征包括粒度、封装效率、体外和体内药物释放,以及傅立叶变换红外光谱(FTIR)、电子稳定性扫描(DSC)、X射线衍射(XRD)和扫描电子显微镜(SEM)等技术。统计分析确保了配方优化和性能评估的稳健性。优化后的氟比洛芬负载聚合物纳米颗粒的平均直径、PDI、zeta 电位、药物释放和 EE% 分别为 306.1 ± 6.00 nm、0.184 ± 0.02 Mw、-23.6 ± 1.51 mV、85.46 ± 0.53% 和 92.31 ± 0.84(% w/w)。药代动力学分析进一步证实,与纯氟比洛芬相比,该药物的持续释放时间可延长至 12 小时,且渗透性更强。负载氟比洛芬的聚合物纳米粒子的持续释放大大提高了对炎症的治疗效果。
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Development, QbD-based optimisation, in-vivo pharmacokinetics, and ex-vivo evaluation of Eudragit® RS 100 loaded flurbiprofen nanoparticles for oral drug delivery.

This study aims to develop and evaluate flurbiprofen-loaded polymeric nanoparticles to achieve sustained drug release, enhancing therapeutic efficacy and minimising dosing frequency for improved patient outcomes. Flurbiprofen-loaded polymeric nanoparticles were prepared using a tubular microreactor and spray drying, optimised via Box-Behnken Design. Characterisation included particle size, encapsulation efficiency, in vitro and in vivo drug release, and techniques like FTIR, DSC, XRD, and SEM. Statistical analysis ensured robust formulation optimisation and evaluation of performance. The optimised batch of flurbiprofen-loaded polymeric nanoparticles was characterised for mean diameter, PDI, zeta potential, drug release, and EE% were found to be 306.1 ± 6.00 nm, 0.184 ± 0.02 Mw, -23.6 ± 1.51 mV, 85.46 ± 0.53% and 92.31 ± 0.84 (% w/w) respectively. Pharmacokinetic analysis further confirmed the sustained release, extending up to 12 hours and enhancing permeation compared to the pure flurbiprofen. Sustained release of flurbiprofen-loaded polymeric nanoparticles significantly enhances therapeutic effectiveness for inflammatory conditions.

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来源期刊
Journal of microencapsulation
Journal of microencapsulation 工程技术-工程:化工
CiteScore
6.30
自引率
2.60%
发文量
39
审稿时长
3 months
期刊介绍: The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.
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