Effect of poly(ε-caprolactone) microspheres on population pharmacokinetic/pharmacodynamic model of a simple coumarin.

IF 3 4区医学 Q2 CHEMISTRY, APPLIED Journal of microencapsulation Pub Date : 2024-12-01 Epub Date: 2024-10-26 DOI:10.1080/02652048.2024.2418606

Paola A Cárdenas, Izabel Almeida Alves, Bibiana Verlindo De Araujo, Diana Marcela Aragón

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Abstract

This study aims to evaluated the impact of poly(ε-caprolactone) (PCL) microspheres on the pharmacokinetics and pharmacodynamics (PopPK/PD) of 6-methylcoumarin (6MC). For this, PCL microspheres loaded with 6MC were prepared using the emulsification-evaporation method. Particle size, zeta potential, drug loading, and entrapment efficiency were characterised by dynamic light scattering and UV spectrophotometry. In vitro release and pharmacokinetics in Wistar rats were assessed for free and encapsulated 6MC. Anti-inflammatory activity was evaluated using the carrageenan-induced paw edoema model, with PopPK and PopPK/PD models developed. Microspheres showed diameters between 2.9 and 7.1 µm, zeta potentials of -10 to -15 mV, and drug loading of 0.24 mg/mg. Encapsulation efficiency was 45.5% to 75.9%. PopPK models showed enhanced absorption and distribution, with increased anti-inflammatory potency of encapsulated 6MC. PCL microspheres significantly improved the pharmacokinetic and pharmacodynamic profiles of 6MC, enhancing its therapeutic potential for lipophilic drugs.

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聚（ε-己内酯）微球对一种简单香豆素的群体药代动力学/药效学模型的影响

本研究旨在评估聚(ε-己内酯)（PCL）微球对 6-甲基香豆素（6MC）药代动力学和药效学（PopPK/PD）的影响。为此，采用乳化-蒸发法制备了负载 6MC 的 PCL 微球。采用动态光散射法和紫外分光光度法对粒度、ZETA电位、载药量和包埋效率进行了表征。对游离和包封的 6MC 在 Wistar 大鼠体内的体外释放和药代动力学进行了评估。使用卡拉胶诱导的爪水肿模型评估了抗炎活性，并建立了 PopPK 和 PopPK/PD 模型。微球的直径在 2.9 至 7.1 微米之间，zeta 电位为 -10 至 -15 mV，载药量为 0.24 毫克/毫克。封装效率为 45.5% 至 75.9%。PopPK 模型显示，包封的 6MC 的吸收和分布均有所改善，抗炎效力也有所提高。PCL 微球明显改善了 6MC 的药代动力学和药效学特征，提高了其作为亲脂性药物的治疗潜力。

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

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.