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基于脂肪酸的低共熔混合物作为相变材料在药物微囊化中的应用:制备、表征及释放行为

Application of fatty acid-based eutectic mixture as a phase change material in microencapsulation of drugs: preparation, characterization and release behavior.

作者信息

Ghaffari Fariba, Shekaari Hemayat

机构信息

Department of Physical Chemistry, University of Tabriz, Tabriz, Iran.

出版信息

BMC Chem. 2025 Feb 17;19(1):42. doi: 10.1186/s13065-025-01406-4.

Abstract

Recently, microencapsulation has developed in various industries with its versatile applications. Its profound impact is particularly notable in the chemical, food, and pharmaceutical sectors. Among its research areas, the microencapsulation of drugs using phase change materials (PCMs) stands out as a groundbreaking advancement in drug delivery systems. This innovative approach involves encasing drugs within a PCM shell, significantly enhancing their stability and delivery regulation. The focus of our study is the microencapsulation of certain drugs with poor water solubility namely, cyclosporine, baclofen, and biotin within a bio-based PCM. It has identified PCMs with phase transition temperatures near human body temperature ( 310 K) as ideal candidates for this purpose. A eutectic mixture of stearic-lauric acid in a 1:3 mole ratio was selected for its optimal phase change properties to create microcapsules with core-shell morphology in spherical form. Our comprehensive characterization of the microcapsules, validated by FT-IR and SEM techniques, confirms their proper formation. All studied drugs microencapsulated with the PCM exhibited an excellent thermal stability at working temperature from thermal stability analysis based on TGA results. Furthermore, differential scanning calorimetry (DSC) tests conducted on the microencapsulated drugs obtained the melting point of all three microencapsulated drugs near the melting point of PCM. Also, the release behavior of drugs from drug delivery method was investigated in PBS (pH 7.4) and two temperatures (310.15 and 318.15) K. Drug release occurred sustainably, such that 50% and about 60% of the total of each drug was released from the microcapsules at mentioned temperatures respectively during 24 h.

摘要

近年来,微胶囊化技术凭借其广泛的应用在各个行业得到了发展。其深远影响在化工、食品和制药领域尤为显著。在其研究领域中,使用相变材料(PCM)对药物进行微胶囊化是药物递送系统中的一项突破性进展。这种创新方法涉及将药物包裹在PCM壳内,显著提高了药物的稳定性和递送调控能力。我们研究的重点是将某些水溶性差的药物,即环孢素、巴氯芬和生物素,包裹在生物基PCM中。已确定相变温度接近人体体温(310 K)的PCM是实现这一目的的理想候选材料。选择了摩尔比为1:3的硬脂酸 - 月桂酸低共熔混合物,因其具有最佳的相变特性,以制备具有核壳形态的球形微胶囊。通过傅里叶变换红外光谱(FT - IR)和扫描电子显微镜(SEM)技术对微胶囊进行的全面表征证实了它们的正确形成。基于热重分析(TGA)结果的热稳定性分析表明,所有用PCM微胶囊化的研究药物在工作温度下均表现出优异的热稳定性。此外,对微胶囊化药物进行的差示扫描量热法(DSC)测试得出,所有三种微胶囊化药物的熔点接近PCM的熔点。同时,在磷酸盐缓冲液(PBS,pH 7.4)和两个温度(310.15和318.15)K下研究了药物从药物递送方法中的释放行为。药物持续释放,使得在上述温度下,每种药物总量的50%和约60%分别在24小时内从微胶囊中释放出来。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a606/11834564/5349b22c7ab6/13065_2025_1406_Fig1a_HTML.jpg

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