Nakipekova Aidana, Kudaibergenova Bates, Abdurashitov Arkady S, Sukhorukov Gleb B
Faculty of Chemistry and Chemical Technology, Al-Farabi Kazakh National University, 71 Al-Farabi Ave., Almaty 050042, Kazakhstan.
Vladimir Zelman Center for Neurobiology and Brain Restoration, Skoltech, 3 Nobel Str., Moscow 121205, Russia.
Pharmaceutics. 2025 Jul 15;17(7):916. doi: 10.3390/pharmaceutics17070916.
This research focuses on the development of fabrication approaches for microparticles intended for controlled drug delivery. The primary objective is to identify the most suitable polymer type, particle size, and morphology for encapsulating a water-soluble crystalline drug. Optimizing these parameters may enhance structural stability and prolong the release of this active substance. The microparticles were fabricated through the encapsulation of a drug substance within a polymer carrier and employing polymer casting on prepatterned surfaces, followed by the loading of drug precipitates and the application of a sealing layer. The crystalline powder 1-allyl-2,5-dimethylpiperidol-4 hydrochloride served as the core cargo material, while the walls of these particles were composed of polylactic acid (PLA) and a poly (α-caprolactone) (PCL) in a 70:30 composition ratio. The size and volume of the microparticles were found to be dependent on the geometric parameters of the template and the concentration of the polymer solutions. The study demonstrates the formation, physical dimensions, and particle count at varied polymer compositions and concentrations. The formation of the PLA and PCL mixture occurred solely through physical interactions. Scanning electron microscopy (SEM) and optical microscopy were employed to observe the appearance and physical dimensions of the microparticles. The obtained data confirm that tailored polymer compositions can yield consistent particle morphology and a suitable drug elution rate. The results indicate that microparticles sealed with an optimal polymer composition exhibit enhanced release properties. This finding highlights the feasibility of microencapsulation at precise ratios and concentrations of polymers to achieve the long-lasting effects of water-soluble drugs.
本研究聚焦于用于控释给药的微粒制备方法的开发。主要目标是确定用于包封水溶性结晶药物的最合适的聚合物类型、粒径和形态。优化这些参数可能会增强结构稳定性并延长这种活性物质的释放时间。微粒是通过将药物包裹在聚合物载体中，并在预先图案化的表面上进行聚合物浇铸，随后加载药物沉淀物并施加密封层来制备的。结晶粉末1-烯丙基-2,5-二甲基哌啶-4盐酸盐作为核心载药材料，而这些微粒的壁由聚乳酸（PLA）和聚（α-己内酯）（PCL）按70:30的组成比例构成。发现微粒的尺寸和体积取决于模板的几何参数和聚合物溶液的浓度。该研究展示了在不同聚合物组成和浓度下微粒的形成、物理尺寸和颗粒数量。PLA和PCL混合物的形成仅通过物理相互作用发生。使用扫描电子显微镜（SEM）和光学显微镜观察微粒的外观和物理尺寸。获得的数据证实，定制的聚合物组成可以产生一致的颗粒形态和合适的药物洗脱速率。结果表明，用最佳聚合物组成密封的微粒具有增强的释放特性。这一发现突出了在精确的聚合物比例和浓度下进行微囊化以实现水溶性药物长效作用的可行性。
