Boyuklieva Radka, Hristozova Asya, Pilicheva Bissera
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.
Research Institute, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.
Biomedicines. 2023 May 22;11(5):1491. doi: 10.3390/biomedicines11051491.
The present work is focused on the preparation of an optimal model of poly-ε-caprolactone nanoparticles as potential carriers for nasal administration of idebenone. A solvent/evaporation technique was used for nanoparticle preparation. Poly-ε-caprolactone with different molecular weights (14,000 and 80,000 g/mol) was used. Polysorbate 20 and Poloxamer 407, alone and in combination, were used as emulsifiers at different concentrations to obtain a stable formulation. The nanoparticles were characterized using dynamic light scattering, SEM, TEM, and FTIR. The resulting structures were spherical in shape and their size distribution depended on the type of emulsifier. The average particle size ranged from 188 to 628 nm. The effect of molecular weight and type of emulsifier was established. Optimal models of appropriate size for nasal administration were selected for inclusion of idebenone. Three models of idebenone-loaded nanoparticles were developed and the effect of molecular weight on the encapsulation efficiency was investigated. Increased encapsulation efficiency was found when poly-ε-caprolactone with lower molecular weight was used. The molecular weight also affected the drug release from the nanostructures. Dissolution study data were fitted into various kinetic models and the Korsmeyer-Peppas model was found to be indicative of the release mechanism of idebenone.
本研究聚焦于制备聚己内酯纳米颗粒的优化模型，作为艾地苯醌鼻腔给药的潜在载体。采用溶剂蒸发技术制备纳米颗粒。使用了不同分子量（14,000和80,000 g/mol）的聚己内酯。聚山梨酯20和泊洛沙姆407单独或组合使用，以不同浓度作为乳化剂来获得稳定的制剂。使用动态光散射、扫描电子显微镜、透射电子显微镜和傅里叶变换红外光谱对纳米颗粒进行表征。所得结构呈球形，其尺寸分布取决于乳化剂的类型。平均粒径范围为188至628 nm。确定了分子量和乳化剂类型的影响。选择适合鼻腔给药的合适尺寸的优化模型以包载艾地苯醌。开发了三种载艾地苯醌纳米颗粒模型，并研究了分子量对包封率的影响。发现使用较低分子量的聚己内酯时包封率增加。分子量也影响药物从纳米结构中的释放。将溶出研究数据拟合到各种动力学模型中，发现Korsmeyer-Peppas模型可指示艾地苯醌的释放机制。
