Department of Mechanical Engineering, University College London, Torrington Place, London WC1E 7JE, UK.
Department of Physics & Astronomy, University College London, Gower Street, London WC1E 6BT, UK.
Int J Pharm. 2022 Nov 25;628:122279. doi: 10.1016/j.ijpharm.2022.122279. Epub 2022 Oct 13.
Coaxial electrospray is advantageous for the production of multidrug-releasing nanocarriers because it permits precise control over particle size, inhibits initial burst release, and offers moderate preparation conditions. In this study, a single-step coaxial electrospray technique is presented that achieves over 90 % co-encapsulation of the saxagliptin and dapagliflozin, two drugs treating type 2 diabetes, into biodegradable poly (-lactide-co-glicolide) (PLGA) nanoparticles. Scanning electron microscopy reveals spherical and smooth shapes with diameters ranging from 534.8 to 708.6 nm. Transmission electron microscopy revealed clear core-shell and trilayer nanostructures. Fourier transform infrared spectroscopy confirmed the presence of PLGA, saxagliptin, and dapagliflozin in all the evaluated formulations. The results of the drug release investigation indicated the prolonged and regulated release of saxagliptin and dapagliflozin from bi- and trilayer structures, as compared to monolayer particles. Computational modelling showed good agreement with the experimental drug release profile in vitro. Further, cytotoxicity assay demonstrates that the formulated nanoparticles display good cytocompatibility. This study indicates that with the controllable and distinctive sustained release profiles, the hybrid nanoparticle-based drug delivery system can effectively co-encapsulate multiple drugs treating type 2 diabetes in a protectively shell of PLGA for therapeutically-benefit controlled release.
同轴电喷雾在制备多药物释放纳米载体方面具有优势,因为它可以精确控制粒径、抑制初始突释,并提供温和的制备条件。本研究提出了一种单步同轴电喷雾技术,可将两种治疗 2 型糖尿病的药物——沙格列汀和达格列净——超过 90%共包封到可生物降解的聚(乳酸-共-乙醇酸)(PLGA)纳米颗粒中。扫描电子显微镜显示,粒径范围为 534.8 至 708.6nm 的纳米颗粒呈球形且表面光滑。透射电子显微镜显示出清晰的核壳和三层纳米结构。傅里叶变换红外光谱证实了所有评估配方中均存在 PLGA、沙格列汀和达格列净。药物释放研究结果表明,与单层颗粒相比,双和三层结构中沙格列汀和达格列净的释放具有延长和调节的特点。计算模型显示与体外实验药物释放曲线吻合良好。此外,细胞毒性试验表明,所制备的纳米颗粒具有良好的细胞相容性。本研究表明,具有可控和独特的持续释放曲线的混合纳米粒子给药系统可以有效地将多种治疗 2 型糖尿病的药物共包封在 PLGA 的保护性外壳中,实现治疗效益控制释放。