Department of Drug Sciences, University of Pavia, 27100 Pavia, Italy.
Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
Mar Drugs. 2018 Nov 15;16(11):447. doi: 10.3390/md16110447.
Most of the methods of poly-lactic-glycolic acid (PLGA) preparation involve the passage through the emulsification of a PLGA organic solution in water followed by solvent evaporation or extraction. The choice of the droplet stabilizer during the emulsion step is critical for the dimensions and the surface characteristics of the nanoparticles (NPs). In the present work, a recently described ionic amphiphilic chitosan derivative, chitosan oleate salt (CS-OA), was proposed for the first time to prepare PLGA NPs. A full factorial design was used to understand the effect of some formulation and preparation parameters on the NP dimensions and on encapsulation efficiency (EE%) of Nile red, used as a tracer. On the basis of the DoE study, curcumin loaded NPs were prepared, having 329 ± 42 nm dimensions and 68.75% EE%. The presence of a chitosan coating at the surface was confirmed by positive zeta potential and resulted in mucoadhesion behavior. The expected improvement of the interaction of the chitosan surface modified nanoparticles with cell membrane surface was confirmed in Caco-2 cell culture by the internalization of the loaded curcumin.
大多数聚乳酸-乙醇酸(PLGA)的制备方法都涉及将 PLGA 有机溶剂溶液乳化在水中,然后进行溶剂蒸发或萃取。在乳化步骤中,选择液滴稳定剂对于纳米颗粒(NPs)的尺寸和表面特性至关重要。在本工作中,首次提出了一种最近描述的离子两亲性壳聚糖衍生物,油酸钠壳聚糖(CS-OA),用于制备 PLGA NPs。采用完全析因设计来了解一些制剂和制备参数对 NPs 尺寸和尼罗红包封效率(EE%)的影响,尼罗红被用作示踪剂。基于 DOE 研究,制备了负载姜黄素的 NPs,其尺寸为 329±42nm,EE%为 68.75%。表面存在壳聚糖涂层通过正zeta 电位得到证实,导致具有粘膜粘附性。通过负载姜黄素的内化,在 Caco-2 细胞培养中证实了表面改性的壳聚糖纳米颗粒与细胞膜表面的预期改善的相互作用。