Dipartimento di Scienze del Farmaco e Prodotti per la Salute, Università di Messina, Piazza Pugliatti 1, Messina, Italy.
Istituto di Bioscienze e Biorisorse - CNR, Via Pietro Castellino 111, Napoli, Italy; Istituto di Genetica e Biofisica "ABT" - CNR, Via Pietro Castellino 111, Napoli, Italy.
Int J Pharm. 2017 Mar 30;520(1-2):21-28. doi: 10.1016/j.ijpharm.2017.01.049. Epub 2017 Jan 24.
In this work, curcumin (CURC)-encapsulating nanoparticles (NPs), made up of an amphiphilic blend of poloxamers and PLGA (PPC NPs) at different polymer concentrations, were prepared by nanoprecipitation. CURC was preliminarily complexed with (2-hydroxypropyl)-β-cyclodextrin (HPβCD) to improve its loading efficiency. The formation of host-guest complexes of CURC with HPβCD (CD-CURC) was confirmed by means of HNMR studies and differential scanning calorimetry (DSC). Nanoprecipitation allowed to obtain NPs with a small size (90-120nm depending on the polymer concentration), a narrow size distribution and stable in water for 30days at 4°C and in RPMI-1640 cell culture medium up to 72h at 37°C. The in vitro release of CD-CURC, sustained up to 5days, was governed mainly by a diffusive mechanism. It was also found that the produced NPs were efficiently internalized by mesothelioma cells (MSTO-211H) in the cytoplasmic space, at an extent strongly dependent on NP size and polydispesity index, therefore pointing at the importance of NP preparation method in improving their uptake.
在这项工作中，通过纳米沉淀法制备了由两亲性泊洛沙姆和 PLGA（PPC NPs）组成的姜黄素（CURC）纳米胶囊（NPs），聚合物浓度不同。CURC 与（2-羟丙基）-β-环糊精（HPβCD）初步络合，以提高其包载效率。通过 HNMR 研究和差示扫描量热法（DSC）证实了 CURC 与 HPβCD 的主体客体络合（CD-CURC）的形成。纳米沉淀法可获得粒径为 90-120nm（取决于聚合物浓度）、粒径分布窄且在 4°C 下在水中稳定 30 天、在 37°C 下在 RPMI-1640 细胞培养液中稳定 72h 的 NPs。CD-CURC 的体外释放持续 5 天，主要受扩散机制控制。还发现所制备的 NPs 能够有效地被间皮瘤细胞（MSTO-211H）内吞到细胞质空间，其程度强烈依赖于 NP 尺寸和多分散指数，因此指出 NP 制备方法对于提高其摄取能力的重要性。
