LEPABE, Department of Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal.
Beilstein J Nanotechnol. 2015 Jun 12;6:1306-18. doi: 10.3762/bjnano.6.135. eCollection 2015.
Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were studied as drug delivery vehicles for calcitriol, the active form of vitamin D3. In vitro effects of calcitriol encapsulated in PLGA nanoparticles were evaluated with respect to free calcitriol on human pancreatic cell lines, S2-013 and hTERT-HPNE, and the lung cancer cell line A549. Encapsulated calcitriol retained its biological activity, reducing the cell growth. Cytotoxicity assays demonstrated that encapsulation of calcitriol enhanced its inhibitory effect on cell growth at a concentration of 2.4 μM for the S2-013 cells (91%) and for A549 cells (70%) comparared to the free calcitriol results. At this concentration the inhibitory effect on nontumor cells (hTERT-HPNE) decreased to 65%. This study highlights the ability of PLGA nanoparticles to deliver vitamin D3 into cancer cells, with major effects regarding cancer cell cycle arrest and major changes in the cell morphological features.
聚（乳酸-共-乙醇酸）（PLGA）纳米粒被研究作为钙三醇（维生素 D3 的活性形式）的药物传递载体。用游离钙三醇对人胰腺细胞系 S2-013 和 hTERT-HPNE 以及肺癌细胞系 A549 进行评价，研究了包封在 PLGA 纳米粒中的钙三醇的体外效应。包封的钙三醇保留了其生物活性，降低了细胞生长。细胞毒性试验表明，与游离钙三醇相比，在浓度为 2.4 μM 时，钙三醇的包封增强了其对 S2-013 细胞（91%）和 A549 细胞（70%）的生长抑制作用。在该浓度下，对非肿瘤细胞（hTERT-HPNE）的抑制作用降低至 65%。这项研究强调了 PLGA 纳米粒将维生素 D3 递送至癌细胞的能力，其对癌细胞周期停滞和细胞形态特征的重大变化具有主要影响。
