用于新型细胞药物递送系统的杂化改良聚（D，L-丙交酯-共-乙交酯）纳米球。
Hybrid-modified poly(D,L-lactide-co-glycolide) nanospheres for a novel cellular drug delivery system.
机构信息
Laboratory of Pharmaceutical Engineering, School of Pharmacy, Aichi Gakuin University, Nagoya, Aichi, Japan.
出版信息
Int J Pharm. 2010 Jun 15;392(1-2):311-3. doi: 10.1016/j.ijpharm.2010.03.042. Epub 2010 Mar 25.
We prepared surface-modified poly(D,L-lactide-co-glycolide) (PLGA) nanospheres (NS) for use as cellular drug and gene delivery systems using an emulsion solvent diffusion method. In this study, we screened for an appropriate surface modifier to improve NS cellular uptake. Poly-L-lysine (PLL)-modified PLGA NS were taken up by A549 cells in significantly higher amounts (17-fold) than unmodified NS. In order to provide a novel function, PLGA NS were hybrid-modified using both; a cationic polymer, PLL, and a nonionic surfactant, polysorbate 80, to improve cellular uptake in serum-containing medium (SCM). Hybrid modification abrogated the decreased PLGA NS cellular uptake in SCM as a result of better dispersion in serum compared to PLL-PLGA NS, which aggregated in SCM. Luciferase activity of Hybrid-NS/pCMV-Luc complexes in A549 cells in SCM was 122-fold higher than PLL-NS. Hybrid-PLGA NS were not cytotoxic for A549 cells. In conclusion, Hybrid-PLGA NS have great potential as effective cellular drug delivery carriers.
我们使用乳化溶剂扩散法制备了用于细胞药物和基因传递系统的表面修饰的聚（D，L-丙交酯-共-乙交酯）（PLGA）纳米球（NS）。在这项研究中，我们筛选了一种合适的表面修饰剂来提高 NS 的细胞摄取率。与未修饰的 NS 相比，聚-L-赖氨酸（PLL）修饰的 PLGA NS 的摄取量明显更高（17 倍）。为了提供新的功能，使用阳离子聚合物 PLL 和非离子表面活性剂聚山梨酯 80 对 PLGA NS 进行混合修饰，以改善含血清培养基（SCM）中的细胞摄取。与 PLL-PLGA NS 相比，混合修饰使 NS 在血清中的分散性更好，从而消除了其在 SCM 中摄取率降低的问题，因为 PLL-PLGA NS 在 SCM 中会聚集。在 SCM 中，A549 细胞中 Hybrid-NS/pCMV-Luc 复合物的荧光素酶活性比 PLL-NS 高 122 倍。混合 PLGA NS 对 A549 细胞没有细胞毒性。总之，混合 PLGA NS 具有作为有效的细胞药物传递载体的巨大潜力。
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