CIRIMAT Carnot Institute, University of Toulouse, CNRS/INPT/UPS, ENSIACET, 118 route de Narbonne, 31077 Toulouse, France.
Langmuir. 2009 Oct 20;25(20):12256-65. doi: 10.1021/la901671j.
Intracellular drug delivery using colloidal biomimetic calcium phosphate apatites as nanocarriers is a seducing concept. However, the colloid preparation to an industrial scale requires the use of easily handled raw materials as well as the possibility to tailor the nanoparticles size. In this work, the stabilization of the colloids was investigated with various biocompatible agents. Most interestingly, nanoscale colloids were obtained without the need for toxic and/or hazardous raw materials. Physico-chemical characteristics were investigated by chemical analyses, dynamic light scattering, FTIR/Raman spectroscopies, XRD, and electron microscopy. A particularly promising colloidal system associates biomimetic apatite stabilized with a natural phospholipid moiety (AEP(r), 2-aminoethylphosphoric acid). Complementary data described such colloids as apatite nanocrystals covered with surface Ca(2+)(AEP(r)(-))(2) complexes involving "supernumerary" Ca(2+) ions. The effects of the concentration in AEPr, synthesis temperature, duration of aging in solution, pH, and sonication were followed, showing that it is possible to modulate the mean size of the nanoparticles, typically in the range 30-100 nm. The perfect biocompatibility of such colloids allied to the possibility to prepare them from innocuous compounds shows great promise for intracellular drug delivery.
使用胶体仿生磷酸钙磷灰石作为纳米载体进行细胞内药物输送是一个诱人的概念。然而，将胶体制备到工业规模需要使用易于处理的原材料以及能够定制纳米颗粒尺寸的可能性。在这项工作中，用各种生物相容性试剂研究了胶体的稳定性。最有趣的是，无需使用有毒和/或危险的原材料即可获得纳米级胶体。通过化学分析、动态光散射、FTIR/Raman 光谱、XRD 和电子显微镜研究了物理化学特性。一种特别有前途的胶体系统是由仿生磷灰石与天然磷脂部分（AEP(r)，2-氨基乙基磷酸）稳定的胶体。补充数据将这种胶体描述为纳米晶磷灰石，表面覆盖有 Ca(2+)(AEP(r)(-))(2) 配合物，其中涉及“多余”的 Ca(2+) 离子。研究了 AEPr 的浓度、合成温度、溶液中老化时间、pH 值和超声处理的影响，结果表明可以调节纳米颗粒的平均尺寸，通常在 30-100nm 范围内。这种胶体的完美生物相容性以及能够用无害化合物制备它们的可能性为细胞内药物输送展示了巨大的前景。
