Rajaonarivony M, Vauthier C, Couarraze G, Puisieux F, Couvreur P
Laboratorie de Physio-chimie, Biopharmacie, Pharmacotechnie, URA CNRS 1218, Université de Paris XI, Faculté de Pharmacie, Chatenay-Malabry, France.
J Pharm Sci. 1993 Sep;82(9):912-7. doi: 10.1002/jps.2600820909.
A new approach for the preparation of nanoparticles is presented. The method is based on control of the gelification phenomenon of alginate by calcium ions, and it leads to small particles of a wide range of very well-defined sizes (250-850 nm) depending on the alignate concentration. The particles are formed in a sodium alginate solution by addition of calcium chloride and then poly-L-lysine. The concentrations of sodium alginate and of calcium chloride were lower than those required for gel formation and corresponded to the formation of a pregel state. The size of the particles formed is greatly dependent on the order of addition of calcium and poly-L-lysine to the sodium alginate solution. This phenomenon can be attributed to the difference in the nature of the interactions between calcium and alginate and between poly-L-lysine and alginate. Furthermore, the data indicate that the formation of the particles probably occurs during the addition of the first component to the sodium alginate solution. Evaluation of the drug-loading capacity was done with doxorubicin as a drug model. The results indicate that alginate nanoparticles are interesting carriers because the drug-loading capacity could be > 50 mg of doxorubicin per 100 mg of alginate.
本文提出了一种制备纳米颗粒的新方法。该方法基于钙离子对藻酸盐凝胶化现象的控制,根据藻酸盐浓度的不同,可制备出尺寸范围很广(250 - 850纳米)且粒径明确的小颗粒。通过向海藻酸钠溶液中加入氯化钙,然后加入聚-L-赖氨酸来形成颗粒。海藻酸钠和氯化钙的浓度低于凝胶形成所需的浓度,对应于预凝胶状态的形成。所形成颗粒的大小很大程度上取决于向海藻酸钠溶液中添加钙和聚-L-赖氨酸的顺序。这种现象可归因于钙与藻酸盐之间以及聚-L-赖氨酸与藻酸盐之间相互作用性质的差异。此外,数据表明颗粒的形成可能发生在向海藻酸钠溶液中添加第一种成分的过程中。以阿霉素作为药物模型对载药能力进行了评估。结果表明,藻酸盐纳米颗粒是一种有吸引力的载体,因为每100毫克藻酸盐的载药能力可以> 50毫克阿霉素。