Bravo-Osuna I, Ponchel G, Vauthier C
CNRS, UMR CNRS 8612, Faculté de Pharmacie, 5 Rue J.B. Clément, 92296 Chatenay-Malabry, France.
Eur J Pharm Sci. 2007 Feb;30(2):143-54. doi: 10.1016/j.ejps.2006.10.007. Epub 2006 Nov 7.
The aim of the work was to develop a new family of chitosan-coated acrylic nanoparticles to increase the specificity of absorption of drugs associated given by the mucosal route. To achieve this goal, techniques of radical and anionic emulsion polymerisation of isobutylcyanoacrylate (IBCA) were used. Changes in the shell composition were made by using chitosan of different molecular weight and thiolated chitosan to modify the particle surface properties in order to vary the mucosae-nanoparticle interactions. The core was also modified by the inclusion of methyl methacrylate (MMA) as second monomer potentially able to improve the control of drug release. Finally, the labelling of nanoparticles core with a fluorophore, methacryloxyethyl thiocarbamoyl rhodamine B (Polyfluor), was successfully achieved, necessary for the in vitro and in vivo evaluation of the systems created. Results showed that nanoparticle size varied from 200 to 500 nm, depending on the molecular weight of chitosan used. Positive surface charge values were obtained in all cases. In addition, evidences of the presence of thiol groups were obtained (0.03-0.16 x 10(-3)micromol/cm(2) of nanoparticle).
这项工作的目的是开发一种新型的壳聚糖包衣丙烯酸纳米颗粒，以提高经粘膜途径给药相关药物的吸收特异性。为实现这一目标，采用了异丁基氰基丙烯酸酯（IBCA）的自由基和阴离子乳液聚合技术。通过使用不同分子量的壳聚糖和硫醇化壳聚糖来改变壳层组成，以修饰颗粒表面性质，从而改变粘膜与纳米颗粒之间的相互作用。还通过加入甲基丙烯酸甲酯（MMA）作为第二种单体来修饰核心，该单体可能有助于改善药物释放的控制。最后，成功实现了用荧光团甲基丙烯酰氧基乙基硫代氨基甲酰罗丹明B（Polyfluor）对纳米颗粒核心进行标记，这对于所制备系统的体外和体内评估是必要的。结果表明，纳米颗粒的尺寸在200至500纳米之间变化，这取决于所用壳聚糖的分子量。在所有情况下均获得了正表面电荷值。此外，还获得了存在硫醇基团的证据（纳米颗粒为0.03 - 0.1⑥× 10(-3)微摩尔/平方厘米）。
