Andrieu V, Fessi H, Dubrasquet M, Devissaguet J P, Puisieux F, Benita S
Laboratoire de Pharmacie Galenique et Biopharmacie, UA CNRS 1218, Universite Paris XI, Chatenay-Malabry, France.
Drug Des Deliv. 1989 Jun;4(4):295-302.
Indomethacin-loaded polyisobutylcyanoacrylate nanocapsules were prepared by interfacial polymerization of the alkylcyanoacrylate monomer. Mean particle size of the nanocapsules ranged from 200 to 300 nm. Comparison of the results following intravenous infusion of indomethacin solution and nanocapsules to rats revealed that nanoencapsulation accelerated the extravascular distribution of indomethacin due partly to enhanced uptake of the colloidal carrier by the liver reticuloendothelial system. Following intragastric administration, the oral bioavailability of indomethacin in solution was 90%--indicating complete absorption of this drug from the gastrointestinal tract of the rat. Absorption of indomethacin nanocapsules by this route was more rapid. This was attributed either to an increase in the intensity and/or the duration of contact of the encapsulated drug with the gut wall, or to a more efficient absorption process involving paracellular pathways.
通过烷基氰基丙烯酸酯单体的界面聚合制备了载有吲哚美辛的聚异丁基氰基丙烯酸酯纳米胶囊。纳米胶囊的平均粒径在200至300纳米之间。将吲哚美辛溶液和纳米胶囊静脉输注给大鼠后的结果比较表明，纳米包封加速了吲哚美辛的血管外分布，部分原因是肝脏网状内皮系统对胶体载体的摄取增加。胃内给药后，吲哚美辛溶液在大鼠体内的口服生物利用度为90%，表明该药物从大鼠胃肠道完全吸收。通过该途径吸收吲哚美辛纳米胶囊更快。这归因于包封药物与肠壁接触强度和/或持续时间的增加，或者归因于涉及细胞旁途径的更有效的吸收过程。
