Losa C, Calvo P, Castro E, Vila-Jato J L, Alonso M J
Laboratorio de Farmacia Galénica, Facultad de Farmacia, Santiago de Compostela, España.
J Pharm Pharmacol. 1991 Aug;43(8):548-52. doi: 10.1111/j.2042-7158.1991.tb03534.x.
The main objective of this paper was to investigate the ability of polycyanoacrylate nanoparticles to improve the corneal penetration of hydrophilic drugs. Three different nanoparticle formulations were prepared by changing the nature of the stabilizer agent (Dextran 70000, Synperonic F 68 and sodium lauryl sulphate). The significant influence of the stabilizer type on the particle size, electrophoretic mobility and on the drug loading efficiency was proved. Moreover, the ocular disposition of amikacin was affected by its association to nanoparticles, displaying the most interesting results when Dextran 70000 was employed for preparation of nanoparticles. The increase of the amikacin concentration in cornea and aqueous humour was statistically significant for this nanoparticle formulation with respect to the other formulations and the control solution. The in-vitro release profiles obtained using a dialysis system were similar for all the nanoparticle formulations and for the control solution, indicating that drug molecules are desorbed from the nanoparticles quickly enough to maintain the equilibrium concentration in the dialysis system.
本文的主要目的是研究聚氰基丙烯酸酯纳米颗粒改善亲水性药物角膜渗透的能力。通过改变稳定剂(葡聚糖70000、泊洛沙姆F68和十二烷基硫酸钠)的性质制备了三种不同的纳米颗粒制剂。证明了稳定剂类型对粒径、电泳迁移率和药物负载效率有显著影响。此外,阿米卡星与纳米颗粒的结合影响了其眼部分布,当使用葡聚糖70000制备纳米颗粒时显示出最有趣的结果。相对于其他制剂和对照溶液,这种纳米颗粒制剂在角膜和房水中阿米卡星浓度的增加具有统计学意义。使用透析系统获得的所有纳米颗粒制剂和对照溶液的体外释放曲线相似,表明药物分子从纳米颗粒上快速解吸,以维持透析系统中的平衡浓度。