Kim M-S
Department of Pharmaceutical Engineering, Inje University, Gimhae, Korea.
Drug Res (Stuttg). 2013 Jun;63(6):326-30. doi: 10.1055/s-0033-1341425. Epub 2013 Mar 22.
The present study sought to evaluate the pharmacokinetics of dutasteride-loaded Eudragit E nanoparticle in rats. In addition, the study investigated the effect of increasing drug load on the in vitro solubility and dissolution behavior of dutasteride together with its in vivo oral absorption characteristics. The suspension of dutasteride-loaded Eudragit E nanoparticles prepared by the nanoprecipitation method showed blue opalescence and the particles were uniform in appearance. The entrapment efficiency and the mean particle size of these nanoparticles were in the range of 98.1-99.3% and 120.5-128.4 nm, respectively, and no significant difference in these parameters was observed between the nanoparticles in the sample. Eudragit E nanoparticles containing a drug load of 5% showed an increase in bioavailability by 550% as compared to dutasteride suspension. This finding is attributable to enhanced solubility and dissolution of dutasteride when formulated as nanoparticles. Furthermore, the oral absorption of dutasteride in rats increased as a function of the extent of supersaturation of dutasteride in Eudragit E nanoparticles. Therefore, the preliminary results from our study suggest that dutasteride-loaded Eudragit E nanoparticles may have significant potential for clinical application.
本研究旨在评估载有度他雄胺的Eudragit E纳米颗粒在大鼠体内的药代动力学。此外，该研究还考察了增加药物载量对度他雄胺体外溶解度和溶出行为及其体内口服吸收特性的影响。通过纳米沉淀法制备的载有度他雄胺的Eudragit E纳米颗粒混悬液呈现蓝色乳光，颗粒外观均匀。这些纳米颗粒的包封率和平均粒径分别在98.1 - 99.3%和120.5 - 128.4 nm范围内，样品中的纳米颗粒在这些参数上未观察到显著差异。与度他雄胺混悬液相比，载药量为5%的Eudragit E纳米颗粒的生物利用度提高了550%。这一发现归因于度他雄胺制成纳米颗粒后溶解度和溶出度的提高。此外，大鼠体内度他雄胺的口服吸收随着其在Eudragit E纳米颗粒中的过饱和程度而增加。因此，我们研究的初步结果表明，载有度他雄胺的Eudragit E纳米颗粒可能具有显著的临床应用潜力。
