Sanzhakov M A, Ignatov D V, Kostryukova L V, Druzhilovskaya O S, Medvedeva N V, Prozorovskyi V N, Ipatova O M
Institute of Biomedical Chemistry, Moscow, Russia.
Biomed Khim. 2016 Mar-Apr;62(2):150-3. doi: 10.18097/PBMC20166202150.
The use of targeted transport systems for drug delivery is a promising approach to improve pharmacokinetics of drug substances, accumulation in the lesion. In this study we have obtained and characterized the pharmaceutical composition of doxorubicin in colloidal nanoparticles equipped with targeted conjugates based on folic acid and biotin with dodecylamine. The inclusion of the address fragments into colloidal nanopartical was carried out without surface and drug substance modification The accumulation of anthracycline antibiotic doxorubicin in tumor tissue was compared in Lewis lung carcinoma mouse models after intravenous administration of the composition of colloidal nanoparticles with targeted conjugates biotin-dodecylamine and folic acid-dodecylamine or free doxorubicin. It was shown that the doxorubicin accumulation in tumor tissue when administered in drug compositions with targeted fragments are 2 times higher for the folic acid-dodecylamine conjugate and 1.4 times higher for the biotin-dodecylamine conjugate.
使用靶向转运系统进行药物递送是一种改善药物物质药代动力学、提高病变部位药物蓄积的有前景的方法。在本研究中，我们制备并表征了阿霉素在配备基于叶酸和生物素与十二胺的靶向缀合物的胶体纳米颗粒中的药物组合物。将靶向片段纳入胶体纳米颗粒的过程未对表面和药物物质进行修饰。在Lewis肺癌小鼠模型中，静脉注射含有生物素 - 十二胺和叶酸 - 十二胺靶向缀合物的胶体纳米颗粒组合物或游离阿霉素后，比较了蒽环类抗生素阿霉素在肿瘤组织中的蓄积情况。结果表明，当与靶向片段一起制成药物组合物给药时，阿霉素在肿瘤组织中的蓄积量，对于叶酸 - 十二胺缀合物而言高出2倍，对于生物素 - 十二胺缀合物而言高出1.4倍。
