Конструирование стерически стабилизированной липосомальной формы доксорубицина путем модификации поверхности по реакции 1,3-диполярного циклоприсоединения

The first aim of any therapy is the drug delivery to the cellular and intracellular targets with minimal accumulation and effects on the non-specific sites. To achieve this goal different vectors have been used, the most common of which are liposomes. However, liposomes are rapidly captured by the mononuclear phagocyte system and removed from the blood circulation, and do not reach the affected areas. To increase the circulation time as well as other purposes liposomal surface are being modified by the flexible water-soluble polymers such as polyethylene glycol (PEG). Traditional methods of steric stabilization are based on the incorporation of PEG-lipid conjugates in the formation of liposomes. In this paper we investigated the applicability of the 1,3-dipolar cycloaddition reaction in order to modify the liposomal surface with polyethylene glycol monomethyl ether and the effectiveness of the incorporation of doxorubicin into their composition was determined. References Kolb H. C., Sharpless K. B. / Drug Discov. Today. 2003. V. 8. P. 1128–1137. Hassane S. F., Frisch B., Schuber F. / Bioconjugate Chem. 2006. V. 17. P. 849–854. Sebyakin Ju.L., Budanova U.A., Gur'eva L.Ju. / Biologich. membrany.  2007.  V. 24. №3. P. 273–279. Jayakumar R., Murugesan M. Rafiuddin Ahmed M ./ Bioorg. Med. Chem. Lett. 2000. V. 10. P. 1547-1550. Horne W. S., Stout C. D., Ghadiri M. R. / J. Am. Chem. Soc. 2003. V. 125. P. 9372–9376. Normal 0