Lecithinization of IL-6 enhances its thrombopoietic activity in mice.
This study was conducted to assess the merit of lecithinization of recombinant human interleukin-6 (IL-6) as a drug delivery system. IL-6 was lecithinized by covalently binding it with a phosphatidylcholine (lecithin, PC) derivative. The in-vivo thrombopoietic potency of lecithinized IL-6 (PC-IL-6) was greater than that of native IL-6 when administered subcutaneously, although the in-vitro bioactivity of PC-IL-6 was markedly reduced by lecithinization. When PC-IL-6 and native IL-6 were given in doses that produced the same level of thrombopoietic activity, the former stimulated less production of IgG1, a marker of the adverse effects of IL-6, than did the latter. Furthermore, PC-IL-6 persisted in the blood longer than native IL-6. Based on the above, PC-IL-6 appears to be useful as a drug delivery system and may also be useful in the treatment of drug-induced thrombocytopenia.
Igarashi
R
R
Division of Drug Delivery Systems, St. Marianna University, Kawasaki, Japan.
Tsutsumi
Y
Y
Fujii
H
H
Tsunoda
S
S
Ochiai
A
A
Takenaga
M
M
Morizawa
Y
Y
Mayumi
T
T
Mizushima
Y
Y
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects* / Q000502:physiology; D016503:Drug Delivery Systems; D006207:Half-Life; D006410:Hematopoiesis / Q000187:drug effects*; D006801:Humans; D007074:Immunoglobulin G / Q000097:blood; D015850:Interleukin-6 / Q000008:administration & dosage*; D008297:Male; D051379:Mice; D008809:Mice, Inbred C3H; D010713:Phosphatidylcholines / Q000008:administration & dosage*; D011994:Recombinant Proteins / Q000008:administration & dosage
D007074:Immunoglobulin G; D015850:Interleukin-6; D010713:Phosphatidylcholines; D011994:Recombinant Proteins