[Primary studies on synthesis and properties of mitoxantrone-insulin conjugates].
OBJECTIVE
Mitoxantrone-insulin conjugate was prepared through covalent bond, where mitoxantrone was an anticancer model drug and insulin acted as a vector. Its stability in vitro was discussed.


METHODS
Spacer was used to join insulin and mitoxantrone. The intermediate and the final conjugate were characterized by infra-red spectroscopy (IR), 1H NMR, mass spectrometray (MS) and ultra-violet spectrophotometry (UV). Stability trials of the conjugate were carried out in different pH buffer solutions and mouse plasma at 37 degrees C.


RESULTS
Drug loading of the conjugate was 11.68%. The conjugate was stable in phosphate buffer solution of pH 2-8 and mouse plasma at 37 degrees C.


CONCLUSIONS
Stable mitoxantrone-insulin conjugate was obtained to ensure further tumor targeted study in vivo.
Liu
Wen-sheng
WS
Department of Pharmaceatics, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Zhang
Zhi-rong
ZR
Huang
Yuan
Y
Li
Yan
Y
D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D007328:Insulin / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008942:Mitoxantrone / Q000008:administration & dosage / Q000737:chemistry*; D013055:Spectrophotometry, Infrared
D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D007328:Insulin; D008942:Mitoxantrone