[Study on mitoxantrone albumin microspheres for liver targeting].
An optimum procedure was established for preparing mitoxantrone albumin microspheres (DHAQ-BSA-MS) with emulsion-heating solidification. The morphology, diameters, drug loading, release characteristics, stability and its distribution in vivo of the drug-loaded albumin microspheres were studied. The results showed that the surface was regular, the average diameter was 0.99 micron, mean surface diameter was 1.24 microns and mean volume diameter was 1.44 microns, apparent drug loading was 2.558 +/- 0.101 micrograms.mg-1 (n = 5), effective drug loading was 1.503% +/- 0.127% (n = 5), embedding ratio was 92.82% +/- 6.48% (n = 5), and the release characteristics were in accord with "biphase kinetics equation": 1 - Q = 0.6428e-0.2132t + 0.3988e-0.00150t (gamma 1 = -0.9951, gamma 2 = -0.9982); T1/2 alpha = 3.250 h, T1/2 beta = 461.7 h. The stability of the drug-loaded albumin microspheres was good after three months storage at room temperature. The results determined by HPLC showed that the drug accumulated about 77.6% +/- 1.38% of the dose in the liver 20 minutes after intravenous injection to mice. This indicates that DHAQ-BSA-MS showed remarkable targeting for liver, and it seems to have important value for increasing the antihepatoma effect and decreasing the toxicity of mitoxantrone.
Zhang
Z R
ZR
School of Pharmacy, West China University of Medical Sciences, Chengdu 610041.
Qian
W J
WJ
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D016503:Drug Delivery Systems; D005260:Female; D008297:Male; D051379:Mice; D008863:Microspheres; D008942:Mitoxantrone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011897:Random Allocation; D013678:Technology, Pharmaceutical / Q000379:methods
D000970:Antineoplastic Agents; D008942:Mitoxantrone