[Human recombinant interferon-alpha 2a polybutylcyanoacrylate sustained release lyophilized nanospheres for liver-targeting].
OBJECTIVE
To evaluate the liver-targeted and sustained release characteristics of human recombinant interferan-alpha 2a polybutylcyanoacrylate lyophilized nanospheres (rIFN alpha 2a-PBCA-NS).


METHODS
Emulsification/polymerization method was used to prepare the nanospheres which was lyophilized to obtain rIFN alpha 2a-PBCA-NS, and cell pathological embarrassment (CPE) was used to determine the rIFN alpha 2a concentration in the preparations and biological samples. The in vivo distribution and pharmacokinetics in liver after intravenous injection (i.v.) of rIFN alpha 2a-PBCA-NS and rIFN alpha 2a in mice were evaluated.


RESULTS
The rate of entrapment of the nanospheres was (56.2 +/- 4.3)%; the particle diameter, span of rIFN alpha 2a-PBCA-NS were (108 +/- 37) nm and 0.55, respectively, and their biological activity had little change after being stored at 3-5 degrees C for 6 months. The distribution ratio of rIFN alpha 2a after i.v. in mice liver increased from 13.1% (for rIFN alpha 2a) to 50.6% (for rIFN alpha 2a-PBCA-NS), and the mean retain time from 1.41 h (for rIFN alpha 2a) to 8.35 h (for rIFN alpha 2a-PBCA-NS). Of the distribution parameters (te for rIFN alpha 2a, re and te for rIFN alpha 2a-PBCA-NS) in 5 main organs, the largest ones were in liver and both re and te for rIFN alpha 2a-PBCA-NS in liver larger than one.


CONCLUSIONS
The rIFN alpha 2a-PBCA-NS showed obviously liver-targeting and sustained release characteristics.
Department of Pharmaceutical Sciences, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Bin
B
Lu
Jian-fang
JF
Feng
Xiu-cen
XC
Yang
D000818:Animals; D001692:Biological Transport; D003692:Delayed-Action Preparations / Q000138:chemical synthesis; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004655:Emulsions; D004659:Enbucrilate / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008099:Liver / Q000378:metabolism*; D051379:Mice; D008863:Microspheres; D036103:Nanotechnology; D010316:Particle Size; D011108:Polymers; D011897:Random Allocation; D011994:Recombinant Proteins
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D000077190:Interferon alpha-2; D016898:Interferon-alpha; D011108:Polymers; D011994:Recombinant Proteins; D004659:Enbucrilate