[Studies on preparation of recombinant hirudin-2 liposome and its pharmacokinetics by nasal delivery in rats].
OBJECTIVE
To promote the nasal absorption of recombinant hirudin-2, the preparation and physicochemical properties of recombinant hirudin-2 liposomes, as well as its pharmacokinetic characteristics and bioavailability in rats after nasal administration were investigated.


METHODS
Recombinant hirudin-2 liposomes were prepared by reversal phase evaporation; the test of physicochemical properties including encapsulation efficiency, particle size and stability of liposome suspensions were determined by HPLC; Recombinant hirudin-2 concentration in plasma was determined by chromogenic substrate method and the relative bioavailability and pharmacokinetic parameters were also calculated using software program 3p87.


RESULTS
The encapsulation efficiency of recombinant hirudin-2 liposome reached greater than 76.95%, with an average particle size of about 168.3 nm, size distribution ranging from 24 to 286 nm, relative peak width of +/- 0.47, and a good stability.


CONCLUSIONS
Compared with recombinant hirudin-2 solution, liposome preparation enhanced the nasal absorption of recombinant hirudin-2.
Zhang
Yu-Jie
YJ
School of Chinese Medicines, Beijing University of Traditional Chinese Medicine, Beijing 100102, China. zhyj227@126.com
Wang
Xiao-Liang
XL
Wu
Jian-Mei
JM
Cheng
Ming-Xia
MX
D000281:Administration, Intranasal; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D004337:Drug Carriers; D004355:Drug Stability; D006629:Hirudins / Q000008:administration & dosage* / Q000235:genetics / Q000493:pharmacokinetics*; D008081:Liposomes; D008297:Male; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D013678:Technology, Pharmaceutical / Q000379:methods*
D004337:Drug Carriers; D006629:Hirudins; D008081:Liposomes; D011994:Recombinant Proteins; C072299:hirudin HV2