Guo Huiling,Du Gaiping,Hu Lianna,Wang Dajiang,Wang Liqiang,Huang Yifei.Distribution of a novel immunosuppressant J2 nano-suspension in peripheral blood and eyes in rabbits after subconjunctival injection[J].J Amry Med Univ (J Third Mil Med Univ),2013,35(12):1225-1228.
Guo Huiling,Du Gaiping,Hu Lianna,Wang Dajiang,Wang Liqiang,Huang Yifei.Distribution of a novel immunosuppressant J2 nano-suspension in peripheral blood and eyes in rabbits after subconjunctival injection[J].J Amry Med Univ (J Third Mil Med Univ),2013,35(12):1225-1228.DOI:
Distribution of a novel immunosuppressant J2 nano-suspension in peripheral blood and eyes in rabbits after subconjunctival injection
Objective To investigate the distribution of a novel immunosuppressant
J2 nano-suspension (NS)
in the peripheral blood and intraocular tissues in rabbits after subconjunctival injection. Methods Totally 18 healthy New Zealand white rabbits (36 eyes)
8- to 12-week-old
were given an subconjunctival injection of 0.2 ml 1% J2-NS. Drug concentration in the cornea
aqueous humor
and iris (6 eyes in each time point) and peripheral blood was detected by high-performance liquid chromatography (HPLC) on the days 1 and 3
and the
weeks of 1
2
3 and 4 respectively after injection. The main pharmacokinetic parameters were calculated by pharmacokinetic software
WinNonlin. Results J2-NS at different concentrations was found in all detected organs during the observation period after injection. The serum concentration of J2-NS was 11.19±0.33 to 13.23±0.84 ng/mL from the day 1 to week 4 after injection. The cornea had the highest dose in all the eye tissues
but it was at lower dose in the aqueous humor and iris. The concentration was 5.72±1.67 to 11.86±4.35 ng/mg in the cornea from the day 1 to week 4 after injection
with Cmax of 11.861 3 ng/mg
Tmax of 1 d
and area under curve (AUC) of 201.561 5 ng/(mg·d)and T
1/2
of 45 d. Conclusion Single subconjunctival injection of J2-NS leads the drug mainly being distributed in the peripheral blood and cornea
and being maintained at the effective drug concentration for a long time.