Intranasal administration of melatonin starch microspheres.
Using melatonin as model drug, starch microspheres for intranasal administration were prepared by an emulsification-crosslinking technique using a uniform design to optimize preparation conditions. The entrapment ratio of melatonin in the microspheres was 11.0% and particle sizes ranged from 30 to 60 microm. Melatonin was released from the microspheres in a sustained manner in vitro. Nasal clearance of 99mTC labeled starch microspheres was investigated using gamma scintigraphy. It was revealed that >80% of the starch microspheres could be detected in the nasal tissue 2h after administration, compared to 30% for a solution. The pharmacokinetics of melatonin starch microspheres was investigated after intranasal administration. The absorption rate was rapid (T(max) min), and the absolute bioavailability was high, 84.07%. A good correlation was found between in vitro release and in vivo absorption data.
Mao
Shirui
S
College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China. mao@staff.uni-marburg.de
Chen
Jianming
J
Wei
Zhenping
Z
Liu
Huan
H
Bi
Dianzhou
D
D000281:Administration, Intranasal; D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004655:Emulsions; D007275:Injections, Intravenous; D008297:Male; D008550:Melatonin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008863:Microspheres; D009297:Nasal Mucosa / Q000378:metabolism; D010316:Particle Size; D011817:Rabbits; D013213:Starch; D013997:Time Factors
D003692:Delayed-Action Preparations; D004655:Emulsions; D013213:Starch; D008550:Melatonin