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 6...

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Bibliographic Details
Published in:International journal of pharmaceutics 2004-03, Vol.272 (1), p.37-43
Main Authors: Mao, Shirui, Chen, Jianming, Wei, Zhenping, Liu, Huan, Bi, Dianzhou
Format: Article
Language:English
Subjects:
Administration, Intranasal
Animals
Biological and medical sciences
Biological Availability
Delayed-Action Preparations
Emulsions
General pharmacology
Injections, Intravenous
Intranasal administration
Male
Medical sciences
Melatonin
Melatonin - administration & dosage
Melatonin - blood
Melatonin - pharmacokinetics
Microspheres
Nose - metabolism
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rabbits
Starch
Starch microspheres
Time Factors
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Summary: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 μm. Melatonin was released from the microspheres in a sustained manner in vitro. Nasal clearance of 99 m Tc labeled starch microspheres was investigated using gamma scintigraphy. It was revealed that >80% of the starch microspheres could be detected in the nasal tissue 2 h 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=7.8 min), and the absolute bioavailability was high, 84.07%. A good correlation was found between in vitro release and in vivo absorption data.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2003.11.028