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In vivo evaluation of alginate microspheres of carvedilol for nasal delivery.
- Source :
-
Journal of biomedical materials research. Part B, Applied biomaterials [J Biomed Mater Res B Appl Biomater] 2012 Jan; Vol. 100 (1), pp. 249-55. Date of Electronic Publication: 2011 Nov 24. - Publication Year :
- 2012
-
Abstract
- Mucoadhesive alginate microspheres of carvedilol (CRV) for nasal administration intended to avoid first pass metabolism and to improve bioavailability were prepared and evaluated. The microspheres were prepared by emulsification cross-linking method. Radiolabeling of CRV and its microspheres was performed by direct labeling with reduced technetium-99m ((99m) Tc). In vivo studies were performed on New Zealand white rabbits by administering the microspheres intranasally using monodose nasal insufflator. The radioactivity was measured in a well-type gamma scintillation counter. The noncompartmental pharmacokinetic analysis was performed. The pattern of deposition and clearance of the microspheres were evaluated using a radioactive tracer and the noninvasive technique of gamma scintigraphy. The clearance of alginate microsphere was compared with that of control lactose. The microspheres were nonaggregated, free flowing powders with spherical shape, and smooth surface. Pharmacokinetics study displayed an increase in area under the curve and hence in relative bioavailability when compared with intravenous administration of drug. The nasal bioavailability was 67.87% which indicates that nasal administration results in improved absorption of CRV. The results of gamma scintigraphy showed that the alginate microspheres had significantly reduced rates of clearance from the rabbit nasal cavity when compared with the control lactose.<br /> (Copyright © 2011 Wiley Periodicals, Inc.)
- Subjects :
- Administration, Intranasal
Adrenergic alpha-1 Receptor Antagonists pharmacology
Alginates pharmacology
Animals
Biological Availability
Carbazoles pharmacology
Carvedilol
Drug Carriers
Drug Evaluation, Preclinical
Glucuronic Acid pharmacokinetics
Glucuronic Acid pharmacology
Hexuronic Acids pharmacokinetics
Hexuronic Acids pharmacology
Isotope Labeling
Lactose pharmacokinetics
Lactose pharmacology
Nasal Cavity diagnostic imaging
Nasal Cavity metabolism
Propanolamines pharmacology
Rabbits
Radionuclide Imaging
Sheep
Technetium pharmacokinetics
Technetium pharmacology
Adrenergic alpha-1 Receptor Antagonists pharmacokinetics
Alginates pharmacokinetics
Carbazoles pharmacokinetics
Microspheres
Propanolamines pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1552-4981
- Volume :
- 100
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of biomedical materials research. Part B, Applied biomaterials
- Publication Type :
- Academic Journal
- Accession number :
- 22113887
- Full Text :
- https://doi.org/10.1002/jbm.b.31947