Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

The purpose of this research was to prepare acyclovir niosomes in a trial to improve its poor and variable oral bioavailability. The nonionic surfactant vesicles were prepared by the conventional thin film hydration method. The lipid mixture consisted of cholesterol, span 60, and dicetyl phosphate i...

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Bibliographic Details
Published in:AAPS PharmSciTech 2007-10, Vol.8 (4), p.E106-212
Main Authors: Attia, Ismail A, El-Gizawy, Sanaa A, Fouda, Medhat A, Donia, Ahmed M
Format: Article
Language:English
Subjects:
Acyclovir - administration & dosage
Acyclovir - chemistry
Acyclovir - pharmacokinetics
Administration, Oral
Animals
Antiviral Agents - administration & dosage
Antiviral Agents - chemistry
Antiviral Agents - pharmacokinetics
Biological Availability
Chemistry, Pharmaceutical
Cholesterol - chemistry
Delayed-Action Preparations
Drug Compounding
Hexoses - chemistry
Liposomes
Male
Organophosphates - chemistry
Particle Size
Rabbits
Solubility
Technology, Pharmaceutical - methods
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Summary:The purpose of this research was to prepare acyclovir niosomes in a trial to improve its poor and variable oral bioavailability. The nonionic surfactant vesicles were prepared by the conventional thin film hydration method. The lipid mixture consisted of cholesterol, span 60, and dicetyl phosphate in the molar ratio of 65:60:5, respectively. The percentage entrapment was approximately 11% of acyclovir used in the hydration process. The vesicles have an average size of 0.95 microm, a most probable size of 0.8 microm, and a size range of 0.4 to 2.2 microm. Most of the niosomes have unilamellar spherical shape. In vitro drug release profile was found to follow Higuchi's equation for free and niosomal drug. The niosomal formulation exhibited significantly retarded release compared with free drug. The in vivo study revealed that the niosomal dispersion significantly improved the oral bioavailability of acyclovir in rabbits after a single oral dose of 40 mg kg(-1). The average relative bioavailability of the drug from the niosomal dispersion in relation to the free solution was 2.55 indicating more than 2-fold increase in drug bioavailability. The niosomal dispersion showed significant increase in the mean residence time (MRT) of acyclovir reflecting sustained release characteristics. In conclusion, the niosomal formulation could be a promising delivery system for acyclovir with improved oral bioavailability and prolonged drug release profiles.
ISSN:1530-9932
1530-9932
DOI:10.1208/pt0804106