Effect of different polymers on avanafil–β-cyclodextrin inclusion complex: in vitro and in vivo evaluation

[Display omitted] In this study, we examined the effect of different polymers on the chemical, physical and pharmacokinetic properties of avanafil–β-cyclodextrin (β-CD) inclusion complex. Equimolar mixtures of drug and β-CD were used to prepare 25 ternary drug–β-CD-polymer inclusion complexes using...

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Bibliographic Details
Published in:International journal of pharmaceutics 2016-10, Vol.512 (1), p.168-177
Main Authors: Soliman, Kareem AbuBakr, Ibrahim, Howida Kamal, Ghorab, Mahmoud Mohammed
Format: Article
Language:English
Subjects:
Animals
beta-Cyclodextrins - chemistry
Bioavailability
Biological Availability
Crystallinity
Drug Liberation
Drug Stability
Polyethylene glycol
Polymers - chemistry
Polyvinyl pyrrolidone
Pyrimidines - chemistry
Pyrimidines - pharmacokinetics
Rabbits
Solubility
Stability
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Summary:[Display omitted] In this study, we examined the effect of different polymers on the chemical, physical and pharmacokinetic properties of avanafil–β-cyclodextrin (β-CD) inclusion complex. Equimolar mixtures of drug and β-CD were used to prepare 25 ternary drug–β-CD-polymer inclusion complexes using five different polymers, polyethylene glycol (PEG 4000), polyvinyl pyrrolidone (PVP K-30), chitosan, hydroxypropylmethyl cellulose, and hydroxyethyl cellulose, each in five different concentrations, 1, 3, 5, 7, and 10% (w/w). The addition of 10% (w/w) PEG 4000 resulted in a significant decrease of drug solubility, where the infrared spectra and differential scanning thermograms revealed an interaction between PEG 4000 and avanafil which hindered drug inclusion. In contrast, addition of 7% (w/w) PVP K-30 facilitated drug inclusion as concluded from differential scanning thermograms, X-ray diffraction patterns and scanning electron micrographs. This resulted in a subsequent improvement in drug solubility and in vitro dissolution. This ‎formula was chemically and physically stable for 6 ‎months under accelerated storage conditions. The formula had a relative bioavailability of 125.56% in rabbits as compared to conventional commercially available avanafil‎ tablets (Spedra®).
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2016.08.044