title: Effect of different polymers on avanafil-β-cyclodextrin inclusion complex: in vitro and in vivo evaluation.
abstract: 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(®)).
authors: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt. Electronic address: karim.mohamed@pharma.cu.edu.eg.
authors: Kareem AbuBakr
authors: KA
authors: Soliman
authors: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors: Howida Kamal
authors: HK
authors: Ibrahim
authors: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors: Mahmoud Mohammed
authors: MM
authors: Ghorab
mesh_terms: D000818:Animals; D001682:Biological Availability; D065546:Drug Liberation; D004355:Drug Stability; D011108:Polymers / Q000737:chemistry*; D011743:Pyrimidines / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D011108:Polymers; D011743:Pyrimidines; D047392:beta-Cyclodextrins; C553414:avanafil
keywords: Bioavailability; Crystallinity; Polyethylene glycol; Polyvinyl pyrrolidone; Stability