title: Formulation of avanafil in a solid self-nanoemulsifying drug delivery system for enhanced oral delivery.
abstract: Avanafil was incorporated into solid self-nanoemulsifying systems with the aim of improving its oral bioavailability. Labrafil, Labrafac, and Miglyol 812 N were investigated as oils, Tween 80 and Cremophor EL as surfactants, and Transcutol HP as a co-surfactant. Nine formulations produced clear solutions of 13.89-38.09nm globules after aqueous dilution. Adsorption of preconcentrate onto Aeroperl 300 Pharma at a 2:1 ratio had no effect on nanoemulsion particle size. Differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy indicated that avanafil was molecularly dispersed within the solid nanosystems. A formulation containing 10% Labrafil, 60% Tween 80, and 30% Transcutol HP had the highest drug loading (44.48mg/g) and an acceptable in vitro dissolution profile (96.42% within 30min). This formulation was chemically and physically stable for 6months under accelerated storage conditions and it produced a 3.2-fold increase in bioavailability 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. Electronic address: howida.ibrahim@pharma.cu.edu.eg.
authors: Howida Kamal
authors: HK
authors: Ibrahim
authors: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt. Electronic address: mah.mohamed@cu.edu.eg.
authors: Mahmoud Mohammed
authors: MM
authors: Ghorab
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004655:Emulsions; D008055:Lipids / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000648:ultrastructure; D010316:Particle Size; D058986:Phosphodiesterase 5 Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D033362:Powder Diffraction; D011743:Pyrimidines / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D004655:Emulsions; D008055:Lipids; D058986:Phosphodiesterase 5 Inhibitors; D011743:Pyrimidines; D013501:Surface-Active Agents; C553414:avanafil
keywords: Aeroperl; Amorphous; Bioavailability; Dissolution; Nanoemulsion; Stability