Transdermal delivery of tadalafil using a novel formulation.
The aim of this work was to investigate the transdermal gel loaded with tadalafil, a practically insoluble selective phosphodiesterase-5 inhibitor (PDE5) in order to improve the solubility and bioavailability. The solubility of tadalafil in mixed solution of hydroxypropyl-β-cyclodextrin (HPCD), polyethylene glycol (PEG) 400 and tween 80 (T2 solution) was 260.8 ± 4.3 µg/mL and that of tadalafil in modified T2 (M-T2) solution, which tadalafil was dissolved in 20% (w/v) HPCD at first and then mixture solutions of PEG 400 and tween 80 were added, was increased to 344.9 ± 30.6 µg/mL. Four gel formulae were prepared, subsequently in vitro and in vivo skin permeation studies were carried out. Interestingly, tadalafil gel in M-T2 and oleic acid (OA) (F3) could promote the percutaneous absorption of tadalafil by 179.4% in vitro and increase AUC by 223% in vivo compared with tadalafil gel in the absence of M-T2 and OA (F1). Also, there was a finding that tadalafil gel in M-T2 and OA did not cause dermal irritations in an experimental animal.
a College of Pharmacy and Institute of Drug Research and Development, Chungnam National University , Daejeon , South Korea.
Jong-Suep
JS
Baek
a College of Pharmacy and Institute of Drug Research and Development, Chungnam National University , Daejeon , South Korea.
Cheong-Weon
CW
Cho
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000279:Administration, Cutaneous; D000818:Animals; D001682:Biological Availability; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry*; D011136:Polysorbates / Q000008:administration & dosage* / Q000737:chemistry; D012867:Skin / Q000737:chemistry / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D000068581:Tadalafil / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D047392:beta-Cyclodextrins / Q000737:chemistry*
D011136:Polysorbates; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D011092:Polyethylene Glycols; D000068581:Tadalafil
Hydroxypropyl-β-cyclodextrin; pharmacokinetic; solubility; tadalafil; transdermal drug delivery