title: Tadalafil-loaded nanostructured lipid carriers using permeation enhancers.
abstract: Tadalafil is a phosphodiesterase-5 inhibitor indicated for the treatment of erectile dysfunction. In this study, we prepared and evaluated transdermal nanostructured lipid carriers (NLC) to improve the skin permeability of tadalafil. Tadalafil-loaded NLC dispersions were prepared using glyceryl monostearate as a solid lipid, oleic acid as a liquid lipid, and Tween 80 as a surfactant. We characterized the dispersions according to particle size, polydispersity index, zeta potential, encapsulation efficiency, and transmission electron microscopy. In vitro skin permeation studies were carried out using Franz diffusion cells, and cytotoxicity was examined using HaCaT keratinocyte cell lines. Tadalafil skin permeability increased for all tadalafil-loaded NLC formulations. The tadalafil-loaded NLC dispersion with ethanol and limonene as skin permeation enhancers exhibited the highest flux (∼4.8-fold) compared to that observed with tadalafil solution alone. Furthermore, a tadalafil-loaded NLC gel with selected permeation enhancers showed tolerance against toxicity in HaCaT cells. These results suggest that the NLC formulations with ethanol and limonene as skin permeation enhancers could be a promising dermal delivery carrier for tadalafil.
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea.
authors.forename: Jong-Suep
authors.initials: JS
authors.lastname: Baek
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea.
authors.forename: Cuong Viet
authors.initials: CV
authors.lastname: Pham
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea.
authors.forename: Chang-Seon
authors.initials: CS
authors.lastname: Myung
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea. Electronic address: chocw@cnu.ac.kr.
authors.forename: Cheong-Weon
authors.initials: CW
authors.lastname: Cho
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects / Q000378:metabolism; D008055:Lipids / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures; D010316:Particle Size; D058986:Phosphodiesterase 5 Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D000068581:Tadalafil / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D004337:Drug Carriers; D005079:Excipients; D008055:Lipids; D058986:Phosphodiesterase 5 Inhibitors; D000068581:Tadalafil
keywords: Nanostructured lipid carriers; Permeation enhancer; Tadalafil; Transdermal drug delivery