Iontophoretic delivery of lipophilic and hydrophilic drugs from lipid nanoparticles across human skin.
The combined effects of iontophoresis and lipid nanoparticles on drug delivery across human epidermal membrane (HEM) were investigated. The delivery of lipophilic and hydrophilic drugs, all trans-retinoic acid (ATRA), salicylate (SA), and acyclovir (ACV), across HEM from lipid nanoparticles, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), was compared in passive and iontophoresis experiments in vitro. Iontophoresis experiments were also performed with synthetic Nuclepore membrane for comparison. Drug distribution in the skin after iontophoretic delivery with the lipid nanoparticles was examined using a model probe rhodamine B base (RhoB). The drug-loaded lipid nanoparticles had average sizes of ∼ 118-169 nm and a negative zeta potential. Iontophoresis did not enhance the delivery of ATRA across HEM from SLN and NLC. However, HEM distribution study of RhoB suggested that lipophilic drugs could be delivered into the deeper layer of the skin following iontophoretic delivery of the drugs from the lipid nanoparticles. Iontophoresis enhanced the delivery of hydrophilic drug SA with the lipid nanoparticles. Similarly, iontophoresis enhanced the delivery of ACV when it was loaded in SLN. These results suggest that lipid nanoparticles are a promising drug delivery method that can be combined with iontophoresis to improve skin delivery of hydrophilic drugs.
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.
Ponwanit
P
Charoenputtakun
Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, Ohio 45267-0004, USA. Electronic address: kevin.li@uc.edu.
S Kevin
SK
Li
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.
Tanansait
T
Ngawhirunpat
D000212:Acyclovir / Q000008:administration & dosage / Q000493:pharmacokinetics; D000279:Administration, Cutaneous; D016503:Drug Delivery Systems / Q000379:methods*; D004817:Epidermis / Q000378:metabolism; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007478:Iontophoresis / Q000379:methods*; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012459:Salicylates / Q000008:administration & dosage / Q000493:pharmacokinetics; D012869:Skin Absorption / Q000502:physiology; D014212:Tretinoin / Q000008:administration & dosage / Q000493:pharmacokinetics
D008055:Lipids; D012459:Salicylates; D014212:Tretinoin; D000212:Acyclovir
Diffusion; Iontophoresis; Lipid nanoparticles; Nanostructured lipid carriers; Solid lipid nanoparticles; Transdermal delivery