Increased bioavailability of a transdermal application of a nano-sized emulsion preparation.
The aim of this study was to compare the transdermal application of a nano-sized emulsion versus a micron-sized emulsion preparation of delta tocopherol as it relates to particle size and bioavailability. Two separate experiments were performed using seven F1B Syrian Golden hamsters, 1 week apart. Each emulsion preparation consisted of canola oil, polysorbate 80, deionized water and delta tocopherol; the only difference between the two preparations was processing the nano-sized emulsion with the Microfluidizer Processor. Both were formulated into a cream and applied to the shaven dorsal area. The particle size of the micron-sized emulsion preparation was 2788 nm compared to 65 nm for the nano-sized emulsion formulation. Two hours post-application, hamsters that were applied the nano-sized emulsion had a 36-fold significant increase of plasma delta tocopherol, where as hamsters that were applied the micron-sized emulsion only had a 9-fold significant increase, compared to baseline, respectively. At 3h post-application, plasma delta tocopherol had significantly increased 68-fold for hamsters applied the nano-sized emulsion, whereas only an 11-fold significant increase was observed in hamsters applied the micron-sized emulsion, compared to baseline, respectively. Significant differences were also observed between the nano-sized and micron-sized emulsion at 2 and 3h post-application. This study suggests that nano-sized emulsions significantly increase the bioavailability of transdermally applied delta tocopherol.
Kotyla
T
T
Department of Clinical Laboratory and Nutritional Sciences, Center for Health and Disease Research, University of Massachusetts Lowell, Lowell, MA 01854, USA.
Kuo
F
F
Moolchandani
V
V
Wilson
T
T
Nicolosi
R
R
D000279:Administration, Cutaneous; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D006224:Cricetinae; D004655:Emulsions; D005079:Excipients / Q000737:chemistry; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry; D008027:Light; D008297:Male; D036103:Nanotechnology / Q000379:methods*; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D000074262:Rapeseed Oil; D012542:Scattering, Radiation; D024505:Tocopherols / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D014783:Viscosity
D000975:Antioxidants; D004655:Emulsions; D005079:Excipients; D005229:Fatty Acids, Monounsaturated; D011136:Polysorbates; D000074262:Rapeseed Oil; C479072:delta-tocopherol; D024505:Tocopherols