Production and characterization of testosterone undecanoate-loaded NLC for oral bioavailability enhancement.
OBJECTIVE
Nanostructured lipid carriers were loaded with testosterone undecanoate (TU), which has a low oral bioavailability.


METHODS
Different NLC dispersions were produced using the hot high pressure homogenization method. Particles were characterized using dynamic and static light scattering techniques, differential scanning calorimetry and X-ray diffraction. And the bioavailability was compared to a marketed product.


RESULTS
Nanostructured lipid carriers with up to 30% TU load and sizes of about 600 and 200 nm could be achieved, allowing a direct comparison of the size effect in in vivo bioavailability studies. The zeta potentials varied between - 20 and - 40 mV. The bioavailability of Andriol Testocaps® in the fed state was matched.


CONCLUSIONS
This opens the perspective of administering a single dose of dose of TU in one oral dosage unit and simultaneously having a bioavailability less dependent on the fed state.
Department of Pharmaceutics, Biopharmaceutics and NutriCosmetics, Freie Universität Berlin, Berlin, Germany.
M
M
Muchow
P
P
Maincent
R H
RH
Müller
C M
CM
Keck
D000284:Administration, Oral; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D004355:Drug Stability; D008055:Lipids / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D013739:Testosterone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D014961:X-Ray Diffraction / Q000379:methods
D004337:Drug Carriers; D008055:Lipids; D013739:Testosterone; C010792:testosterone undecanoate