albumin - publications

Predict more albumin - ligand interactions now!

1. Int J Pharm. 2012 Feb 2. [Epub ahead of print]

Preparation, characterization and pharmacokinetic studies of
tacrolimus-dimethyl-β-cyclodextrin inclusion complex-loaded albumin

Gao S, Sun J, Fu D, Zhao H, Lan M, Gao F.

Department of Pharmaceutics, School of Pharmacy, East China University of Science
and Technology, Shanghai 200237, PR China.

The purpose of the study is to develop a new formulation for clinically used
anti-cancer agent tacrolimus (FK506) to minimize the severe side effects. Toward
this end, a new formulation method has been developed by complexation of FK506
with an hydrophilic cyclodextrin derivative, heptakis
(2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD) using ultrasonic means. The resulting
complex displays dramatically enhanced solubility of FK506. Then bovine serum
albumin (BSA) nanoparticles were prepared directly from the preformed
FK506/DM-β-CD inclusion complex by the desolvation-chemical crosslinking method,
with the size of 148.4-262.9nm. Stable colloidal dispersions of the nanoparticles
were formed with zeta potentials of the range of -24.9 to -38.4mV. The entrapment
efficiency of FK506 was increased as high as 1.57-fold. Moreover, notably FK506
was released from the nanoparticles in a sustained manner. As demonstrated,
pharmacokinetic studies reveal that, as compared with FK506-loaded BSA
nanoparticles, the FK506/DM-β-CD inclusion complex-loaded BSA nanoparticles have
significant increase at T(max), t(1/2), MRT and decrease at C(max). In summary,
these results suggest that the drug/DM-β-CD inclusion complex-loaded BSA
nanoparticles display significantly improved delivery efficiency for poorly
soluble FK506 or its derivatives.

Copyright © 2012. Published by Elsevier B.V.

PMID: 22326299 [PubMed - as supplied by publisher]