H. Mizuguchi et al., A COMPARISON OF DRUG TRANSPORT THROUGH CULTURED MONOLAYERS OF BOVINE BRAIN CAPILLARY AND BOVINE AORTIC ENDOTHELIAL-CELLS, Biological & pharmaceutical bulletin, 17(10), 1994, pp. 1385-1390
To examine how efficient primary cultured brain capillary endothelial
cells are as an in vitro blood-brain barrier (BBB) system with regard
to drug transport, we compared bovine brain capillary endothelial cell
s (BBCEC) with bovine aortic endothelial cells (BAEC). Paracellular an
d transcellular transport were examined. [C-14]Sucrose and fluorescein
isothiocyanate-dextran (FITC-dextran)(average molecular weight about
4400 and 71200) were used as indices of paracellular transport. The pe
rmeability coefficients of [C-14]sucrose and FITC-dextran through BBCE
C monolayers were about 3 and 30-40 fold lower than those through BAEC
monolayers, respectively. Transcellular transport was examined by mea
ns of [H-3]leucine and [H-3]alanine uptake studies. The K-m value (Mic
haelis constant) of the amino acid uptake was lower in BBCEC than in B
AEC. BBCEC had higher alkaline phosphatase (ALP) and gamma-glutamyl tr
anspeptidase (gamma-GTP) activity than BAEC when cultured in vitro. Th
ese results suggest that BBCEC are suitable for drug transport studies
across the BBB in vitro.