Drug delivery studies in Caco-2 monolayers. II. Absorption enhancer effects of lysophosphatidylcholines
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Drug delivery studies in Caco-2 monolayers. II. Absorption enhancer effects of lysophosphatidylcholines. / Hovgaard, Lars; Brøndsted, Helle; Nielsen, Hanne Mørck.
I: International Journal of Pharmaceutics, Bind 114, Nr. 2, 14.02.1995, s. 141-149.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Drug delivery studies in Caco-2 monolayers. II. Absorption enhancer effects of lysophosphatidylcholines
AU - Hovgaard, Lars
AU - Brøndsted, Helle
AU - Nielsen, Hanne Mørck
PY - 1995/2/14
Y1 - 1995/2/14
N2 - This paper concerns the mechanistic elucidation of a certain class of absorption enhancers within the group of phospholipids, lysophosphatidylcholines. The studies were performed in Caco-2 monolayers. Physico-chemical characteristics and effects on the integrity and viability of the Caco-2 monolayers were found to be correlated with the absorption promoting effects of the phospholipids. Comparing enhancers with varying size of the lipophilic moiety, the lipophilicity was shown to be of the utmost importance for all of the observed effects. As the chain length increased from 6 to 16 methylene groups, the effects measured on the monolayers were amplified. The acute effects were evaluated by various microscopic staining techniques as well as by transport studies. The transport rates of the vasopressin analogue 1-deamino-8-d-arginine-vasopressin (DDAVP) were determined as a measure of the monolayer integrity. Based on the apparent permeability coefficient, Papp, it could be concluded that phospholipid treatment increased DDAVP transport even under circumstances where the cell monolayer integrity was only slightly altered.
AB - This paper concerns the mechanistic elucidation of a certain class of absorption enhancers within the group of phospholipids, lysophosphatidylcholines. The studies were performed in Caco-2 monolayers. Physico-chemical characteristics and effects on the integrity and viability of the Caco-2 monolayers were found to be correlated with the absorption promoting effects of the phospholipids. Comparing enhancers with varying size of the lipophilic moiety, the lipophilicity was shown to be of the utmost importance for all of the observed effects. As the chain length increased from 6 to 16 methylene groups, the effects measured on the monolayers were amplified. The acute effects were evaluated by various microscopic staining techniques as well as by transport studies. The transport rates of the vasopressin analogue 1-deamino-8-d-arginine-vasopressin (DDAVP) were determined as a measure of the monolayer integrity. Based on the apparent permeability coefficient, Papp, it could be concluded that phospholipid treatment increased DDAVP transport even under circumstances where the cell monolayer integrity was only slightly altered.
KW - Absorption enhancer
KW - Caco-2
KW - Cell culture
KW - DDAVP
KW - Intestinal absorption
KW - Lysophosphatidylcholine
KW - Peptide absorption
KW - Phospholipid
UR - http://www.scopus.com/inward/record.url?scp=0028924771&partnerID=8YFLogxK
U2 - 10.1016/0378-5173(94)00232-T
DO - 10.1016/0378-5173(94)00232-T
M3 - Journal article
AN - SCOPUS:0028924771
VL - 114
SP - 141
EP - 149
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 2
ER -
ID: 239817159