Intestinal lymphatic transport of three retinoids in the rat after oral administration: Effect of lipophilicity and lipid vehicle

Nankervis, R., Davis, S.S., Day, N.H. and Shaw, P.N. (1996) Intestinal lymphatic transport of three retinoids in the rat after oral administration: Effect of lipophilicity and lipid vehicle. International Journal of Pharmaceutics, 130 1: 57-64. doi:10.1016/0378-5173(95)04265-2


Author Nankervis, R.
Davis, S.S.
Day, N.H.
Shaw, P.N.
Title Intestinal lymphatic transport of three retinoids in the rat after oral administration: Effect of lipophilicity and lipid vehicle
Journal name International Journal of Pharmaceutics   Check publisher's open access policy
ISSN 0378-5173
1873-3476
Publication date 1996-03
Sub-type Article (original research)
DOI 10.1016/0378-5173(95)04265-2
Volume 130
Issue 1
Start page 57
End page 64
Total pages 8
Place of publication Amsterdam, Netherlands
Publisher Elsevier
Language eng
Abstract The retinoids are highly lipophilic molecules and are known to be transported in the intestinal lymph after oral administration. Three retinoids, isotretinoin, etretinate and temarotene were used to study the effects of solubility and lipophilicity on lymphatic uptake in the rat after oral administration in each of three oily vehicles, cottonseed oil, Miglyol 812 and linoleic acid. Lipid solubility showed a general increase with increasing log P of the retinoid. The most lipophilic retinoid, temarotene, showed solubilities between 109.5 mg/ml (linoleic acid) and 170.6 mg/ml (Miglyol 812), whereas the least lipophilic retinoid, isotretinoin showed much lower solubilities between 5.1 (cottonseed oil) and 30.5 mg/ml (linoleic acid). Lymphatic uptake of temarotene was 4000-times and from etretinate 1000-times greater than that for isotretinoin after administration in linoleic acid. The lymphatic uptake of temarotene and etretinate from cottonseed oil were 27- and 26-times greater than that for isotretinoin and from Miglyol 812, 22-and 10-times greater than isotretinoin. These decreases in absorption via the lymphatic route reflect a decrease in log P value from temarotene (log P ≈ 8.7) to etretinate (log P ≈ 7.8) to isotretinoin (log P ≈ 6.8). The rank order of increasing lymphatic uptake from each of the three oils shows an inverse relationship with solubility of the retinoid in each of the oils
Keyword Retinoid
Isotretinoin
Etretinate
Temarotene
Lymphatic Uptake
Lipophilicity
Solubility
Oil Vehicle
Absorption
Oils
Ddt
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Pharmacy Publications
 
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Created: Mon, 20 Dec 2010, 14:09:29 EST