LIPIDIC CONJUGATES OF LUTEINIZING-HORMONE-RELEASING HORMONE (LHRH)+ AND THYROTROPIN-RELEASING-HORMONE (TRH)+ THAT RELEASE AND PROTECT THE NATIVE HORMONES IN HOMOGENATES OF HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS

被引：51

作者：

TOTH, I ^{[1
]}

FLINN, N ^{[1
]}

HILLERY, A ^{[1
]}

GIBBONS, WA ^{[1
]}

ARTURSSON, P ^{[1
]}

机构：

[1] UNIV UPPSALA,BIOMEDICUM,S-75123 UPPSALA,SWEDEN

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1994年 / 105卷 / 03期

关键词：

LIPIDIC AMINO ACID; LIPIDIC PEPTIDE; DRUG DELIVERY; LHRH; TRH; CACO-2 CELL HOMOGENATE; ENZYME DEGRADATION;

D O I：

10.1016/0378-5173(94)90108-2

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The enzymatically labile peptides LHRH and TRH were conjugated to various lipidic peptides. The conjugates and free peptides were incubated with Caco-2 cell homogenates and their respective degradation profiles were studied following incubation. Conjugation to lipidic peptides increased the half-life of LHRH and TRH. The Caco-2 cell homogenates were capable of cleaving the conjugated lipidic peptide, to release the parent LHRH or TRH. The released LHRH or TRH subsequently demonstrated a longer half-life than when present alone in the incubation mixture, suggesting that the cleaved lipidic peptide is capable of inhibiting enzymes.

引用

页码：241 / 247

页数：7

共 19 条

[1] EPITHELIAL TRANSPORT OF DRUGS IN CELL-CULTURE .1. A MODEL FOR STUDYING THE PASSIVE DIFFUSION OF DRUGS OVER INTESTINAL ABSORPTIVE (CACO-2) CELLS [J].