[Characteristics of drug-release in vitro of different dextran-dexamethasone conjugates].

AIM

To evaluate the effects of molecular weight of dextran on drug-release of conjugate in vitro by screening colon-specific conjugates.

METHODS

The conjugates, synthesized with different molecular-weight dextran and dexamethasone, were incubated in the contents of different parts of rat gastrointestinal tract at 37 degrees C. The release of dexamethasone(Dex) and dexamethasonehemisuccinate was determined by HPLC. The mobile phase consisted of 35% acetonitrile and 65% trisodium citrate (50 mmol.L-1, adjusted to pH 4.1 with phosphoric acid).

RESULTS

There was no release of dexamethasone or dexamethasonehemisuccinate from conjugates in the stomach contents. The amount of Dex (including dexamethasonehemisuccinate) released from DexD26 in the contents of colon and cecum was shown to be 4.0 times higher than that released in the contents of proximal and distal small intestine while the amount of Dex (including dexamethasonehemisuccinate) released from DexD50 was shown to be 3.6 times higher. The amount of Dex (including dexamethasonehemisuccinate) released from DexD2 in the contents of colon and cecum and from DexD7.6 were 2.0 times and 1.9 times higher, respectively, than that released in contents of proximal and distal small intestine.

CONCLUSION

The molecular weight of dextran showed marked effect on drug-release of the conjugate in vitro, and the conjugates with larger molecular-weight dextran have great potential in colon-specific delivery of dexamethasone.