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


CONCLUSIONS
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.
Zhou
Si-yuan
SY
Department of Pharmacology, Fourth Military Medical University, Xi'an 710032, China.
Mei
Qi-bing
QB
Liu
Li
L
Zhang
Bang-le
BL
Li
Chen
C
Zhou
Jin
J
D000818:Animals; D003106:Colon / Q000378:metabolism*; D003907:Dexamethasone / Q000008:administration & dosage* / Q000378:metabolism; D003911:Dextrans / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005260:Female; D005753:Gastric Mucosa / Q000378:metabolism; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000378:metabolism; D008297:Male; D008970:Molecular Weight; D051381:Rats; D017207:Rats, Sprague-Dawley
D003911:Dextrans; D004337:Drug Carriers; D003907:Dexamethasone