Biodegradable hydrophilic carriers for the oral delivery of hematological factor IX for hemophilia B treatment.

摘要: Current protein replacement therapies for hemophilia B, a genetic bleeding disorder caused by deficiency in coagulation factor IX, rely on IV injections and infusions. Oral delivery of IX is desirable needle-free option, especially prophylaxis. We have developed biodegradable, pH-responsive hydrogel microcarrier system based the poly(methacrylic acid)-grafted-poly(ethylene glycol) [P(MAA-g-EG)]. Incorporation an enzymatically degradable peptide crosslinking agent allows site-specific degradation trypsin small intestine. P(MAA-g-EG) polymer was synthesized UV polymerization, then subsequently crosslinked with using EDC-NHS chemistry. Physical characterization included FTIR determining composition SEM microparticle morphology. The swelling enzyme-specific were confirmed bright-field microscopy corresponding kinetics determined turbidimetric measurements. Evaluating drug application this system, release studies showed release, vitro transport resulted improved absorption. significantly potential as compared to previously reported non-degradable systems. Using vehicle can possibly lead orally administered prophylactic treatment B patients.