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Photo courtesy of the CDC
Researchers say they have developed biodegradable hydrophilic carriers that could provide oral delivery of factor IX (FIX) to treat hemophilia B.
Preclinical experiments have shown these carriers can be loaded with FIX and release it in response to environmental
stimuli.
Sarena Horava, PhD, of Triton Systems, Inc. in Chelmsford, Massachusetts, and her colleagues described the carriers in the International Journal of Pharmaceutics.
The current work builds on a previous delivery system devised by Dr Horova and Nicholas A. Peppas, ScD, of The University of Texas at Austin.
Although that system was successful in transporting FIX, the researchers found that modifications were needed to improve the oral bioavailability of FIX.
The team noted that FIX is delicate and unstable in the body’s various pH environments. So the new system is designed to capitalize on the body’s pH and changes in enzymes inside the gastrointestinal tract.
Specifically, the researchers developed a biodegradable, pH-responsive hydrogel microcarrier system based on the poly(methacrylic acid)-grafted-poly(ethylene glycol) [P(MAA-g-EG)].
The team said the incorporation of an enzymatically degradable peptide crosslinking agent allows for site-specific degradation by trypsin in the small intestine.
The carrier is designed to remain intact as it moves through the body. Once it reaches the small intestine, the carrier should begin to swell with the increase in pH. The carrier should then be degraded by trypsin and slowly release FIX over time.
The researchers said their experiments confirmed that the peptide crosslinked P(MAA-g-EG) microparticles are capable of loading FIX and releasing it under intestinal conditions.
They said the biodegradable component allowed for increased levels of FIX to be released, when compared to the previous system.
Furthermore, both the microparticles and the degradation products enhanced the in vitro absorption of FIX.
“Based on the current capabilities of this system, approximately 2 capsules would be equivalent to 1 injection [of FIX],” Dr Horava said. “However, we anticipate that we will make further improvements to the delivery capacity of the oral delivery system and therefore decrease the capsule amount.”
The researchers plan to conduct additional preclinical experiments with this system before starting clinical trials. 
Photo courtesy of the CDC
Researchers say they have developed biodegradable hydrophilic carriers that could provide oral delivery of factor IX (FIX) to treat hemophilia B.
Preclinical experiments have shown these carriers can be loaded with FIX and release it in response to environmental
stimuli.
Sarena Horava, PhD, of Triton Systems, Inc. in Chelmsford, Massachusetts, and her colleagues described the carriers in the International Journal of Pharmaceutics.
The current work builds on a previous delivery system devised by Dr Horova and Nicholas A. Peppas, ScD, of The University of Texas at Austin.
Although that system was successful in transporting FIX, the researchers found that modifications were needed to improve the oral bioavailability of FIX.
The team noted that FIX is delicate and unstable in the body’s various pH environments. So the new system is designed to capitalize on the body’s pH and changes in enzymes inside the gastrointestinal tract.
Specifically, the researchers developed a biodegradable, pH-responsive hydrogel microcarrier system based on the poly(methacrylic acid)-grafted-poly(ethylene glycol) [P(MAA-g-EG)].
The team said the incorporation of an enzymatically degradable peptide crosslinking agent allows for site-specific degradation by trypsin in the small intestine.
The carrier is designed to remain intact as it moves through the body. Once it reaches the small intestine, the carrier should begin to swell with the increase in pH. The carrier should then be degraded by trypsin and slowly release FIX over time.
The researchers said their experiments confirmed that the peptide crosslinked P(MAA-g-EG) microparticles are capable of loading FIX and releasing it under intestinal conditions.
They said the biodegradable component allowed for increased levels of FIX to be released, when compared to the previous system.
Furthermore, both the microparticles and the degradation products enhanced the in vitro absorption of FIX.
“Based on the current capabilities of this system, approximately 2 capsules would be equivalent to 1 injection [of FIX],” Dr Horava said. “However, we anticipate that we will make further improvements to the delivery capacity of the oral delivery system and therefore decrease the capsule amount.”
The researchers plan to conduct additional preclinical experiments with this system before starting clinical trials.
Photo courtesy of the CDC
Researchers say they have developed biodegradable hydrophilic carriers that could provide oral delivery of factor IX (FIX) to treat hemophilia B.
Preclinical experiments have shown these carriers can be loaded with FIX and release it in response to environmental
stimuli.
Sarena Horava, PhD, of Triton Systems, Inc. in Chelmsford, Massachusetts, and her colleagues described the carriers in the International Journal of Pharmaceutics.
The current work builds on a previous delivery system devised by Dr Horova and Nicholas A. Peppas, ScD, of The University of Texas at Austin.
Although that system was successful in transporting FIX, the researchers found that modifications were needed to improve the oral bioavailability of FIX.
The team noted that FIX is delicate and unstable in the body’s various pH environments. So the new system is designed to capitalize on the body’s pH and changes in enzymes inside the gastrointestinal tract.
Specifically, the researchers developed a biodegradable, pH-responsive hydrogel microcarrier system based on the poly(methacrylic acid)-grafted-poly(ethylene glycol) [P(MAA-g-EG)].
The team said the incorporation of an enzymatically degradable peptide crosslinking agent allows for site-specific degradation by trypsin in the small intestine.
The carrier is designed to remain intact as it moves through the body. Once it reaches the small intestine, the carrier should begin to swell with the increase in pH. The carrier should then be degraded by trypsin and slowly release FIX over time.
The researchers said their experiments confirmed that the peptide crosslinked P(MAA-g-EG) microparticles are capable of loading FIX and releasing it under intestinal conditions.
They said the biodegradable component allowed for increased levels of FIX to be released, when compared to the previous system.
Furthermore, both the microparticles and the degradation products enhanced the in vitro absorption of FIX.
“Based on the current capabilities of this system, approximately 2 capsules would be equivalent to 1 injection [of FIX],” Dr Horava said. “However, we anticipate that we will make further improvements to the delivery capacity of the oral delivery system and therefore decrease the capsule amount.”
The researchers plan to conduct additional preclinical experiments with this system before starting clinical trials.