Oral administration has the advantages of convenience
safety
and strong patient dependence which is an ideal route of administration. However
protein drugs are easily degraded by gastric acid and protease during oral administration resulting in low bioavailability. In this paper
a drug carrier was designed for oral administration of protein drugs
which solved the problem that protein drugs were easily inactivated in the gastrointestinal tract. Glucose oxidase nanocapsules were prepared by
in-situ
free radical polymerization on the surface of the protein using glucose oxidase as a protein drug model
and the nanocapsules were grounded into powder and encapsulated in the capsul after dried at low temperature. Hypromellose was used as a raw material to prepare hypromellose acetate succinate
which was used as an enteric coating material to coat the above-mentioned capsules to obtain enteric capsules. By simulating the environment in the gastrointestinal tract
in vitro
release experiments and activity tests were performed. The results showed that the enteric-coated capsule did not dissolve within 2h under the environment of gastric juice
and the glucose oxidase in the capsule maintained high activity. Under the environment of intestinal juice
the enteric-coated capsule was dissolved and the activity of the glucose oxidase encapsulated by the nanocapsules was significantly higher than that of free glucose oxidase. The above experimental results proved that the drug-carrying system could solve the problem that oral protein drugs were easily decomposed by gastric acid and protease in the gastrointestinal tract and became inactivated.
关键词
蛋白类药物口服给药纳米微囊醋酸羟丙甲纤维素琥珀酸酯蛋白活性
Keywords
Protein drugsOral administrationNanocapsulesHypromellose succinateProtein activity