Novel polymeric film coatings for colon targeting: Drug release from coated pellets.
The aim of this study was to prepare and characterize novel types of polymer coated pellets allowing for the site-specific delivery of drugs to the colon. 5-Aminosalicylic acid (5-ASA)-loaded beads were prepared by extrusion-spheronization and coated with different Nutriose:ethylcellulose blends. In vitro drug release from these systems was measured under various conditions, including the exposure to fresh fecal samples from inflammatory bowel disease patients under anaerobic conditions. Nutriose is a starch derivative, which is preferentially degraded by enzymes secreted by the microflora in the colon of Crohn's disease and ulcerative colitis patients. Interestingly, the release of 5-ASA (which is commonly used for the local treatment of inflammatory bowel diseases) could effectively be suppressed upon exposure to release media simulating the conditions in the upper GIT, irrespective of the degree of agitation and presence or absence of enzymes. But as soon as the pellets came into contact with fecal samples of inflammatory bowel disease patients, the release rate significantly increased and the drug was released in a time-controlled manner. Thus, this novel type of colon targeting system is adapted to the pathophysiology of the patient. Furthermore, culture media containing specific colonic bacteria are presented providing an interesting potential as substitutes for fresh fecal samples.
Karrout
Youness
Y
College of Pharmacy, JE 2491, Universite Lille Nord de France, 3 rue du Professeur Laguesse, 59006 Lille, France.
Neut
Christel
C
Wils
Daniel
D
Siepmann
Florence
F
Deremaux
Laëtitia
L
Flament
Marie-Pierre
MP
Dubreuil
Luc
L
Desreumaux
Pierre
P
Siepmann
Juergen
J
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry; D002214:Capsules; D002482:Cellulose / Q000031:analogs & derivatives; D003106:Colon / Q000378:metabolism*; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D005243:Feces / Q000737:chemistry; D041981:Gastrointestinal Tract / Q000378:metabolism; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy / Q000378:metabolism; D019804:Mesalamine / Q000008:administration & dosage / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D013608:Tablets, Enteric-Coated
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D003692:Delayed-Action Preparations; D005079:Excipients; D011108:Polymers; D013608:Tablets, Enteric-Coated; D019804:Mesalamine; C013517:ethyl cellulose; D002482:Cellulose