Use of floating alginate gel beads for stomach-specific drug delivery.
Two types of alginate gel beads capable of floating in the gastric cavity were prepared. The first, alginate gel bead containing vegetable oil (ALGO), is a hydrogel bead and its buoyancy is attributable to vegetable oil held in the alginate gel matrix. The model drug, metronidazole (MZ), contained in ALGO was released gradually into artificial gastric juice, the release rate being inversely related to the percentage of oil. The second, alginate gel bead containing chitosan (ALCS), is a dried gel bead with dispersed chitosan in the matrix. The drug-release profile was not affected by the kind of chitosan contained in ALCS. When ALCS containing MZ was administered orally to guinea pigs, it floated on the gastric juice and released the drug into the stomach. Furthermore, the concentration of MZ at the gastric mucosa after administration of ALCS was higher than that in the solution, though the MZ serum concentration was the same regardless of which type of gel was administered. These release properties of alginate gels are applicable not only for sustained release of drugs but also for targeting the gastric mucosa.
Murata
Y
Y
Faculty of Pharmaceutical Science, Hokuriku University, Kanazawa, Japan. y-murata@hokuriku-u.ac.jp
Sasaki
N
N
Miyamoto
E
E
Kawashima
S
S
D000464:Alginates / Q000008:administration & dosage*; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage*; D002686:Chitin / Q000008:administration & dosage / Q000031:analogs & derivatives; D048271:Chitosan; D016503:Drug Delivery Systems; D005753:Gastric Mucosa / Q000378:metabolism*; D005782:Gels; D020723:Glucuronic Acid; D006168:Guinea Pigs; D006603:Hexuronic Acids; D008297:Male; D008795:Metronidazole / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012995:Solubility
D000464:Alginates; D000890:Anti-Infective Agents; D005782:Gels; D006603:Hexuronic Acids; D002686:Chitin; D008795:Metronidazole; D020723:Glucuronic Acid; D048271:Chitosan