Preparation and properties of carrageenan microspheres containing allopurinol and local anesthetic agents for the treatment of oral mucositis.
For the treatment of oral mucositis, carrageenan microspheres containing allopurinol and local anesthetic agents, such as lidocaine hydrochloride, dibucaine hydrochloride and tetracaine hydrochloride were prepared using a spray-drying method. As base materials, kappa-carrageenan and iota-carrageenan were evaluated, since carrageenan mitigates bitter taste of lidocaine hydrochloride, dibucaine hydrochloride and tetracaine hydrochloride. The microspheres were spherical and their average diameters were about 10 microm. The drug loading efficiency was more than 70%. Allopurinol and local anesthetic agents became amorphous by the spray drying. Allopurinol and the local anesthetic agents were released from the microspheres for at least 400 min when iota-carrageenan was used as a base material. On the other hand, the release was prolonged to 600 min when kappa-carrageenan was used. The microspheres were spread and made membranes at the air/water interfaces immediately after dropped on the water surfaces. The properties of the microspheres such as dispersing efficacy and membrane production on the water surfaces suggest that the microspheres can uniformly cover inner surfaces of oral cavity to prevent and treat oral mucositis.
Tomoda
Keishiro
K
Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Asahiyama
Masato
M
Ohtsuki
Emi
E
Nakajima
Takehisa
T
Terada
Hiroshi
H
Kanebako
Makoto
M
Inagi
Toshio
T
Makino
Kimiko
K
D000493:Allopurinol / Q000737:chemistry / Q000627:therapeutic use; D000777:Anesthetics / Q000737:chemistry* / Q000627:therapeutic use*; D002351:Carrageenan / Q000737:chemistry* / Q000648:ultrastructure; D004337:Drug Carriers / Q000737:chemistry*; D008012:Lidocaine / Q000737:chemistry / Q000627:therapeutic use; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D013280:Stomatitis / Q000188:drug therapy*; D013499:Surface Properties
D000777:Anesthetics; D004337:Drug Carriers; D000493:Allopurinol; D002351:Carrageenan; D008012:Lidocaine