Design of pH-sensitive microspheres for the colonic delivery of the immunosuppressive drug tacrolimus

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 58, Issue 1, 2004, Pages 37-43

  Lamprecht, Alf ^a   Yamamoto, Hiromitsu ^a   Takeuchi, Hirofumi ^a   Kawashima, Yoshiaki ^a  

^a GIFU PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

Colon delivery; Eudragit; FK506; Microspheres; pH dependent; Tacrolimus

Indexed keywords

IMMUNOSUPPRESSIVE AGENT; MICROSPHERE; TACROLIMUS; WATER OIL CREAM;

ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG RELEASE; EMULSION; ENCAPSULATION; EVAPORATION; EXTRACTION; MOLECULAR DYNAMICS; PH MEASUREMENT; X RAY ANALYSIS;

COLON; DRUG DELIVERY SYSTEMS; HYDROGEN-ION CONCENTRATION; IMMUNOSUPPRESSIVE AGENTS; MICROSPHERES; TACROLIMUS;

EID: 2942665785     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2004.01.003     Document Type: Article

References (21)

1. Friend D.R. Colon-specific drug delivery. Adv. Drug Deliv. Rev. 7:1991;149-199
2. McLeod A., Friend D.R., Tozer T.N. Glucocorticoid-dextran conjugates as potential prodrugs colon-specific delivery: hydrolysis in rat gastrointestinal tract contents. J. Pharm. Sci. 83:1994;1284-1288
3. Fedorak R., Haeberlin B., Empey L.R., Cui N., Nolen H. III, Jewell L.D., Friend D.R. Colonic delivery of dexamethasone from a prodrug accelerates healing of colitis in rats without adrenal suppression. Gastroenterology. 108:1995;1688-1699
4. Rubinstein A. Approaches and opportunities in colon-specific drug delivery. Crit. Rev. Ther. Drug Carrier Syst. 12:1995;101-149
5. Watts P.J., Illum L. Colonic drug delivery. Drug Dev. Ind. Pharmcol. 23:1997;893-913
6. Kinget R., Kalala W., Vervoort L., van den Mooter G. Colonic drug targeting. J. Drug Target. 6:1998;129-149
7. Hardy F.H., Davis S.S., Khosla R., Robertson C.S. Gastrointestinal transit of small tablets in patients with ulcerative colitis. Int. J. Pharmcol. 48:1988;79-82
8. Watts P.J., Barrow L., Steed K.P., Wilson C.G., Spiller R.C., Melia C.D., Davies M.C. The transit rate of different-sized model dosage forms through the human colon and the effects of a lactulose-induced catharsis. Int. J. Pharmcol. 87:1992;215-221
9. Fellermann K., Ludwig D., Stahl M., David-Walek T., Stange E.F. Steroid-unresponsive acute attacks of inflammatory bowel disease: immunomodulation by tacrolimus (FK506). Am. J. Gastroenterol. 93:1998;1860-1866
10. Matsuhashi N., Nakajima A., Watanabe K., Komeno Y., Suzuki A., Ohnishi S., Omata M., Kondo K., Usui Y., Iwadare J.I., Watanabe T., Nagawa H., Muto T. Tacrolimus in corticoid-resistant ulcerative colitis. J. Gastroenterol. 35:2000;655-657
11. Rudolph M., Klein S., Beckert T.E., Petereit H.U., Dressman J.B. A new 5-aminosalicylic acid multi-unit dosage form for the therapy of ulcerative colitis. Eur. J. Pharmcol. Biopharm. 51:2001;183-190
12. Jeong Y.I., Prasad Y.R., Ohno T., Yoshikawa Y., Shibata N., Kato S., Takeuchi K., Takada K. Application of Eudragit P-4135F for the delivery of ellagic acid to the rat lower small intestine. J. Pharm. Pharmacol. 53:2001;1079-1085
13. Hu Z., Shimokawa T., Ohno T., Kimura G., Mawatari S.S., Kamitsuna M., Yoshikawa Y., Masuda S., Takada K. Characterization of norfloxacine release from tablet coated with a new pH-sensitive polymer, P-4135F. J. Drug Target. 7:1999;223-232
14. Lin S.Y., Ayres J.W. Calcium alginate beads as core carriers of 5-aminosalicylic acid. Pharmcol. Res. 9:1992;1128-1131
15. Lorenzo-Lamosa M.L., Remunan-Lopez C., Vila-Jato J.L., Alonso M.J. Design of microencapsulated chitosan microspheres for colonic drug delivery. J. Control. Release. 52:1998;109-118
16. Rodriguez M., Vila-Jato J.L., Torres D. Design of a new multiparticulate system for potential site-specific and controlled drug delivery to the colonic region. J. Control. Release. 55:1998;67-77
17. Akashi T., Nefuji T., Yoshida M., Hosoda J. Quantitative determination of tautomeric FK506 by reversed-phase liquid chromatography. J. Pharmcol. Biomed. Anal. 14:1996;339-346
18. K. Lehmann, W. Höss, Thermoplastic resin for enteric pharmaceutical coating, European patent EP 704, 207, July 25, 2001.
19. Lamprecht A., Yamamoto H., Takeuchi H., Kawashima Y. Microsphere design for the colonic delivery of 5-fluorouracil. J. Control. Release. 90:2003;313-322
20. Barichello J.M., Morishita M., Takayama K., Nagai T. Encapsulation of hydrophilic and lipophilic drugs in PLGA nanoparticles by the nanoprecipitation method. Drug Dev. Ind. Pharmcol. 25:1999;471-476
21. Lamprecht A., Ubrich N., Yamamoto H., Schafer U., Takeuchi H., Lehr C.M., Maincent P., Kawashima Y. Design of rolipram-loaded nanoparticles: comparison of two preparation methods. J. Control. Release. 71:2001;297-306