Depot injectable microcapsules of leuprorelin acetate (Lupron Depot)

Biodrug Delivery Systems: Fundamentals, Applications and Clinical Development

Volumn , Issue , 2016, Pages 370-383

  Okada, Hiroaki ^a  

^a TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

INJECTABLE MICROCAPSULES;

EID: 84947208306     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter

References (24)

1. Fujino M, Fukuda T, Shinagawa S, et al. Synthetic analogs of luteinizing hormonereleasing hormone (LH-RH) substituted in position 6 and 10. Biochem Biophys Res Commun 1974; 60:406-413.
2. Okada H, Yamazaki I, Ogawa Y, et al. Vaginal absorption of a potent luteinizing hormone-releasing hormone analog (leuprolide) in rats: I. Absorption by various routes and absorption enhancement. J Pharm Sci 1982; 71:1367-1371.
3. Okada H, Yamazaki I, Yashiki T, et al. Vaginal absorption of a potent luteinizing hormone-releasing hormone analog (leuprolide) in rats: IV. Evaluation of the vaginal absorption and gonadotropin responses by radioimmunoassay. J Pharm Sci 1984; 73:298-302.
4. Okada H, Sakura Y, Kawaji H, et al. Regression of rat mammary tumors by a potent luteinizing hormone-releasing hormone analogue (leuprolide) administered vaginally. Cancer Res 1983; 43:1869-1874.
5. Okada H. Vaginal route of peptide and protein drug delivery. In: Lee VHL, ed. Peptide and Protein Drug Delivery. New York: Marcel Dekker, 1991:633-666.
6. Okada H, Ogawa Y, Yashiki T. Prolonged release microcapsule and its production. US Patent 1987:4652441 ( Jpn Patent Appl 1983: 207760/1983).
7. Okada H, Heya T, Igari Y, et al. One-month release injectable microspheres of a superactive agonist of LH-RH, leuprolide acetate. In: Marshak D, Lie D, eds. Current Communications in Molecular Biology: Therapeutic Peptides and Proteins: Formulation, Delivery and Targeting. New York: Cold Spring Harbor Laboratory 1989:107-112.
8. Okada H, Yamamoto M, Heya T, et al. Drug delivery using biodegradable microspheres. J Control Release 1994; 28:121-129.
9. Okada H, Toguchi H, Biodegradable microspheres in drug delivery. Crit Rev Ther Drug Carrier Syst 1995; 12:1-99.
10. Okada H. One-and three-month release injectable microspheres of the LH-RH superagonist leuprorelin acetate. Adv Drug Deliv Rev 1997; 28:43-70.
11. Okada H, Heya T, Ogawa Y, et al. One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats. J Pharmacol Exp Ther 1988; 244:744-750.
12. Okada H, Heya T, Igari Y, et al. One-month release injectable microspheres of leuprolide acetate inhibit steroidogenesis and genital organ growth in rats. Int J Pharm 1989; 54:231-239.
13. Ogawa Y, Okada H, Heya T, et al. Controlled release of LH-RH agonist, leuprolide acetate, from microcapsules: serum drug level profiles and pharmacological effects in animals. J Pharm Pharmacol 1989; 41:439-444.
14. Okada H, Heya T, Ogawa Y, et al. Sustained pharmacological activities in rats following single and repeated administration of once-a-month injectable microspheres of leuprolide acetate. Pharm Res 1991; 8:584-587.
15. Okada H, Inoue Y, Heya T, et al. Pharmacokinetics of once-a-month injectable microspheres of leuprolide acetate. Pharm Res 1991; 8:787-791.
16. Yamamoto M, Takada S, Ogawa Y. Method for producing microcapsule. Jpn Patent Appl 1985:22978/1985.
17. Ogawa Y, Yamamoto M, Okada H, et al. A new technique to efficiently entrap leuprolide acetate into microcapsules of polylactic acid or copoly(lactic/glycolic) acid. Chem Pharm Bull 1988; 36:1095-1103.
18. Okada H, Inoue Y, Ogawa Y. Prolonged release microcapsules. US Patent 1996:5480656 (Jpn Patent App l1990: 33133/90).
19. Okada H, Doken Y, Ogawa Y, et al. Preparation of three-month depot injectable microspheres of leuprorelin acetate using biodegradable polymers. Pharm Res 1994; 11:1143-1147.
20. Okada H, Doken Y, Ogawa Y, et al. Sustained suppression of the pituitary-gonadal axis by leuprorelin three-month depot microspheres in rats and dogs. Pharm Res 1994; 11:1199-1203.
21. Okada H, Doken Y, Ogawa Y. Persistent suppression of the pituitary-gonadal system in female rats by three-month depot injectable microspheres of leuprorelin acetate. J Pharm Sci 1996; 85:1044-1048.
22. Heya T, Okada H, Tanigawara Y, et al. Effects of counteranion of TRH and loading amount on control of TRH release from copoly(DL-lactic/glycolic acid) microspheres, prepared by an in-water drying method. Int J Pharm 1991; 69:69-75.
23. Yoshioka T, Okada H, Ogawa Y. Sustained release microcapsule for water-soluble drug. US Patent 1993:5271945 ( Jpn Patent Appl 1988: 167490/1988).
24. Murata N, Takashima Y, Toyoshima K, et al. Anti-tumor effects of anti-VEGF siRNA encapsulated with PLGA microspheres in mice. J Control Release 2008; 126:246-254.