One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats
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⤵ 12 in-corpus citations
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Injectable microcapsules of leuprolide acetate provided one-month sustained release of the LHRH agonist for treating experimental endometriosis in rats.
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Abstract
Leuprolide acetate is a highly potent analog of luteinizing hormone-releasing hormone. We have prepared 1-month release injectable microcapsules of leuprolide acetate using a biodegradable polymer, poly (dl-lactide-co-glycolide), to treat an endocrine-dependent tumor, prostate cancer. In the present study, the possibility using the microcapsules to treat endometriosis was investigated. In rats, the microcapsules exhibited a pseudo-zero order release from the injection site for 1 month after being administered s.c. and i.m., and maintained effective constant serum levels of the analog during the 4-week treatment. A single injection of the microcapsules (100 micrograms/kg/day as leuprolide acetate) suppressed luteinizing hormone, follicle-stimulating hormone and estradiol for more than 4 weeks, and caused a dramatic regression of growth of Jones experimental endometriosis model in female rats. These results encourage the belief that a 1-month release parenteral preparation of leuprolide acetate may be potentially useful in the therapy of endometriosis in human beings.
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Cited by (12)
- Validation of rat endometriosis model by using raloxifene as a positive control for the evaluation of novel SERM compounds 2005
- A prospective randomized study comparing endocrinological and clinical effects of two types of GnRH agonists in cases of uterine leiomyomas or endometriosis 2000
- Inhibitory effects of a novel aromatase inhibitor, YM511, on growth of endometrial explants and insulin-like growth factor-I gene expression in rats with experimental endometriosis 1997
- Individual and combined effects of triptoreline and gestrinone on experimental endometriosis in rats 1996
- Effects of gonadotropin-releasing hormone agonist (GnRHa) and ovariectomy on leukocyte subpopulations in rats with autotransplanted endometrium 1996
- Persistent suppression of the pituitary-gonadal system in female rats by three-month depot injectable microspheres of leuprorelin acetate 1996
- Leukocyte subpopulation changes in rats with autotransplanted endometrium and the effect of danazol 1995
- Leuprorelin. A review of its pharmacology and therapeutic use in prostatic cancer, endometriosis and other sex hormone-related disorders 1994
- Time-related effects of gonadotropin-releasing hormone analog treatment in experimentally induced endometriosis in the rat 1991
- Effects of TAP-144-SR, a sustained-release formulation of a potent GnRH agonist, on experimental endometriosis in the rat 1991
- Effects of danazol, gonadotropin-releasing hormone agonist, and a combination of danazol and gonadotropin-releasing hormone agonist on experimental endometriosis 1990
- Histological studies on the therapeutic effect of sustained-release microspheres of a potent LHRH agonist (leuprorelin acetate) in an experimental endometriosis model in rats 1990
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