[Once-a-month injectable microcapsules of leuprorelin acetate]

H Toguchi, Y Ogawa, H Okada, M Yamamoto
Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan · 1991 · doi:10.1248/yakushi1947.111.8_397 · PMID:1795229
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⚙ AI-generated summary by claude@2026-06, 2026-06-14 ⓘ

Injectable microcapsules of leuprorelin acetate were developed to provide a once-a-month depot formulation, achieving prolonged depression of the pituitary-gonadal axis in experimental animals.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-14 · read from full text ⓘ

The paper describes the development of once-a-month injectable microcapsules containing leuprorelin acetate (a potent LH-RH/LHRH agonist), produced using a novel in-water drying method. Using copoly(lactic/glycolic acid) as wall material, the microcapsule depot was designed to release leuprorelin over one month at an apparent zero-order rate driven by bioerosion. In experimental animals, once-a-month injection produced a dramatic, prolonged depression of the pituitary-gonadal axis (chemical castration), and the paper summarizes dosage-design studies for this delivery system. Relevance to endometriosis: the paper explicitly states that this formulation is expected for treating hormone-dependent conditions including endometriosis, though the reported experimental details are in general terms for hormone-dependent cancers and chemical castration in animals.

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Abstract

Leuprorelin (leuprolide, D-Leu6-(des-Gly10-NH2)-LH-RH ethylamide) acetate is a super-active agonist of luteinizing hormone-releasing hormone (LH-RH). We developed once-a-month injectable microcapsules of this agonist by our novel in-water drying method. This depot formulation can release the drug at an apparent zero-order rate over one month with bioerosion of copoly (lactic/glycolic acid) utilized as a wall material of the polycore microcapsules. A dramatic prolonged depression of pituitary-gonadal axis, chemical castration, was achieved by the once-a-month injection in experimental animals; it expects a reliable efficacy for treating hormone-dependent prostatic, breast cancers and endometriosis. Studies on the dosage design of this new delivery system of leuprorelin are summarized.
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抄録 Leuprorelin (leuprolide, D-Leu6-(des-Gly10-NH2)-LH-RH ethylamide) acetate is a superactive agonist of luteinizing hormone-releasing hormone (LH-RH). We developed once-a-month injectable microcapsules of this agonist by our novel in-water drying method. This depot formulation can release the drug at an apparent zero-order rate over one month with bioerosion of copoly (lactic/glycolic acid) utilized as a wall material of the polycore microcapsules. A dramatic prolonged depression of pituitary-gonadal axis, chemical castration, was achieved by the once-a-month injection in experimental animals ; it expects a reliable effcacy for treating hormone-dependent prostatic, breast cancers and endometriosis. Studies on the dosage design of this new delivery system of leuprorelin are summarized. © by the PHARMACEUTICAL SOCIETY OF JAPAN

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Condition tags

endometriosis

MeSH descriptors

Drug Delivery Systems Leuprolide Amino Acid Sequence Animals Breast Neoplasms Breast Neoplasms Capsules Delayed-Action Preparations Endometriosis Endometriosis Glycolates Humans Injections Lactates Lactic Acid Leuprolide Leuprolide Leuprolide Male Molecular Sequence Data

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