Controlled Release of LHRH Agonist, Leuprolide Acetate, from Microcapsules: Serum Drug Level Profiles and Pharmacological Effects in Animals

A new technique to efficiently entrap leuprolide acetate into microcapsules of polylactic acid or copoly(lactic/glycolic) acid.

Ogawa, Y., Yamamoto, M., Okada, H., Yashiki, T., & Shimamoto, T. (1988) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.36.1095 · Cited by 506

Resorption rate, route of elimination, and ultrastructure of the implant site of polylactic acid in the abdominal wall of the rat

Brady, J. M., Cutright, D. E., Miller, R. A., Battistone, G. C., & Hunsuck, E. E. (1973) · Journal of Biomedical Materials Research · doi:10.1002/jbm.820070204 · Cited by 280

Controlled Release of a Luteinizing Hormone-Releasing Hormone Analogue from Poly(d,l-lactide—co-glycolide) Microspheres

Sanders, L. M., Kent, J. S., McRae, G. I., VICKERY, B. H., Tice, T. R., & Lewis, D. H. (1984) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600730927 · Cited by 253

Controlled-release of leuprolide acetate from polylactic acid or copoly(lactic/glycolic) acid microcapsules: Influence of molecular weight and copolymer ratio of polymer.

Ogawa, Y., Yamamoto, M., Takada, S., Okada, H., & Shimamoto, T. (1988) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.36.1502 · Cited by 173

In vivo release profiles of leuprolide acetate from microcapsules prepared with polylactic acids or copoly(lactic/glycolic) acids and in vivo degradation of these polymers.

Ogawa, Y., Okada, H., YAMAMOTO, Y., & Shimamoto, T. (1988) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.36.2576 · Cited by 171

One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats.

Okada, H., Heya, T., Ogawa, Y., & Shimamoto, T. (1988) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)24466-4 · Cited by 116

Controlled delivery of an LHRH analogue from biodegradable injectable microspheres

Sanders, L. M., McRae, G. I., Vitale, K. M., & Kell, B. A. (1985) · Journal of Controlled Release · doi:10.1016/0168-3659(85)90044-6 · Cited by 113

Delay of Puberty and Inhibition of Reproductive Processes in the rat by a Gonadotropin-Releasing Hormone Agonist Analog

Johnson, E. S., Gendrich, R. L., & White, W. F. (1976) · Fertility and Sterility · doi:10.1016/s0015-0282(16)41963-1 · Cited by 104

A radioimmunoassay for a highly active luteinizing hormone-releasing hormone analogue and relation between the serum level of the analogue and that of gonadotropin.

Yamazaki, I., & Okada, H. (1980) · Endocrinologia Japonica · doi:10.1507/endocrj1954.27.593 · Cited by 48

Biopolymeric controlled release systems

Wise, D. L. (1984) · CRC Press eBooks · Cited by 46

Histological Studies on the Therapeutic Effect of Sustained-Release Microspheres of a Potent LHRH Agonist (Leuprorelin Acetate) in an Experimental Endometriosis Model in Rats.

Sakura, Y., Masaki, T., Sudo, K., Nomura, M., & Shino, A. (1990) · Endocrinologia Japonica · doi:10.1507/endocrj1954.37.719 · Cited by 9

Usefulness of pharmacokinetic/efficacy analysis of an investigational kisspeptin analog, TAK-448, in quantitatively evaluating anti-tumor growth effect in the rat VCaP androgen-sensitive prostate cancer model

Ishikawa, K., Tanaka, A., Kogame, A., Watanabe, T., Tagawa, Y., & Matsui, H. (2018) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2018.03.032 · Cited by 8

Surface Dissolution-Bulk Erosion Model of Drug Release from Biodegradable Polymer Rods.

Tojo, K. J., Aoyagi, H., & Kurita, T. (1998) · JOURNAL OF CHEMICAL ENGINEERING OF JAPAN · doi:10.1252/jcej.31.648 · Cited by 8

In Vitro=In Vivo Release from Injectable Dispersed Systems

Clark, B. C., Dickinson, P. A., & Pyrah, I. T. (2005) · CRC Press eBooks · doi:10.1201/9780849350610-8 · Cited by 8

Possible use of diethyl-.BETA.-cyclodextrin in preparation of sustained-release oily injection of buserelin acetate (LHRH agonist).

Matsubara, K., 栗木武男, Arima, H., 浩太郎, 若., Irie, T., & Uekama, K. (1990) · Drug Delivery System · doi:10.2745/dds.5.95 · Cited by 8

Application of plug–plug technique to ACE experiments for discovery of peptides binding to a larger target protein: A model study of calmodulin‐binding fragments selected from a digested mixture of reduced BSA

Saito, K., Nakato, M., Mizuguchi, T., Wada, S., Uchimura, H., Kataoka, H., Yokoyama, S., Hirota, H., & Kiso, Y. (2013) · Electrophoresis · doi:10.1002/elps.201300339 · Cited by 7

Tissue Reaction to a Novel Bone Substitute Material Fabricated With Biodegradable Polymer-Calcium Phosphate Nanoparticle Composite

Shimizu, H., Jinno, Y., Ayukawa, Y., Atsuta, I., ARAHIRA, T., Todo, M., & Koyano, K. (2016) · Implant Dentistry · doi:10.1097/id.0000000000000447 · Cited by 7

Hydrogen‐Bonded Films for Zero‐Order Release of Leuprolide

Fu, M., Zhuang, X., Zhang, T., Guan, Y., Meng, Q., & Zhang, Y. (2020) · Macromolecular Bioscience · doi:10.1002/mabi.202000050 · Cited by 6

Preparation and in-vitro/in-vivo evaluation of surface-modified poly (lactide-co-glycolide) fluorescent nanoparticles

Pamujula, S., Hazari, S., Bolden, G., Graves, R. A., Chinta, D. M. D., Dash, S., Kishore, V., & Mandal, T. K. (2010) · Journal of Pharmacy and Pharmacology · doi:10.1211/jpp.62.04.0003 · Cited by 6

The Enhancement of Subcutaneous First-Pass Metabolism Causes Nonlinear Pharmacokinetics of TAK-448 after a Single Subcutaneous Administration to Rats

Moriya, Y., Kogame, A., Tagawa, Y., Morohashi, A., Kondo, T., Asahi, S., & Benet, L. Z. (2019) · Drug Metabolism and Disposition · doi:10.1124/dmd.119.087148 · Cited by 6

In-vivo Release of a GnRH Agonist from a Slow-release Poly(lactide-glycolide) Copolymer Preparation: Comparison in Rat, Rabbit and Guinea-Pig

Heinrich, N., Fechner, K., Berger, H., Lorenz, D., Albrecht, E., Rafler, G., Schäfer, H., & MEHLIS, B. (1991) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.1991.tb03478.x · Cited by 6

Endocrinological Studies on TAP-144-SR, a Sustained-Release Formulation of a Potent GnRH Agonist (D-Leu6-(des-Gly10-NH2)-GnRH Ethylamide), in male Rats.

Sudo, K., Masaki, T., Shiota, K., Kawase, M., & Fujita, T. (1990) · Endocrinologia Japonica · doi:10.1507/endocrj1954.37.685 · Cited by 6

Puberty Blocker, Leuprolide, Reduces Sex Differences in Rough-and-Tumble Play and Anxiety-like Behavior in Juvenile Rats

Oliveira, G. D. F., Nguyen, A. T., Carreras-Simons, L., Niepsuj, T., Gadelhak, S. H., Johnson, A. K., Abdalla, A., Lev, E., Torres Román, S. G., Fuchs, S. N., et al. (2024) · Endocrinology · doi:10.1210/endocr/bqae046 · Cited by 5

Regulation of LH.BETA. Subunit mRNA in Immature Female Rats during GnRH Agonist Treatment.

Uemura, T., Shirasu, K., Sakakibara, H., KONDO, Y., & MINAGUCHI, H. (1990) · Endocrinologia Japonica · doi:10.1507/endocrj1954.37.695 · Cited by 4

Biodegradable Microparticles for the Development of Less-Painful and Less-Irritating Parenterals

Fattal, E., Quaglia, F., Gupta, P., & Brazeau, G. A. (1999) · CRC Press eBooks · doi:10.1201/b14378-19 · Cited by 4

Effects of luteinizing hormone-releasing hormone (LH-RH) analogue on the function of the isolated rabbit corpus cavernosum.

Itoh, Y., Ando, M., Ohmura, M., Kondo, A., Miyake, K., & Saito, M. (1996) · PubMed · Cited by 3

Long-Term Controlled Delivery of Therapeutic Agents via an Implantable Osmotically Driven System: The DUROS Implant

Wright, J. C., Chester, A. E., Skowroński, R., & Lucas, C. (2002) · CRC Press eBooks · doi:10.1201/9780203910337-58 · Cited by 3

In Vitro/In Vivo Release from Injectable Dispersed Systems

Pyrah, I. T. G., Dickinson, P., & Clark, B. (2005) · Drugs and the pharmaceutical sciences · doi:10.1201/9780849350610.ch4 · Cited by 2

The effects of two formulations of deslorelin on the reproduction of male African wild dogs (Lycaon pictus)

Newell‐Fugate, A. E. (2008) · UpSpace Institutional Repository (University of Pretoria) · Cited by 2

Local injection of a sustained‐release antiandrogen formulation into a target prostatic site: an experimental study

Goya, N., Gotanda, K., Sasaki, T., Okada, M., Tomizawa, Y., & Toma, H. (2006) · British Journal of Urology · doi:10.1111/j.1464-410x.2006.06440.x · Cited by 1

Microencapsulation of Insulin into Biodegradable Microcapsules by the High Voltage Field Method

Zhou, W., Li, B., & Du, W. (2005) · Annual International Conference of the IEEE Engineering in Medicine and Biology Society (EMBC) · doi:10.1109/iembs.2005.1616655 · Cited by 1

Depot Microcapsules Containing Biologic Nanoparticles and Cytoplasm-Responsive Nanocarriers for Nucleotides

Okada, H. (2015) · Methods in pharmacology and toxicology · doi:10.1007/978-1-4939-3121-7_16 · Cited by 1

Effects of TAP-144-SR Administration on the Prostates of Male and Female Mastomys.

Akihiko, O. H. T. A., MIZOGUCHI, Y., & KANOH, Y. (1994) · Journal of Reproduction and Development · doi:10.1262/jrd.40.329 · Cited by 1

Core-cross-linked polymeric micelles: a versatile nanomedicine platform with broad applicability

Hu, Q. (2015) · doi:10.3990/1.9789036539470 · Cited by 1

Exploring the follicular route for transcutaneous vaccination using nanoparticles

Mittal, A. (2014) · Publications of the UdS (Saarland University) · doi:10.22028/d291-22973

Die mikroverkapselte Monatsdepotform von Leuprorelin: Tierversuche und interne Struktur der Mikrokapseln

Ogawa, Y. (1995) · Springer eBooks · doi:10.1007/978-3-642-79669-2_7

Worin besteht die galenische Innovation bei Enantone® Monats-Depot?

Hübner, R. (1992) · Springer eBooks · doi:10.1007/978-3-642-76866-8_7

Sürekli etkili implant sistemlerin veteriner alandaki uygulamaları : veterinary applications of sustained release implant systems

ALĞIN, E. (1956) · Ankara Universitesi Eczacilik Fakultesi Dergisi · doi:10.1501/eczfak_0000000070

Monthly Microcapsule Depot Form of Leuprorelin: Animal Studies and Internal Structure of Microcapsules

Ogawa, Y. (1996) · Springer eBooks · doi:10.1007/978-3-642-79947-1_7

Drug delivery system in hormonal agents: long-term release LH-RH agonist

Οhyama, C., & Kato, T. (2003) · Drug Delivery System · doi:10.2745/dds.18.431

Use of sensitive gonadotropin assays to monitor response to depot-leuprolide in central precocious puberty

GARIBALDI, L. R., Aceto, T., Weber, C., & Levy, R. A. (1993) · Journal of Pediatric and Adolescent Gynecology · doi:10.1016/s0932-8610(12)80006-5

Methods and models for the investigation ofthe uptake of nanoparticles into hair follicles

Raber, A. S. (2014) · Publications of the UdS (Saarland University) · doi:10.22028/d291-23017

Therapiefortschritt mit GnRH-Analoga durch galenische Weiterentwicklung des Leuprorelinacetats zum Enantone®-Gyn Monats-Depot

Hübner, R. (1992) · Springer eBooks · doi:10.1007/978-3-642-77666-3_5

Therapeutische Kontroverse

Becker, H., Bichler, K.-H., Flüchter, S. H., Tunn, U. W., Ludwig, G., Fosså, S. D., Rubben, H., Studer, U. E., Putz, A., Bandhauer, K., et al. (1991) · Springer eBooks · doi:10.1007/978-3-642-84264-1_17

Formulation of Peptides

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Sustained release of estrogens from PEGylated nanoparticles for treatment of secondary spinal cord injury

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From molecular bridge to macro-encapsulation: Unraveling the HEPES-porosity synergy for ultra-high peptide loading in PLGA microspheres

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Persistent Suppression of the Pituitary-Gonadal System in Female Rats by Three-Month Depot Injectable Microspheres of Leuprorelin Acetate

Okada, H., Doken, Y., & Ogawa, Y. (1996) · Journal of Pharmaceutical Sciences · doi:10.1021/js960123a · Cited by 35

The pharmacokinetics and pharmacodynamics of a new sustained-release leuprolide acetate depot compared to market references

Leitner, J. M., Mayr, F., Spiel, A. O., Firbas, C., Savulsky, C. I., Mis, R., Corrado, M. E., & Jilma, B. (2008) · International Journal of Clinical Pharmacology and Therapeutics · doi:10.5414/cpp46407 · Cited by 12

Pharmacokinetics of Once-a-Month Injectable Microspheres of Leuprolide Acetate

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Sustained Pharmacological Activities in Rats Following Single and Repeated Administration of Once-a-Month Injectable Microspheres of Leuprolide Acetate

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Randomized head-to-head prospective study of pharmacokinetic and pharmacodynamic properties of leuprolide acetate formulations: 7.5 mg single depot subcutaneous vs 7.5 mg intramuscular microsphere.

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