Biodegradable PLGA Microspheres as a Sustained Release System for a New Luteinizing Hormone-Releasing Hormone (LHRH) Antagonist
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概要
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A sustained release poly(DL-lactide-co-glycolide) (PLGA) microsphere delivery system to treat prostate cancer for a luteinizing hormone-releasing hormone (LHRH) antagonists, LXT-101 was prepared and evaluated in the paper. LXT-101 microspheres were prepared from PLGA by three methods: (1) double-emulsion solvent extraction/evaporation technique, (2) single-emulsion solvent extraction/evaporation technique, and (3) S/O/O(solid-in-oil-in-oil) method. The microspheres were investigated on drug loading, particle size, surface morphology and in vitro release profiles. An accelerated release approach was also established in order to expedite the evaluation periods. The in vivo evaluation of the microspheres was made by monitoring testosterone levels after subcutaneous administration to rats. The LXT-101 PLGA microspheres showed smooth and round surfaces according to a scanning electron microscopic investigation, and average particle size of ca. 30μm according to laser diffractometry. The drug encapsulation efficiency of microspheres was influenced by LA/GA ratio of PLGA, salt concentrations, solvent mixture and preparation methods. Moreover, LA/GA ratio of PLGA, different preparation methods and different peptide stabilizers affected in vitro release of drugs. In vivo study, the testosterone levels were suppressed to castration up to 42d as for the 7.5mg/kg dose. And in vivo performance of LXT-101 microspheres was dose-dependent. The weights of rat sexual organs decreased and histopathological appearance of testes had little changes after 4-month microspheres therapy. This also testified that LXT-101 sustained release microspheres could exert the efficacy to suppress the testosterone level to castration with little toxicity. In conclusion, the PLGA microspheres could be a well sustained release system for LXT-101.
- 社団法人日本薬学会の論文
- 2006-09-01
著者
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LIU Yan
Department of Nutrition and Food Hygiene, School of Public Health, Nanjing Medical University
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Qie Jiankun
Department Of Pharmaceutical Chemistry Beijing Institute Of Pharmacology And Toxicology
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DU Lina
Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology
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CHENG Junping
Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology
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CHI Qiang
Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology
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MEI Xingguo
Department of Pharmaceutical Chemistry, Beijing Institute of Pharmacology and Toxicology
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Liu Yan
Department Of Cardiology Daping Hospital The Third Military Medical University
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Du Lina
Department Of Pharmaceutical Chemistry Beijing Institute Of Pharmacology And Toxicology
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Chi Qiang
Department Of Pharmaceutical Chemistry Beijing Institute Of Pharmacology And Toxicology
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Mei Xingguo
Department Of Pharmaceutical Chemistry Beijing Institute Of Pharmacology And Toxicology
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Cheng Junping
Department Of Pharmaceutical Chemistry Beijing Institute Of Pharmacology And Toxicology
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Liu Yan
Department Of Pharmaceutical Chemistry Beijing Institute Of Pharmacology And Toxicology
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Liu Yan
Department of Applied Physics, South China Agricultural University, Guangzhou 510642, China
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