{"title":"mPEG-PCL共聚物作为依那普利模型亲水药物递送聚合物的合成与表征","authors":"H. Danafar","doi":"10.22034/IJPS.2018.33691","DOIUrl":null,"url":null,"abstract":"Purpose: Enalapril maleate (EPM), was used for hypertension and congestive heart failure. In this way, an innovative delivery system with mPEG–PCL was synthesized and the release profile of the EPM from the drug-loaded polymersomes was evaluated. Methods: Di-block methoxy)-poly (ethylene glycol) - Poly (caprolactone) (mPEG-PCL) copolymers were synthesized and used to prepare of polymersomes for controlled release of EPM as hydrophilic model drug. MPEG-PCL copolymer was characterized in vitro by HNMR, FTIR, DSC and GPC techniques. The resulting polymersomes were characterized further by various techniques such as dynamic light scattering (DLS) and transmission electron microscopy (TEM). Results: The results of TEM shows the polymersomes formed had spherical structure and the size of nanoparticles is 80 nm. The loading and encapsulation efficiency of EPM were determinate by HPLC at 215 nm with loading and encapsulation efficiency 19.8% ± 2.12% and 85.6% ± 1.26%, respectively. Study on DSC results exposed strong interaction between EPM and copolymer. In vitro release of EPM from polymersomes was clearly sustained in all the time tested for this purpose. The sustained release of drug was hypothetically due to the entrapment of EPM in core of polymersomes. Polymersomes also showed acceptable stability for long periods of time. Conclusion: The results indicate the successful formulation of EPM loaded m-PEG/PCL polymersomes. Overall, the results was showed that m-PEG-PCL polymersomes can be considered as a promising carrier for hydrophilic drugs such as EPM.","PeriodicalId":14582,"journal":{"name":"Iranian Journal of Pharmaceutical Sciences","volume":"14 1","pages":"25-38"},"PeriodicalIF":0.0000,"publicationDate":"2018-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Synthesis and characterization of mPEG-PCL copolymers as a polymersomes for delivery of enalapril as a model hydrophilic drug\",\"authors\":\"H. Danafar\",\"doi\":\"10.22034/IJPS.2018.33691\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Purpose: Enalapril maleate (EPM), was used for hypertension and congestive heart failure. In this way, an innovative delivery system with mPEG–PCL was synthesized and the release profile of the EPM from the drug-loaded polymersomes was evaluated. Methods: Di-block methoxy)-poly (ethylene glycol) - Poly (caprolactone) (mPEG-PCL) copolymers were synthesized and used to prepare of polymersomes for controlled release of EPM as hydrophilic model drug. MPEG-PCL copolymer was characterized in vitro by HNMR, FTIR, DSC and GPC techniques. The resulting polymersomes were characterized further by various techniques such as dynamic light scattering (DLS) and transmission electron microscopy (TEM). Results: The results of TEM shows the polymersomes formed had spherical structure and the size of nanoparticles is 80 nm. The loading and encapsulation efficiency of EPM were determinate by HPLC at 215 nm with loading and encapsulation efficiency 19.8% ± 2.12% and 85.6% ± 1.26%, respectively. Study on DSC results exposed strong interaction between EPM and copolymer. In vitro release of EPM from polymersomes was clearly sustained in all the time tested for this purpose. The sustained release of drug was hypothetically due to the entrapment of EPM in core of polymersomes. Polymersomes also showed acceptable stability for long periods of time. Conclusion: The results indicate the successful formulation of EPM loaded m-PEG/PCL polymersomes. Overall, the results was showed that m-PEG-PCL polymersomes can be considered as a promising carrier for hydrophilic drugs such as EPM.\",\"PeriodicalId\":14582,\"journal\":{\"name\":\"Iranian Journal of Pharmaceutical Sciences\",\"volume\":\"14 1\",\"pages\":\"25-38\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2018-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Iranian Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.22034/IJPS.2018.33691\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Iranian Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.22034/IJPS.2018.33691","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Synthesis and characterization of mPEG-PCL copolymers as a polymersomes for delivery of enalapril as a model hydrophilic drug
Purpose: Enalapril maleate (EPM), was used for hypertension and congestive heart failure. In this way, an innovative delivery system with mPEG–PCL was synthesized and the release profile of the EPM from the drug-loaded polymersomes was evaluated. Methods: Di-block methoxy)-poly (ethylene glycol) - Poly (caprolactone) (mPEG-PCL) copolymers were synthesized and used to prepare of polymersomes for controlled release of EPM as hydrophilic model drug. MPEG-PCL copolymer was characterized in vitro by HNMR, FTIR, DSC and GPC techniques. The resulting polymersomes were characterized further by various techniques such as dynamic light scattering (DLS) and transmission electron microscopy (TEM). Results: The results of TEM shows the polymersomes formed had spherical structure and the size of nanoparticles is 80 nm. The loading and encapsulation efficiency of EPM were determinate by HPLC at 215 nm with loading and encapsulation efficiency 19.8% ± 2.12% and 85.6% ± 1.26%, respectively. Study on DSC results exposed strong interaction between EPM and copolymer. In vitro release of EPM from polymersomes was clearly sustained in all the time tested for this purpose. The sustained release of drug was hypothetically due to the entrapment of EPM in core of polymersomes. Polymersomes also showed acceptable stability for long periods of time. Conclusion: The results indicate the successful formulation of EPM loaded m-PEG/PCL polymersomes. Overall, the results was showed that m-PEG-PCL polymersomes can be considered as a promising carrier for hydrophilic drugs such as EPM.
期刊介绍:
Iranian Journal of Pharmaceutical Sciences (IJPS) is an open access, internationally peer-reviewed journal that seeks to publish research articles in different pharmaceutical sciences subdivisions: pharmacology and toxicology, nanotechnology, pharmaceutics, natural products, biotechnology, pharmaceutical chemistry, clinical pharmacy and other pharmacy related topics. Each issue of the journal contents 16 outstanding research articles in area of pharmaceutical sciences plus an editorial written by the IJPS editors on one of the most up to date advances topics in pharmacy. All articles published by IJPS would be permanently accessible online freely without any subscription charges. Authors of the published articles have granted the right to use and disseminate their article to third parties.