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Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin
Zhang, Yueling1,2; Wei, Wei1,2; Lv, Piping1,2; Wang, Lianyan1; Ma, Guanghui1; Ma, GH
2011
Source PublicationEUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
ISSN0939-6411
Volume77Issue:1Pages:11-19
AbstractThe alginate-chitosan microspheres with narrow size distribution were prepared by membrane emulsification technique in combination with ion (Ca(2+)) and polymer (chitosan) solidification. The preparation procedure was observed, and the physical properties (particle size distribution, surface morphology, chitosan distribution, zeta potential) of the microspheres were characterized. Subsequently, the microspheres were employed to load model peptide of insulin. The effect of loading ways on the loading efficiency and immunological activity of insulin were investigated. It was shown that the higher loading efficiency (56.7%) and remarkable activity maintenance (99.4%) were obtained when the insulin was loaded during the chitosan solidification process (Method B). Afterward, the release profile in vitro for the optimal insulin-loaded microspheres was investigated. Under the pH conditions of gastrointestinal environment, only 32% of insulin released during the simulated transit time of drug (2 h in the stomach and 4 h in the intestinal). While under the pH condition of blood environment, insulin release was stable and sustained for a long time (14 days). Furthermore, the chemical stability of insulin released from the microspheres was well preserved after they were treated with the simulated gastric fluid containing pepsin for 2 h. Finally, the blood glucose level of diabetic rats could be effectively reduced and stably kept for a long time (similar to 60 h) after oral administration of the insulin-loaded alginate-chitosan microspheres. Therefore, the alginate-chitosan microspheres were found to be promising vectors showing a good efficiency in oral administration of protein or peptide drugs. (C) 2010 Elsevier B.V. All rights reserved.
KeywordNarrow Size Distribution Alginate-chitosan Microspheres Protein Or Peptide Oral Administration Insulin Sustained Release
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
DOI10.1016/j.ejpb.2010.09.016
Indexed BySCI
Language英语
WOS KeywordDRUG-DELIVERY ; PROTEIN DRUGS ; CONTROLLED-RELEASE ; INTERNAL GELATION ; SODIUM ALGINATE ; GEL BEADS ; CARRIER ; PEPTIDE ; SYSTEM ; RAT
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000286687500003
Citation statistics
Cited Times:168[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Version出版稿
Identifierhttp://ir.ipe.ac.cn/handle/122111/5387
Collection生化工程国家重点实验室
Corresponding AuthorMa, GH
Affiliation1.Chinese Acad Sci, Inst Proc Engn, Natl Key Lab Biochem Engn, Beijing, Peoples R China
2.Chinese Acad Sci, Grad Univ, Beijing, Peoples R China
Recommended Citation
GB/T 7714
Zhang, Yueling,Wei, Wei,Lv, Piping,et al. Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin[J]. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,2011,77(1):11-19.
APA Zhang, Yueling,Wei, Wei,Lv, Piping,Wang, Lianyan,Ma, Guanghui,&Ma, GH.(2011).Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin.EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,77(1),11-19.
MLA Zhang, Yueling,et al."Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin".EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS 77.1(2011):11-19.
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