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Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin.
Eur J Pharm Biopharm. 2011 Jan; 77(1):11-9.EJ

Abstract

The 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 (∼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.

Authors+Show Affiliations

National Key Lab of Biochemical Engineering, Institute of Process Engineering, Chinese Academy of Sciences, Beijing, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Evaluation Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20933083

Citation

Zhang, Yueling, et al. "Preparation and Evaluation of Alginate-chitosan Microspheres for Oral Delivery of Insulin." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 77, no. 1, 2011, pp. 11-9.
Zhang Y, Wei W, Lv P, et al. Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin. Eur J Pharm Biopharm. 2011;77(1):11-9.
Zhang, Y., Wei, W., Lv, P., Wang, L., & Ma, G. (2011). Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 77(1), 11-9. https://doi.org/10.1016/j.ejpb.2010.09.016
Zhang Y, et al. Preparation and Evaluation of Alginate-chitosan Microspheres for Oral Delivery of Insulin. Eur J Pharm Biopharm. 2011;77(1):11-9. PubMed PMID: 20933083.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and evaluation of alginate-chitosan microspheres for oral delivery of insulin. AU - Zhang,Yueling, AU - Wei,Wei, AU - Lv,Piping, AU - Wang,Lianyan, AU - Ma,Guanghui, Y1 - 2010/10/07/ PY - 2010/05/28/received PY - 2010/09/15/revised PY - 2010/09/29/accepted PY - 2010/10/12/entrez PY - 2010/10/12/pubmed PY - 2011/5/6/medline SP - 11 EP - 9 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 77 IS - 1 N2 - The 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 (∼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. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/20933083/Preparation_and_evaluation_of_alginate_chitosan_microspheres_for_oral_delivery_of_insulin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(10)00259-6 DB - PRIME DP - Unbound Medicine ER -