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Oral delivery of insulin from alginate/chitosan crosslinked by glutaraldehyde.
Int J Biol Macromol. 2013 Jul; 58:160-8.IJ

Abstract

Insulin is mainly administered via subcutaneous route by injection which is the cause of painful and possible infections. Oral insulin administration would present a more convenient form of application because it is less invasive. Oral delivery of insulin to the gastrointestinal tract is one of the most challenging issues, because it numerous barriers to overcome in order to create an effective system for insulin delivery. In the present study, insulin-loaded alginate/chitosan blend gel beads were prepared with different mass ratios. Chitosan was depolymerized by gamma irradiation at a dose of 80 kGy reducing its molecular weight for ideal blend with sodium alginate. The homogeneous solution of alginate and chitosan was dripped into CaCl2 solution (2%), the resultant calcium crosslinked beads were dipped in glutaraldehyde (2%) solution sequentially to prepare dual crosslinked beads with improved mechanical properties so as to withstand the simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). Morphological structure, FTIR analysis, thermogravimetry analysis, specific surface area, gel fraction, swelling kinetics in SGF and SIF, loading efficiency, insulin release behavior, mucoadhesivity of the alginate/chitosan beads were investigated. The cumulative insulin release of pure alginate beads (10:0) reached as maximum level 100% in 3h after they were dipped in SIF. Concerning the beads Alg/Chi (8:2), Alg/Chi (7:3) and Alg/Chi (6:4) the cumulative release of insulin reached 90.5%, 89.2% and 70.2%, respectively in 6h. The rate of 100% was reached after 24h for Alg/Chi (8:2), Alg/Chi (7:3) and after 73 h for Alg/Chi (6:4). The presence of chitosan in the blend beads decreased the cumulative insulin release in gastric media and enhanced behavior of alginate/chitosan beads in intestinal medium due to the crosslinking. The alginate/chitosan beads crosslinked by glutaraldehyde may be considered as potential insulin carriers for oral drug delivery system.

Authors+Show Affiliations

Department of Irradiation Technology, Nuclear Research Center of Algiers, Algiers, Algeria. tahtatdja@yahoo.frNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

23567292

Citation

Tahtat, Djamel, et al. "Oral Delivery of Insulin From Alginate/chitosan Crosslinked By Glutaraldehyde." International Journal of Biological Macromolecules, vol. 58, 2013, pp. 160-8.
Tahtat D, Mahlous M, Benamer S, et al. Oral delivery of insulin from alginate/chitosan crosslinked by glutaraldehyde. Int J Biol Macromol. 2013;58:160-8.
Tahtat, D., Mahlous, M., Benamer, S., Khodja, A. N., Oussedik-Oumehdi, H., & Laraba-Djebari, F. (2013). Oral delivery of insulin from alginate/chitosan crosslinked by glutaraldehyde. International Journal of Biological Macromolecules, 58, 160-8. https://doi.org/10.1016/j.ijbiomac.2013.03.064
Tahtat D, et al. Oral Delivery of Insulin From Alginate/chitosan Crosslinked By Glutaraldehyde. Int J Biol Macromol. 2013;58:160-8. PubMed PMID: 23567292.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Oral delivery of insulin from alginate/chitosan crosslinked by glutaraldehyde. AU - Tahtat,Djamel, AU - Mahlous,Mohamed, AU - Benamer,Samah, AU - Khodja,Assia Nacer, AU - Oussedik-Oumehdi,Habiba, AU - Laraba-Djebari,Fatima, Y1 - 2013/04/06/ PY - 2012/12/31/received PY - 2013/02/28/revised PY - 2013/03/28/accepted PY - 2013/4/10/entrez PY - 2013/4/10/pubmed PY - 2014/1/3/medline SP - 160 EP - 8 JF - International journal of biological macromolecules JO - Int J Biol Macromol VL - 58 N2 - Insulin is mainly administered via subcutaneous route by injection which is the cause of painful and possible infections. Oral insulin administration would present a more convenient form of application because it is less invasive. Oral delivery of insulin to the gastrointestinal tract is one of the most challenging issues, because it numerous barriers to overcome in order to create an effective system for insulin delivery. In the present study, insulin-loaded alginate/chitosan blend gel beads were prepared with different mass ratios. Chitosan was depolymerized by gamma irradiation at a dose of 80 kGy reducing its molecular weight for ideal blend with sodium alginate. The homogeneous solution of alginate and chitosan was dripped into CaCl2 solution (2%), the resultant calcium crosslinked beads were dipped in glutaraldehyde (2%) solution sequentially to prepare dual crosslinked beads with improved mechanical properties so as to withstand the simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). Morphological structure, FTIR analysis, thermogravimetry analysis, specific surface area, gel fraction, swelling kinetics in SGF and SIF, loading efficiency, insulin release behavior, mucoadhesivity of the alginate/chitosan beads were investigated. The cumulative insulin release of pure alginate beads (10:0) reached as maximum level 100% in 3h after they were dipped in SIF. Concerning the beads Alg/Chi (8:2), Alg/Chi (7:3) and Alg/Chi (6:4) the cumulative release of insulin reached 90.5%, 89.2% and 70.2%, respectively in 6h. The rate of 100% was reached after 24h for Alg/Chi (8:2), Alg/Chi (7:3) and after 73 h for Alg/Chi (6:4). The presence of chitosan in the blend beads decreased the cumulative insulin release in gastric media and enhanced behavior of alginate/chitosan beads in intestinal medium due to the crosslinking. The alginate/chitosan beads crosslinked by glutaraldehyde may be considered as potential insulin carriers for oral drug delivery system. SN - 1879-0003 UR - https://www.unboundmedicine.com/medline/citation/23567292/Oral_delivery_of_insulin_from_alginate/chitosan_crosslinked_by_glutaraldehyde_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0141-8130(13)00164-5 DB - PRIME DP - Unbound Medicine ER -