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Nanoparticles of quaternized chitosan derivatives as a carrier for colon delivery of insulin: ex vivo and in vivo studies.
Int J Pharm. 2008 May 22; 356(1-2):259-66.IJ

Abstract

The aim of the present study was to develop insulin nanoparticulate systems by using chitosan (CS), triethylchitosan (TEC) and dimethyl-ethylchitosan (DMEC, a new quaternized derivative of chitosan) for colon delivery. The nanoparticles were prepared by the polyelectrolyte complexation (PEC) method. Particle size distribution, zeta potential and polydispersity index of the nanoparticles were determined using dynamic light scattering technique. Transmission electron microscopy (TEM) was also used to observe the morphology of the nanoparticles. It was found that the nanoparticles carried positive charges and showed a size distribution in the range of 170-270 nm with spherical morphology and smooth surface structure. The amount of insulin loaded into the nanoparticles was determined by measuring the association efficiency and also the content of insulin in the nanoparticles. Insulin loading was found to be more than 80% for all of the nanoparticles. In vitro release studies showed a small burst effect at the beginning and then a sustained release characteristic for 5h. Ex vivo investigations revealed better insulin transport across the colon membrane of rats for nanoparticles made with quaternized derivatives than those made of chitosan. In vivo studies in rats have showed enhanced colon absorption of insulin by using these nanoparticles compared to free insulin in diabetic rats. The insulin absorption from the rat's colon was evaluated by its hypoglycemic effect.

Authors+Show Affiliations

Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

18289808

Citation

Bayat, Akbar, et al. "Nanoparticles of Quaternized Chitosan Derivatives as a Carrier for Colon Delivery of Insulin: Ex Vivo and in Vivo Studies." International Journal of Pharmaceutics, vol. 356, no. 1-2, 2008, pp. 259-66.
Bayat A, Dorkoosh FA, Dehpour AR, et al. Nanoparticles of quaternized chitosan derivatives as a carrier for colon delivery of insulin: ex vivo and in vivo studies. Int J Pharm. 2008;356(1-2):259-66.
Bayat, A., Dorkoosh, F. A., Dehpour, A. R., Moezi, L., Larijani, B., Junginger, H. E., & Rafiee-Tehrani, M. (2008). Nanoparticles of quaternized chitosan derivatives as a carrier for colon delivery of insulin: ex vivo and in vivo studies. International Journal of Pharmaceutics, 356(1-2), 259-66. https://doi.org/10.1016/j.ijpharm.2007.12.037
Bayat A, et al. Nanoparticles of Quaternized Chitosan Derivatives as a Carrier for Colon Delivery of Insulin: Ex Vivo and in Vivo Studies. Int J Pharm. 2008 May 22;356(1-2):259-66. PubMed PMID: 18289808.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Nanoparticles of quaternized chitosan derivatives as a carrier for colon delivery of insulin: ex vivo and in vivo studies. AU - Bayat,Akbar, AU - Dorkoosh,Farid A, AU - Dehpour,Ahmad Reza, AU - Moezi,Leila, AU - Larijani,Bagher, AU - Junginger,Hans E, AU - Rafiee-Tehrani,Morteza, Y1 - 2008/01/05/ PY - 2007/09/18/received PY - 2007/11/14/revised PY - 2007/12/18/accepted PY - 2008/2/22/pubmed PY - 2008/8/19/medline PY - 2008/2/22/entrez SP - 259 EP - 66 JF - International journal of pharmaceutics JO - Int J Pharm VL - 356 IS - 1-2 N2 - The aim of the present study was to develop insulin nanoparticulate systems by using chitosan (CS), triethylchitosan (TEC) and dimethyl-ethylchitosan (DMEC, a new quaternized derivative of chitosan) for colon delivery. The nanoparticles were prepared by the polyelectrolyte complexation (PEC) method. Particle size distribution, zeta potential and polydispersity index of the nanoparticles were determined using dynamic light scattering technique. Transmission electron microscopy (TEM) was also used to observe the morphology of the nanoparticles. It was found that the nanoparticles carried positive charges and showed a size distribution in the range of 170-270 nm with spherical morphology and smooth surface structure. The amount of insulin loaded into the nanoparticles was determined by measuring the association efficiency and also the content of insulin in the nanoparticles. Insulin loading was found to be more than 80% for all of the nanoparticles. In vitro release studies showed a small burst effect at the beginning and then a sustained release characteristic for 5h. Ex vivo investigations revealed better insulin transport across the colon membrane of rats for nanoparticles made with quaternized derivatives than those made of chitosan. In vivo studies in rats have showed enhanced colon absorption of insulin by using these nanoparticles compared to free insulin in diabetic rats. The insulin absorption from the rat's colon was evaluated by its hypoglycemic effect. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/18289808/Nanoparticles_of_quaternized_chitosan_derivatives_as_a_carrier_for_colon_delivery_of_insulin:_ex_vivo_and_in_vivo_studies_ DB - PRIME DP - Unbound Medicine ER -