Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Millotti, G; Laffleur, F; Perera, G; Vigl, C; Pickl, K; Sinner, F; Bernkop-Schnürch, A.
In vivo evaluation of thiolated chitosan tablets for oral insulin delivery.
J Pharm Sci. 2014; 103(10):3165-3170
Doi: 10.1002/jps.24102
Web of Science
PubMed
FullText
FullText_MUG
- Co-Autor*innen der Med Uni Graz
- Sinner Frank Michael
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- Abstract:
- Chitosan-6-mercaptonicotinic acid (chitosan-6-MNA) is a thiolated chitosan with strong mucoadhesive properties and a pH-independent reactivity. This study aimed to evaluate the in vivo potential for the oral delivery of insulin. The comparison of the nonconjugated chitosan and chitosan-6-MNA was performed on several studies such as mucoadhesion, release, and in vivo studies. Thiolated chitosan formulations were both about 80-fold more mucoadhesive compared with unmodified ones. The thiolated chitosan tablets showed a sustained release for 5 h for the polymer of 20 kDa and 8 h for the polymer of 400 kDa. Human insulin was quantified in rats' plasma by means of ELISA specific for human insulin with no cross-reactivity with the endogenous insulin. In vivo results showed thiolation having a tremendous impact on the absorption of insulin. The absolute bioavailabilities were 0.73% for chitosan-6-MNA of 20 kDa and 0.62% for chitosan-6-MNA 400 kDa. The areas under the concentration-time curves (AUC) of chitosan-6-MNA formulations compared with unmodified chitosan were 4.8-fold improved for the polymer of 20 kDa and 21.02-fold improved for the polymer of 400 kDa. The improvement in the AUC with regard to the most promising aliphatic thiomer was up to 6.8-fold. Therefore, chitosan-6-MNA represents a promising excipient for the oral delivery of insulin. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.
- Find related publications in this database (using NLM MeSH Indexing)
- Administration, Oral -
- Animals -
- Chitosan - administration & dosage
- Chitosan - chemistry
- Insulin - administration & dosage
- Male -
- Rats -
- Rats, Wistar -
- Sulfhydryl Compounds - chemistry
- Tablets -
- Find related publications in this database (Keywords)
- Bioavailability
- oral drug delivery
- chitosan
- in vivo
- in vitro corrlations (IVIC)
- Polymeric drug delivery systems
- solid dosage forms
- thiolated chitosan
- mucoadhesion
- drug release
- oral delivery of insulin in vivo studies