Tf ligand-receptor-mediated exenatide-Zn2+ complex oral-delivery system for penetration enhancement of exenatide

Autor:	Youxin Li, Yina Song, Kaoxiang Sun, Yanan Shi, Xuemei Zhang, Liping Zhang, Dongyu Duan
Rok vydání:	2018
Předmět:	inorganic chemicals 0301 basic medicine chemistry.chemical_classification Chemistry technology industry and agriculture Pharmaceutical Science 02 engineering and technology Pharmacology 021001 nanoscience & nanotechnology In vitro Bioavailability 03 medical and health sciences Subcutaneous injection 030104 developmental biology Pharmacokinetics In vivo Oral administration Transferrin medicine 0210 nano-technology Exenatide medicine.drug
Zdroj:	Journal of Drug Targeting. 26:931-940
ISSN:	1029-2330 1061-186X
Popis:	Safe and effective oral delivery of peptide is a challenge. Here, we used exenatide and zinc ions (Zn2+) to form a complex to explore a meaningful oral-targeted drug-delivery system. Polyethylene glycol-poly(lactic acid-co-glycolic acid) (PEG-PLGA) was used to prepare nanoparticles (NPs) to escape the degradation caused by gastrointestinal enzymes. Transferrin (Tf) was used as a targeting group. PEG-PLGA-NPs and Tf-modified exenatide-Zn2+-loaded NPs (Tf-PEG-PLGA-NPs) were uniformly sized spheres according to transmission electron microscopy. The results of pharmacodynamic and pharmacokinetic investigations in vivo were consistent with in vitro studies using Caco-2 cells. Tf enhanced NPs transport in cell-uptake and transmembrane-transport experiments. Our results showed that the relative bioavailability of Tf-exenatide-Zn2+-NPs was higher than that of exenatide-Zn2+-NPs. The relative bioavailability of Tf-exenatide-Zn2+-NPs versus subcutaneous injection of exenatide was 6.45%. This was a preliminary exploration of the oral administration of exenatide, that data from which can be used for future investigations.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::4faa5ec6bbcf154030618ef7aff7913a https://doi.org/10.1080/1061186x.2018.1455839 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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