Development of chitosan coated calcium-alginate nanocapsules for oral delivery of liraglutide to diabetic patients

摘要

Increasing prevalence, variable pathogenesis and naturalhistory of progressive type II diabetes, highlight the necessityof immediate development of new therapeutic strategiesGlucagon-like peptide-1 receptor agonists are a new class ofinjectable antidiabetic drugs. Chitosan coated calcium-alginate nanocapsules were developed for oral sustaineddelivery of liraglutide, a long-acting analog of glucagon likepeptid-1. The aim of such drug delivery system is to recoverdiabetic patient compliance which otherwise demandsprolonged repeatedly injections. The effect of coatingcomponents including sodium alginate, calcium chloride andchitosan concentrations on the particle size was studied basedon response surface methodology. The beads werecharacterized through dynamic light scattering (DLS),scanning and transmission electron microscopy (SEM andTEM) as well as fourier transform infrared spectroscopy(FTIR). It was shown that the diameter of the formed beadswas most dependent on the encapsulation technique andalginate concentration. SEM revealed spherical and smoothparticles of up to 100 nm diameter for optimum compositionof alginate 0.5%, chitosan 0.5% and calcium chloride 0.5%in the ratio of 3:1:1. The resulting bead formulation had aloading efficiency of 92.5% and loading capacity of 54.16 %.In-vitro release studies in simulated gastrointestinalconditions were carried out in a sequential technique and theamount of drug release was found to be 39.1% after 8 hours.