CNR ExploRA

Articolo in rivista, 2020, ENM, 10.3390/pharmaceutics12010060

Zein Beta-Cyclodextrin Micropowders for Iron Bisglycinate Delivery

Diletta Esposito , Giovanni Dal Poggetto , Aurélie Demont, Nicolai Kraut, Agnese Miro, Francesca Ungaro, Paola Laurienzo and Fabiana Quaglia

Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Via Domenico Montesano 49, 80131 Napoli, Italy; Institute for Polymers, Composites and Biomaterials CNR, Via Campi Flegrei 34, 80078 Pozzuoli, Italy; BÜCHI Labortechnik AG, Meierseggstrasse 40, 9230 Flawil, Switzerland

Given the limited number of materials available to design delivery platforms for nutrients, the rational combination of raw materials already approved as food ingredients and their processing through nano-micro technology can offer a unique tool for innovation. Here,we propose a nano-in-micro strategy to produce powders based on the hydrophobic protein zein, useful for the oral delivery of a hydrophilic iron source (iron bisglycinate) in anaemic patients. Iron-loaded powders were prepared through a two-step strategy consisting in the formation of a zein pseudolatex followed by a spray-drying step. To extend the manipulation space for zein and entrap iron bisglycinate, -cyclodextrin (CD) was selected as helping excipient. Addition of CD allowed iron loading in the pseudolatex and greatly increased product yields after the drying process as compared to zein alone. Iron-loaded micro-sized powders were characterised by attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectra, thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC) to elucidate the role of CD as a compatibilizer for the zein-iron system. Remarkably, micropowders released only 20% of FeBIS in a simulated gastric fluid, whereas release in a simulated intestinal fluid was almost completed in 7 h. In summary, CD association to zein is a novel strategy to expand applications in the oral delivery of iron bisglycinate and, prospectively, to micronutrient chelates.

Pharmaceutics 12