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Merck

Complex Polysaccharide-Based Nanocomposites for Oral Insulin Delivery.

Marine drugs (2020-01-19)
Mar Collado-González, M Cristina Ferreri, Alessandra R Freitas, Ana Cláudia Santos, Nuno R Ferreira, Guzmán Carissimi, Joana A D Sequeira, F Guillermo Díaz Baños, Gloria Villora, Francisco Veiga, Antonio Ribeiro
ABSTRACT

Polyelectrolyte nanocomposites rarely reach a stable state and aggregation often occurs. Here, we report the synthesis of nanocomposites for the oral delivery of insulin composed of alginate, dextran sulfate, poly-(ethylene glycol) 4000, poloxamer 188, chitosan, and bovine serum albumin. The nanocomposites were obtained by Ca2+-induced gelation of alginate followed by an electrostatic-interaction process among the polyelectrolytes. Chitosan seemed to be essential for the final size of the nanocomposites and there was an optimal content that led to the synthesis of nanocomposites of 400-600 nm hydrodynamic size. The enhanced stability of the synthesized nanocomposites was assessed with LUMiSizer after synthesis. Nanocomposite stability over time and under variations of ionic strength and pH were assessed with dynamic light scattering. The rounded shapes of nanocomposites were confirmed by scanning electron microscopy. After loading with insulin, analysis by HPLC revealed complete drug release under physiologically simulated conditions.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Chitosan, low molecular weight
Sigma-Aldrich
Chitosan, medium molecular weight
Sigma-Aldrich
Bovine Serum Albumin, chromatographically purified, New Zealand origin, low endotoxin, suitable for cell culture, pH 7, ≥98%
Sigma-Aldrich
DL-Lactic acid, ~90% (T)