Influence of the surface properties of nanocapsules on their interaction with intestinal barriers

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Abstract

Despite the convenience of the oral route for drug administration, the existence of different physiological barriers associated with the intestinal tract greatly lowers the bioavailability of many active compounds. We have previously suggested the potential polymeric nanocapsules, consisting of an oily core surrounded by a polymer shell, as oral drug delivery carriers. Here we present a systematic study of the influence of the surface properties of these nanocapsules on their interaction with the intestinal barriers. Two different surfactants, Pluronic®F68 (PF68) and F127 (PF127), and two polymeric shells, chitosan (CS) and polyarginine (PARG) were chosen for the formulation of the nanocapsules. We analyzed nine different combinations of these polymers and surfactants, and studied the effect of each specific combination on their colloidal stability, enzymatic degradation, and mucoadhesion/mucodiffusion. Our results indicate that both, the polymer shell and the surfactants located at the oil/water interface, influence the interaction of the nanocapsules with the intestinal barriers. More interestingly, according to our observations, the shell components of the nanosystems may have either synergic or disruptive effects on their capacity to overcome the intestinal barriers

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Irene Santalices, Dolores Torres, Mª Victoria Lozano, Mª Mar Arroyo-Jiménez, María José Alonso, Manuel J. Santander-Ortega, Influence of the surface properties of nanocapsules on their interaction with intestinal barriers, European Journal of Pharmaceutics and Biopharmaceutics, Volume 133, 2018, Pages 203-213

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The authors acknowledge financial support from the TRANS‐INT European Consortium −FP7, under grant agreement No. 281035 and the Xunta de Galicia (Competitive Reference Groups ‐FEDER Funds; Ref 2014/043). Irene Santalices acknowledges a predoctoral grant from the FPU program (No. FPU13/02015) from the Ministry of Education, Culture and Sports, MECD, Spain. The authors acknowledge Servier for providing Servier Medical Art (http://smart.servier.com/), being the small intestine, intestinal villi and laboratory material and equipment (https://creativecommons.org/licenses/by/3.0/) modified from the original work and used for the creation of the graphical abstract and Figure 1.

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CC BY-NC-ND