Multi-responsive starch-based nanocapsules for colon-targeting delivery of peptides: In vitro and in vivo evaluation.

Colon-targeting delivery of insulin is surging great interests in revolutionizing diabetes. Herein, insulin-loaded starch-based nanocapsules developed by layer-by-layer self-assembly technology were rationally structured. Interactions between starches and the structural changes of the nanocapsules were unraveled to understand in vitro and in vivo insulin release properties. By increasing the deposition layers of starches, the structural compactness of nanocapsules increased and in turn retarded insulin release in the upper gastrointestinal tract. Spherical nanocapsules deposited at least five layers of starches could deliver insulin to the colon in a high efficiency according to the in vitro and in vivo insulin release performance. The underlying mechanism of the insulin colon-targeting release should ascribe to the suitable changes in compactness of the nanocapsules and the interactions between deposited starches after multi-response to the changes in pH, time and enzymes in gastrointestinal tract. Starch molecules interacted with each other much stronger at the intestine than that at the colon, which guaranteed a compact structure in the intestine but a loose structure in the colon for the colon-targeting nanocapsules. It suggested that rather than controlling the deposition layer of the nanocapsules, controlling the interaction between starches could also regulate the structures of the nanocapsules for colon-targeting delivery system.

In vitro digestibility and structural control of rice starch-unsaturated fatty acid complexes by high-pressure homogenization.

This study emphasized on structural alteration of rice starch-unsaturated fatty acid complexes by adding trans-2-dodecaenoic acid (t12), trans-oleic acid (t18), cis-oleic acid (c18) and linoleic acid (loa) with different concentration under high-pressure homogenization treatment, and further illustrated the underlying mechanism of modulating digestibility. Results showed that the complex primarily presented as V6 or type IIa polymorph; complex index, content of ordered structure and thermal stability appeared to be positively correlated to the concentration of unsaturated fatty acids. t12 was too mobile to form single helix, leading to the formation of loose matrix; t18 fitted better within the cavity of starch than c18, and formed structural domain with higher compactness and thermal stability; Rloa had lower complex index but higher degree of short-range order, and tended to form alternating amorphous and crystalline structure. The digestibility was higher in the order of Rloa, Rt18, Rc18 and Rt12.