Nano-in-Micro Delivery System Prepared by Co-Axial Air Flow for Oral Delivery of Conjugated Linoleic Acid.

ABSTRACT

The preparation of a nano-in-micro delivery system (NiMDS) under mild conditions without using toxic organic solvents and expensive equipment still faces challenges. In this study, we introduced the co-axial air flow method to prepare NiMDS for the oral delivery of conjugated linoleic acid (CLA). The chitosan nanoparticles were prepared using the stearic-acid-modified chitosan through self-aggregation. Then, the chitosan nanoparticles were incorporated into alginate microparticles by the co-axial air flow method. The obtained chitosan nanoparticles and NiMDS were spherical in shape with the average sizes of 221⁻243 nm and 130⁻160 µm, respectively. Compared with alginate microparticles, the hybrid particles were of fewer fragments, were bigger in size, had a higher mechanical strength, and showed a controlled release in the phosphate buffer solution (pH 1.2 or 7.4). The release kinetics study showed that encapsulating the chitosan nanoparticles into the alginate microparticles inhibited the dissolution of alginate microparticles at the initial stage. These results revealed the potential of NiMDS as an ideal oral carrier for the sustained release of CLA in the gastrointestinal environment.