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.

Highlights

  • Micro- or nano-sized particles have found numerous applications as oral delivery vehicles for lipid nutraceuticals

  • As the lining of fatty core were used to increase water dispersion of conjugated linoleic acid (CLA), CLA-loaded nanoparticles the digestive tract is aqueous in nature, to be assimilated, it is important to enhance the water were encapsulated into the alginate microparticles to achieve a controlled release in the stomach and dispersion of lipid nutraceuticals

  • 95% for for all all groups groups when when the the concentrations concentrations of of nano, nano, micro, micro, nano-in-micro nano-in-micro particles ranged from from5050toto μg/mL, was no difference in cell viability particles ranged μg/mL, and and therethere was no difference in cell viability betweenbetween chitosan chitosan nanoparticles, alginate microparticles and the

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Summary

Introduction

Micro- or nano-sized particles have found numerous applications as oral delivery vehicles for lipid nutraceuticals. Hybrid matrix is Conjugated acid (CLA), a family of the essential fattyalginate–chitosan acids for humans, is aof great good candidate for the controlled release of the lipid nutraceuticals in the gastrointestinal importance in health and disease prevention [11]. It induces diverse biological activities in humans environment [9,10]. As the lining of fatty core were used to increase water dispersion of CLA, CLA-loaded nanoparticles the digestive tract is aqueous in nature, to be assimilated, it is important to enhance the water were encapsulated into the alginate microparticles to achieve a controlled release in the stomach and dispersion of lipid nutraceuticals.

Results and of Discussion
Characterization of Chitosanconcentration
In Vitro Release Studies of Loaded CLA
Release Kinetics
Materials
Synthesis and Characterization of Amphiphilic Chitosan
Preparation of CLA-Loaded Nanoparticles
Preparation of CLA-Loaded NiMDS
Characterization of Nanoparticles and NiMDS
CLA Loading Efficiency and Loading Capacity
In Vitro Release Study
In Vitro Cytotoxicity Assay
Conclusions
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