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pH-Responsive Emulsions with β‑Cyclodextrin/Vitamin E Assembled Shells for Controlled Delivery of Polyunsaturated Fatty Acids
journal contribution
posted on 2019-10-18, 15:43 authored by Yongkang Xi, Yuxiao Zou, Zhigang Luo, Liang Qi, Xuanxuan LuLipid-based
delivery systems (LBDSs) are widely applied in pharmaceuticals
and health care because of the increased bioavailability of lipophilic
components when they are coadministered with high-fat meals. However,
how to accurately control their in vivo release and stability is still
challenging. Here, after introducing the simple esterification and
coprecipitation, we created the dual-functional composite ODS-β-CD-VE
by the coassembly of β-cyclodextrin (β-CD), octadecenyl
succinic anhydride (ODSA), and vitamin E (VE). The resulting dual-functional
particle presented a uniform sheetlike shape and nanometer size. In
addition, its chemical structure was clarified in detail via nuclear
magnetic resonance (NMR), Fourier transform infrared spectroscopy
(FTIR), and X-ray diffraction (XRD). Benefiting from the antioxygenation
of VE, lipid oxidation in the ODS-β-CD-VE-stabilized Pickering
emulsion was effectively inhibited. Meanwhile, pH-induced protonation/deprotonation
of carboxyl groups guaranteed that the emulsions kept steady at pH
≤4 but were unsteady under neutral conditions. In this way,
the lipids contained in the emulsion were protected from gastric juice
and then digested and accurately released as n-3 polyunsaturated fatty
acids (PUFA) in the simulated intestine environment. This strategy
sheds some light on the rational and efficient construction of LBDSs
for nutrient supplements and even pharmaceuticals in a living digestive
tract.
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lipid oxidationvitamin EPUFAODS -β-CD Pickering emulsionLBDSuniform sheetlike shapeX-ray diffractionvivo releaseXRDn -3intestine environmentFTIRnanometer sizepharmaceuticalchemical structureODS -β-CDNMRODSAhealth carePolyunsaturated Fatty Acids Lipid-based delivery systemshigh-fat mealslipophilic componentsVEControlled Deliverycarboxyl groupsdual-functional particlepH-Responsive Emulsions
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