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Augmenting Therapeutic Potential of Polyphenols by Hydrogen-Bonding Complexation for the Treatment of Acute Lung Inflammation
journal contribution
posted on 2020-08-05, 20:17 authored by Zhicheng Le, Zhijia Liu, Lilong Sun, Lixin Liu, Yongming ChenDysregulated
inflammation is considered as an essential pathological
process in inflammation-associated diseases, which would be aggravated
by high levels of reactive oxygen species (ROS) generation inducing
oxidative stress. Currently, extensive attention has been paid to
polyphenolic compounds owing to their broad spectrum biological activities,
such as antioxidant and anti-inflammatory effects, while their therapeutic
potential has been compromised by the poor stability, short plasma
half-life, and low bioavailability. Given that polyphenols have a
wide range of structural characteristics and various physicochemical
properties, there remains a real challenge toward green, mass production
of universal nanocarriers for effective entrapment of these active
pharmaceutical ingredients. In this study, we adopted a flash nanocomplexation
(FNC) platform to prepare nanocomplexes comprising polyphenols and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)
enabled by hydrogen bonding. We confirmed that the molecular structure
of polyphenols has a great influence on their complexation with TPGS,
and stable nanocomplexes were formed when the number of phenolic hydroxyl
groups of polyphenols was above the value of 8. These hydrogen-bonded
nanocomplexes produced by an FNC apparatus exhibited well-controlled
quality with uniform size, good colloidal stability, and high batch-to-batch
repeatability, thus improving the druggability as potent nanotherapeutics
for antioxidant and anti-inflammatory applications. In vivo experiments indicated that the optimal nanocomplex (EGCG-NC) can
be applied to ameliorate acute lung injury in a mice model after nasal
administration. These results proved that polyphenols formulated with
TPGS for nanocomplex formation through hydrogen-bonding complexation
could augment their therapeutic potential for modulating hyperactive
inflammation in the treatment of acute lung inflammation.
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EGCG-NCstabilitylung injuryhydrogen-bonding complexationlung inflammationmass productionphenolic hydroxyl groupsAugmenting TherapeuticAcute Lung Inflammation Dysregulate...mice modelbatch-to-batch repeatabilityROSreactive oxygen speciesantioxidantanti-inflammatory applicationsuniform sizeinflammation-associated diseases-α-tocopheryl polyethylene glycol 1...FNC apparatusoxidative stressphysicochemical propertiesnanocomplex formationvivo experimentsflash nanocomplexationpolyphenolic compoundsanti-inflammatory effectsplasma half-lifeHydrogen-Bonding ComplexationTPGShydrogen-bonded nanocomplexeswell-controlled quality
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