首页|β-Lactoglobulin stabilized lipid nanoparticles enhance oral absorption of insulin by slowing down lipolysis

β-Lactoglobulin stabilized lipid nanoparticles enhance oral absorption of insulin by slowing down lipolysis

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Lipid-based nanocarriers have staged a remarkable comeback in the oral delivery of proteins and pep-tides,but delivery efficiency is compromised by lipolysis.β-Lactoglobulin(β-lg)stabilized lipid nanopar-ticles,including nanoemulsions(NE@β-lg)and nanocapsules(NC@β-lg),were developed to enhance the oral absorption of insulin by slowing down lipolysis due to the protection from β-lg.Cremophor EL sta-bilized nanoemulsions(NE@Cre-EL)were prepared and set as a control.The lipid nanoparticles produced mild and sustained hypoglycemic effects,amounting to oral bioavailability of 3.0％±0.3％,7.0％±1.1％,and 7.7％±0.8％for NE@Cre-EL,NE@β-lg,and NC@β-lg,respectively.Aggregation-caused quenching(ACQ)probes enabled the identification of intact nanoparticles,which were used to investigate the in vivo and intracellular fates of the lipid nanoparticles.In vitro digestion/lipolysis and ex vivo imaging confirmed de-layed lipolysis from β-lg stabilized lipid nanoparticles.NC@β-lg was more resistant to intestinal lipolysis than NE@β-lg due to the Ca2+-induced crosslinking.Live imaging revealed the transepithelial transport of intact nanoparticles and their accumulation in the liver.Cellular studies confirmed the uptake of intact nanoparticles.Slowing down lipolysis via food proteins represents a good strategy to enhance the oral absorption of lipid nanoparticles and thus co-formulated biomacromolecules.

β-LactoglobulinLipid nanoparticlesOral absorptionInsulinLipolysisAggregation-caused quenching

Lu Li、Suticha Chunta、Xianzi Zheng、Haisheng He、Wei Wu、Yi Lu

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School of Pharmacy & Key Laboratory of Smart Drug Delivery of MOE,Fudan University,Shanghai 201203,China

Department of Clinical Chemistry,Faculty of Medical Technology,Prince of Songkla University,Songkhla 90110,Thailand

Shanghai Skin Disease Hospital,Tongji University School of Medicine,Shanghai 200433,China

Fudan Zhangjiang Institute,Shanghai 201203,China

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Science and Technology Com-mittee of Shanghai MunicipalityScience and Technology Com-mittee of Shanghai MunicipalityScience and Technology Com-mittee of Shanghai MunicipalityScience and Technology Com-mittee of Shanghai Municipality国家自然科学基金国家自然科学基金

1943074140023S1190150023ZR1413100214307608008197324782030107

2024

10.1016/j.cclet.2023.108662

中国化学快报(英文版)
中国化学会

中国化学快报(英文版)

CSTPCD
影响因子：0.771
ISSN：1001-8417
年,卷(期)：2024.35(4)
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