Simple but effective methods are required to incorporate multiple bioactive polyphenols into delivery systems to increase their dispersibility,stability and bioavailability.We developed and tested three p Hdriven prot...Simple but effective methods are required to incorporate multiple bioactive polyphenols into delivery systems to increase their dispersibility,stability and bioavailability.We developed and tested three p Hdriven protocols for creating nanoemulsions loaded with multiple lipophilic polyphenols.These protocols differed in how the different polyphenols were incorporated into the nanoemulsions.The impact of these three methods on the formation,properties,and gastrointestinal fate of nanoemulsions loaded with curcumin,resveratrol,and quercetin was investigated.The three methods produced nanoemulsions with similar initial particle properties:droplet diameters(0.15,0.16,and 0.15μm)and zeta-potentials(–59,–58,and–58 m V),respectively.However,the average encapsulation efficiencies(82%,88%,and 61%),gastrointestinal stabilities(83%,97%,and 29%)and bioaccessibilities(77%,90%,and 73%)for curcumin,resveratrol,and quercetin were somewhat different.In particular,more quercetin degradation occurred using the approach that held it under alkaline conditions for extended periods.In general,the p H-driven method provides researchers with a versatile approach of incorporating multiple polyphenols with different characteristics into functional food and beverages using a simple and inexpensive method.展开更多
尿石素A具有许多优良的生理活性,但其极低的水溶性和生物利用率限制了尿石素A的应用。为克服上述限制,该文采用pH驱动法结合高压均质技术制备尿石素A脂质体(urolithin A liposomes,UA-LPs),并考察其结构特性、稳定性及体外消化特性。结...尿石素A具有许多优良的生理活性,但其极低的水溶性和生物利用率限制了尿石素A的应用。为克服上述限制,该文采用pH驱动法结合高压均质技术制备尿石素A脂质体(urolithin A liposomes,UA-LPs),并考察其结构特性、稳定性及体外消化特性。结果表明,大豆卵磷脂为20 mg/mL所制得的UA-LPs的平均粒径为(97.46±0.83)nm,多分散系数为(0.27±0.01),Zeta电位为(-40.3±1.06)mV,包埋率为(98.11±0.26)%,负载率为(2.39±0.01)%。UA-LPs在原子力显微镜下为分布均匀的球状结构。热稳定性实验表明,不同大豆卵磷脂浓度的UA-LPs的包埋率均随热处理时间的延长有所下降,20 mg/mL的大豆卵磷脂制备的UA-LPs具有最好的热稳定性,其在80℃处理180 min后仍可保留45%的尿石素A,且粒径、多分散系数变化趋势较小。pH稳定性表明UA-LPs在酸性条件下包埋率较低,随着pH的升高,粒径、多分散系数变化不显著(P>0.05),20 mg/mL的大豆卵磷脂制备的UA-LPs的Zeta电位绝对值上升5.5,稳定性升高。体外模拟消化实验表明,UA-LPs能有效提高尿石素A的转化率以及生物可接受度,其中20 mg/mL大豆卵磷脂制备的UA-LPs的体外转化率相比游离的尿石素A增加了3.26倍,生物可接受度提高2.07倍。因此,利用pH驱动法可以成功制备出UA-LPs,且高大豆卵磷脂浓度的UA-LPs物理稳定性更好,以上研究结果为扩展尿石素A在食品工业及生物医药领域的应用提供依据。展开更多
Hemin is recognized as a superior biological iron-fortifier in the prevention and treatment of iron deficiency anemia.Nevertheless,free hemin could have low bioavailability due to its insolubility in intestinal fluid ...Hemin is recognized as a superior biological iron-fortifier in the prevention and treatment of iron deficiency anemia.Nevertheless,free hemin could have low bioavailability due to its insolubility in intestinal fluid after passing through the digestive tract,so hemin as a direct fortifier is not as effective as it should be.In this study,a novel hemin-delivery system with good water-solubility was developed by fabricating soy protein isolate(SPI)-hemin complex nanoparticles through pH-driven method,and the formation mechanism and bioavailability were also investigated.Hemin could bind to SPI and form nanoparticles with a diameter ranging from 100 to 300 nm in the process of pH dropping from 12.0 to 7.0,and thereby significantly improve the water-solubility of hemin.It was proved that the nanoparticles were produced mainly through hydrophobic interaction between SPI and hemin,and driven by entropy.The results from in vitro simulated gastrointestinal digestion experiments indicated that bioavailability of hemin was also significantly improved(P<0.05),and the value in SPI-hemin nanoparticles reached nearly 80%at the concentrations of 1.0%(w/v)SPI and 0.25%(w/v)hemin.SPI-hemin nanoparticles could be an innovation for improving the solubility and bioavailability of hemin and an easily acceptable candidate for the design of novel iron-fortified foods.展开更多
As known,the benefits of photothermal therapy(PTT)are greatly limited by the heat tolerance of cancer cells resulting from overexpressed heat shock proteins(HSPs).Then HSPs further trigger the formation of stress gran...As known,the benefits of photothermal therapy(PTT)are greatly limited by the heat tolerance of cancer cells resulting from overexpressed heat shock proteins(HSPs).Then HSPs further trigger the formation of stress granules(SGs)that regulate protein expression and cell viability under various stress conditions.Inhibition of SG formation can sensitize tumor cells to PTT.Herein,we developed PEGylated pH(low)insertion peptide(PEG-pHLIP)-modified hollow copper sulfide nanoparticles(HCuS NPs)encapsulating the SG inhibitor ISRIB,with the phase-change material lauric acid(LA)as a gatekeeper,to construct a pH-driven and NIR photo-responsive controlled smart drug delivery system(IL@H-PP).The nano medicine could specifically target slightly acidic tumor sites.Upon irradiation,IL@H-PP realized PTT,and the light-controlled release of ISRIB could effectively inhibit the formation of PTT-induced SG to sensitize tumor cells to PTT,thereby increasing the antitumor effect and inducing potent immunogenic cell death(ICD).Moreover,IL@H-PP could promote the production of reactive oxygen species(ROS)by tumor-associated macrophages(TAMs),repolarizing them towards the M1 phenotype and remodeling the immunosuppressive microenvironment.In vitro/vivo results revealed the potential of PTT combined with SG inhibitors,which provides a new paradigm for antitumor and antimetastases.展开更多
基金the supporting from the USDA National Institute of Food and Agriculture,Agricultural and Food Research Initiative Competitive Program(2020-03921)partly supported by funding from the Good Food Institute。
文摘Simple but effective methods are required to incorporate multiple bioactive polyphenols into delivery systems to increase their dispersibility,stability and bioavailability.We developed and tested three p Hdriven protocols for creating nanoemulsions loaded with multiple lipophilic polyphenols.These protocols differed in how the different polyphenols were incorporated into the nanoemulsions.The impact of these three methods on the formation,properties,and gastrointestinal fate of nanoemulsions loaded with curcumin,resveratrol,and quercetin was investigated.The three methods produced nanoemulsions with similar initial particle properties:droplet diameters(0.15,0.16,and 0.15μm)and zeta-potentials(–59,–58,and–58 m V),respectively.However,the average encapsulation efficiencies(82%,88%,and 61%),gastrointestinal stabilities(83%,97%,and 29%)and bioaccessibilities(77%,90%,and 73%)for curcumin,resveratrol,and quercetin were somewhat different.In particular,more quercetin degradation occurred using the approach that held it under alkaline conditions for extended periods.In general,the p H-driven method provides researchers with a versatile approach of incorporating multiple polyphenols with different characteristics into functional food and beverages using a simple and inexpensive method.
基金supported by the National Natural Science Foundation of China(31371741).
文摘Hemin is recognized as a superior biological iron-fortifier in the prevention and treatment of iron deficiency anemia.Nevertheless,free hemin could have low bioavailability due to its insolubility in intestinal fluid after passing through the digestive tract,so hemin as a direct fortifier is not as effective as it should be.In this study,a novel hemin-delivery system with good water-solubility was developed by fabricating soy protein isolate(SPI)-hemin complex nanoparticles through pH-driven method,and the formation mechanism and bioavailability were also investigated.Hemin could bind to SPI and form nanoparticles with a diameter ranging from 100 to 300 nm in the process of pH dropping from 12.0 to 7.0,and thereby significantly improve the water-solubility of hemin.It was proved that the nanoparticles were produced mainly through hydrophobic interaction between SPI and hemin,and driven by entropy.The results from in vitro simulated gastrointestinal digestion experiments indicated that bioavailability of hemin was also significantly improved(P<0.05),and the value in SPI-hemin nanoparticles reached nearly 80%at the concentrations of 1.0%(w/v)SPI and 0.25%(w/v)hemin.SPI-hemin nanoparticles could be an innovation for improving the solubility and bioavailability of hemin and an easily acceptable candidate for the design of novel iron-fortified foods.
基金supported by the National Natural Science Foundation of China(82173762,China)the Key Research and Development Program of Science and Technology Department of Sichuan Province(2022YFS0334,2022JDJQ0500,China)+1 种基金111 Project(B18035,China)the Fundamental of Research Funds for the Central Universities。
文摘As known,the benefits of photothermal therapy(PTT)are greatly limited by the heat tolerance of cancer cells resulting from overexpressed heat shock proteins(HSPs).Then HSPs further trigger the formation of stress granules(SGs)that regulate protein expression and cell viability under various stress conditions.Inhibition of SG formation can sensitize tumor cells to PTT.Herein,we developed PEGylated pH(low)insertion peptide(PEG-pHLIP)-modified hollow copper sulfide nanoparticles(HCuS NPs)encapsulating the SG inhibitor ISRIB,with the phase-change material lauric acid(LA)as a gatekeeper,to construct a pH-driven and NIR photo-responsive controlled smart drug delivery system(IL@H-PP).The nano medicine could specifically target slightly acidic tumor sites.Upon irradiation,IL@H-PP realized PTT,and the light-controlled release of ISRIB could effectively inhibit the formation of PTT-induced SG to sensitize tumor cells to PTT,thereby increasing the antitumor effect and inducing potent immunogenic cell death(ICD).Moreover,IL@H-PP could promote the production of reactive oxygen species(ROS)by tumor-associated macrophages(TAMs),repolarizing them towards the M1 phenotype and remodeling the immunosuppressive microenvironment.In vitro/vivo results revealed the potential of PTT combined with SG inhibitors,which provides a new paradigm for antitumor and antimetastases.
