Lipid-based nanostructures have garnered considerable interests over the last two decades,and have achieved tremendous clinical success including thefirst clinical approval of a liposome(Doxil)for cancer therapy in 199...Lipid-based nanostructures have garnered considerable interests over the last two decades,and have achieved tremendous clinical success including thefirst clinical approval of a liposome(Doxil)for cancer therapy in 1995 and the recent COVID-19 mRNA lipid nanoparticle vaccines.Compared to liposomes which have a lipid bilayer surrounding an aqueous core,lipid nanoparticles with a particle structure have several attractive advantages for encapsulating poorly water-soluble drugs such as better stability due to the particle structure,high drug encapsulation efficiency because of a pre-or co-drug-loading strategy.While many studies have reported the synthesis of lipid nanoparticles for hydrophobic drug encapsulation,the pre-cise control of drug loading and encapsulation efficiency remains a significant challenge.This work reports a new concentration-controlled nanoprecipitation plat-form technology for fabricating lipid nanoparticles with tunable drug loading up to 70 wt%.This method is applicable for encapsulating a wide range of drugs from very hydrophobic to slightly hydrophilic.Using this facile method,nanoparticles with tunable drug loading exhibited excellent properties such as small particle size,narrow size distribution,good particle stability,showing great promise for future drug delivery applications.展开更多
Increasing drug loading remains a critical challenge in the development and translation of nanomedicine.High drug-loading nanoparticles have demonstrated unique advantages such as less carrier material used,better-con...Increasing drug loading remains a critical challenge in the development and translation of nanomedicine.High drug-loading nanoparticles have demonstrated unique advantages such as less carrier material used,better-controlled drug release,and improved efficacy and safety.Herein,we report a simple and efficient salt concentration screening method for making polymer nanoparticles with exceptionally high drug loading(up to 66.5 wt%)based on phase separation-induced nanoprecipitation.Upon addition of salt,phase separation occurs in a miscible solvent-water solution delaying the precipitation time of drugs and polymers to different extents,facilitating their co-precipitation thus the formation of high drug-loading nanoparticles with high encapsulation efficiency(>90%)and excellent stability(>1 month).This technology is versatile and easy to be adapted to various hydrophobic drugs,different polymers,and solvents.This salt-induced nanoprecipitation strategy offers a novel approach to fabricating polymer nanoparticles with tunable drug loading,and opens great potentials for future nanomedicines.展开更多
基金Australian Research Council Projects,Grant/Award Number:DP200101238Australian National Health and Medical Research Council projects of Australia,Grant/Award Number:APP2008698+1 种基金Australian Research Council Discovery Early Career Researcher Award,Grant/Award Number:DE230101044Australian Government Research Training Program Scholarships。
文摘Lipid-based nanostructures have garnered considerable interests over the last two decades,and have achieved tremendous clinical success including thefirst clinical approval of a liposome(Doxil)for cancer therapy in 1995 and the recent COVID-19 mRNA lipid nanoparticle vaccines.Compared to liposomes which have a lipid bilayer surrounding an aqueous core,lipid nanoparticles with a particle structure have several attractive advantages for encapsulating poorly water-soluble drugs such as better stability due to the particle structure,high drug encapsulation efficiency because of a pre-or co-drug-loading strategy.While many studies have reported the synthesis of lipid nanoparticles for hydrophobic drug encapsulation,the pre-cise control of drug loading and encapsulation efficiency remains a significant challenge.This work reports a new concentration-controlled nanoprecipitation plat-form technology for fabricating lipid nanoparticles with tunable drug loading up to 70 wt%.This method is applicable for encapsulating a wide range of drugs from very hydrophobic to slightly hydrophilic.Using this facile method,nanoparticles with tunable drug loading exhibited excellent properties such as small particle size,narrow size distribution,good particle stability,showing great promise for future drug delivery applications.
基金Australian Research Council,Grant/Award Number:DP200101238National Health and Medical Research Council projects of Australia,Grant/Award Number:APP2008698。
文摘Increasing drug loading remains a critical challenge in the development and translation of nanomedicine.High drug-loading nanoparticles have demonstrated unique advantages such as less carrier material used,better-controlled drug release,and improved efficacy and safety.Herein,we report a simple and efficient salt concentration screening method for making polymer nanoparticles with exceptionally high drug loading(up to 66.5 wt%)based on phase separation-induced nanoprecipitation.Upon addition of salt,phase separation occurs in a miscible solvent-water solution delaying the precipitation time of drugs and polymers to different extents,facilitating their co-precipitation thus the formation of high drug-loading nanoparticles with high encapsulation efficiency(>90%)and excellent stability(>1 month).This technology is versatile and easy to be adapted to various hydrophobic drugs,different polymers,and solvents.This salt-induced nanoprecipitation strategy offers a novel approach to fabricating polymer nanoparticles with tunable drug loading,and opens great potentials for future nanomedicines.
