2018
DOI: 10.1038/s41467-018-04225-5
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Reversible glycosidic switch for secure delivery of molecular nanocargos

Abstract: Therapeutic drugs can leak from nanocarriers before reaching their cellular targets. Here we describe the concept of a chemical switch which responds to environmental conditions to alternate between a lipid-soluble state for efficient cargo loading and a water-soluble state for stable retention of cargos inside liposomes. A cue-responsive trigger allows release of the molecular cargo at specific cellular sites. We demonstrate the utility of a specific glycosidic switch for encapsulation of potent anticancer dr… Show more

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Cited by 18 publications
(14 citation statements)
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“…Prodrugs, which can be converted into pharmacological drugs at desired sites, are widely used in cancer chemotherapy . To date, overexpressed enzymes (e.g., matrix metalloproteinase, glutathione S‐transferase, and β‐glucuronidase) within tumor tissues that can direct the conversion of the prodrugs have been broadly reported owing to their higher catalytic activity. However, certain restrictive factors for this strategy remained, such as limited number of enzymes that can be used and poor adjustability of endogenous enzymes .…”
Section: Methodsmentioning
confidence: 99%
“…Prodrugs, which can be converted into pharmacological drugs at desired sites, are widely used in cancer chemotherapy . To date, overexpressed enzymes (e.g., matrix metalloproteinase, glutathione S‐transferase, and β‐glucuronidase) within tumor tissues that can direct the conversion of the prodrugs have been broadly reported owing to their higher catalytic activity. However, certain restrictive factors for this strategy remained, such as limited number of enzymes that can be used and poor adjustability of endogenous enzymes .…”
Section: Methodsmentioning
confidence: 99%
“…When activated, the clue-responsive trigger releases the original drug molecule. Liposomes with “On” and “Off” responsive glucosidase (triggered by reaction with lysosomal beta-glucuronidase) switches [ 245 ] and thermosensitive leucine zipper lipopeptide anchored in the liposomal bilayer [ 246 ] have been constructed. Using the insertion of a copolymer consisting of an azobenzene group linked with PDPA, reversible get-in and get-out blocks in the liposome bilayer were obtained that could ultimately realize complete drug release under UV-irradiation and pH stimuli [ 247 ].…”
Section: Dual-sensitive Liposomesmentioning
confidence: 99%
“…Nowadays, edible and multifunctional nanocarriers such as proteins, lipids and polysaccharides have gained much attention in drug delivery engineering owing to their eco‐friendly, safety and biocompatibility characteristics 1‐4 . In addition to those polymeric molecules, for delivery of hydrophobic molecules in aqueous media, micellar solubilization driven by small molecular surfactants has been considered as a promising technology due to the simplicity and low cost 5,6 …”
Section: Introductionmentioning
confidence: 99%