title: In vivo gastrointestinal drug-release monitoring through second near-infrared window fluorescent bioimaging with orally delivered microcarriers.
abstract: Non-invasive monitoring of gastrointestinal drug release in vivo is extremely challenging because of the limited spatial resolution and long scanning time of existing bioimaging modalities, such as X-ray radiation and magnetic resonance. Here, we report a novel microcarrier that can retain drugs and withstand the harsh conditions of gastrointestinal tract. Significantly, we can track the microcarrier fate and semi-quantitatively monitor the content of drug released in vivo in real time by measuring the fluorescence signals in the second near-infrared window of lanthanide-based downconversion nanoparticles with an absorption competition-induced emission bioimaging system. The microcarriers show a prolonged residence time of up to 72 h in the gastrointestinal tract, releasing up to 62% of their content. Moreover, minimal deposition of the microcarriers is found in non-target organs, such as the liver, spleen and kidney. These findings provide novel insights for the development of therapeutic and bioimaging strategies of orally administered drugs.
authors.affiliation: Department of Chemistry, Laboratory of Advanced Materials, Collaborative Innovation Center of Chemistry for Energy Materials, State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, China.
authors.forename: Rui
authors.initials: R
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Laboratory of Advanced Materials, Collaborative Innovation Center of Chemistry for Energy Materials, State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Zhou
authors.affiliation: Department of Chemistry, Laboratory of Advanced Materials, Collaborative Innovation Center of Chemistry for Energy Materials, State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, China.
authors.forename: Wenxing
authors.initials: W
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Laboratory of Advanced Materials, Collaborative Innovation Center of Chemistry for Energy Materials, State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, China.
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Li
authors.affiliation: Department of Chemistry, Laboratory of Advanced Materials, Collaborative Innovation Center of Chemistry for Energy Materials, State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, China.
authors.forename: Fan
authors.identifier: 0000-0001-7886-6144
authors.initials: F
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D040761:Biomimetic Materials / Q000737:chemistry; D004337:Drug Carriers / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D004339:Drug Compounding; D065546:Drug Liberation; D005260:Female; D005459:Fluorides / Q000737:chemistry; D005682:Gadolinium / Q000737:chemistry; D005750:Gastric Juice / Q000737:chemistry; D005753:Gastric Mucosa / Q000378:metabolism; D007211:Indoles / Q000493:pharmacokinetics*; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000000981:diagnostic imaging*; D007668:Kidney / Q000000981:diagnostic imaging / Q000378:metabolism; D008099:Liver / Q000000981:diagnostic imaging / Q000378:metabolism; D051379:Mice; D061848:Optical Imaging / Q000295:instrumentation / Q000379:methods*; D010714:Phosphatidylethanolamines / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D012822:Silicon Dioxide / Q000737:chemistry; D019265:Spectroscopy, Near-Infrared / Q000295:instrumentation / Q000379:methods*; D013154:Spleen / Q000000981:diagnostic imaging / Q000378:metabolism; D013270:Stomach / Q000000981:diagnostic imaging*; D014018:Tissue Distribution
chemical_list: C519184:1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000); D004337:Drug Carriers; D007211:Indoles; D010714:Phosphatidylethanolamines; C028418:tetrasulfophthalocyanine; D011092:Polyethylene Glycols; D012822:Silicon Dioxide; D005682:Gadolinium; D005459:Fluorides