Effect of particle size on the cellular uptake and anti-inflammatory activity of oral nanotherapeutics. 2020

Xin Zhou, and Yao Liu, and Xianfeng Wang, and Xiaomeng Li, and Bo Xiao
State Key Laboratory of Silkworm Genome Biology, School of Materials and Energy, Southwest University, Chongqing, 400715, PR China.

To elucidate the impacts of particle size on the cell internalization and anti-inflammatory activity of oral nanotherapeutics, curcumin (CUR)-loaded polymeric nanoparticles (NPs) with different particle sizes were fabricated. The obtained NPs with particle sizes (185-884 nm) and negative zeta potentials (approximately -25 mV) had desirable CUR loading amounts (5.1-6.1 %) and high CUR encapsulation efficiency (73.2-89.6 %). In vitro cellular uptake assays revealed that the cell internalization efficiencies of NPs were increased with the increase of their particle sizes, and NPs (900) showed the highest phagocytosis efficiency in macrophages among all the tested NPs. Importantly, NPs (900) exhibited significantly stronger capability to downregulate the production of the main pro-inflammatory cytokines from macrophages when they were compared with NPs (200) and NPs (500). Further animal studies suggested that oral administration of hydrogel (chitosan and alginate)-embedding NPs (900) could efficiently accumulate in colitis tissue in a manner that was comparable to that of NPs (200) and NPs (500) and could achieve the best treatment efficacy against ulcerative colitis (UC). Collectively, these findings can serve as a guideline for the rational design of nanotherapeutics with desirable accumulation profiles in colitis tissue, maximized cellular uptake efficiency in macrophages, and good therapeutic outcomes against UC.

UI MeSH Term Description Entries
D008264 Macrophages The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.) Bone Marrow-Derived Macrophages,Monocyte-Derived Macrophages,Macrophage,Macrophages, Monocyte-Derived,Bone Marrow Derived Macrophages,Bone Marrow-Derived Macrophage,Macrophage, Bone Marrow-Derived,Macrophage, Monocyte-Derived,Macrophages, Bone Marrow-Derived,Macrophages, Monocyte Derived,Monocyte Derived Macrophages,Monocyte-Derived Macrophage
D008855 Microscopy, Electron, Scanning Microscopy in which the object is examined directly by an electron beam scanning the specimen point-by-point. The image is constructed by detecting the products of specimen interactions that are projected above the plane of the sample, such as backscattered electrons. Although SCANNING TRANSMISSION ELECTRON MICROSCOPY also scans the specimen point by point with the electron beam, the image is constructed by detecting the electrons, or their interaction products that are transmitted through the sample plane, so that is a form of TRANSMISSION ELECTRON MICROSCOPY. Scanning Electron Microscopy,Electron Scanning Microscopy,Electron Microscopies, Scanning,Electron Microscopy, Scanning,Electron Scanning Microscopies,Microscopies, Electron Scanning,Microscopies, Scanning Electron,Microscopy, Electron Scanning,Microscopy, Scanning Electron,Scanning Electron Microscopies,Scanning Microscopies, Electron,Scanning Microscopy, Electron
D010316 Particle Size Relating to the size of solids. Particle Sizes,Size, Particle,Sizes, Particle
D010587 Phagocytosis The engulfing and degradation of microorganisms; other cells that are dead, dying, or pathogenic; and foreign particles by phagocytic cells (PHAGOCYTES). Phagocytoses
D003093 Colitis, Ulcerative Inflammation of the COLON that is predominantly confined to the MUCOSA. Its major symptoms include DIARRHEA, rectal BLEEDING, the passage of MUCUS, and ABDOMINAL PAIN. Colitis Gravis,Idiopathic Proctocolitis,Inflammatory Bowel Disease, Ulcerative Colitis Type,Ulcerative Colitis
D003474 Curcumin A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes. 1,6-Heptadiene-3,5-dione, 1,7-bis(4-hydroxy-3-methoxyphenyl)-, (E,E)-,Curcumin Phytosome,Diferuloylmethane,Mervia,Turmeric Yellow,Phytosome, Curcumin,Yellow, Turmeric
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D000067996 RAW 264.7 Cells A transformed macrophage cell line isolated from ASCITES of mice infected with ABELSON MURINE LEUKEMIA VIRUS. RAW 264.7 Cell Line,264.7 Cell, RAW,264.7 Cells, RAW,Cell, RAW 264.7,Cells, RAW 264.7,RAW 264.7 Cell
D000077182 Polylactic Acid-Polyglycolic Acid Copolymer A co-polymer that consists of varying ratios of polylactic acid and polyglycolic acid. It is used as a matrix for drug delivery and for BONE REGENERATION. PLGA Acid,LactoSorb,PL-PG Copolymer,PLG Polymer,PLGA Compound,Poly (D,L-lactic-co-glycolic Acid),Poly (Lactic-co-glycolic Acid) -,Poly(D,L-lactide-co-glycolide),Poly(DL-lactide-co-glycolic Acid),Poly(Glycolide-co-lactide),Poly(L-lactide)-co-glycolide,Poly(Lactic-co-glycolic Acid),Poly-L-lactic-polyglycolic Acid,Polylactic-co-glycolic Acid Copolymer,RG 502,Acid, PLGA,Acids, PLGA,Copolymer, PL-PG,Copolymer, Polylactic-co-glycolic Acid,Copolymers, PL-PG,Copolymers, Polylactic-co-glycolic Acid,PL PG Copolymer,PL-PG Copolymers,PLG Polymers,PLGA Acids,PLGA Compounds,Poly L lactic polyglycolic Acid,Poly-L-lactic-polyglycolic Acids,Polylactic Acid Polyglycolic Acid Copolymer,Polylactic co glycolic Acid Copolymer,Polylactic-co-glycolic Acid Copolymers,Polymer, PLG,Polymers, PLG
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations

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