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. 2020 Dec 9;10(12):2460. doi: 10.3390/nano10122460

Table 2.

Few examples of therapeutic nanoparticles/microparticles that have experimentally (in vitro, in vivo, and ex vivo conditions) used in the treatment of IBD.

Nanoparticles Therapeutic Agent Characteristics
Cationic Polymethacrylate
(Eudragit RL) NPs
Clodronate Decreased MPO activity in TNBS- and OXA-induced-colitis compared to free clodronate [175]
Polymeric (poly 1,4-phenyl acetone dimethylene-thioketal) NPs complexed with DOTAP TNF-α small interfering ribonucleic acid (siRNA) Thioketal NPs degrade in response to ROS, and DOTAP enhances mucosal transport. Protects UC by decreasing TNF-α level [182]
Nitroxide-radical NPs comprising of block copolymer methoxy-poly(ethylene glycol)-b-poly(4-(2,26,6-tetramethyl-piperidine-1-oxyl)oxymethylstyrene (MeO-PEG-b-PMOT) TEMPOL Reduction in colitis with successful scavenging of ROS [183]
Poly(lactic-co-glycolic acid) (PLGA) NPs encapsulated inside Eudragit P4135F microspheres Tacrolimus Provided protection to the drug at acidic pH [189]
PLGA/Eudragit NPs Budesonide (BSD) Sustained release of BSD at colonic pH and improved therapeutic effects of BSD against TNBS-induced colitis [192]
PLGA/Eudragit S100 NPs Curcumin Reduced TNF-α secretion in LPS-activated macrophages. Reduced neutrophil infiltration in a DSS-colitis model [187]
Pectin coated-chitosan-hydroxide biohybrid beads 5-ASA Protection to NPs to transport through gastric juices in upper GIT and sustained release of the drugs at 7.4 [193]
PLGA-coated Eudragit S100 nanospheres Cyclosporine Sustained release at 7.4 and used in UC therapy [194]
Eudragit S100/ethyl cellulose nanofibers Budesonide (BSD) Sustained release of drug at a pH of 7.4 [195]
Chitosan and alginate coated with Eudragit S100
microcrystals
Dexamethasone Release of drug in colonic pH and alleviate inflammation in DSS-colitis model [197]
Chitosan and alginate hydrogel/PLA NPs Anti-inflammatory tripeptide Lys–Pro–Val (KPV) Reduced MPO activity and colitis symptoms [202]
Cross-linked pectin microspheres Indomethacin Increased colon-specific delivery at a pH of 7.4 [206]
Calcium pectin–silica gel beads Mesalazine Controlled release of mesalazine at the simulated upper GIT condition and increased mesalazine release in the simulated colonic fluid [207]
Grapefruit-derived nanovesicles Methotrexate Downregulation of IL-1β and TNF-α by upregulating release of heme-oxygenase I and induced anti-inflammatory properties against DSS-IBD [211]
Ginger-derived NPs Ginger Elevated anti-inflammatory cytokines and downregulated concertation’s of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 [212]
PEI NPs Anti-cluster of differentiation (CD)98 siRNA Reduction of CD98 expression in DSS-induced colitis [215]
Mannosylated bio-reducible cationic polymeric NPs TNF-α siRNA Reduction in TNF-α expression in DSS-induced colitis [218]
Galactosylated trimethyl chitosan cysteine NPs Mitogen-Activated Protein Kinase Kinase Kinase Kinase (Map4k4) siRNA Blocks the TNF-α production in DSS-induced UC [219]
Peanut and wheat germ-lecithin decorated NPs Betamethasone Specificity towards inflamed tissues having high expression of lecithin [222]
PLA-PEG (poly (lactic acid) poly (ethylene glycol) block copolymer) grafted with the Fab’ portion of F4/F80 Ab TNF-α Enhanced macrophage-targeting and endocytosis of NPs. Oral administration led to attention in DSS-induced colitis [229]
Folic acid-conjugated PLGA NPs Resveratrol Oral delivery reduced colitis in TNBS-induced rat model [223]
Chitosan microparticle Quercetin Oral administration reduced colitis in an acetic acid-induced rabbit model compared to free quercetin
[210]

Abbreviations used: MPO: myeloperoxidase; TNBS: 2,4,6-trinitrobenzene sulfonic acid; OXA: oxazolone; DOTAP: 1,2-dioleoyl-3-trimethylammonium-propan; TNF-α: tumor necrosis factor; IL: interleukins; ROS: reactive oxygen species; UC: ulcerative colitis; TEMPOL: 4-hydroxy-2,2,6,6-tetramethylpiperidin-1-oxyl; LPS: lipopolysaccharide; DSS: dextran sulfate sodium; 5-ASA: aminosalicylic acid; GIT: gastrointestinal tract; NP: nanoparticle; PEI: polyethyleneimine.