Study summary · research use only
Drug-loaded nanoparticles targeted to the colon with polysaccharide hydrogel reduce colitis in a mouse model
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
In this mouse study with in vitro work, the authors engineered nanoparticles (NPs) to deliver the anti-inflammatory tripeptide Lys-Pro-Val (KPV) to the colon and assessed efficacy in a colitis model. NPs were synthesized by double-emulsion/solvent evaporation with KPV loaded during synthesis, then encapsulated in an alginate-chitosan polysaccharide gel. NPs (400 nm) did not affect cell viability or barrier functions. The hydrogel with labeled NPs collapsed in the colon, releasing KPV near colonocytes. Inflammatory responses to lipopolysaccharide were reduced in Caco2-BBE cells exposed to NP-KPV versus NPs alone, dose-dependently. Mice given dextran sodium sulfate followed by NP-KPV showed less inflammatory and histologic change than mice given only DSS. The authors report KPV could be delivered at a concentration 12,000-fold lower than free KPV with similar therapeutic efficacy.
Abstract
One of the challenges to treating inflammatory bowel disease (IBD) is to target the site of inflammation. We engineered nanoparticles (NPs) to deliver an anti-inflammatory tripeptide Lys-Pro-Val (KPV) to the colon and assessed its therapeutic efficacy in a mouse model of colitis. NPs were synthesized by double-emulsion/solvent evaporation. KPV was loaded into the NPs during the first emulsion of the synthesis process. To target KPV to the colon, loaded NPs (NP-KPV) were encapsulated into a polysaccharide gel containing 2 polymers: alginate and chitosan. The effect of KPV-loaded NPs on inflammatory parameters was determined in vitro as well as in the dextran sodium sulfate-induced colitis mouse model. NPs (400 nm) did not affect cell viability or barrier functions. A swelling degree study showed that alginate-chitosan hydrogel containing dextran-fluorescein isothiocyanate-labeled NPs collapsed in the colon. Once delivered, NPs quickly released KPV on or within the closed area of colonocytes. The inflammatory responses to lipopolysaccharide were reduced in Caco2-BBE (brush border enterocyte) cells exposed to NP-KPV compared with those exposed to NPs alone, in a dose-dependent fashion. Mice given dextran sodium sulfate (DSS) followed by NP-KPV were protected against inflammatory and histologic parameters, compared with mice given only DSS. Nanoparticles are a versatile drug delivery system that can overcome physiologic barriers and target anti-inflammatory agents such as the peptide KPV to inflamed areas. By using NPs, KPV can be delivered at a concentration that is 12,000-fold lower than that of KPV in free solution, but with similar therapeutic efficacy. Administration of encapsulated drug-loaded NPs is a novel therapeutic approach for IBD.
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