Self-assembled micelles based on N-octyl-N’-phthalyl-O-phosphoryl chitosan derivative as an effective oral carrier of paclitaxel

Add time:08/22/2019    Source:sciencedirect.com

Herein, we describe a novel amphipathic chitosan derivative (N-octyl-N’-phthalyl-O-phosphoryl chitosan, abbreviated as OPPC) as an effective oral delivery platform for P-gp substrates, especially paclitaxel (PTX). OPPC could readily self-assemble into micelles, solubilize and encapsulate PTX into the hydrophobic inner core of OPPC with superior loading capacity to chitosan. PTX/OPPC micelles possessed improved intestinal epithelial permeability and oral bioavailability of PTX evaluated by in situ perfusion and pharmacokinetic studies. In vivo fluorescence imaging revealed enhanced stability and integrity of OPPC micelles in mice gastrointestine. Furthermore, cellular uptake studies revealed effective transport and accumulation of OPPC micelles loading PTX or rhodamine-123 into Caco-2 cells via clathrin/cavelin-mediated endocytosis and OPPC-mediated P-gp inhibition. Mechanistically, the inhibition of P-gp efflux pumps by OPPC resulted from the reduction of membrane fluidity and decreased P-gp ATPase activity. In summary, OPPC micelles may serve as an efficient and promising delivery system for enhancing oral bioavailability of P-gp substrates.

We also recommend Trading Suppliers and Manufacturers of octyl hydrogen sulphate (cas 110-11-2). Pls Click Website Link as below: cas 110-11-2 suppliers

Prev:Leaching of chalcopyrite with hydrogen peroxide in 1-hexyl-3-methyl-imidazolium hydrogen sulfate ionic liquid aqueous solution
Next:Precipitation transformation of rare earth sulfate into chloride with p-dodecylphenoxy carboxylic acids☆)