Intracellular delivery of doxorubicin encapsulated in novel pH-responsive chitosan/heparin nanocapsules

Abstract

A novel polyelectrolyte nanocapsule system composed of biopolymers, chitosan and heparin has been fabricated by the layer-by-layer technique on silica nanoparticles followed by dissolution of the silica core. The nanocapsules were of the size range 200 ± 20 nm and loaded with the positively charged anticancer drug doxorubicin with an efficiency of 89%. The loading of the drug into the capsule happens by virtue of the pH-responsive property of the capsule wall, which is determined by the pKa of the polyelectrolytes. As the pH is varied, about 64% of the drug is released in acidic pH while 77% is released in neutral pH. The biocompatibility, efficiency of drug loading, and enhanced bioavailability of the capsule system was confirmed by MTT assay and in vivo biodistribution studies.

Biopolymer-Based Multilayer Capsules and Beads Made via Templating: Advantages, Hurdles and Perspectives

“…Despite this slight drawback, they present numerous advantages due to their little-to-no toxicity, ease of biodegradability, and intrinsic biocompatibility [94]. Polysaccharides (typically glycosaminoglycans [95,96], functionalised chitosans [96,97], alginates [29,98], etc.) and polyamino acids (poly-L-glutamic acid (PGLU), poly-L-lysine (PLL), etc.)…”

Polyelectrolyte Multilayer Capsule (PEMC)-Based Scaffolds for Tissue Engineering

“…For the elimination of these organic cores, pure organic solvents or rather concentrated acids (0.1 M HCl) are required, which obstructs their use for bioapplications [133,135]. However, inorganic templates have become increasingly popular, including silica nanoparticles (SNPs) [136,137]. SNPs were the first inorganic cores investigated and were predicted to be superior candidates to PS and MF cores.…”

Biopolymer-based strategies in the design of smart medical devices and artificial organs

“…These nanoparticle systems entail functionalizing chitosan with different polymers, such as heparin or dimethylmaleic acid/urocanic acid; the pH sensitivity of chitosan accelerates drug release in an acidic environment due to protonation of the chitosan amine groups and subsequent nanoparticle swelling. 160 , 161 …”