Preparation and characterization of chitosan and trimethyl-chitosanmodified poly-(ε-caprolactone) nanoparticles as DNA carriers

Abstract

The purpose of this research was to prepare poly-(e-caprolactone) (PCL) particles by an emulsion-diffusion-evaporation method using a blend of poly-(vinyl alcohol) and chitosan derivatives as stabilizers. The chitosan derivatives used were chitosan hydrochloride and trimethyl chitosans (TMC) with varying degrees of quaternization. Particle characteristics-size, zeta potential, surface morphology, cytotoxicity, and transfection efficiency-were investigated. The developed method yields PCL nanoparticles in the size range of 250 to 300 nm with a positive surface charge (2.5 to 6.8 mV). The cytotoxicity was found to be moderate and virtually independent of the stabilizersÕ concentration with the exception of the highly quaternized TMC (degree of substitution 66%) being significantly more toxic. In immobilization experiments with gel electrophoresis, it could be shown that these cationic nanoparticles (NP) form stable complexes with DNA at a NP:DNA ratio of 3:1. These nanoplexes showed a significantly higher transfection efficiency on COS-1 cells than naked DNA.

Polysaccharide-Based Nanocarriers for Drug Delivery

“…HA, have also been reported. 78,128,[196][197][198][199] CS nanocarriers have shown high transfection levels not only in HEK293 cell lines, 137,200,201 but also in HeLa, CaLu-3 and MDCK cell lines, known to be more challenging for transfection. 78,92,137,191,[202][203][204][205][206][207] Supporting this high efficacy, siRNA-loaded CS nanocarriers have also been reported to reduce gene expression to similar levels to those obtained with lipofectaminee (~50%).…”

Doxorubicin-chitin-poly(caprolactone) composite nanogel for drug delivery

“…The aim of the present work is to develop a pH responsive Dox-chitin-PCL CNGs system for tumor site specific delivery and for providing a controlled release profile at action site. Chitin based nanogel is more hydrophilic and incorporation of PCL will enhance its lipophilicity to support passive uptake process [19]. In addition, we have evaluated the physicochemical properties, swelling, in vitro degradation and in vitro cytotoxicity studies of the developed composite nanogels.…”

Carriers for the targeted delivery of aerosolized macromolecules for pulmonary pathologies

“…Furthermore, they can be actively targeted to the site of action and have mechanisms for controlled release with a net gain of reduced dosing frequency and improved patient compliance. Moreover, they can be easily formulated from a wide variety of natural and polymeric biodegradable and biocompatible materials such as chitosan, alginate, poly Lactic-co-Glycolic acid (PLGA), polyethylenimine (PEI), and poly (l-lysine) (PLL) [45]. However, the formulation processes to produce NPs and MPs from the above polymers include harsh steps and solvents that can potentially denature the macromolecule or alter its structure such as emulsification/solvent evaporation, spray dryer, freeze dryer, and supercritical fluid technology [46,47].…”