Xyloglucan‐block‐Poly(ϵ‐Caprolactone) Copolymer Nanoparticles Coated with Chitosan as Biocompatible Mucoadhesive Drug Delivery System

Abstract

The development of novel xyloglucan-block-poly(ϵ-caprolactone) (XGO-b-PCL) nanoparticles coated with the mucoadhesive polysaccharide chitosan is described. XGO-b-PCL nanoparticles show monodisperse size distribution (Rh = 50 nm). Curcumin is successfully encapsulated within the PCL core within drug to polymer ratio of 1:5 (w/w). The coating of nanoparticles with chitosan results in an increased particle size and positive surface charge due to the polycation nature of the chitosan. Mucoadhesive properties of chitosan-coated nanoparticles are demonstrated by its exceptional ability to interact with mucin through electrostatic forces. Finally, in vitro studies show that curcumin-loaded nanoparticles exhibit higher cytotoxic effects against B16F10 melanoma cells than L929 fibroblast cells.

Chitosan‐based delivery systems for curcumin: A review of pharmacodynamic and pharmacokinetic aspects

“…In vitro mucoadhesion study Mazzarino, Coche-Guérente et al (2014), Mazzarino, Otsuka et al (2014) ICL (genipin and sodium salts)…”

“…The %EE of curcumin in the NPs was reported to be approximately 99%. Chitosan also creates a positively‐charged surface and strong hydrogen bonds with poloxamer surfactants and consequently, creates highly mucoadhesive nanoparticles (Mazzarino et al, ; Mazzarino, Borsali, & Lemos‐Senna, ; Mazzarino, Coche‐Guérente et al, ; Mazzarino, Otsuka et al, ). These authors indicated that Cur/PCL‐chitosan NPs showed significant toxicity to an SCC‐9 human oral cancer cell line (Mazzarino et al, ).…”

“…To achieve greater mucoadhesion and thus, facilitate oral delivery of curcumin,Mazzarino et al synthesized Cur-loaded polycaprolactone nanoparticles coated with three different molar masses of chitosan (Cur/PCL-chitosan NPs) using a nano-precipitation method. The %EE of curcumin in the NPs was reported to be approximately 99%.Chitosan also creates a positively-charged surface and strong hydrogen bonds with poloxamer surfactants and consequently, creates highly mucoadhesive nanoparticles(Mazzarino et al, 2012;Mazzarino, Coche-Guérente et al, 2014;Mazzarino, Otsuka et al, 2014). These authors indicated that Cur/PCL-chitosan NPs showed significant toxicity to an SCC-9 human oral cancer cell line(Mazzarino et al, 2015).Mazzarino et al also created an amphiphilic copolymer, PCL, nanoparticle containing Cur using the co-solvent technique and showed that the chitosan-coated nanoparticles demonstrated improved mucoadhesion.…”

Evaluation of photodynamic activity, photostability and in vitro drug release of zinc phthalocyanine-loaded nanocapsules

“…Nano C -ZnPc loaded lipid-core PCL nanocapsules coated with chitosan Nano C was prepared by simple adsorption of chitosan onto Nano B, following the method suggested by Mazzarino et al (2014). Briefly, the adsorption of chitosan was carried out by dropwise addition of a 6.25 mL of chitosan solution (10 mg/mL dissolved in 1% acetic acid) over 17 mL of preformed Nano B.…”

Bioadhesive drug delivery systems: Overview and recent advances

“…Coating of chitosan increases the particle size as well as imparts positive charge, due to its positive surface, to the nanoparticles. The mucoadhesive property of chitosan can be attributed to its exceptional ability to interact with mucin through electrostatic forces (Mazzarino et al, 2014).…”