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

• Published in: Macromolecular bioscience Vol. 14; no. 5; pp. 709 - 719
• Main Authors: Mazzarino, Letícia, Otsuka, Issei, Halila, Sami, Bubniak, Lorena dos Santos, Mazzucco, Suelen, Santos-Silva, Maria C., Lemos-Senna, Elenara, Borsali, Redouane
• Format: Journal Article
• Language: English
• Published: Germany Blackwell Publishing Ltd 01.05.2014; Wiley Subscription Services, Inc; Wiley-VCH Verlag
• Subjects: Adhesives - chemistry; Apoptosis - drug effects; Biocompatible Materials - chemical synthesis; Biocompatible Materials - chemistry; block copolymer nanoparticles; Chitosan; Chitosan - chemistry; chitosan-coated nanoparticles; Coating; Copolymers; curcumin; Curcumin - administration & dosage; Curcumin - chemistry; Curcumin - pharmacology; cytotoxicity; Drug Delivery Systems - methods; Drugs; Encapsulation; Fibroblasts; Glucans - chemistry; In vitro testing; Microscopy, Electron, Transmission; Microscopy, Fluorescence; Models, Molecular; Molecular Structure; mucoadhesive nanoparticles; Nanoparticles; Nanoparticles - chemistry; Plasmons; Polyesters - chemistry; polysaccharide coating; Surface Plasmon Resonance; Xylans - chemistry; mucoadhesive nanoparticles; chitosan-coated nanoparticles; cytotoxicity; polysaccharide coating; block copolymer nanoparticles; curcumin
• ISSN: 1616-5187; 1616-5195
• DOI: 10.1002/mabi.201300465

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. Monodisperse self‐assembled nanoparticles are prepared from the new diblock copolymer XGO‐b‐PCL. The ability of nanoparticles to load hydrophobic drugs is demonstrated using curcumin. Mucoadhesive properties are achieved by coating the nanoparticles with chitosan, as evidenced by surface plasmon resonance measurements. In vitro studies indicate that curcumin‐loaded nanoparticles show higher cytotoxic effects on B16F10 melanoma cells than L929 fibroblast cells.