PUBLICATION

Surface modification of nanostructure lipid carrier (NLC) by oleoyl-quaternized-chitosan as a mucoadhesive nanocarrier

Authors
Yostawonkul, J., Surassmo, S., Iempridee, T., Pimtong, W., Suktham, K., Sajomsang, W., Gonil, P., Ruktanonchai, U.R.
ID
ZDB-PUB-161026-2
Date
2017
Source
Colloids and surfaces. B, Biointerfaces   149: 301-311 (Journal)
Registered Authors
Pimtong, Wittaya
Keywords
Alpha-mangostin, Mucoadhesive, Nanostructure lipid carrier, Oleoyl-quaternized-chitosan
MeSH Terms
  • Apoptosis/drug effects
  • Caco-2 Cells
  • Cell Survival/drug effects
  • Chitosan/analogs & derivatives*
  • Cyclin D1/genetics
  • Cyclin D1/metabolism
  • Cyclin-Dependent Kinase 4/genetics
  • Cyclin-Dependent Kinase 4/metabolism
  • Drug Carriers*
  • Drug Compounding
  • Drug Liberation
  • Gene Expression/drug effects
  • HeLa Cells
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Nanoparticles/chemistry*
  • Nanoparticles/ultrastructure
  • Particle Size
  • Protein Kinase Inhibitors/chemistry
  • Protein Kinase Inhibitors/pharmacology*
  • Proto-Oncogene Proteins c-bcl-2/genetics
  • Proto-Oncogene Proteins c-bcl-2/metabolism
  • Surface Properties
  • Xanthones/chemistry
  • Xanthones/pharmacology*
  • bcl-2-Associated X Protein/genetics
  • bcl-2-Associated X Protein/metabolism
  • bcl-X Protein/genetics
  • bcl-X Protein/metabolism
PubMed
27780087 Full text @ Colloids Surf. B Biointerfaces
Abstract
A nanostructure lipid carrier (NLC) composed of solid, and liquid lipid as a core has been developed as a delivery system for hydrophobic drug molecules. The aim of this research was to fabricate an oleoyl-quaternized-chitosan (CS)-coated NLC, where the mucoadhesive property of nanoparticles is enhanced for more efficient drug delivery. NLC loaded with alpha-mangostin (AP), a model hydrophobic drug, were fabricated using a high pressure homogenization process and subsequently coated with CS. The fabricated nanoparticles showed particle sizes in the range of 200-400nm, with low polydispersity, high physical stability and excellent encapsulation efficiency (EE>90%). Additionally, in vitro viability, cytotoxicity and ability of NLC and CS-NLC to affect apoptosis in carcinoma Caco-2 cells were determined using the Triplex assay. Gene expressiom analysis were performed using quantitative reverse transcription Polymerase Chain Reaction (RT-qPCR). Moreover, in vivo toxicological testing of NLCs was conducted in zebrafish embryos. Results indicated that CS-NLC provieded high cytotoxicity than NLC itself. In the case of AP loaded nanoparticles, NLC loaded with AP (AP-NLC), and CS-NLC loaded with AP (CS-AP-NLC) exhibited higher cytotoxicity to Caco-2 over Hela cells. These results indicate that CS-NLC shows enhanced cellular uptake but increased cytotoxicity characteristics over NLC and therefore careful optimization of dosage and loading levels in CS-NLC is needed to allow cancer cell targeting, and for exploiting the potential of these systems in cancer therapy.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping