TY - JOUR

T1 - Nicotine-magnesium aluminum silicate microparticle surface modified with chitosan for mucosal delivery

AU - Kanjanakawinkul, Watchara

AU - Rades, Thomas

AU - Puttipipatkhachorn, Satit

AU - Pongjanyakul, Thaned

N1 - Copyright © 2012 Elsevier B.V. All rights reserved.

PY - 2013/4/1

Y1 - 2013/4/1

N2 - Magnesium aluminum silicate (MAS), a negatively charged clay, and nicotine (NCT), a basic drug, can interact electrostatically to form microparticles. Chitosan (CS) was used for the surface modification of the microparticles, and a lyophilization method was used to preserve the original particle morphology. The microparticles were characterized in terms of their physicochemical properties, NCT content, mucoadhesive properties, and release and permeation across porcine esophageal mucosa. The results showed that the microparticles formed via electrostatic interaction between MAS and protonated NCT had an irregular shape and that their NCT content increased with increasing NCT ratios in the microparticle preparation solution. High molecular weight CS (800 kDa) adsorbed to the microparticle surface and induced a positive surface charge. CS molecules intercalated into the MAS silicate layers and decreased the crystallinity of the microparticles, leading to an increase in the release rate and diffusion coefficient of NCT from the microparticles. Moreover, the microparticle surface modified with CS was found to have higher NCT permeation fluxes and mucoadhesive properties, which indicated the significant role of CS for NCT mucosal delivery. However, the enhancement of NCT permeation and of mucoadhesive properties depended on the molecular weight and concentration of CS. These findings suggest that NCT-MAS microparticle surface modified with CS represents a promising mucosal delivery system for NCT.

AB - Magnesium aluminum silicate (MAS), a negatively charged clay, and nicotine (NCT), a basic drug, can interact electrostatically to form microparticles. Chitosan (CS) was used for the surface modification of the microparticles, and a lyophilization method was used to preserve the original particle morphology. The microparticles were characterized in terms of their physicochemical properties, NCT content, mucoadhesive properties, and release and permeation across porcine esophageal mucosa. The results showed that the microparticles formed via electrostatic interaction between MAS and protonated NCT had an irregular shape and that their NCT content increased with increasing NCT ratios in the microparticle preparation solution. High molecular weight CS (800 kDa) adsorbed to the microparticle surface and induced a positive surface charge. CS molecules intercalated into the MAS silicate layers and decreased the crystallinity of the microparticles, leading to an increase in the release rate and diffusion coefficient of NCT from the microparticles. Moreover, the microparticle surface modified with CS was found to have higher NCT permeation fluxes and mucoadhesive properties, which indicated the significant role of CS for NCT mucosal delivery. However, the enhancement of NCT permeation and of mucoadhesive properties depended on the molecular weight and concentration of CS. These findings suggest that NCT-MAS microparticle surface modified with CS represents a promising mucosal delivery system for NCT.

KW - Adhesiveness

KW - Administration, Mucosal

KW - Aluminum Compounds

KW - Animals

KW - Calorimetry, Differential Scanning

KW - Chitosan

KW - Drug Delivery Systems

KW - Hydrogen-Ion Concentration

KW - Magnesium Compounds

KW - Microspheres

KW - Nicotine

KW - Particle Size

KW - Permeability

KW - Silicates

KW - Spectroscopy, Fourier Transform Infrared

KW - Static Electricity

KW - Surface Properties

KW - Sus scrofa

KW - X-Ray Diffraction

U2 - 10.1016/j.msec.2012.12.086

DO - 10.1016/j.msec.2012.12.086

M3 - Journal article

C2 - 23827630

VL - 33

SP - 1727

EP - 1736

JO - Materials Science and Engineering C: Materials for Biological Applications

JF - Materials Science and Engineering C: Materials for Biological Applications

SN - 1873-0191

IS - 3

ER -