Nicotine-magnesium aluminum silicate microparticle surface modified with chitosan for mucosal delivery
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Nicotine-magnesium aluminum silicate microparticle surface modified with chitosan for mucosal delivery. / Kanjanakawinkul, Watchara; Rades, Thomas; Puttipipatkhachorn, Satit; Pongjanyakul, Thaned.
In: Materials science & engineering. C, Materials for biological applications, Vol. 33, No. 3, 01.04.2013, p. 1727-36.Research output: Contribution to journal › Journal article › peer-review
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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 -
ID: 104573304