چکیده (انگلیسی):

The aim of the investigation was to prepare and characterize wheat germ agglutinin(WGA)-
conjugated poly(D,L-lactic-co-glycolic) acid nanoparticles encapsulating mometasone furoate (MF) as a
model drug and assess changes in its fate in terms of cellular interactions. MF loaded nanoparticles were
prepared using emulsion–solvent evaporation technique. WGA-conjugation was done by carbodiimide
coupling method. The nanoparticles were characterized for size, zeta potential, entrapment efficiency and
in-vitro drug release. The intracellular uptake of nanoparticles, drug cellular levels, and anti-proliferative
activity studies of wheat germ agglutinin-conjugated and unconjugated nanoparticles were assessed on
alveolar epithelial (A549) cells to establish cellular interactions. Prepared nanoparticles were spherical
with 10–15 μg/mg of WGA conjugated on nanoparticles. The size of nanoparticles increased after
conjugation and drug entrapment and zeta potential reduced from 78±5.5% to 60±2.5% and −15.3±1.9
to −2.59±2.1 mV respectively after conjugation. From the cellular drug concentration–time plot, AUC
was found to be 0.4745, 0.6791 and 1.24 for MF, MF-nanoparticles and wheat germ agglutinin-
MF-nanoparticles respectively. The in-vitro antiproliferative activity was improved and prolonged
significantly after wheat germ agglutinin-conjugation. The results conclusively demonstrate improved
availability and efficacy of antiasthmatic drug in alveolar epithelial cell lines. Hence, a drug once
formulated as mucoadhesive nanoparticles and incorporated in dry powder inhaler formulation may be
used for targeting any segment of lungs for more improved therapeutic response in other lung disorders
as well.