The aim of this study was to design and systematically optimize
triclosan loaded nanoparticles (TCS-loaded NPs) formulation for the treatment
of periodontal disease. Triclosan (TCS) is a broad spectrum antimicrobial
agent that has been used in the treatment of the disease. The free drug has
poor aqueous solubility and therefore may encounter permeability problems
when applied to the oral cavity. Resolution IV model of Design-Expert®
software (version 10) was used for the design of experiment and optimization
of TCS-loaded NPs. The nanoparticles (NPs) were prepared using the solvent
displacement method. Effect of factors that were investigated include drugpolymer ratio, surfactant concentration, stirring speed, stirring duration, and
drug-polymer injection rate. Particle size, zeta potential, polydispersity index
(PDI) and entrapment efficiency (EE) were the critical quality attributes
selected for the study. Desirability function determined by the software for
optimized TCS-loaded NPs was 0.704. The observed particle size, PDI, zeta
potential and EE of the optimized TCS-loaded NPs was found to be 135 ± 2.3
nm, 0.1 ± 0.012, -30 ± -4 mV and 75 ± 6%, respectively. It was found that
particle size increases by elevating the concentration of polymer and
decreases with an increase in surfactant concentration and stirring speed.
Zeta potential was found to increase when surfactant concentration was
reduced. Both surfactant concentration and drug to polymer ratio were found
to negatively affect PDI while % EE was positively influenced by the increase
in polymer concentration and decrease in surfactant concentration. The use of
Design-Expert®
software helped in identifying suitable levels of critical quality
parameters for preparing improved NPs formulation for delivery of TCS into
the periodontal pocket.