Development and Optimization of Polymeric Nanoparticles and their In vitro Deposition Studies Using Modified TSI

Abstract

Background: To deliver the drug through the pulmonary route, polymers like oleoylcarboxymethyl chitosan (O-CMC), chitosan, and HPMC (hydroxypropyl methylcellulose) K4M are well known for their effective mucoadhesive properties. Drug-loaded polymeric nanoparticles have the potential for a therapeutic response for the targeted site is a beneficial approach. background: To deliver the drug through the pulmonary route, polymers like oleoyl-carboxymethyl chitosan (O-CMC), chitosan, and HPMC (hydroxypropyl methyl cellulose) K4M are well known for their effective mucoadhesive properties. Drug-loaded polymeric nanoparticles have potential for therapeutic response for the targeted site is a beneficial approach. Objective: The present study is to develop polymeric nanoparticles (PNPs) utilizing mucoadhesive polymers with varying concentrations as well as to develop the PNPs for pulmonary delivery. objective: The present study is to develop polymeric nanoparticles (PNPs) utilizing mucoadhesive polymers with varying concentrations as well as to developed the PNPs for pulmonary delivery. Methods: Polymeric nanoparticles are developed by homogenization and solvent evaporation methods and characterized by modified twin-stage impinger to study in vitro deposition. Results: The characterization of pirfenidone-loaded polymeric nanoparticles (PFD-PNPs) reveals that the mean particle size of O-CMC-PNPs is 140.8 nm ± 20, found to be less than CS-PNPs and HPMC-PNPs. The polydispersibility index reveals that the particles of all prepared formulations are homogenous. At the same time, the zeta potential of O-CMC-PNPs is 40.8 mV ± 5.64, and the entrapment efficiency is 91% ± 1.2, which is better as compared to Chitosan and HPMC K4M PNPs and makes them efficient for pulmonary delivery. Findings from the in vitro deposition study using modified TSI show that 88.5% of the drug delivered through nebulization from both the stage of right and left sides of the TSI suggests effective deposition in the lungs of O-CMC PNPs, and it may move to the deeper regions because of the lowest diameter of the particles. Sustaining release of the drug was found in the O-CMC PNPs for 8 hours, compared with 5 and 7 hours for HPMC PNPs and Chitosan PNPs, respectively. Conclusions: Overall, the results of the O-CMC-PNPs highlight that the prepared nanoparticles with O-CMC would be effective for pulmonary delivery instead of chitosan and HPMC K4M.