The effect of different excipients on the nasal delivery performance of levodopa microparticles
XIE Shuaiyu
LI Mengyuan
YAN Shen
ZHANG Shengyu
WU Duo
Abstract：Objective Excipients play a crucial role in enhancing the delivery performance of nasal powders.This study aimed to establish an in vitro evaluation method for nasal delivery performance to investigate the effects of excipients and process parameters on the structure of levodopa microparticles,as well as their correlation with in vitro nasal release and ad-hesion performance.Methods Levodopa microparticles were fabricated via a self-designed micro-fluidic jet spray freeze drying technology with different excipients.The in vitro nasal release and adhesion properties of the microparticles were eval-uated using a modified Franz diffusion cell and a self-designed multi-channel microparticles adhesion property measurement device.Results The spray freeze dried samples showed spherical and porous morphology,and samples contai-ning higher molecular weight excipients formed a film on their surfaces.The porous structure of the microparticles dominated their in vitro release behavior,with the best release performance achieved by formulation L1M4,reaching a cumulative re-lease rate of 86.57％at 60 minutes.The in vitro adhesion performance was best for formulation L1C4,with a surface retention of about 61.75％at 10 minutes,influenced by the hydrophilicity of the microparticles and their surface film structure.Con-clusion This study elucidates the cross-influence of excipient types and microparticle structure on the in vitro nasal release and adhesion properties of levodopa microparticles and proposes corresponding formulations and process parameters to enhance these performances.
Keywords：LevodopaNasal administrationSpray freeze dryingIn vitro nasal release performanceIn vitro nasal adhe-sion performance
Publication Date：2025-05-31
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：7( 429-435 )