A comparison study of lipid and polymeric nanoparticles in the nasal delivery of meloxicam: Formulation, characterization, and in vitro evaluation

Abstract

With the increasingly widespread of central nervous system (CNS) disorders and the lack of sufficiently effective medication, meloxicam (MEL) has been reported as a possible medication for Alzheimer's disease (AD) management. Unfortunately, following the conventional application routes, the low brain bioavailability of MEL forms a significant limitation. The intranasal (IN) administration route is considered revolutionary for CNS medications delivery. The objective of the present study was to develop two types of nanocarriers, poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) and solid lipid nanoparticles (SLNs), for the IN delivery of MEL adapting the Quality by Design approach (QbD). Turning then to further enhance the optimized nanoformulation behavior by chitosan-coating. SLNs showed higher encapsulation efficacy (EE) and drug loading (DL) than PLGA NPs 87.26% (EE) and 2.67% (DL); 72.23% (EE) and 2.55% (DL), respectively. MEL encapsulated into the nanoformulations improved in vitro release, mucoadhesion, and permeation behavior compared to the native drug with greater superiority of chitosan-coated SLNs (C-SLNs). In vitro-in vivo correlation (IVIVC) results estimated a significant in vivo brain distribution of the nanoformulations compared to native MEL with estimated greater potential in the C-SLNs. Hence, MEL encapsulation into C-SLNs towards IN route can be promising in enhancing its brain bioavailability.

Keywords: Mucoadhesion; Nose-to-brain delivery; PLGA nanoparticles; Permeability; Quality by Design; Solid lipid nanoparticles.