Spray Dried Levodopa-Doped Powder Potentially for Intranasal Delivery

Abstract

This work was aimed to develop levodopa (L-dopa) nasal powder to achieve controllable drug release and high nasal deposition efficiency. A series of uniform microparticles, composed of amorphous L-dopa and excipients of hydroxypropyl methyl cellulose (HPMC), polyvinylpyrrolidone (PVP), or hydroxypropyl-β-cyclodextrin (CD), were fabricated by a self-designed micro-fluidic spray dryer. The effects of excipient type and drug/excipient mass ratio on the particle size, morphology, density, and crystal property, as well as the in vitro performance of drug release, mucoadhesion, and nasal deposition, were investigated. Increased amounts of added excipient, regardless of its type, could accelerate the L-dopa release to different extent. The addition of CD showed the most obvious effect, i.e., ~83% of L-dopa released in 60 min for SD-L1CD2, compared to 37% for raw L-dopa. HPMC could more apparently improve the particle mucoadhesion than PVP and CD, with respective adhesive forces of ~269, 111, and 26 nN for SD-L1H2, -L1P2, and -L1CD2. Nevertheless, the deposition fractions in the olfactory region for such samples were almost the same (~14%), probably ascribable to their quite similar particle aerodynamic diameter (~30 μm). This work demonstrates a feasible methodology for the development of nasal powder.

Comparative Analysis of Micrometer-Sized Particle Deposition in the Olfactory Regions of Adult and Pediatric Nasal Cavities: A Computational Study

“…The 3D printing of the nasal cavity model utilized resin material, and a coating was applied to the surface to simulate mucus. The experimental procedure has been delineated in our prior work [ 40 ]. The experimental outcomes and the corresponding simulation results at an aerosol flow rate of 15 LPM with a particle diameter of 10 μm are illustrated in Figure 6 .…”

Cold Plasma for the Modification of the Surface Roughness of Microparticles

“…Currently, the experimental work related to the adhesion between microparticles and a flat surface is limited due to the complexity of the required techniques. ,, Even more limited is the evaluation of the impact of inhalable microparticles’ morphological properties on the nasal mucosa’s adhesion. While it is well known that the material properties, such as mucoadhesivity, of inhalable microparticles’ surfaces are fundamental for efficient nasal delivery, other morphological aspects have been poorly investigated. − For example, the size of inhalable microparticles is linked to the deposition location, suggesting important physical scaling. As previously observed, inhalable microparticles with a diameter between 50 and 150 μm deposit mostly in the nasal cavity. , Furthermore, surface roughness can affect microparticles’ self-adhesion and microparticles’ adhesion to the nasal tissue .…”