Polymer-Lipid Microparticles for Pulmonary Delivery

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery

Background:

• Optimizing inhaled drug delivery requires precise control over particle characteristics like size, morphology, and mucoadhesion.
• Current inhaler formulations often face challenges in achieving desired aerosolization and lung deposition properties.

Purpose of the Study:

• To engineer multicomponent polymer-lipid systems based on spray-dried α-lactose monohydrate microparticles.
• To optimize particle size, morphology, and mucoadhesion for improved inhaler formulations.
• To evaluate the physicochemical properties, cytocompatibility, and drug release profiles of the developed systems.

Main Methods:

• Preparation of multicomponent microparticles via spray-drying using α-lactose monohydrate as a base.
• Incorporation of budesonide (active drug), dipalmitoylphosphatidylcholine (lung surfactant), polyvinyl alcohol (morphology modifier), l-leucine (aerosolization enhancer), and chitosan (mucoadhesion promoter).
• Physicochemical characterization, in vitro mucoadhesion studies using Calu-3 cell monolayers, and budesonide release assessment in simulated lung fluid.

Main Results:

• Spray-drying successfully produced engineered α-lactose monohydrate microparticles with tunable morphology and particle size.
• Formulation composition significantly influenced particle characteristics and in vitro mucoadhesion profiles.
• Calu-3 cell data demonstrated good cytocompatibility of the microparticles.
• Simulated lung fluid studies indicated therapeutically relevant budesonide release kinetics.

Conclusions:

• Multicomponent polymer-lipid systems based on spray-dried microparticles offer a promising approach for optimizing inhaler formulations.
• The engineered microparticles exhibit favorable physicochemical properties, good cytocompatibility, and controlled drug release.
• These findings support the potential of these systems for enhanced pulmonary drug delivery.