Inflammatory-Targeted Lipid Carrier as a New Nanomaterial to Formulate an Inhaled Drug Delivery System

Area of Science:

• Nanotechnology
• Pharmacology
• Respiratory Medicine

Background:

• Efficacious therapies are needed for respiratory diseases and infections.
• Lipid nanocarriers (LNPs) administered via aerosols offer targeted drug delivery to the lungs, minimizing systemic exposure.
• Palmitoylethanolamide (PEA), an endogenous lipid, possesses anti-inflammatory properties, making it a candidate for novel nanomaterials.

Purpose of the Study:

• To explore the in vitro characteristics of inhalable lipid nanoparticles formulated with Palmitoylethanolamide (PEA-LNPs).
• To evaluate the aerosol performance and safety of PEA-LNPs as a potential drug carrier for respiratory applications.

Main Methods:

• PEA-LNPs were prepared and characterized for size, shape, and solubility.
• Aerosol performance of freeze-dried PEA-LNP powders was assessed using a twin glass impinger, with varying mannose concentrations.
• Cytotoxicity assays on MH-S alveolar macrophage cell lines and particle internalization studies were conducted.

Main Results:

• PEA-LNPs displayed a size of approximately 250 nm with improved PEA solubility.
• Higher mannose concentrations enhanced the emitted dose and fine particle fraction of the dry powder formulation.
• PEA-LNPs demonstrated no toxicity to macrophages up to 0.64 mg/mL and were rapidly internalized.

Conclusions:

• Palmitoylethanolamide is a suitable material for developing inhalable lipid nanocarriers.
• PEA-LNPs are safe, efficiently internalized by macrophages, and possess favorable aerosol properties for respiratory drug delivery.
• These findings suggest PEA-LNPs are a promising platform for treating respiratory diseases and infections.