Peptide loaded polymeric nanoparticles by non-aqueous nanoprecipitation

Area of Science:

• Materials Science
• Nanotechnology
• Pharmaceutical Sciences

Background:

• Encapsulating water-soluble peptides in polymer nanoparticles (NPs) presents significant challenges.
• Existing methods often struggle with maintaining drug integrity and achieving high loading efficiency for hydrophilic compounds.

Purpose of the Study:

• To develop and validate a novel non-aqueous nanoprecipitation method for encapsulating neuropeptides.
• To assess the drug loading, particle characteristics, and in vitro release profiles of polymer NPs containing neuro-peptides.

Main Methods:

• A solvent-antisolvent process was employed under strictly anhydrous conditions to prepare poly(sebacic anhydride) (PSA) NPs.
• Neuro-peptides like oxytocin and Luteinizing hormone-releasing hormone (LHRH) were encapsulated.
• Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), and Transmission Electron Microscopy (TEM) were used for characterization.

Main Results:

• The method successfully produced spherical PSA NPs of approximately 300 nm with uniform morphology.
• High drug loading was achieved, with oxytocin showing a rapid initial release and LHRH exhibiting slower release kinetics.
• The method was validated for other polymers (PLGA, PLA, PCL) and Thyrotropin releasing hormone (TRH), demonstrating 100% drug loading.

Conclusions:

• The developed non-aqueous nanoprecipitation method is highly effective for co-encapsulating hydrophilic drugs in polymer NPs.
• The resulting NPs exhibit desirable characteristics for potential direct nasal delivery of neuropeptides to the olfactory epithelium.
• This technique offers a promising approach for enhancing the delivery of challenging peptide-based therapeutics.