Preparation and characterization of solid lipid nanoparticles containing peptide

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Drug Delivery Systems

Background:

• Solid lipid nanoparticles (SLN) offer controlled drug delivery but struggle with hydrophilic peptide incorporation.
• Hydrophilic peptides are challenging to integrate into the lipophilic matrix of SLN.

Purpose of the Study:

• To develop a novel solvent diffusion method for preparing peptide-loaded SLN.
• To characterize gonadorelin-loaded SLN for entrapment efficiency, size, zeta potential, and drug release.
• To evaluate the suitability of SLN for prolonged release of hydrophilic peptides.

Main Methods:

• Peptide-loaded SLN were prepared using a novel solvent diffusion method in an aqueous system.
• Gonadorelin and monostearin were dissolved in organic solvents and poured into an aqueous solution with polyvinyl alcohol (PVA).
• SLN were separated by centrifugation and characterized for size, zeta potential, and in vitro drug release.

Main Results:

• The novel method successfully produced gonadorelin-loaded SLN with an average diameter of 421.7 nm and a zeta potential of -21.1 mV.
• Entrapment efficiency of gonadorelin reached 69.4%.
• In vitro release studies showed a biphasic pattern with a burst release followed by prolonged release over 12 days, demonstrating suitability for sustained drug delivery.

Conclusions:

• A novel and effective method for preparing peptide-loaded SLN was established.
• Solid lipid nanoparticles are suitable for the prolonged release formulation of hydrophilic peptide drugs.
• The developed SLN system shows promise for enhancing the delivery of peptide therapeutics.