Nifedipine-loaded polymeric nanoparticles: Preparation and in vitro characterization

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Nifedipine (NF) is a widely used calcium channel blocker with a short half-life, necessitating frequent dosing.
• Developing sustained-release formulations of NF can improve therapeutic efficacy and patient compliance while minimizing side effects.

Purpose of the Study:

• To prepare poly(lactic-co-glycolic) acid (PLGA) nanoparticles loaded with nifedipine (NF) using two distinct methods: nanoprecipitation (N-2) and emulsion-solvent evaporation (N-4).
• To characterize the in vitro properties of the prepared NF-loaded PLGA nanoparticles, including morphology, particle size, encapsulation efficiency, and drug release kinetics.
• To evaluate the potential of these nanoparticles for achieving sustained NF release and reducing associated side effects.

Main Methods:

• Preparation of nifedipine-loaded PLGA nanoparticles via nanoprecipitation (N-2) and emulsion-solvent evaporation (N-4).
• Characterization of nanoparticles using Scanning Electron Microscopy (SEM) for surface morphology.
• Determination of particle size, size distribution, and zeta potential.
• Quantification of encapsulation efficiency.
• In vitro drug release studies in phosphate-buffered saline (PBS) at pH 7.4.

Main Results:

• SEM analysis confirmed the spherical morphology of the prepared nanoparticles.
• Mean particle sizes ranged from 294.27±7.93 nm to 424.92±4.96 nm, with near-neutral zeta potentials.
• Encapsulation efficiencies were 13.03±1.82% for N-2 and 18.96±1.95% for N-4 (p=0.05).
• Sustained release of NF was observed, with cumulative drug release reaching approximately 100% within 38 days for N-2 and 22 days for N-4 (p<0.05).

Conclusions:

• PLGA nanoparticles prepared by both methods are effective in encapsulating nifedipine.
• The developed nanoparticle formulations demonstrate sustained drug release capabilities.
• These nifedipine-loaded PLGA nanoparticles represent a viable system for improving drug delivery, potentially reducing side effects, and enhancing patient compliance.