Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability.

Area of Science:

• Pharmaceutical Nanotechnology
• Drug Delivery Systems
• Materials Science

Background:

• Poorly soluble drugs often exhibit low bioavailability.
• Enhancing drug dissolution rates is crucial for improving therapeutic efficacy.
• Lipid nanoparticles offer a promising platform for drug delivery.

Purpose of the Study:

• To develop stable solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for spironolactone (SP).
• To enhance the dissolution rate and bioavailability of poorly soluble SP.
• To optimize NLC formulations for improved drug delivery.

Main Methods:

• SLNs and NLCs were prepared using probe ultra-sonication.
• Formulations were characterized for particle size, zeta potential, morphology, thermal behavior, stability, and in vitro release.
• NLCs incorporated stearic acid (solid lipid) and oleic acid (liquid lipid).

Main Results:

• Increased oleic acid concentration in NLCs reduced particle size and zeta potential but improved entrapment efficiency.
• Nanoparticles were spherical with an average size of ~170 nm.
• NLCs exhibited superior physical stability and higher drug release (5.1- to 7.2-fold increase) compared to SLNs.

Conclusions:

• NLCs, particularly with a 70:30 solid:liquid lipid ratio, are highly effective for enhancing spironolactone dissolution.
• These optimized NLC formulations demonstrate excellent entrapment efficiency and long-term physical stability.
• Lipid nanoparticles represent a viable strategy for improving the delivery of poorly soluble drugs.