New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion...

Area of Science:

• Pharmaceutical Nanotechnology
• Drug Delivery Systems
• Materials Science

Background:

• Quercetin (QCT) possesses valuable pharmacological properties but suffers from poor pharmacokinetics, limiting its therapeutic application.
• Solid lipid nanoparticles (SLNs) are a promising nanocarrier system to enhance the delivery of poorly soluble compounds.
• Novel methods for SLN preparation are needed to improve drug loading and stability.

Purpose of the Study:

• To investigate the preparation of quercetin-loaded solid lipid nanoparticles (QCT-SLNs) using a novel phase-inversion temperature method incorporating volatile oil.
• To evaluate the effect of rosemary oil (RMO) and different solid lipids on SLN characteristics, including particle size, stability, and drug encapsulation.
• To assess the in vitro drug release profile and safety of the developed QCT-SLNs.

Main Methods:

• QCT-SLNs were prepared using the phase-inversion temperature method with various solid lipids and rosemary oil (RMO).
• Particle size, polydispersity index, and zeta potential were analyzed.
• Entrapment efficiency, drug loading, and stability were determined using HPLC.
• In vitro drug release studies and cytotoxicity assays (cell viability) were performed.
• Computer simulations were used to model the effect of RMO on SLN formation.

Main Results:

• Trilaurin (TLR) based SLNs demonstrated optimal particle size and stability.
• An RMO to TLR ratio of 1:3 yielded QCT-SLNs with >60% entrapment efficiency and ~2% w/w drug loading.
• Polyoxyethylene-hydrogenated castor oil RH40 was crucial for achieving the smallest particle size.
• QCT-SLNs exhibited a prolonged biphasic release profile over 24 hours.
• The formulation showed good safety with >75% cell viability at <2% v/v.
• Computer simulations confirmed that RMO incorporation leads to smaller SLN sizes.

Conclusions:

• A novel, safe, and efficient method for preparing QCT-loaded SLNs using phase-inversion temperature and volatile oil (RMO) was established.
• The developed RMO-incorporated SLNs significantly improve quercetin encapsulation and offer sustained drug release, addressing pharmacokinetic challenges.
• This approach holds considerable potential for the nanodelivery of lipophilic compounds, enhancing their therapeutic efficacy.