Systematic approach for the formulation and optimization of atorvastatin loaded solid lipid NANOAPARTICLES using...

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Drug Delivery

Background:

• Atorvastatin exhibits poor oral bioavailability (12%) due to low solubility and extensive first-pass hepatic metabolism.
• Solid lipid nanoparticles (SLNs) offer a potential strategy to overcome these limitations in drug delivery.

Purpose of the Study:

• To optimize atorvastatin-loaded solid lipid nanoparticles (ATOR-SLNs) using response surface methodology.
• To improve the physicochemical properties and drug release profile of atorvastatin.

Main Methods:

• Formulation of ATOR-SLNs using glyceryl tripalmitate, poloxamer 407, and soya lecithin.
• Optimization of formulation parameters using a central composite rotatable design (response surface methodology).
• Characterization of ATOR-SLNs using FTIR, DSC, particle size analysis, zeta potential, drug loading (DL), and entrapment efficiency (EE).

Main Results:

• Optimized formulation achieved a drug/lipid ratio of 1:3.64, 1.5% surfactant, and 5 min sonication time.
• ATOR-SLNs exhibited an optimal particle size of 338.5 nm, zeta potential of -24.7mV, DL of 17.7%, and EE of 81.06%.
• In vitro studies showed initial burst release followed by sustained drug release; optimized SLNs were more stable at 4±2°C.

Conclusions:

• ATOR-SLNs represent a promising approach for enhancing atorvastatin bioavailability.
• The developed nanoparticle formulation improves physicochemical properties and offers sustained drug release.
• Solid lipid nanoparticles provide an effective strategy for improving the delivery of poorly bioavailable drugs like atorvastatin.