Preparation, characterization, and optimization of altretamine-loaded solid lipid nanoparticles using Box-Behnken...

Area of Science:

• Nanotechnology
• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Altretamine (ALT) is an antineoplastic agent with limitations in its current delivery methods.
• Solid lipid nanoparticles (SLNs) offer a promising platform for enhancing drug solubility, stability, and targeted delivery.
• Developing efficient SLN formulations requires careful optimization of preparation parameters.

Purpose of the Study:

• To prepare and characterize solid lipid nanoparticles (SLNs) encapsulating altretamine (ALT).
• To optimize the SLN formulation using Box-Behnken design (BBD) and response surface methodology (RSM).
• To evaluate the in vitro release profile and physicochemical properties of the optimized ALT-loaded SLNs.

Main Methods:

• Altretamine (ALT) loaded SLNs were prepared using the hot homogenization and ultrasonication technique.
• Box-Behnken design (BBD) combined with response surface methodology (RSM) was employed for formulation optimization.
• Characterization included mean particle size, entrapment efficiency (EE), and drug-loading (DL) analysis.

Main Results:

• The optimized SLN formulation achieved a high entrapment efficiency of 93.21 ± 1.5% and drug-loading of 1.15 ± 0.6%.
• The mean particle size of the optimized SLNs was found to be 100.6 ± 2.1 nm.
• In vitro release studies exhibited a biphasic release pattern over 24 hours, closely matching predicted values.

Conclusions:

• The hot homogenization and ultrasonication method, optimized via BBD and RSM, successfully produced stable ALT-loaded SLNs.
• The optimized SLNs possess favorable physicochemical properties and controlled drug release characteristics.
• These findings suggest that ALT-loaded SLNs are a viable strategy for improving altretamine delivery and therapeutic efficacy.