Solid nano-lipoidal intelligent premix (SNIP): designing, optimization, and characterization

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Bicalutamide exhibits poor oral bioavailability due to low solubility and P-gp efflux.
• Developing effective delivery systems is crucial for improving Bicalutamide's therapeutic efficacy.
• Natural excipients offer potential for enhanced drug formulation.

Purpose of the Study:

• To improve Bicalutamide solubility and absorption using Epigallocatechin-3-gallate (EGCG).
• To design a patient- and industry-friendly solid nanolipoidal intelligent premix (SNIP).
• To explore natural excipients for advanced drug delivery.

Main Methods:

• Investigated Bicalutamide solubility in various oils, surfactants, and cosurfactants.
• Utilized EGCG to enhance Bicalutamide absorption via P-gp interaction.
• Optimized SNIP formulation using pseudo-ternary phase diagrams and D-optimal mixture design.
• Characterized SNIP for morphology, globule size, stability, and dissolution.

Main Results:

• Identified optimal SNIP formulation with sunflower oil, Tween 20, and Span 80.
• Achieved immediate emulsification, nano-sized uniform globules (254.4 nm), and high stability.
• Demonstrated enhanced Bicalutamide solubility and amorphous nature in SNIP.
• Confirmed EGCG's efficacy in improving ex vivo drug absorption (96.75%).

Conclusions:

• Developed a novel, stable, and effective SNIP formulation for Bicalutamide.
• SNIP enhances Bicalutamide solubility and dissolution, potentially bypassing first-pass metabolism.
• EGCG significantly improves Bicalutamide absorption, offering a patient-convenient delivery system.