Amphiphilic, lauric acid-coupled pluronic-based nano-micellar system for efficient glipizide delivery

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biomedical Engineering

Background:

• Glipizide, a sulfonylurea, manages type 2 diabetes but requires frequent dosing.
• Sustained-release nano-formulations offer potential advantages over conventional antidiabetic drugs.
• Orally active drug delivery systems are crucial for improving patient compliance and therapeutic outcomes.

Purpose of the Study:

• To develop and characterize orally active sustained-release nano-micelles for glipizide delivery.
• To evaluate the efficacy and safety of the novel nano-formulation in a diabetic rat model.
• To explore the potential of lauric acid-conjugated-F127 (LAF127) block copolymer for drug delivery applications.

Main Methods:

• Synthesis and characterization of amphiphilic LAF127 block copolymer.
• Formulation of glipizide-loaded nano-micelles (GNM) using the thin-film hydration technique.
• Evaluation of particle size, polydispersity index (PDI), surface charge, in vitro drug release, and in vivo antidiabetic activity and toxicity.

Main Results:

• Optimized GNM exhibited a particle size of 341.40 ± 3.21 nm, PDI < 0.2, and a surface charge of -17.11 ± 6.23 mV.
• In vitro studies demonstrated a sustained release profile for glipizide from the nano-micelles.
• In vivo studies showed significant reduction in blood glucose levels in diabetic rats for up to 24 hours with no observed toxicity.

Conclusions:

• The synthesized LAF127 block copolymer is suitable for developing effective oral sustained-release nano-micelles.
• Glipizide-loaded nano-micelles demonstrate promising therapeutic potential for type 2 diabetes management.
• The developed nano-formulation offers a safe and effective alternative to conventional glipizide administration.