LINAGLIPTIN AND GLICLAZIDE DI-LOADED EXTENDED-RELEASE NANOPARTICLES: FORMULATION AND EVALUATION

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Drug Delivery Systems

Background:

• Diabetes mellitus management often requires combination therapy with oral hypoglycemic agents.
• Achieving sustained drug release is crucial for improving patient compliance and therapeutic efficacy.
• Nanoparticle formulations offer potential for enhanced drug delivery and controlled release profiles.

Purpose of the Study:

• To formulate and characterize extended-release nanoparticles for co-delivery of gliclazide and linagliptin.
• To evaluate the in-vitro release kinetics of dual-drug loaded nanoparticles.
• To identify an optimal nanoparticle formulation for sustained drug release.

Main Methods:

• Development and validation of a simultaneous HPLC method for gliclazide and linagliptin quantification.
• Nanoparticle preparation using emulsion solvent evaporation with hydroxypropyl methylcellulose (HPMC) and xanthan gum.
• Characterization of nanoparticles including drug content, yield, entrapment efficiency, zeta potential, particle size, morphology (TEM), and in-vitro release studies.

Main Results:

• A validated HPLC method enabled simultaneous determination of both drugs without interference.
• Nanoparticles were successfully prepared and characterized for various physicochemical properties.
• Formula GHX1, utilizing xanthan gum, demonstrated sustained release of both gliclazide (>80%) and linagliptin (>75%) within 8 hours.

Conclusions:

• The GHX1 nanoparticle formulation, with a xanthan gum to drug ratio of 0.5:1, proved optimal for co-delivery.
• This formulation achieved significant in-vitro release of both gliclazide and linagliptin, exceeding 80% within 8 hours.
• The developed nanoparticles show promise for achieving a 24-hour extended release profile for combination therapy in diabetes management.