Gastroretentive Cosolvent-Based In Situ Gel as a Promising Approach for Simultaneous Extended Delivery and Enhanced...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Ion cross-linking in situ gels are advanced liquid sustained-release drug delivery systems.
• Poorly water-soluble drugs, like mitiglinide calcium (MTG), present formulation challenges for these systems.
• Short half-life drugs require strategies for sustained release and enhanced bioavailability.

Purpose of the Study:

• To formulate a gastroretentive in situ gel for mitiglinide calcium (MTG) using a cosolvency approach.
• To enhance the bioavailability and achieve sustained release of MTG.
• To overcome the limitations of in situ gels for poorly water-soluble drugs.

Main Methods:

• Development of MTG in situ gel formulations utilizing propylene glycol as a cosolvent.
• Characterization of formulations for viscosity, gel strength, and floating-lag time.
• In vitro release studies and in vivo pharmacokinetic evaluations were performed.

Main Results:

• The optimized formulation (1% gellan gum, 0.75% sodium alginate, 0.75% calcium carbonate, 7.5% propylene glycol) formed a firm, buoyant gel in simulated gastric fluid, remaining so for 24 hours.
• The formulation demonstrated a sustained in vivo release of MTG over 24 hours.
• Significant enhancement in drug bioavailability was observed.

Conclusions:

• Cosolvency is a viable strategy for formulating sustained-release liquid delivery systems for hydrophobic drugs like MTG.
• The developed gastroretentive in situ gel improves drug bioavailability and extends release duration.
• This approach offers potential for improved patient compliance in managing diabetes through reduced dosing frequency.