Alginate-Polymethacrylate Hybrid Microparticles as Multi-Unit Enteric Drug Carriers for Posaconazole

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Enteric drug formulations aim to control drug release, protecting against stomach degradation and irritation.
• Posaconazole (POS) bioavailability is pH-dependent and variable with current oral suspension, impacting treatment efficacy.
• Existing POS formulations include delayed-release tablets and oral suspensions with bioavailability concerns.

Purpose of the Study:

• To design and develop novel multi-unit drug forms for delayed and sustained release of posaconazole (POS).
• To create polymeric microparticles using sodium alginate (ALG) and methacrylic acid-ethyl acrylate copolymer (EUD) via spray-drying.
• To evaluate the in vitro performance of these microparticles for improved POS delivery.

Main Methods:

• Spray-drying technique to prepare polymeric microparticles of ALG, EUD, or their blends.
• In vitro dissolution testing to assess enteric release according to pharmacopoeia standards.
• Evaluation of swelling, mucoadhesion, antifungal activity, ATR-FTIR, and thermal properties of microparticles.

Main Results:

• EUD formulations (5-6%) showed enteric release; ALG (1.5%) demonstrated sustained release.
• Optimal blended formulations (EAP15-EAP18) met enteric dosage form criteria with sustained release (2-3 hours).
• Developed microparticles exhibited favorable swelling, mucoadhesion, and inherent antifungal properties.

Conclusions:

• The developed multi-unit microparticles show promise for a sustained-release enteric dosage form of POS.
• These formulations offer a potential strategy to overcome the bioavailability challenges of current POS oral products.
• Further in vivo investigations are warranted to confirm the therapeutic potential of these novel POS delivery systems.