Fast-dissolving mucoadhesive microparticulate delivery system containing piroxicam

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Sublingual drug delivery aims to improve therapeutic efficacy through rapid absorption.
• Piroxicam, an NSAID, requires enhanced delivery systems for better sublingual residence and dissolution.
• Developing mucoadhesive systems can prolong drug contact time with the mucosa.

Purpose of the Study:

• To investigate the feasibility of creating fast-dissolving, mucoadhesive microparticulate systems for piroxicam.
• To enhance piroxicam's sublingual residence time and dissolution rate.
• To evaluate novel mucoadhesive carriers, Eudragit L100 (EuLNa) and Eudragit S100 (EuSNa) sodium salts.

Main Methods:

• Spray drying was employed to prepare microparticles containing piroxicam and EuLNa or EuSNa at various ratios.
• Characterization included analysis of microparticle morphology, physical state, drug release kinetics, and mucoadhesion.
• Investigated the impact of drug/copolymer ratios on piroxicam's physical state and system performance.

Main Results:

• Piroxicam was successfully incorporated in an amorphous form within the microparticles across all drug/copolymer ratios.
• Amorphous piroxicam formation, attributed to hydrogen bonding, improved dissolution rate and apparent drug solubility.
• Mucoadhesive properties varied with composition; formulations with >50% piroxicam in Series 2 lacked mucoadhesion.

Conclusions:

• The piroxicam/EuLNa 70/30% (m/m) microparticle system demonstrated significant promise for sublingual delivery.
• This optimal formulation requires a minimal polymer content while conferring mucoadhesive properties and enhancing drug solubility.
• The developed microparticles offer a viable strategy for improving piroxicam's pharmacokinetic profile via sublingual administration.