Development and characterization of buccoadhesive nifedipine tablets.

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Nifedipine is a crucial drug for cardiovascular conditions.
• Developing effective controlled-release drug delivery systems is essential for improving patient compliance and therapeutic outcomes.
• Buccoadhesive systems offer potential for sustained drug release and localized delivery.

Purpose of the Study:

• To develop and characterize buccoadhesive controlled-release tablets for nifedipine delivery.
• To evaluate the bioadhesion properties and drug release kinetics of these tablets.
• To assess the in vivo performance and safety of the optimized formulation.

Main Methods:

• Tablets were prepared by direct compression using carboxymethyl cellulose (CMC) and carbomer (CP).
• Bioadhesion was assessed using a modified tensiometry method in vitro.
• Drug release studies were conducted in vitro and in vivo in human volunteers.
• Zero-order release kinetics and adhesion forces were analyzed based on CP:CMC ratios.

Main Results:

• CMC and CP demonstrated superior bioadhesion compared to other polymers.
• The optimal CP:CMC ratio (8:2) yielded the highest adhesion force.
• Tablets with 15% CMC and 35% CP adhered for over 8 hours and showed sustained nifedipine release in vivo (56% at 8h).
• A strong correlation (r²=0.989) was found between in vitro and in vivo drug release.

Conclusions:

• Buccoadhesive tablets formulated with CMC and CP provide effective controlled release of nifedipine.
• The developed system exhibits promising bioadhesion and sustained drug delivery properties.
• The in vitro release profile accurately predicts in vivo performance, supporting its clinical potential.