Montmorillonite Poly-L-Lactide Microcomposites of Procainamide for controlled drug delivery: In vitro and In vivo...

Area of Science:

• Materials Science
• Pharmacology
• Nanotechnology

Background:

• Procainamide hydrochloride is an antiarrhythmia drug.
• Intercalation into Na(+)-clay (montmorillonite) is a method for drug delivery.
• Previous research explored procainamide hydrochloride intercalation in montmorillonite.

Purpose of the Study:

• To create and characterize microcomposite particles of procainamide-montmorillonite hybrid and poly L-lactide.
• To evaluate the in vitro drug release profile and in vivo pharmacokinetics and biodistribution.
• To assess the toxicity profile of the novel formulation compared to the free drug.

Main Methods:

• Preparation of microcomposite particles using procainamide-montmorillonite hybrid and poly L-lactide.
• Characterization via scanning electron microscopy (SEM) and atomic force microscopy (AFM).
• In vitro drug release studies in simulated intestinal and gastric fluids.
• In vivo pharmacokinetic, biodistribution, and toxicity assessments in rats.

Main Results:

• Microcomposite particles were successfully prepared and characterized.
• Controlled drug release observed up to 72 hours in intestinal fluid, with reduced release in gastric environment.
• In vivo studies showed therapeutic plasma/tissue drug levels and significantly reduced drug toxicity compared to the free drug.

Conclusions:

• The montmorillonite/poly L-lactide formulation provides a controlled release of procainamide hydrochloride.
• This novel formulation enhances therapeutic efficacy by maintaining drug levels within the therapeutic window.
• The formulation significantly reduces drug toxicity, offering improved patient therapy with fewer side effects.