Aceclofenac delivery by microencapsulation using LBL self-assembly for delayed release

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery

Background:

• Colonic drug delivery is crucial for treating local diseases and protecting sensitive peptide drugs from digestion.
• Conventional oral delivery often fails to deliver drugs effectively to the colon due to degradation in the upper gastrointestinal tract.

Purpose of the Study:

• To develop Aceclofenac microcapsules using Layer-By-Layer (LBL) self-assembly for enhanced colonic targeting.
• To optimize the formulation factors influencing microcapsule properties and drug release using the Taguchi approach.

Main Methods:

• Utilized LBL self-assembly with chitosan and pectin on Aceclofenac microcrystals.
• Applied Taguchi methodology to optimize chitosan concentration, pectin concentration, centrifugation speed, and incubation time.
• Characterized microcapsules for size, zeta potential, encapsulation efficiency, and morphology (SEM).
• Evaluated in-vitro release kinetics in simulated colonic conditions (rat fecal matter).

Main Results:

• Successfully fabricated single bilayer Aceclofenac microcapsules with sequential charge reversal indicating successful LBL assembly.
• Optimized microcapsules (F5) exhibited an average size of 20µm and 63.83% encapsulation efficiency.
• Achieved 98.40% cumulative drug release ex-vivo in the presence of colonic fecal matter.
• Release kinetics followed first-order release (R²=0.950) in simulated colonic environment.

Conclusions:

• LBL self-assembly is an effective technique for developing Aceclofenac microcapsules for targeted colonic delivery.
• The optimized microcapsules demonstrate significant potential for delivering drugs to the colon with high efficiency and controlled release.