Floating or pulsatile drug delivery systems based on coated effervescent cores

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Developing advanced drug delivery systems is crucial for improving therapeutic efficacy and patient compliance.
• Floating and pulsatile drug delivery systems offer distinct advantages for controlling drug release kinetics.
• Reservoir systems with effervescent cores and polymeric coatings present a versatile platform for these advanced delivery strategies.

Purpose of the Study:

• To develop and evaluate floating and pulsatile drug delivery systems (DDS) based on effervescent cores and polymeric coatings.
• To characterize the mechanical and permeability properties of acrylic and cellulosic polymers for system design.
• To optimize core and coating compositions for controlled drug release and specific release profiles.

Main Methods:

• Characterization of mechanical properties (puncture strength, elongation) of acrylic and cellulosic polymers in dry and wet states.
• Formulation of floating DDS using Eudragit RL coating for rapid effervescence and flotation.
• Formulation of pulsatile DDS using ethyl cellulose coating for controlled lag time and subsequent rapid drug release.

Main Results:

• Selected Eudragit RL/acetyltributyl citrate coating for floating systems due to high elongation and controlled permeability.
• Selected ethyl cellulose/dibutyl sebacate coating for pulsatile systems, creating a weak, semipermeable film for rupture after a lag time.
• Drug release in floating systems was not retarded by the coating; release control was achieved by adding polymers to the core.
• Lag time in pulsatile systems increased with core hardness and coating thickness, while core composition and coating influenced flotation time in floating systems.

Conclusions:

• Tailored polymer selection and formulation strategies enable the development of distinct floating and pulsatile drug delivery systems.
• Mechanical and permeability properties of polymers are critical determinants for achieving desired drug release profiles.
• The study successfully demonstrated control over flotation time and lag time through precise manipulation of core and coating characteristics.