Dissolution and permeation properties of naproxen from solid-state systems with chitosan

Area of Science:

• Pharmaceutical Science
• Materials Science

Background:

• Naproxen, a non-steroidal anti-inflammatory drug (NSAID), exhibits poor water solubility, limiting its bioavailability.
• Chitosan, a biocompatible polymer, is explored for drug delivery applications to enhance solubility and permeation.

Purpose of the Study:

• To evaluate the impact of various chitosan types and preparation techniques on naproxen's dissolution and permeation.
• To identify optimal drug-chitosan combinations and methods for improving naproxen's biopharmaceutical properties.

Main Methods:

• Naproxen-chitosan systems were prepared using physical mixing, kneading, cogrinding, or coevaporation.
• Five chitosan types (base, glutamate, hydrochloride salts at two molecular weights) were utilized.
• Drug dissolution and permeation through Caco-2 cells and artificial membranes were assessed.

Main Results:

• Chitosan base significantly enhanced naproxen dissolution, attributed to its amorphizing effect.
• Chitosan glutamate demonstrated the highest improvement in naproxen apparent permeability, followed by the hydrochloride salt.
• Cogrinding emerged as the most effective preparation technique for improving both dissolution and permeation.

Conclusions:

• The choice of chitosan type and preparation method critically influences the enhancement of naproxen's dissolution and permeation.
• Cogrinding is a promising technique for developing effective naproxen-chitosan drug delivery systems.
• Artificial lipophilic membranes serve as a suitable alternative for rapid preformulation screening of drug-carrier systems.