Stearoyl-Chitosan Coated Nanoparticles Obtained by Microemulsion Cold Dilution Technique

Area of Science:

• Biomaterials Science
• Nanotechnology
• Pharmacology

Background:

• Chitosan is a well-researched excipient known for muco-adhesiveness and epithelial tight junction modulation.
• Lipophilic modification of chitosan can enhance its utility in nanoparticle formulation.
• Curcumin, a model drug, has therapeutic potential but faces delivery challenges.

Purpose of the Study:

• To synthesize lipophilic stearoyl chitosan (ST-CS) for nanoparticle coating.
• To prepare and characterize ST-CS-coated nanoparticles (ST-CS-NP) encapsulating curcumin (CURC).
• To evaluate the in vitro and in vivo performance of CURC-ST-CS-NP.

Main Methods:

• Synthesis of stearoyl chitosan and preparation of ST-CS-NP via microemulsion cold dilution.
• Characterization of nanoparticles: size, zeta potential, drug entrapment, and release kinetics.
• In vitro cytotoxicity on HUVEC cells and anti-cancer efficacy on PANC-1 cells.
• In vivo pharmacokinetic and biodistribution studies in rats.

Main Results:

• ST-CS-NP exhibited mean diameters of 200-400 nm with up to 73% curcumin entrapment.
• No cytotoxicity observed on HUVEC cells; enhanced efficacy against PANC-1 cells compared to free curcumin.
• Nanoparticle encapsulation prolonged curcumin's systemic circulation time, suggesting stealth properties.
• Biodistribution studies indicated lower curcumin concentration in reticuloendothelial system (RES) organs.

Conclusions:

• ST-CS-NP represent a viable system for curcumin delivery, enhancing its anti-cancer properties.
• The nanoparticle formulation improves drug circulation and potentially reduces RES uptake.
• This approach holds promise for developing advanced drug delivery systems utilizing modified chitosan.