فاطمه پورتوكلي چترودي

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) with very low aqueous solubility, a characteristic that significantly limits its bioavailability. The primary objective of this research was the synthesis, optimization, an‎d comprehensive characterization of Nanostructured Lipid Carriers (NLCs) loaded with celecoxib. This was aimed at assessing the potential of this system to overcome the challenges of low solubility an‎d bioavailability, thereby offering an advanced drug delivery platform with improved therapeutic efficacy an‎d safety. The NLCs were prepared using the High-Speed Homogenization followed by Ultrasonication method an‎d were finally converted into a powder form using a freeze dryer (lyophilizer). The formulation utilized Glyceryl Monostearate as the solid lipid, Triacetin as the liquid lipid, a combination of Pluronic 188 (Poloxamer 188) an‎d Tween 80 as surfactants, an‎d sucrose as the cryoprotectant during the drying stage. The final formulation was developed through the optimization of key parameters. Comprehensive characterization of the produced nanoparticles was performed via Dynamic Light Scattering (DLS), Zeta Potential (ZP), Transmission Electron Microscopy (TEM), Field-Emission Scanning Electron Microscopy (FE-SEM), Fourier-Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), an‎d X-Ray Diffraction (XRD). Finally, the Drug Encapsulation Efficiency (EE%), drug release kinetics, an‎d physical stability of the nanocarriers were investigated. The results demonstrated that the optimized formulation consisted of nanoparticles with an average size of 119 nm, a polydispersity index (PDI) of 0.5, an‎d a zeta potential of -39.6 mV. Microscopic images confirmed the spherical structure an‎d uniform distribution of the nanoparticles. The drug encapsulation efficiency reached 93.33%, indicating the high efficacy of the method in entrapping celecoxib. FTIR an‎d DSC analyses confirmed the absence of undesirable chemical interaction between the drug an‎d carrier components, as well as the dispersal of the drug within the lipid matrix. The drug release profile exhibited a two-phase pattern, including an initial rapid release (burst release) followed by a slow an‎d sustained release. Approximately 31.16% of the drug was released in the gastric environment (pH = 1.2) an‎d 42.57% was released in the intestinal environment (pH = 7.4) over 24 hours. Furthermore, in 30-day stability studies, the nanoparticles showed good physical stability by maintaining their size, PDI, an‎d ZP values with negligible changes. Therefore, this research successfully developed an‎d optimized celecoxib-loaded NLCs that serve as a highly promising system for improving the pharmacological characteristics of hydro‎phobic drugs such as celecoxib.

سلكوكسيب , حامل‌هاي ليپيدي نانوساختار , دارورساني , رهايش كنترل‌شده , نانو فرمولاسيون , حلاليت

Celecoxib , Nanostructured Lipid Carriers (NLCs) , Drug Delivery , Controlled Release , Nanoformulation , Solubility

Fatemeh pourtavakoli

Prof. Ahmad Rahbar Kelishami