DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate

EZETIMIBE NANOSTRUCTURED LIPID CARRIERS (NLCs): A NEW TECHNIQUE TO OVERCOME THE LIMITATIONS OF ORAL ADMINISTRATION

Objective: Ezetimibe (EMB) is a commonly used lipid-lowering medication that lowers cholesterol and triglycerides. Because of its lower water solubility and hepatic metabolism, it necessitates the formulation of drug delivery systems that are capable of improving solubility and avoiding hepatic effect. Methods: Ezetimibe nanostructured lipid carriers (EMB-NLCs) were formulated and examined. They were formulated through emulsification with a high homogenization speed and ultrasonication (The method and evaluation parameters have been mentioned under method section in Formulation of EMB-NLCs paragraph). Results: The formulated NLCs have exhibited particle size (P. S.) between 163.6±7.20 and 866.66±18.65 nm and the zeta potential (Z. P.) values have ranged between-24±1.25 and-35±0.25 mV. Besides, they exhibited higher EE% than 77 percent and the drug encapsulated in lipid matrix was in amorphous state. Pharmacokinetics of optimized formula (F1; composed of 2% w/w Gelucire® 43/01, 8% w/w Miglyol® 812 N, 0.5% w/w lecithin and 2% w/w Poloxmer® 188) have exhibited 2.63-and 2.33-fold increase in oral bioavailability in comparison with EMB suspension and marketing product (Ezetrol® 10 mg tablet), respectively. Conclusion: These studies have demonstrated that, NLCs are superior for enhancing in vivo behavior and oral bioavailability of EMB

Design and Optimization of Omeprazole-Curcumin-Loaded Hydrogel Beads Coated with Chitosan for Treating Peptic Ulcers

This study aimed to formulate a pharmaceutical dosage form containing omeprazole (OMP) and curcumin (CURC) to treat experimental peptic ulcers. OMP and CURC were preliminarily complexed with hydroxypropyl-β-cyclodextrin for enhancing their solubilization. After that, the combined complex (CURC/OMP) was loaded to alginate beads to sustain their release and then coated with chitosan. Finally, we tested the anti-ulcerogenic impact of the best formula versus free OMP or OMP-only-loaded beads. The formulated spherical beads’ diameter ranged from a minimum value of 1.5 ± 0.08 mm to 2.6 ± 0.24 mm; the swelling results ranged from 400.00 ± 8.5% to 800.00 ± 6.2%. The entrapment efficiency was in a range from 60.85 ± 1.01% to 87.44 ± 1.88%. The optimized formula (F8) showed a maximum EE% (87.44 ± 1.88%), swelling (800.00 ± 6.2%), and diameter in the range of 2.60 ± 0.24, with a desirability of 0.941. In the first hour following the administration of the free drug complex, 95% of OMP and 98% of CURC were released. This is unacceptable for medications that require a delayed release in the stomach. The initial drug release from hydrogel beads was 23.19% for CURC and 17.19% for OMP after 2 h and 73.09% for CURC and 58.26% for OMP after 12 h; however, after 24 h, 87.81% of CURC and 81.67% of OMP had been released. The OMP/CURC beads showed a more stable particle size (0.52 ± 0.01 mm) after 6 weeks. In conclusion, the OMP/CURC hydrogel beads give stronger anti-ulcer effectiveness compared to free OMP, CURC-only beads, and OMP-only-loaded beads, indicating a prospective application for managing peptic ulcers