Novel pyrrolo [2,3-b] pyrrole derivatives were synthesized and their hypolipidemic activity was assessed in hyperlipidemic rats. The chemical structures of the new derivatives were confirmed through spectral analysis. Compounds 5 and 6 were revealed to be the most effective hypolipidemic agents, with considerable hypocholesterolemic and hypotriglyceridemic effects. They appear to be promising candidates for creating new powerful derivatives with anti-atherosclerotic and hypolipidemic properties. As for antimicrobial activity, some of the tested compounds showed moderate activity against Pseudomonas aeruginosa: compound 2 revealed an MIC value of 50 μg/mL, compared to 25 μg/mL for ciprofloxacin. Compound 3 showed good antimicrobial activity against Staphylococcus aureus, comparable to ciprofloxacin, and roughly half the activity of ampicillin, according to MIC values. Compound 2 has an MIC approximately 25% of that of clotrimazole against Candida albicans. Compound 2 also showed the highest antioxidant activity with 59% inhibition of radical scavenging activity. Additionally, the cytotoxic activity of these new derivatives 1–7 was investigated and most of them showed good anticancer activity against the three tested cell lines.

Eye inflammation is considered one of the most common co-morbidities associated with
ocular disorders and surgeries. Conventional management of this condition with non-steroidal antiinflammatory
drugs as eye drops is associated with low corneal bioavailability and ocular irritancy.
In the current study, we first investigated the capacity of different solvent systems to enhance the
solubility of Meloxicam (MLX). Then, we prepared chitosan nanoparticles loaded with meloxicam
(MLX-CS-NPs) through electrostatic interaction between the cationic chitosan and the anionic MLX
using either 100% v/v polyethylene glycol 400 or 0.25% w/v tripolyphosphate solution as solvents
based on the MLX solubility data. In further studies, MLX-CS-NPs were characterized in vitro and
assessed for their ex vivo corneal and scleral permeability. The morphology, average particle size
(195–597 nm), zeta potential (25–54 mV), and percent entrapment efficiencies (70–96%) of the prepared
MLX-CS-NPs were evaluated. The in vitro release study of MLX from the selected MLX-CS-NPs
showed a sustained drug release for 72 h with accepted flux and permeation through the cornea
and sclera of rabbits. In the in vivo studies, MLX-CS-NPs eye drop dispersion showed enhanced
anti-inflammatory activity and no ocular irritancy compared to MLX-eye drop solution. Our findings
suggest the potential for using chitosan nanotechnology for ocular delivery of MLX with high contact
time and activity.