Conjunctivitis is considered as a common infection of ocular surfaces. Eye drop is most commonly used for treatment of conjunctivitis, but has some drawback like 95% drug eliminated after administration. Administration of levofloxacin to the anterior site in form of chitosan coated poly (lactic-co-glycolic acid) nanoparticles (LFV-CS-PLGA-NPs) expected to overcome these problem and increasing corneal contact time and permeability for effective treatment of bacterial conjunctivitis. The Nanoparticles were developed by single emulsion solvent evaporationtechnique and optimized for different variables (chitosan, poly (lactide-co-glycolic acid) and polyvinyl alcohol concentration) by employing three factors, three levels Box-Behnken statistical design. The nanoparticles were evaluated for particle size, drug loading, entrapment efficiency, drug release, ex-vivo permeation, ocular tolerance, antimicrobial study, confocal laser microscopy, and Gamma scintigraphy study. The particle size and PdI of the optimized nanoparticles were 169.968 +/- 15.23 nm and 0.13 +/- 0.03, respectively, where as entrapment efficiency and drug loading is 49.54 +/- 2.43% and 11.29 +/- 2.13% with extended release profile and strong mucoadhesion. DSC data indicated levofloxacin formed molecular dispersion within coated nanoparticles. Corneal flux showed significantly (P < 0.05) higher permeation as compared to marketed formulation. Formulation was nonirritant and possessed good antibacterial activity. Gamma Scintigraphy showed slow drainage compared to drug solution, indicating reduction in nasolachiymal drainage. The Gamma Scintigraphy study indicated the CS coated PLGA-NPs have high corneal residence time as compared to drug solution. So, it is revealed that LFV-CS-PLGA-NPs increase the drug concentration over ocular tissue and potential usefulness for sustained drug delivery.
This study explores a novel approach to managing skin conditions through a combination therapy utilizing a phospholipid-enriched edge activator-based nanoformulation. 5-Fluorouracil (5-FU)- and sesamol (SES)-loaded transliposomes (FS-TL) were developed using a thin film hydration method and optimized using Box-Behnken Design. FS-TL characterization indicated a vesicle size of 165.6 ± 1.1 nm, polydispersity index of 0.28 ± 0.01, and a zeta potential of −33.17 ± 0.9 mV, and the percent entrapment efficiencies for 5-FU and SES were found to be 63.16 ± 1.07% and 75.60 ± 3.68%, respectively. The drug loading percents for 5-FU and SES were found to be 5.87 ± 0.099% and 7.03 ± 0.34%, respectively. The morphological studies exhibit the distinctive spherical shape of the nanoformulation. The in vitro drug release demonstrated sustained release with 82.52 ± 1.2% and 86.28 ± 1.3% releases for 5-FU and SES, respectively. The ex vivo skin permeation exhibited 81.04 ± 2.1% and 78.03 ± 1.7% for 5-FU and SES. Confocal laser microscopy scanning (CLSM) revealed a deeper formulation penetration (30.0 μm) of excised mice skin membranes than for a standard rhodamine solution (10.0 μm). The dermatokinetic investigation revealed that FS-TL gel has significantly higher concentrations of 5-FU and SES (p < 0.001). The efficacy of FS-TL (p < 0.05) in eradicating the A431 melanoma cell line was satisfactory. These findings suggest the potential of FS-TL formulation over conventional approaches in skin cancer management.