
Pharmaceutics, Год журнала: 2025, Номер 17(3), С. 302 - 302
Опубликована: Фев. 25, 2025
Background Despite many studies on polymer-incorporated nanocarriers for ophthalmic drug delivery, few have thoroughly explored the relationship between coating composition and performance. This study aimed to evaluate effects of three commonly used cationic polymers—distearoyl phosphatidylethanolamine-polyethylene glycol 1000-poly(amidoamine) (DSPE-PEG1000-PAMAM), trimethyl chitosan (TMC), (2,3-dioleoyloxypropyl) trimethylammonium chloride (DOTAP)—on corneal behaviors anti-cataract efficacy diosmetin (DIO)-loaded micelles (D-M-P, D-M-T, D-M-D, respectively). Methods The DIO-loaded were prepared using thin-film dispersion method incorporated with polymers through hydrophobic interactions electrostatic adsorption. Structural characterization was demonstrated by TEM imaging particle size analyzer. In vitro release behavior detected dialysis method. Cell viability D-M-P, D-M-D L929 cells CCK-8 assays, cellular uptake performed coumarin 6 as fluorescence indicator. Precorneal retention these vesicles observed Vivo Imaging System. Transcorneal permeability determined modified Franz diffusion permeation routes are investigated. Selenite-induced cataract model established. different evaluated observation lens opacity antioxidant enzyme activities. Eye Irritation DIO in preparations estimated Draize test, along H&E staining corneas. Results revealed that spherical, a uniform distribution around 28 nm, similar surface potential approximately 6.0 mV, high entrapment efficiency about 95%. Compared suspension, all formulations exhibited significant sustained-release effect. They showed no signs irritation increased IC50 values cells, indicating improved biocompatibility. Cellular human epithelial (HLECs) assessed confocal laser scanning microscopy. C-M-T displayed highest signals, internalization 3.2 times greater than solution group. Both C-M-P enhanced vesicle at least 47.8% compared Cou-6 solution. Furthermore, TMC facilitated paracellular transport into deepest layers cornea delivered across cornea, Papp value 3.11 1.49 those respectively. terms therapeutic efficacy, D-M-T most attenuation opacity, activities inhibition lipid peroxidation. Conclusion modification micelle significantly influences their performance ocular delivery. Among tested formulations, stands out due its multiple advantages, including transcorneal DIO, safety, making it promising candidate applications.
Язык: Английский