Chondroitin sulfate-chitosan nanoparticles for ocular delivery of bromfenac sodium: Improved permeation, retention, and penetration

硫酸软骨素-壳聚糖纳米粒子用于眼部递送溴芬酸钠:改善渗透性、保留性和穿透性

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作者:Tara Abdulrahman Abdullah, Naz Jamal Ibrahim, Musarrat Husain Warsi

Conclusion

Encouraging outcomes of in vitro and ex vivo studies indicated that CHS-CS-NPs could be a potential substitute for improved ocular delivery.

Methods

Formulation was developed and optimized for CS, chondroitin, and initial drug concentration. Optimized formulation was evaluated for various in vitro aspects i.e., particles' size, size distribution, zeta potential, shape and morphology, in vitro release profile, corneal permeation, corneal retention, corneal uptake, and ocular tolerance test.

Results

The mean particle size, polydispersity index, zeta potential, and entrapment efficiency of optimized formulation were found to be 245.6 ± 14.22 nm, 0.187 ± 0.016, +37.59 ± 4.05 mV, and 71.72 ± 4.43%, respectively. Transmission electron microscopic analysis revealed a spherical shape of developed formulation. Further, formulation exhibited biphasic release profile and Korsmeyer-Peppas model was found to be the best fit model. Significantly high transcorneal permeation (1.62-fold) and corneal retention (1.92-fold) of bromfenac was observed through ChS-CS-NPs when compared with marketed eyedrops (P < 0.01). Furthermore, high corneal uptake of CHS-CS-NPs was confirmed by confocal laser scanning microscopy (CLSM). Safety profile of the developed formulation was established by hen's egg test-chorioallantoic membrane test.

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