ABSTRACT Mucoadhesion is an effective approach for increasing the retention time of topical ophthalmic therapeutics, particularly in dry eye, as it may mitigate rapid nasolacrimal drainage and improve their limited bioavailability. Using the gelation properties of mucin, the major glycoprotein of the mucosa, to assemble drug loaded nanocarriers that would consolidate considerably on the ocular mucosa and facilitate sustained release is a facile approach to integrate mucoadhesion into topical formulations. However, mucin‐based nanoparticles tend to aggregate due to their limited stability in colloidal solution form. This study reports on the synthesis and stabilization of mucin in nanoparticle form using alginate as an electrostatic stabilizer, and then the subsequent loading of antioxidant coenzyme Q10. Simultaneous ionotropic gelation of both alginate and mucin is employed to obtain self‐assembling polymeric nanocarriers with superior mucoadhesive properties (>80% adheres to the ocular mucosa for 0.25 gm formulation), improved shelf stability, and desired shear‐thinning behavior whereas coenzyme Q10 was encapsulated with high encapsulation efficiency (>96%) and sustained release for up to 4 days. Extensive in vivo assessment reveals the efficacy of the nanocarriers in improving dry eye symptoms. This study demonstrates a novel and straightforward way to synthesize stabilized alginate‐mucin nanoparticles for the effective delivery of coenzyme Q10.
Akram et al. (Thu,) studied this question.