Tailoring Terpesomes and Leciplex for the Effective Ocular Conveyance of Moxifloxacin Hydrochloride (Comparative Assessment): In-vitro, Ex-vivo, and In-vivo Evaluation

Abstract

Aim To compare the ability of both terpesomes (TPs) and leciplex (LPs) loaded moxifloxacin hydrochloride (MOX) for enhancing ocular drug conveyance. Methods Two separate 21.31 full-factorial trials were established to determine the influence of multiple variables upon nanovesicles properties and select the optimized formulae using Design Expert® software. The thin-film hydration method was used to formulate TPs, while the single-step procedure was used for LPs. All formulae were characterized for their entrapment efficiency percent (EE%), particle size distribution (PS), polydispersity index (PDI), and zeta potential (ZP). Then, the optimized formulae were selected, evaluated, and compared for additional assessments. Results The optimized formulae TP4 and LP1 showed EE% of 84.14±0.21 and 78.47±0.17%, PS of 578.65±5.65 and 102.41±3.39 nm, PDI of 0.56±0.04 and 0.28±0.01, ZP of −12.50±0.30 and 32.50±0.50 mV, respectively. Further, LP1 showed enhanced corneal permeation across cow cornea compared to MOX solution and TP4. Besides, confocal laser scanning microscopy assessment viewed valuable infiltration from the fluoro-labeled LP through corneal layers compared to TP. LP1 showed spherical morphology and, its ability to adhere to mucus membranes was justified. Further, LP1 showed superiority over MOX solution in biofilm inhibition and eradication in addition to the treatment of infected mice with methicillin-resistant Staphylococcus aureus without any inflammatory response. Finally, the histopathological study verified the harmlessness and biocompatibility of the assembled LPs. Conclusion The gained outcomes confirmed the capability of utilizing LPs as a successful nanovesicle for the ocular conveyance of MOX over TPs and MOX solution.