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 2 1 .3 1 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.

Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies

“…Considering the DDAB amount (X 3 ), it was found that by increasing the DDAB amount from 5 to 15 mg the amount of LVC entrapped decreased. The previous findings were in accordance with Albash et al, 2021d as they described upon increasing cationic SAA as DDAB the EE% of leciplex loaded Moxifloxacin hydrochloride decreased. In addition, they correlate the lower EE% values at high DDAB concentration owed to the enhancement of PC solubility by SAA, promoting the drug leak from vesicles.…”

Sertaconazole-Nitrate-Loaded Leciplex for Treating Keratomycosis: Optimization Using D-Optimal Design and In Vitro, Ex Vivo, and In Vivo Studies

“…These results may be due to the solubilization of phospholipid by the cationic SAA, leading to decreasing STZN encapsulation into the LP. Contrary to previous literature that pointed out the positive impact of the double-chain cationic SAA (DDAB) with a higher log p -value (11.8) on the EE% of lipophilic drugs compared to the single chain CTAB with a lower log p -value 8 [ 30 , 31 ], CTAB increased the EE% of STZN compared to DDAB ( p = 0.0084). DDAB is a double-chain SAA that could compete with the positively charged drug STZN for affinity with the negative phospholipid groups; therefore, by increasing the DDAB molar ratio, the amount of STZN entrapped was reduced.…”

Syringeable atorvastatin loaded eugenol enriched PEGylated cubosomes in-situ gel for the intra-pocket treatment of periodontitis: statistical optimization and clinical assessment

“…First, appropriate dilution of the sample was performed, and a drop was dried over a carbon-coated copper grid and stained with 2% w/v phosphotungstic acid solution. Subsequently, imaging of the sample was performed using TEM at 80 kV (Albash et al., 2021 ).…”