Formulation and Evaluation of Moxifloxacin Loaded Bilosomes In-Situ Gel: Optimization to Antibacterial Evaluation

Abstract

In this study, moxifloxacin (MX)-loaded bilosome (BS) in situ gel was prepared to improve ocular residence time. MX-BSs were prepared using the thin-film hydration method. They were optimized using a Box–Behnken design (BBD) with bile salt (A, sodium deoxycholate), an edge activator (B, Cremophor EL), and a surfactant (C, Span 60) as process variables. Their effects were assessed based on hydrodynamic diameter (Y1), entrapment efficacy (Y2), and polydispersity index (Y3). The optimized formulation (MX-BSop) depicted a low hydrodynamic diameter (192 ± 4 nm) and high entrapment efficiency (76 ± 1%). Further, MX-BSop was successfully transformed into an in situ gel using chitosan and sodium alginate as carriers. The optimized MX-BSop in situ gel (MX-BSop-Ig4) was further evaluated for gelling capacity, clarity, pH, viscosity, in vitro release, bio-adhesiveness, ex vivo permeation, toxicity, and antimicrobial properties. MX-BSop-Ig4 exhibited an optimum viscosity of 65.4 ± 5.3 cps in sol and 287.5 ± 10.5 cps in gel states. The sustained release profile (82 ± 4% in 24 h) was achieved with a Korsmeyer–Peppas kinetic release model (R2 = 0.9466). Significant bio-adhesion (967.9 dyne/cm2) was achieved in tear film. It also exhibited 1.2-fold and 2.8-fold higher permeation than MX-Ig and a pure MX solution, respectively. It did not show any toxicity to the tested tissue, confirmed by corneal hydration (77.3%), cornea histopathology (no internal changes), and a HET-CAM test (zero score). MX-BSop-Ig4 exhibited a significantly (p < 0.05) higher antimicrobial effect than pure MX against Staphylococcus aureus and Escherichia coli. The findings suggest that bilosome in situ gel is a good alternative to increase corneal residence time, as well as to improve therapeutic activity.

Tailoring of Novel Bile Salt Stabilized Vesicles for Enhanced Transdermal Delivery of Simvastatin: A New Therapeutic Approach against Inflammation

“…The vesicle size of F8 and F3 were 323.1 ± 12.9 nm and 201.3 ± 11.2 nm, respectively. The bile salt imparts bilosomes with a negative charge, which increase the repulsive forces among bilosomal lipid bilayers, leading to an increase in vesicle size [ 39 ]. Furthermore, the bulkiness of SDC (steroidal-like nature) could contribute to the rise in bilosomal vesicle size upon increasing SDC amount [ 40 ].…”

Spanlastic-laden nanogel as a plausible platform for dermal delivery of bimatoprost with superior cutaneous deposition and hair regrowth efficiency in androgenic alopecia

“…6 ). Importantly, the endothermic peak of BIM were completely disappeared in the thermogram of optimized BIM-SLs formula (F1), suggesting a complete entrapment of BIM and its transformation from the crystalline form to the amorphous form ( Zafar et al, 2022 ). Collectively, DSC analysis nullified any incompatibility between BIM and formulation components.…”

Formulation, optimization and evaluation of ocular gel containing nebivolol Hcl-loaded ultradeformable spanlastics nanovesicles: In vitro and in vivo studies

“…The developed formulae were inspected visually on a black-and-white background for physical properties such as color, clarity, and homogeneity ( Zafar et al, 2022 ).…”

“…The pH of each formula was measured three times using a pH meter (3505–Jenway, Bibby Scientific Ltd., Dunmow, UK) and the average of the three values was calculated ( Teaima et al, 2021 ; Zafar et al, 2022 ).…”