Besifloxacin-loaded ocular nanoemulsions: design, formulation and efficacy evaluation

Kassaee, Seyedeh Negin; Mahboobian, Mohammad Mehdi

doi:10.1007/s13346-021-00902-z

Cited by 28 publications

(17 citation statements)

References 53 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The findings of the study indicated that the ingredients used to formulate MX-BS-Ig were safe for ocular administration. This result agreed with previously reported research, i.e., besifloxacin and acyclovir nano-emulsion, and did not show any damage to the CAM with a score closer to zero [15,54].…”

Section: Het-cam Studysupporting

confidence: 93%

“…Now, researchers mainly focus on colloidal delivery systems for the improvement of ocular bioavailability and therapeutic efficacy. Different ocular nanocolloidal delivery systems for drugs such as gatifloxacin [ 7 ], fluorometholone [ 8 ], thymoquinone [ 9 ], pilocarpine hydrochloride [ 10 ], betaxolol [ 11 ], methazolamide [ 12 ], dexamethasone [ 13 ], ciprofloxacin [ 14 ], besifloxacin [ 15 ], doxylamine succinate/pyridoxine hydrochloride [ 16 ], and clarithromycin [ 17 ] have been reported with greater therapeutic activity.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

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

Zafar

Alsaidan

Imam

et al. 2022

Gels

View full text Add to dashboard Cite

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.

show abstract

Section: Het-cam Studysupporting

confidence: 93%

Section: Introductionmentioning

confidence: 99%

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

Zafar

Alsaidan

Imam

et al. 2022

Gels

View full text Add to dashboard Cite

show abstract

“…Distilled water was added dropwise to a mixture of oil and Km under gentle magnetic stirring at 37 until the mixture became clear at a certain point. The critical points between the NE region and other phase regions were recorded when the appearance of the system changed from clear to turbid and vice versa (Shao et al., 2021 ; Kassaee & Mahboobian, 2022 ). The amount of water consumption was used to calculate the final weight percentages of water, oil and Km in order to complete the pseudoternary phase diagrams.…”

Section: Methodsmentioning

confidence: 99%

Preparation and in vitro and in vivo evaluation of an isoliquiritigenin-loaded ophthalmic nanoemulsion for the treatment of corneal neovascularization

Zhang¹,

Yang

Luo

et al. 2022

Drug Delivery

View full text Add to dashboard Cite

Isoliquiritigenin (ISL), as a natural flavonoid, has been proven to have therapeutic potential for corneal neovascularization (CNV) treatment; however, its therapeutic use is restricted due to its poor aqueous solubility and limited bioavailability. To overcome these limitations, a novel ISL-loaded nanoemulsion (ISL-NE) was designed for inhibiting CNV in this study. ISL-NE formulation was composed of propylene glycol dicaprylate (PGD), Cremophor® EL (EL35), polyethylene glycol 400 (PEG 400) and adding water with sodium hyaluronate, its particle size was 34.56 ± 0.80 nm with a low polydispersity index of less than 0.05, which suggested a narrow size distribution. The results demonstrated that ISL-NE released higher and permeated more drug than ISL suspension (ISL-Susp) in in vitro drug release and ex vivo corneal permeation study. ISL-NE showed no cytotoxicity in human corneal epithelial cells toxicity study, which was consistent with the result of ocular irritation study in rabbit eyes. ISL-NE had bioavailability 5.76-fold, 7.80-fold and 2.13-fold higher than ISL-Sups in tears, cornea and aqueous humor after a single dose of ISL-NE, respectively. Furthermore, the efficacy of ISL-NE treatment (0.2% ISL) was comparable to that of dexamethasone treatment (0.025%) in the inhibition of CNV in mice model. Enzyme-linked immunosorbent assay (ELISA) showed that the expressions of corneal vascular endothelial growth factor (VEGF-A) and matrix metalloproteinase (MMP-2) were decreased. In conclusion, the ISL-NE demonstrated excellent physicochemical properties, good tolerance, and enhanced ocular bioavailability. It could be a promising, safe, and effective treatment for CNV.

show abstract

“…Distilled water was added dropwise to a mixture of oil and S/Cos (Km) under gentle magnetic stirring at 37 °C until the mixture became clear at a certain point (Kassaee & Mahboobian, 2021 ; Zeng et al., 2021 ). The system with low viscosity and a clear appearance was considered to be a microemulsion.…”

Section: Methodsmentioning

confidence: 99%

Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: in vitro and in vivo evaluation

Yang

Zhang

et al. 2021

Drug Delivery

View full text Add to dashboard Cite

Naringenin, a flavonoid, possesses antiangiogenic potential and inhibits corneal neovascularization (CNV); however, its therapeutic use is restricted due to poor solubility and limited bioavailability. In this study, we developed a naringenin microemulsion (NAR-ME) for inhibiting CNV. NAR-ME formulation was composed of triacetin (oil phase), Cremophor RH40 (CRH40), PEG400, and water, its droplet size was 13.22 ± 0.13 nm with a narrow size distribution (0.112 ± 0.0014). The results demonstrated that NAR-ME released higher and permeated more drug than NAR suspension (NAR-Susp) in in vitro drug release and ex vivo corneal permeation study. Human corneal epithelial cells (HCECs) toxicity study showed no toxicity with NAR-ME, which is consistent with the result of ocular irritation study. NAR-ME had high bioavailability 1.45-fold, 2.15-fold, and 1.35-fold higher than NAR-Susp in the cornea, conjunctiva, and aqueous humor, respectively. Moreover, NAR-ME (0.5% NAR) presented efficacy comparable to that of dexamethasone (0.025%) in the inhibition of CNV in mice CNV model induced by alkali burning, resulting from the attenuation of corneal vascular endothelial growth factor (VEGF) and matrix metalloproteinase (MMP-14) expression. In conclusion, the optimized NAR-ME formulation demonstrated excellent physicochemical properties and good tolerance, enhanced ocular bioavailability and corneal permeability. This formulation is promising, safe, and effective for the treatment of CNV.

show abstract

Besifloxacin-loaded ocular nanoemulsions: design, formulation and efficacy evaluation

Cited by 28 publications

References 53 publications

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

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

Preparation and in vitro and in vivo evaluation of an isoliquiritigenin-loaded ophthalmic nanoemulsion for the treatment of corneal neovascularization

Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: in vitro and in vivo evaluation

Contact Info

Product

Resources

About