Besifloxacin: A Critical Review of Its Characteristics, Properties, and Analytical Methods

Tótoli, Eliane Gandolpho; Salgado, Hérida Regina Nunes

doi:10.1080/10408347.2018.1429885

Cited by 17 publications

(21 citation statements)

References 68 publications

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“…from Tokyo, Japan (former SS734). It has been approved by the FDA in 2009 and registered under the trade name Besivance (Bausch & Lomb Inc., Rochester, NY, USA) [ 46 , 98 , 101 , 102 ]. Besifloxacin is indicated for the treatment of bacterial conjunctivitis [ 98 , 103 ].…”

Section: Compounds In Therapy Since 2000mentioning

confidence: 99%

“…Gatifloxacin is administered for ophthalmic use only after the withdrawal from systemic use due to its side effects (hypo- and hyperglycemia) [ 43 , 108 , 109 ]. The approved pharmaceutical formulation of besifloxacin is an ophthalmic suspension 0.6%, which contains 6.63 mg of besifloxacin hydrochloride (equivalent to 6 mg of besifloxacin) [ 46 , 95 , 96 , 97 , 107 ]. At present, attempts are being made to develop several ophthalmic pharmaceutical formulas with besifloxacin, such as nanoemulsions [ 110 ], positively charged liposomes [ 111 ], and for the treatment of bacterial keratitis new loaded nanofibrous ocular inserts [ 112 ].…”

Section: Compounds In Therapy Since 2000mentioning

confidence: 99%

“…A second substitution in the C8 position with a chlorine atom add an increased antimicrobial potency through the action on the target enzymes DNA gyrase and topoisomerase IV [ 46 , 123 ]. Also, C8 chlorine increases the antibacterial activity against FQN-resistant mutants of Mycobacterium smegmatis and Staphylococcus aureus [ 121 ].…”

Section: Compounds In Therapy Since 2000mentioning

confidence: 99%

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Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation

et al. 2021

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The evolution of the class of antibacterial quinolones includes the introduction in therapy of highly successful compounds. Although many representatives were withdrawn due to severe adverse reactions, a few representatives have proven their therapeutical value over time. The classification of antibacterial quinolones into generations is a valuable tool for physicians, pharmacists, and researchers. In addition, the transition from one generation to another has brought new representatives with improved properties. In the last two decades, several representatives of antibacterial quinolones received approval for therapy. This review sets out to chronologically outline the group of approved antibacterial quinolones since 2000. Special attention is given to eight representatives: besifloxacin, delafoxacin, finafloxacin, lascufloxacin, nadifloxacin and levonadifloxacin, nemonoxacin, and zabofloxacin. These compounds have been characterized regarding physicochemical properties, formulations, antibacterial activity spectrum and advantageous structural characteristics related to antibacterial efficiency. At present these new compounds (with the exception of nadifloxacin) are reported differently, most often in the fourth generation and less frequently in a new generation (the fifth). Although these new compounds’ mechanism does not contain essential new elements, the question of shaping a new generation (the fifth) arises, based on higher potency and broad spectrum of activity, including resistant bacterial strains. The functional groups that ensured the biological activity, good pharmacokinetic properties and a safety profile were highlighted. In addition, these new representatives have a low risk of determining bacterial resistance. Several positive aspects are added to the fourth fluoroquinolones generation, characteristics that can be the basis of the fifth generation. Antibacterial quinolones class continues to acquire new compounds with antibacterial potential, among other effects. Numerous derivatives, hybrids or conjugates are currently in various stages of research.

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Section: Compounds In Therapy Since 2000mentioning

confidence: 99%

Section: Compounds In Therapy Since 2000mentioning

confidence: 99%

Section: Compounds In Therapy Since 2000mentioning

confidence: 99%

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Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation

et al. 2021

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“…This may minimize resistance because mutations of both enzymes are required for resistance to develop [2]. Besifloxacin is a very important drug for the treatment of infectious conjunctivitis since it presents less occurrence of bacterial resistance than other drugs used for the same purpose and, at the same time, presents great efficacy and tolerability [3]. Besifloxacin is a topical synthetic fluoroquinolone and represents the first chlorofluoroquinolone developed specifically for the topical treatment of ophthalmic infections [4].…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Besifloxacin Non-Erodible Ocular Inserts

PATIL¹,

Patil²

2022

Int J App Pharm

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Objective: Ocular inserts offer many advantages over conventional dosage forms, like increased ocular residence, the possibility of releasing a drug at a slow and constant rate, accurate dosing, exclusion of preservatives, and increased shelf life. Besifloxacin is a very important drug for the treatment of infectious conjunctivitis. The present study was aimed to formulate and evaluate Besifloxacin Non-Erodible Ocular Insert using Pullulan and polyvinyl pyrrolidone as a drug reservoir, PEG 400 as a plasticizer, and Eudragit RS-100 as a rate-controlling membrane. Methods: Central composite design was employed to study the effect of independent variables, i.e., effects of Pullulan amount (X1) and PVP (X2) on the dependent variables, i.e., % moisture absorption and In vitro diffusion rate. After evaluation of all thirteen batches of ocular insert reservoir formulation, BSF2 and BSF4 were selected as a satisfactory formulation and was sandwiched between rate-controlling membrane, which was made up of Eudragit RS-100 (3 and 5%). Results: The drug content of all formulations was found to be in the range of 95.33 to 99.89 %. In vitro diffusion of Besifloxacin from reservoir formulations (BSF1 to BSF13) was found to be 62.44 to 70.62 %. In vitro diffusion rate of an ocular insert of Besifloxacin can offer benefits such as increasing residence time, prolonging drug release in the eye for 24 h. Eudragit RS-100, as a sustained drug release polymer, showed promising sustained released action. Conclusion: The study concluded that Besifloxacin non-erodible ocular inserts can be successfully developed using Pullulan and polyvinyl pyrrolidone, which will sustain the release of the drug also reduce the frequency of administration, and thereby may help to improve patient compliance.

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“…This drug is gaining interest owing to its remedial potential (Tótoli, Regina, & Salgado, ). However, for any drug, stability throughout its shelf‐life with respect to purity, quality and efficacy is important.…”

Section: Introductionmentioning

confidence: 99%

Study of degradation behavior of besifloxacin, characterization of its degradation products by LC–ESI–QTOF–MS and their in silico toxicity prediction

Salunke

Kharkar

Pandita

2019

Biomedical Chromatography

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Knowledge and understanding of the stability profile of a drug is important as it affects its safety and efficacy. In the present work, besifloxacin, a new, fourth-generation fluoroquinolone antibiotic, was subjected to different forced-degradation conditions as per International Conference on Harmonization (ICH) guidelines such as hydrolysis (acid, base and neutral), oxidation, thermal and photolysis. The drug degraded under acidic, basic, oxidative and photolytic conditions while it was found to be stable under dry heat and neutral hydrolytic conditions. In total, five degradation products (DPs) were formed under different conditions-DP1 and DP2 (photolysis), DP3 (oxidation), DP4 (acidic), DP3 and DP5 (basic). The chromatographic separation of besifloxacin and its degradation products was achieved on a Sunfire C 18 (250 mm × 4.6 mm, 5 μm) column with 0.1% aqueous formic acid-acetonitrile as a mobile phase. The gradient RP-HPLC method was developed and validated as per ICH guidelines. The degradation products were characterized with the help of LC-ESI-QTOF mass spectrometric studies and the most likely degradation pathway of the drug was proposed. In silico toxicity assessment of the drug and its degradation products was carried out, which indicated that DP3 and DP4 carry a mutagenicity alert.

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Besifloxacin: A Critical Review of Its Characteristics, Properties, and Analytical Methods

Cited by 17 publications

References 68 publications

Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation

Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation

Formulation and Evaluation of Besifloxacin Non-Erodible Ocular Inserts

Study of degradation behavior of besifloxacin, characterization of its degradation products by LC–ESI–QTOF–MS and their in silico toxicity prediction

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