Besifloxacin liposomes with positively charged additives for an improved topical ocular delivery

Santos, Giselly Almeida dos; Ferreira‐Nunes, Ricardo; Dalmolin, Luciana Facco; Ré, Ana Carolina dos Santos; Anjos, Jorge Luiz Vieira dos; Mendanha, Sebastião Antônio; Aires, Carolina Patrícia; Lopez, Renata Fonseca Vianna; Cunha-Filho, Marcílio; Gelfuso, Guilherme M.; Gratieri, Taís

doi:10.1038/s41598-020-76381-y

Cited by 42 publications

(21 citation statements)

References 76 publications

(115 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The liposome is an ideal drug carrier owing to its remarkable biocompatibility, high degradability, flexibility, nonimmunogenicity, nontoxicity, and being mimetic to cell membrane architect, enabling the encapsulation of both lipophilic and hydrophilic drugs and delivering the medicaments effectively in both anterior and posterior chambers [ 94 ]. Various studies investigated the liposomal drug delivery for improving dissolution, bioavailability, precorneal penetration, increased residence time, and targeted action [ 39 , 95 , 96 ].…”

Section: Novel Ocular Therapeutic Systemsmentioning

confidence: 99%

“…The result anticipated that liposomes LP PC:SPM expressed higher drug penetration than the marketed preparation, Besivance. Therefore, besifloxacin-loaded positive (+) liposomes ameliorated the passive delivery of drug upon topical instillation and could be considered a novel approach to enhance the ophthalmic disease therapy [ 39 ].…”

Section: Novel Ocular Therapeutic Systemsmentioning

confidence: 99%

See 1 more Smart Citation

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Akhter

Ahmad

Alshahrani

et al. 2022

Gels

View full text Add to dashboard Cite

Drug instillation via a topical route is preferred since it is desirable and convenient due to the noninvasive and easy drug access to different segments of the eye for the treatment of ocular ailments. The low dose, rapid onset of action, low or no toxicity to the local tissues, and constrained systemic outreach are more prevalent in this route. The majority of ophthalmic preparations in the market are available as conventional eye drops, which rendered <5% of a drug instilled in the eye. The poor drug availability in ocular tissue may be attributed to the physiological barriers associated with the cornea, conjunctiva, lachrymal drainage, tear turnover, blood–retinal barrier, enzymatic drug degradation, and reflex action, thus impeding deeper drug penetration in the ocular cavity, including the posterior segment. The static barriers in the eye are composed of the sclera, cornea, retina, and blood–retinal barrier, whereas the dynamic barriers, referred to as the conjunctival and choroidal blood flow, tear dilution, and lymphatic clearance, critically impact the bioavailability of drugs. To circumvent such barriers, the rational design of the ocular therapeutic system indeed required enriching the drug holding time and the deeper permeation of the drug, which overall improve the bioavailability of the drug in the ocular tissue. This review provides a brief insight into the structural components of the eye as well as the therapeutic challenges and current developments in the arena of the ocular therapeutic system, based on novel drug delivery systems such as nanomicelles, nanoparticles (NPs), nanosuspensions, liposomes, in situ gel, dendrimers, contact lenses, implants, and microneedles. These nanotechnology platforms generously evolved to overwhelm the troubles associated with the physiological barriers in the ocular route. The controlled-drug-formulation-based strategic approach has considerable potential to enrich drug concentration in a specific area of the eye.

show abstract

Section: Novel Ocular Therapeutic Systemsmentioning

confidence: 99%

Section: Novel Ocular Therapeutic Systemsmentioning

confidence: 99%

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Akhter

Ahmad

Alshahrani

et al. 2022

Gels

View full text Add to dashboard Cite

show abstract

“…It is assumed that liposomes with positive charge diffuse slower in the vitreous body mainly due to the presence of constituents such as hyaluronic acid and heparan sulfate [ 177 ]. In contrast, the liposomal surface charge did not prove to improve the topical ocular besifloxacin delivery via iontophoretic treatment [ 178 ]. Both commercial and liposome formulations demonstrated an identical increase in permeability rate consequent to the electrical charge application.…”

Section: Nanocarriers In Ocular Drug Deliverymentioning

confidence: 99%

Lipid Nanoparticles as a Promising Drug Delivery Carrier for Topical Ocular Therapy—An Overview on Recent Advances

et al. 2022

View full text Add to dashboard Cite

Due to complicated anatomical and physical properties, targeted drug delivery to ocular tissues continues to be a key challenge for formulation scientists. Various attempts are currently being made to improve the in vivo performance of therapeutic molecules by encapsulating them in various nanocarrier systems or devices and administering them via invasive/non-invasive or minimally invasive drug administration methods. Biocompatible and biodegradable lipid nanoparticles have emerged as a potential alternative to conventional ocular drug delivery systems to overcome various ocular barriers. Lipid-based nanocarrier systems led to major technological advancements and therapeutic advantages during the last few decades of ocular therapy, such as high precorneal residence time, sustained drug release profile, minimum dosing frequency, decreased drug toxicity, targeted site delivery, and, therefore, an improvement in ocular bioavailability. In addition, such formulations can be given as fine dispersion in patient-friendly droppable preparation without causing blurred vision and ocular sensitivity reactions. The unique advantages of lipid nanoparticles, namely, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and liposomes in intraocular targeted administration of various therapeutic drugs are extensively discussed. Ongoing and completed clinical trials of various liposome-based formulations and various characterization techniques designed for nanoemulsion in ocular delivery are tabulated. This review also describes diverse solid lipid nanoparticle preparation methods, procedures, advantages, and limitations. Functionalization approaches to overcome the drawbacks of lipid nanoparticles, as well as the exploration of new functional additives with the potential to improve the penetration of macromolecular pharmaceuticals, would quickly progress the challenging field of ocular drug delivery systems.

show abstract

“…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%

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

et al. 2021

View full text Add to dashboard Cite

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.

show abstract

Besifloxacin liposomes with positively charged additives for an improved topical ocular delivery

Cited by 42 publications

References 76 publications

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Drug Delivery Challenges and Current Progress in Nanocarrier-Based Ocular Therapeutic System

Lipid Nanoparticles as a Promising Drug Delivery Carrier for Topical Ocular Therapy—An Overview on Recent Advances

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

Contact Info

Product

Resources

About