Ocular pharmacokinetics of bimatoprost formulated in DuraSite compared to bimatoprost 0.03% ophthalmic solution in pigmented rabbit eyes

Shafiee, Afshin; Bowman, Lyle M.; Hou, Eddie; Hosseini, Kamran

doi:10.2147/opth.s48766

Cited by 16 publications

(10 citation statements)

References 39 publications

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“…In addition, the besifloxacin formulation contains DuraSite, a mucoadhesive polyacrylic acid polymer designed to improve the retention time of a drug on the ocular surface. 40 – 44 It is likely that the polyacrylic acid polymer in the besifloxacin formulation retained besifloxacin on the ocular surface longer, thereby augmenting besifloxacin’s intrinsic bactericidal activity. The formulation of moxifloxacin tested in this investigation contains no vehicle components to increase surface contact time.…”

Section: Discussionmentioning

confidence: 99%

Antibacterial efficacy of prophylactic besifloxacin 0.6% and moxifloxacin 0.5% in patients undergoing cataract surgery

Bucci¹,

Evans²,

Amico³

et al. 2015

OPTH

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BackgroundThe purpose of this study was to investigate the ocular bacterial flora in patients scheduled to undergo cataract surgery and compare the antibacterial effects of besifloxacin ophthalmic suspension 0.6% and moxifloxacin ophthalmic solution 0.5% in these patients.MethodsThis was a prospective, randomized, laboratory-masked clinical trial. Patients received besifloxacin or moxifloxacin “quater in die” or QID (four times a day) for 3 days before cataract surgery in the surgical eye and 1 hour before surgery in the nonsurgical fellow eye. Conjunctival and eyelid swabs were obtained from both eyes at baseline and after treatment, on the day of surgery (Visit 2). Swabs were processed for bacterial colony counts (in terms of colony-forming units) and species identification. In vitro antibiotic susceptibilities of isolates were determined using Clinical and Laboratory Standards Institute breakpoints.ResultsFifty-nine patients (n=28 besifloxacin, n=31 moxifloxacin) completed the study. The majority (73%) of conjunctival samples were culture negative at baseline. The most frequent isolates were coagulase-negative staphylococci (CoNS, 89%), specifically Staphylococcus epidermidis (72%). Both fluoroquinolones reduced the lid CFU values when administered QID for 3 days (P≤0.019), but only besifloxacin reduced the lid CFU estimate 1 hour following instillation of a single drop (P=0.039). Fewer besifloxacin-treated eyes had lids that were culture positive for CoNS at Visit 2 compared with moxifloxacin-treated eyes regardless of dosing regimen (P≤0.03). The minimum inhibitory concentration (MIC90) of besifloxacin against methicillin-resistant S. epidermidis (MRSE) was eightfold lower than that of moxifloxacin.ConclusionBesifloxacin appeared more effective in reducing bacterial counts on eyelids of patients undergoing cataract surgery, with significant reductions as early as 1 hour postdose, compared with moxifloxacin. Besifloxacin was more active in vitro against MRSE.

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Section: Discussionmentioning

confidence: 99%

Antibacterial efficacy of prophylactic besifloxacin 0.6% and moxifloxacin 0.5% in patients undergoing cataract surgery

Bucci¹,

Evans²,

Amico³

et al. 2015

OPTH

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“…DuraSite® is a mucoadhesive material long used to enhance the residence time of a pharmaceutical on the ocular surface, has been evaluated in several other topical ophthalmic formulations, and its efficacy and safety data is well known [ 12 – 16 ].…”

Section: Methodsmentioning

confidence: 99%

Twice-Daily vs. Once-Daily Dosing with 0.075% Bromfenac in DuraSite: Outcomes from a 14-Day Phase 2 Study

Trattler

Hosseini²

2017

Ophthalmol Ther

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IntroductionBromfenac is a well-known topical ophthalmic nonsteroidal anti-inflammatory drug (NSAID) that is commercialized in the USA and other regions of the world. A new formulation, 0.075% bromfenac in DuraSite®, was developed to treat postoperative inflammation and reduce pain in patients who have undergone cataract surgery. We hypothesized that efficacy and safety would be enhanced with twice-daily (BID) dosing compared to once-daily (QD) dosing.MethodsThis was a multicenter, double-masked, comparative study in which 40 and 45 subjects were randomized to groups receiving BID dosing and QD dosing, respectively. Subjects self-instilled the study drug for 14 days postoperative and were followed for an additional 2-week evaluation phase. The primary efficacy endpoint was the proportion of subjects with an anterior chamber cell (ACC) grade of 0 at day 15.ResultsA total of 45 subjects had cleared ACC (grade “0”) at day 15, of whom 21 were in the BID group (52.5%) and 24 were in the QD group (53.5%). A secondary analysis found 7/40 (17.5%) subjects in the BID group and 10/45 (22.2%) subjects in the QD group achieved an ACC grade of 0 at day 8. There were more adverse events in the QD group (n = 16) than in the BID group (n = 12).ConclusionSimilar outcomes were observed for subjects using Bromfenac 0.075% in DuraSite® in the BID and QD dosing regimens for the treatment of post-cataract surgery inflammation.Trial registrationClinicalTrials.gov identifier, NCT01190878.FundingInSite Vision (now a division of Sun Pharma).

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“…DuraSite ® system containing BMT showed ocular bioavailability superior to the conventional eye drops. However these (AzaSite and Besivance) need to be administered daily [66]. Similarly a chitosan-based ocular insert for BMT is also reported, which showed an effectiveness for over a month following sub-conjunctival application [67].…”

Section: Sterility Testingmentioning

confidence: 99%

Bimatoprost loaded nanovesicular long-acting sub-conjunctival in-situ gelling implant: In vitro and in vivo evaluation

Yadav

Guzmán-Aránguez

Lara

et al. 2019

Materials Science and Engineering: C

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Primary treatment for glaucoma relies on chronic instillation (daily) of intraocular pressure (IOP) lowering eye drops. Present study tends to develop and assess a novel sustained release bimatoprost loaded nanovesicular (BMT-NV)-thermosensitive in-situ gelling implant (BMT-NV-GEL-IM), for subconjunctival delivery. BMT-NVs developed using novel composition and method of preparation, (IPA/700/DEL/2014) and industrially viable methodology were characterised and evaluated comprehensively for ocular suitability. Their incorporation into an in-situ gelling formula was safe (in vitro and in vivo) and stable upon sterilization. Autoclavability was an important consideration, as a preservative-free, single-use BMT-NV-GEL-IM will avoid side-effects associated with repetitive application of drops containing preservatives like benzalkonium chloride (BAK). An extended in vitro release of BMT (80.23%) was observed for 10 days while the IOP lowering effect extended over 2 months with single subconjunctival injection of BMT-NV-GEL-IM in rats. No clinical signs of irritation, inflammation, or infection were observed in any injected eye, throughout the study, as also confirmed by histology. Furthermore, single administration of BMT-NV-GEL as topical drop lowered the IOP over 5 days. Presence of significant diffuse fluorescence in confocal microscopy of internal eye tissues post-in vivo application, as subconjunctival implant, even after 2 month and eye drops upto1 week provide direct evidence of successful sustained delivery. We thus provide an

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Ocular pharmacokinetics of bimatoprost formulated in DuraSite compared to bimatoprost 0.03% ophthalmic solution in pigmented rabbit eyes

Cited by 16 publications

References 39 publications

Antibacterial efficacy of prophylactic besifloxacin 0.6% and moxifloxacin 0.5% in patients undergoing cataract surgery

Antibacterial efficacy of prophylactic besifloxacin 0.6% and moxifloxacin 0.5% in patients undergoing cataract surgery

Twice-Daily vs. Once-Daily Dosing with 0.075% Bromfenac in DuraSite: Outcomes from a 14-Day Phase 2 Study

Bimatoprost loaded nanovesicular long-acting sub-conjunctival in-situ gelling implant: In vitro and in vivo evaluation

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