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1.
Acta Cir Bras ; 34(12): e201901206, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32049186

RESUMO

PURPOSE: To evaluate the effects of prednisolone against sodium diclofenac both with ciprofloxacin compared to artificial tears on the symptoms and signs of acute viral conjunctivitis. METHODS: Study included 37 patients diagnosed with acute conjunctivitis and distributed by three groups: A (1% prednisolone acetate + ciprofloxacin (0.3%); B (Sodium diclofenac (0.1%) + ciprofloxacin (0.3%) and C (artificial tears + ciprofloxacin (0.3%). Patients received medication 6/6 hours daily. Signs and symptoms (e.g. lacrimation, burning, photophobia, etc.) were scored at baseline and on the first, third, fifth and seventh days and in the end of treatment using a standardized questionnaire and slit lamp anterior segment examination. RESULTS: All three groups demonstrated an improvement in the signs and symptoms of conjunctivitis in their follow-up visits. There was no significant difference in symptom and sign scores between Group A and B and B and C in the study visits ( p >0.05). However, the comparison between groups A and C showed a clinical trend (p=0.05) on third evaluation suggesting better clinical action using the corticosteroids. CONCLUSION: The prednisolone acetate was not superior to the use of sodium diclofenac or artificial tears in relieving the signs and symptoms of viral conjunctivitis.


Assuntos
Corticosteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/administração & dosagem , Ciprofloxacino/administração & dosagem , Conjuntivite Viral/tratamento farmacológico , Diclofenaco/administração & dosagem , Prednisolona/análogos & derivados , Doença Aguda , Adolescente , Adulto , Idoso , Análise de Variância , Feminino , Humanos , Interferon gama , Interleucinas/análise , Lubrificantes Oftálmicos/administração & dosagem , Masculino , Pessoa de Meia-Idade , Óxido Nítrico Sintase/análise , Soluções Oftálmicas/administração & dosagem , Prednisolona/administração & dosagem , Resultado do Tratamento , Fator de Necrose Tumoral alfa/análise , Adulto Jovem
2.
Niger J Clin Pract ; 23(1): 123-125, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31929219

RESUMO

Autologous serum drop (ASD) is a safe and efficient treatment option for most of the ocular surface diseases. We report a case of a persistent corneal epithelial defect in a patient treated by ASD. A 28 year old male patient presented to our clinic with eye pain and blurry vision in his left eye. Best corrected visual acuity (BCVA) was 20/20 in the right eye and 20/200 in the left eye. Slit lamp examination revealed a central corneal epithelial defect on the left eye and the right eye was normal. Corneal epithelial defect appeared after left upper eyelid chalazion surgery and persisted for 2 months without any response to treatment with eye patching, bandage contact lenses, and artificial eyedrops. We started the treatment with ASD six times daily and preservative-free netilmicin eyedrops four times daily to prevent infection. The drops were used simultaneously with eyepatching for the first two days. The eye was left unpatched after the second day. The corneal epithelial defect resolved after 48 hours. We did not detect a new epithelial defect in the follow up visits. ASD is a quick, safe, and effective treatment option in persistent epithelial defect cases.


Assuntos
Doenças da Córnea/terapia , Epitélio Anterior/efeitos dos fármacos , Dor Ocular/etiologia , Soluções Oftálmicas/administração & dosagem , Soro , Adulto , Calázio/cirurgia , Doenças da Córnea/etiologia , Doenças da Córnea/fisiopatologia , Epitélio Anterior/fisiopatologia , Humanos , Masculino , Soluções Oftálmicas/uso terapêutico , Procedimentos Cirúrgicos Oftalmológicos/efeitos adversos , Complicações Pós-Operatórias , Resultado do Tratamento , Acuidade Visual , Cicatrização
3.
Eur J Ophthalmol ; 30(1): 119-124, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30378440

RESUMO

OBJECTIVES: Complete epithelial wound healing is a milestone in early postoperative care after penetrating keratoplasty. The re-epithelialization rate after penetrating keratoplasty was measured in patients receiving a new matrix therapy agent (regenerating agent, Cacicol®) that mimics heparan sulphates. METHODS: This was a prospective, open-label, uncontrolled, single-centre observational study. A total of 33 consecutive patients (33 eyes) who underwent an 8.25-mm diameter penetrating keratoplasty were treated with regenerating agent eye drops: one drop in the operating theatre immediately after graft, then on alternate days. Patients were divided into those at low risk (13 patients) and high risk (20 patients) of delayed wound healing, and follow-up was performed by digital slit lamp with fluorescein-dye testing repeated daily at a fixed time. Dye area was measured using ImageJ freeware. The main endpoint was epithelial healing after regenerating agent therapy. RESULTS: The mean ± standard deviation time to complete healing for all patients was 2.7 ± 1.1 (median: 3, range: 1-6) days. This was obtained on Day 1 for 15% of patients, Day 2 for 33%, Day 3 for 88%, Day 4 for 94% and Day 6 for 100%. There was no significant difference between low- and high-risk patients. The area of epithelial defect decreased by a mean ± standard deviation of 75% ± 22% between Day 1 and Day 2, corresponding to a mean ± standard deviation wound-healing rate of 11.5 ± 6.5 mm2/D. There were no systemic or local side effects related to regenerating agent. CONCLUSION: These preliminary data suggest that regenerating agent could be a useful, non-invasive therapeutic approach in postoperative management of penetrating keratoplasty with the potential to accelerate re-epithelialization.


Assuntos
Epitélio Anterior/patologia , Glicosaminoglicanos/administração & dosagem , Ceratoplastia Penetrante/métodos , Cuidados Pós-Operatórios/métodos , Cicatrização , Adulto , Idoso , Idoso de 80 Anos ou mais , Úlcera da Córnea/cirurgia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/administração & dosagem , Estudos Prospectivos , Resultado do Tratamento , Adulto Jovem
4.
Am J Vet Res ; 81(1): 41-46, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31887086

RESUMO

OBJECTIVE: To evaluate effects of topical ophthalmic administration of diclofenac on intraocular pressure (IOP) when applied at 4 frequencies to eyes of Beagles. ANIMALS: 8 ophthalmologically normal Beagles. PROCEDURES: The study involved four 5-day experimental periods each separated by a 16-day washout period. During each period, 1 drop of 0.1% diclofenac sodium ophthalmic solution was administered to the right eye at 4 treatment frequencies (1, 2, 3, or 4 times/d); 1 drop of eyewash was administered to the left eye as a control treatment. A complete ophthalmic examination was performed on days 0 (day before first treatment) and 5 of each experimental period. Gonioscopy was performed on day 0 of the first period. The IOPs were measured at 7 am and 7 pm on days 1 through 5. RESULTS: No abnormalities were detected during neuro-ophthalmic and ophthalmic examinations on day 0 of each experimental period. No adverse reactions to administration of diclofenac or eyewash were observed at any time point. No abnormalities were detected during ophthalmic examinations performed on day 5, and IOPs remained < 25 mm Hg in all 4 periods. No significant differences were identified between the treated and control eyes or among the 4 treatment frequencies. CONCLUSIONS AND CLINICAL RELEVANCE: Topical ophthalmic administration of diclofenac up to 4 times/d in dogs with no ophthalmic abnormalities did not significantly increase the IOP. Additional research is needed to evaluate the effect of topical ophthalmic administration of diclofenac on IOP in dogs with anterior uveitis.


Assuntos
Diclofenaco/farmacologia , Pressão Intraocular/efeitos dos fármacos , Soluções Oftálmicas/farmacologia , Administração Oftálmica , Administração Tópica , Animais , Diclofenaco/administração & dosagem , Cães , Esquema de Medicação , Olho/efeitos dos fármacos , Feminino , Masculino , Soluções Oftálmicas/administração & dosagem , Tonometria Ocular/veterinária
5.
Invest Ophthalmol Vis Sci ; 60(15): 5035-5044, 2019 12 02.
Artigo em Inglês | MEDLINE | ID: mdl-31800960

RESUMO

Purpose: To compare the changes in human tear proteome and clinical effects following topical cyclosporine A (CsA) 0.05% or diquafosol tetrasodium (DQS) 3% treatment of dry eye disease (DED), and to identify biomarkers for determining disease severity and treatment effectiveness in DED. Methods: A total of 18 patients were diagnosed with non-Sjögren DED. Nine patients in each group were treated with topical CsA 0.05% or DQS 3% for 4 weeks. Tear samples were collected after evaluation of tear breakup time, corneal and conjunctival erosion staining, and results of Schirmer's test 1 before and after treatment. Proteomes were characterized using liquid chromatography mass spectrometry, and proteins exhibiting a fold change >1.5 or <0.67 (P < 0.05) were considered differentially expressed (DEP). Results: A total of 794 proteins were identified, with no significant difference observed between pretreatment and posttreatment conditions. Proteomic analysis identified 54 and 106 DEPs between treatment groups (CsA and DQS, respectively), with gene ontology analysis indicating that both treatments enhanced innate and adaptive immune responses and cellular detoxification. Protein-network analysis showed that inflammation associated with the immune response was primarily responsible for the therapeutic process in both groups. Conclusions: These results provide insight into the broad scope of changes at the ocular surface in DED and indicated that although both drugs improved the clinical parameters, the activated tear-specific biomarkers differed significantly between treatments. Our findings suggest that the DEPs identified here and those correlated with the clinical parameters might represent candidate biomarkers for DED.


Assuntos
Ciclosporina/administração & dosagem , Síndromes do Olho Seco/tratamento farmacológico , Polifosfatos/administração & dosagem , Proteoma/metabolismo , Lágrimas/metabolismo , Nucleotídeos de Uracila/administração & dosagem , Administração Tópica , Túnica Conjuntiva/metabolismo , Túnica Conjuntiva/patologia , Córnea/metabolismo , Córnea/patologia , Relação Dose-Resposta a Droga , Síndromes do Olho Seco/metabolismo , Feminino , Seguimentos , Humanos , Imunossupressores/administração & dosagem , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/administração & dosagem , Estudos Prospectivos , Método Simples-Cego , Lágrimas/efeitos dos fármacos , Resultado do Tratamento
7.
Exp Eye Res ; 189: 107829, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31605685

RESUMO

Approximately 30-70% of the existing and new chemical entities exhibit poor aqueous solubility. For topical ocular delivery, drug molecules need to possess both hydrophilic and lipophilic nature to enable absorption through the aqueous tear layer and permeation through the corneal lipophilic barrier. To overcome the aqueous solubility related issues, various techniques such as solid dispersion, particle size reduction, cyclodextrin complexation, co-solvency, prodrug, derivatization, and salt formation are being explored in the healthcare sector. Cyclodextrin inclusion complexation techniques have been established by several pharmaceutical industries for systemic administration allowing a transition from the lab to the clinics. Though cyclodextrins are exploited in ocular drug delivery, there are prevailing concerns regarding its absorption enhancing capacity and mechanism, retention at the ocular surfaces and, irritation and toxicity profiles. In the present review, the efforts taken by various research groups to address the concerns of using cyclodextrin and its derivatives in ocular therapeutics are summarized. Also, considerations and utility of cyclodextrin systems in fabricating newer formulations such as contact lens, inserts, and implants have been discussed in the review.


Assuntos
Ciclodextrinas/administração & dosagem , Oftalmopatias/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Humanos , Soluções Oftálmicas/administração & dosagem , Resultado do Tratamento
8.
Drug Deliv ; 26(1): 952-964, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31544551

RESUMO

The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q2) and hexagonal (H2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q2 and H2 phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q2 and H2 gel produces a 5.25-fold and 6.23-fold increase in the Papp value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma.


Assuntos
Córnea/efeitos dos fármacos , Géis/administração & dosagem , Géis/química , Glaucoma/tratamento farmacológico , Cristais Líquidos/química , Pilocarpina/administração & dosagem , Pilocarpina/química , Administração Oftálmica , Animais , Humor Aquoso/efeitos dos fármacos , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos/métodos , Pressão Intraocular/efeitos dos fármacos , Masculino , Nanopartículas/química , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/química , Tamanho da Partícula , Permeabilidade/efeitos dos fármacos , Coelhos
10.
AAPS PharmSciTech ; 20(7): 272, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31372767

RESUMO

Bacterial conjunctivitis is a leading cause of ocular infections requiring short-term therapeutic treatment with frequent administration of drugs on daily basis. Topical dosage forms available in the market for the treatment of bacterial conjunctivitis such as simple drug solutions and suspensions are rapidly eliminated from the precorneal space upon instillation due to tear turn over and nasolacrimal drainage, limiting intraocular bioavailability of drug to less than 10% of the administered dose. To overcome issues related to conventional drop, an effort was made to design and evaluate prolong release ophthalmic solution of levofloxacin hemihydrate (LFH) using ion-sensitive in situ gelling polymer. Gellan gum was used as the in situ gelling agent. Formulations were screened based on in vitro gelation time, in vitro drug release, and stability towards sol to gel conversion upon storage. The prototype formulations exhibiting quick in vitro gelling time (< 15 s), prolonged in vitro drug release (18-24 h), and stability for at least 6 months at 25°C/40% relative humidity (RH) and 40°C/25% RH were evaluated for pharmacokinetic studies using healthy New Zealand white rabbits. Tested formulations were found to be well-tolerated and showed significant increase in AUC0-24 (22,660.39 h ng/mL) and mean residence time (MRT 12 h) as compared with commercially available solution Levotop PF® (Ajanta Pharma Ltd., India)(AUC0-24 6414.63 h ng/mL and MRT 4 h). Thus, solution formulations containing in situ gelling polymer may serve as improved drug delivery system providing superior therapeutic efficacy and better patient compliance for the treatment of bacterial conjunctivitis.


Assuntos
Antibacterianos/síntese química , Sistemas de Liberação de Medicamentos/métodos , Levofloxacino/síntese química , Soluções Oftálmicas/síntese química , Polissacarídeos Bacterianos/síntese química , Animais , Antibacterianos/administração & dosagem , Antibacterianos/farmacocinética , Disponibilidade Biológica , Conjuntivite Bacteriana/tratamento farmacológico , Conjuntivite Bacteriana/metabolismo , Composição de Medicamentos , Avaliação Pré-Clínica de Medicamentos/métodos , Liberação Controlada de Fármacos/fisiologia , Levofloxacino/administração & dosagem , Levofloxacino/farmacocinética , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/farmacocinética , Polissacarídeos Bacterianos/administração & dosagem , Polissacarídeos Bacterianos/farmacocinética , Coelhos
11.
Medicine (Baltimore) ; 98(31): e16710, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31374063

RESUMO

BACKGROUND: Dry eye disease (DED) is a chronic ocular surface disease that affects hundreds of millions of people worldwide. Although 0.05% cyclosporine ophthalmic emulsion (CsA OE) has long been prescribed in the U.S. for the treatment of DED, it is not commercially available in China. Our study aims to compare the efficacy and safety profile of 0.05% CsA OE versus vehicle in Chinese patients with moderate to severe DED. METHODS: This was a multicenter, randomized, double-masked, 2-parallel-arm, 3-month phase III study. Patients with moderate to severe DED were randomized to receive twice-daily 0.05% CsA OE or its vehicle, along with unpreserved hypromellose eye drops 3 times per day. Patients were followed up at day 7, 28, 56, and 84, as well as 2 weeks after the medications were discontinued for safety assessment. RESULTS: A total of 240 patients were randomized. The overall effective rate (OER) and efficacy index were significantly better in the CsA OE than vehicle group at all follow up times (all P < .05), and the OER of CsA OE and vehicle group at month 3 was 70.6% and 27.8%, respectively (P < .001) (primary endpoint). The patients in CsA OE group displayed a significant improvement in dry eye symptoms from day 28 and ocular surface test results from day 7 (all P < .05). The ocular surface disease index scores of 0.05% CsA OE treated patients were significantly better than those treated with vehicle control at day 56 and 84 (P = .0061 and <.001, respectively). Drug related adverse events (AEs) were recorded in 6(5%) and 3(2.5%) patients in the CsA OE and vehicle groups respectively (P = .4061) with ocular pain as the most frequently reported AEs, and it was mostly mild to moderate. There were no detrimental effects on visual acuity, intraocular pressure, or vital signs. CONCLUSIONS: Twice-daily instillation of 0.05% CsA OE was effective and well tolerated for the treatment of moderate to severe DED in Chinese population during the 3 months of the study.


Assuntos
Ciclosporina/administração & dosagem , Síndromes do Olho Seco/tratamento farmacológico , Soluções Oftálmicas/administração & dosagem , Adulto , China , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Índice de Gravidade de Doença , Resultado do Tratamento
12.
Int J Pharm ; 570: 118641, 2019 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-31446026

RESUMO

Current information about the pharmacokinetics of an ocular drug can only be achieved by invasive sampling. However, confocal Raman spectroscopy bears the potential to quantify drug concentrations non-invasively. In this project, we evaluated the detection and quantification of ocular ketorolac tromethamine levels with confocal Raman spectroscopy after topical administration. Confocal Raman spectroscopy and high-performance liquid chromatography (HPLC) were compared in terms of sensitivity of detection. Enucleated pig eyes were treated with different concentrations of ketorolac. Hereafter, ketorolac concentrations in the aqueous humor of pig eyes were analyzed by confocal Raman spectroscopy and HPLC. Subsequently, twelve rabbits were treated with Acular™ for four weeks. At several time points, ketorolac concentrations in aqueous humor of the rabbits were measured by confocal Raman spectroscopy followed by drawing an aqueous humor sample for HPLC analysis. In ketorolac treated pig eyes, both ex vivo Raman spectroscopy as well as HPLC were able to detect ketorolac in a broad concentration range. However, in vivo confocal Raman spectroscopy in rabbits was unable to detect ketorolac in contrast to HPLC. To conclude, confocal Raman spectroscopy has the capacity to detect ketorolac tromethamine in vitro, but currently lacks sensitivity for in vivo detection.


Assuntos
Cetorolaco de Trometamina/administração & dosagem , Cetorolaco de Trometamina/química , Administração Tópica , Animais , Humor Aquoso/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Olho/efeitos dos fármacos , Microscopia Confocal/métodos , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/química , Coelhos , Análise Espectral Raman/métodos , Suínos
13.
Ophthalmic Plast Reconstr Surg ; 35(5): e114-e115, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31365511

RESUMO

Over a 2-year period, a 68-year-old woman suffered multiple recurrences of left giant fornix syndrome during the repeated tailing of intensive topical steroids and antibiotics; she had also undergone surgery to reduce the left upper fornix. After a further recurrence during tailing of topical therapy for bilateral disease, treatment with 4 times daily preservative-free povidone-iodine 5% eyedrops was started-with a marked improvement of symptoms and signs within a week. The patient is maintained, symptom-free, on once-daily povidone-iodine drops and dexamethasone 0.1% drops. The dramatic improvement on topical povidone-iodine therapy might suggest that, as an initial therapy, this might be more effective than the previously-recommended regime of hourly potent topical steroids and antibiotics.


Assuntos
Anti-Infecciosos Locais/administração & dosagem , Conjuntivite Bacteriana/tratamento farmacológico , Povidona-Iodo/administração & dosagem , Infecções Estafilocócicas/tratamento farmacológico , Idoso , Feminino , Humanos , Soluções Oftálmicas/administração & dosagem , Resultado do Tratamento
14.
Cornea ; 38(10): 1259-1265, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31306284

RESUMO

BACKGROUND: Keratoconjunctivitis sicca affects 5% to 33% of the population and is often accompanied by symptoms such as burning and dryness. This pooled analysis evaluated total and central corneal fluorescein staining (CFS) in patients receiving OTX-101 0.09% or vehicle in phase 2b/3 and 3 studies and whether improvements in corneal staining correlated with improved visual acuity. METHODS: In these randomized, vehicle-controlled studies, patients received 1 drop of OTX-101 or vehicle in both eyes twice daily. Corneal staining was performed at baseline and days 28, 56, and 84. CFS was evaluated in each zone (0-to-4 scale); total corneal staining (0-to-20 scale per eye) was averaged over both eyes. Pooled safety assessments included adverse event monitoring. RESULTS: Mean baseline CFS total scores (SD) were 4.2 (2.5) and 4.3 (2.6) for the OTX-101 (n = 523) and vehicle (n = 525) groups, respectively. For total corneal staining, least squares mean changes from baseline (standard error) were -0.9 (0.08) versus -0.5 (0.08) for OTX-101 and vehicle, respectively (P = 0.0008), on day 28 and -1.4 (0.09) versus -0.9 (0.09) on day 84 (P = 0.0002). There was a significantly high correlation (P = 0.0117) between reduced central corneal staining and improved visual acuity on day 84. Treatment-related adverse events were mostly mild, with instillation site pain reported by 21.8% and 4.0% of patients receiving OTX-101 and vehicle, respectively. CONCLUSIONS: Treatment with OTX-101 led to greater improvements versus vehicle in corneal surface staining as early as 4 weeks, and further improvements were seen up to 12 weeks. OTX-101 was well tolerated in patients with keratoconjunctivitis sicca.


Assuntos
Córnea/patologia , Ciclosporina/administração & dosagem , Ceratoconjuntivite Seca/tratamento farmacológico , Acuidade Visual , Córnea/efeitos dos fármacos , Relação Dose-Resposta a Droga , Método Duplo-Cego , Feminino , Humanos , Imunossupressores/administração & dosagem , Ceratoconjuntivite Seca/diagnóstico , Masculino , Micelas , Pessoa de Meia-Idade , Soluções Oftálmicas/administração & dosagem , Oftalmoscopia , Coloração e Rotulagem , Resultado do Tratamento
15.
Drug Des Devel Ther ; 13: 2001-2008, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31354245

RESUMO

Background: Effective and tolerable therapeutic strategies for patients with refractory persistent epithelial defects (PEDs) are limited and generally provide poor outcomes. This retrospective case review describes four refractory cases of PEDs associated with recurrent corneal erosions (RCEs) and dry eye disease (DED), which were successfully treated with cyclosporine eye drops. Methods: Patients were treated with cyclosporine A 0.05% eye drops twice a day for at least 12 months. At enrolling time, each patient was asked to suspend topical steroids or other eye drops used for ocular surface abnormalities with the exception of lubricants and eye washing. A complete evaluation of ocular surface symptoms was performed including the McMonnies Dry Eye Questionnaire, Ocular Surface Disease Index, slit-lamp biomicroscopy, fluorescein break-up time, the fluorescein staining of the cornea and conjunctiva (according to the Oxford grading system), the Schirmer I test, and the meibomian secretion after digital pressure application on the lids. This set of exams was carried out at baseline and repeated at all follow-up assessments. Results: All participants that did not benefit from previous therapies, including corticosteroids tapering schedule, showed an important improvement in the clinical picture after two months with topical cyclosporine medication. Moreover, after 12 months of continuous therapy, all patients showed a clinical improvement in DED signs and symptoms, related to the absence of new RCE episodes. The treatment was well tolerated, and no adverse effects were reported. Conclusion: Although a small number of cases were available of our analysis, the treatment with cyclosporine eye drops represents a promising approach in the management of refractory PEDs with associated ocular comorbidities, since it may reduce the RCE episodes and improve the tear film stability, in absence of systemic or local side effects.


Assuntos
Doenças da Córnea/tratamento farmacológico , Ciclosporina/farmacologia , Síndromes do Olho Seco/tratamento farmacológico , Epitélio Anterior/efeitos dos fármacos , Soluções Oftálmicas/farmacologia , Administração Tópica , Adulto , Doenças da Córnea/patologia , Ciclosporina/administração & dosagem , Síndromes do Olho Seco/patologia , Epitélio Anterior/patologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/administração & dosagem , Tamanho da Partícula , Estudos Retrospectivos , Propriedades de Superfície
16.
J Fr Ophtalmol ; 42(8): 880-893, 2019 Oct.
Artigo em Francês | MEDLINE | ID: mdl-31204088

RESUMO

PURPOSE: To demonstrate a decrease in distance visual acuity (VA) following instillation of mydriatic eyedrops in eyes with exudative age-related macular degeneration (AMD). MATERIALS AND METHODS: A prospective assessment in clinical practice was conducted in our ophthalmology department at the University Hospital of Tours from 7/19/2018 to 8/29/2018. Distance (ETDRS) and near (Parinaud) VA were assessed before and after instilling one drop each of tropicamide 0.5% and phenylephrine 10% in the 40 included eyes with exudative AMD. RESULTS: The mean difference in distance VA before and after pupillary dilation (PD) was 0.06 LogMAR (SD=0.14) (P<0.01), i.e. -3.05 letters read (SD=7.52) on the ETDRS chart (P=0.01). For near VA, the mean difference was 0.16 LogMAR (SD=0.16) (P<0.001), i.e. -1.58 paragraphs read (SD=1.63) on the Parinaud chart (P<0.001). DISCUSSION: The absence of a clinically significant loss in post-dilation distance VA for exudative AMD could be explained by negligible glare coming from the ETDRS chart, milder photophobia, low pre-dilation VA's and a balance between higher order optical aberrations and diffraction. The opposite result for near VA could essentially be explained by greater glare induced by the light illuminating the Parinaud chart. CONCLUSION: Our primary goal was not achieved. A study presuming the absence of a clinically significant decrease in post-dilation distance VA would be necessary to consider directly measuring post-dilation VA in eyes with exudative AMD in our daily practice.


Assuntos
Percepção de Distância/efeitos dos fármacos , Degeneração Macular/fisiopatologia , Midriáticos/administração & dosagem , Acuidade Visual/efeitos dos fármacos , Degeneração Macular Exsudativa/fisiopatologia , Acomodação Ocular/efeitos dos fármacos , Acomodação Ocular/fisiologia , Idoso , Idoso de 80 Anos ou mais , Percepção de Distância/fisiologia , Feminino , Humanos , Masculino , Midriáticos/efeitos adversos , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/efeitos adversos , Padrões de Prática Médica , Acuidade Visual/fisiologia
17.
Eur J Pharm Biopharm ; 142: 83-91, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31195132

RESUMO

The management of ocular infections is challenging due to poor drug bioavailability and vehicle related adverse effects associated with current antibiotic eye drops. Semifluorinated alkanes (SFAs) are reportedly well-tolerated on the ocular surface and can enhance ocular drug bioavailability. Therefore, an SFA-based azithromycin suspension (SFA-AZM) was prepared and its antibacterial efficacy was compared to that of marketed azithromycin eye drops by monitoring the growth of bioluminescent Staphylococcus aureus in ex vivo ocular tissues. Corneal and conjunctival distribution of hydrophobic fluorescent dye particles from an SFA suspension (SFA-BODIPY) resulted in preferential dye localisation in the epithelial layers of both tissues. However, corneal dye absorption was significantly lower than conjunctival absorption, likely due to limited adhesion of suspended dye particles to the corneal compared to the conjunctival epithelium. In line with the dye distribution results, bacterial colonisation in the conjunctiva reduced significantly upon application of SFA-AZM with the efficacy being greater than or at least equal to the marketed azithromycin eye drops. In the cornea, all tested azithromycin eye drops reduced the rate of bacterial growth with similar efficacy. Overall, the SFA-AZM suspension tested here may provide a safe and effective alternative for the management of ocular infections by enhancing conjunctival drug absorption and thus drug efficacy.


Assuntos
Alcanos/administração & dosagem , Azitromicina/administração & dosagem , Córnea/efeitos dos fármacos , Infecções Oculares/tratamento farmacológico , Suspensões/administração & dosagem , Animais , Antibacterianos/administração & dosagem , Disponibilidade Biológica , Túnica Conjuntiva/efeitos dos fármacos , Túnica Conjuntiva/microbiologia , Portadores de Fármacos/química , Infecções Oculares/microbiologia , Interações Hidrofóbicas e Hidrofílicas , Soluções Oftálmicas/administração & dosagem , Infecções Estafilocócicas/tratamento farmacológico , Staphylococcus aureus/efeitos dos fármacos , Suínos
18.
AAPS PharmSciTech ; 20(5): 210, 2019 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-31161269

RESUMO

Dorzolamide HCl (DRZ) ophthalmic drop is one of the most common glaucoma medications which rapidly eliminates after instillation leading to short residence time of the drug on cornea. The purpose of the present study is to develop a pH-triggered in situ gel system for ophthalmic delivery of DRZ for treatment of ocular hypertension. In this study, a 32 full factorial design was used for preparation of in situ gel formulations using different levels of Carbopol® and hydroxyl propyl methyl cellulose (HPMC). Rheological behavior, in vitro drug release, ex vivo corneal permeability, and IOP-lowering activity were investigated. DRZ solution (2% w/v) containing of 0.1% (w/v) Carbopol® and 0.1% (w/v) HPMC was selected as the optimal formulation considering its free flow under non-physiological conditions (initial pH and 25 ± 2°C) and transition to appropriate gel form under physiological circumstance (pH 7.4 and 34°C). This in situ gel presented the mucoadhesive property. Ex vivo corneal permeability of this combined solution was similar to those of DRZ solution. The developed formulation compared to the marketed drop (Biosopt®) and DRZ 2% solution had a better performance in intraocular pressure activity. The efficiency and long duration of IOP reduction could be due to the prolonged residence time of the in situ gel. The presence of Carbopol® as a pH triggered and mucoadhesive polymer causes to attach to the ocular mucosal surface for a long term.


Assuntos
Resinas Acrílicas/farmacocinética , Anti-Hipertensivos/farmacocinética , Portadores de Fármacos/farmacocinética , Derivados da Hipromelose/farmacocinética , Sulfonamidas/farmacocinética , Tiofenos/farmacocinética , Resinas Acrílicas/administração & dosagem , Resinas Acrílicas/síntese química , Administração Oftálmica , Animais , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/síntese química , Córnea/efeitos dos fármacos , Córnea/metabolismo , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/síntese química , Avaliação Pré-Clínica de Medicamentos/métodos , Liberação Controlada de Fármacos , Géis , Glaucoma/tratamento farmacológico , Glaucoma/metabolismo , Concentração de Íons de Hidrogênio , Derivados da Hipromelose/administração & dosagem , Derivados da Hipromelose/síntese química , Pressão Intraocular/efeitos dos fármacos , Pressão Intraocular/fisiologia , Masculino , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/síntese química , Soluções Oftálmicas/farmacocinética , Coelhos , Sulfonamidas/administração & dosagem , Sulfonamidas/síntese química , Suínos , Tiofenos/administração & dosagem , Tiofenos/síntese química
19.
Cornea ; 38(9): 1161-1168, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31180924

RESUMO

PURPOSE: To compare the inhibitory effects of dovitinib and bevacizumab for treatment of corneal neovascularization (CNV). METHODS: Thirty-nine adult female Sprague Dawley rats weighing 180 to 250 g were used. CNV was induced by silver nitrate in the right eye of each rat. After the chemical burn, the animals were randomized into 5 groups. Group 1 did not receive any chemical substance. Group 2 received dimethyl sulfoxide, group 3 received bevacizumab 5 mg/mL, group 4 received dovitinib 5 mg/mL, and group 5 received bevacizumab 5 mg/mL + dovitinib 5 mg/mL topically administered twice daily for 14 days. On the 14th day, slit-lamp examination was performed, and anterior segment photographs were taken. The corneal neovascular area was measured on photographs as the percentage of the cornea's total area using computer imaging analysis. The corneal sections were stained with hematoxylin and eosin for histopathological examination. RESULTS: A statistically significant decrease in the percentage of CNV was found in all treatment groups (group 3, group 4, and group 5) compared with the control group (group 1) (P < 0.01). A statistically significant difference in the percentage of CNV was found among group 3, group 4, and group 5 (P = 0.003). The percentage of CNV in group 4 was significantly higher than that in group 3 and group 5 (P1 = 0.004; P2 = 0.006). There was no statistically significant difference in the percentage of CNV between group 3 and group 5 (P = 0.228). CONCLUSIONS: Dovitinib is a newly developed multitargeted tyrosine kinase inhibitor. Topical administration of dovitinib effectively inhibited CNV, but this effect of dovitinib was found less than topical bevacizumab.


Assuntos
Benzimidazóis/uso terapêutico , Bevacizumab/uso terapêutico , Neovascularização da Córnea/tratamento farmacológico , Quinolonas/uso terapêutico , Administração Tópica , Inibidores da Angiogênese/uso terapêutico , Animais , Queimaduras Químicas/tratamento farmacológico , Modelos Animais de Doenças , Queimaduras Oculares/tratamento farmacológico , Feminino , Soluções Oftálmicas/administração & dosagem , Ratos , Ratos Sprague-Dawley , Fator A de Crescimento do Endotélio Vascular/antagonistas & inibidores
20.
Drug Deliv ; 26(1): 575-585, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31172843

RESUMO

Myricetin (Myr) is a naturally occurring flavonoid exhibiting diverse biological and pharmacological properties, but its characteristics such as water insolubility, poor aqueous stability, and poor bioavailability limit its clinical application, including in ophthalmology. To increase its clinical application in ophthalmology, Myr was designed to be encapsulated in a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCL-PVA-PEG) polymeric micelles to increases its aqueous solubility, stability, and corneal permeability to promote its efficacy in eye disease treatments. Thus, the Myr micelle ophthalmic solution was prepared and characterized encapsulation efficiency (EE), micelle size, and zeta potential. The chemical stability of Myr and the short-term storage stability of the Myr micelle ophthalmic solution were evaluated, followed by in vitro cytotoxicity and in vivo ocular irritation; in vitro cellular uptake and in vivo corneal permeation; and in vitro antioxidant activity and in vivo anti-inflammatory efficacy were also further evaluated. Myr could be incorporated into micelles with high EE. PVCL-PVA-PEG micelles significantly enhanced Myr's aqueous solubility and chemical stability. The Myr micelle ophthalmic solution also showed high storage stability. In rabbits, the Myr micelle ophthalmic solution displayed good in vitro cellular tolerance. Remarkable improvements in in vitro cellular uptake and in vivo corneal permeation were also observed in the Myr micelle ophthalmic solution, and significant improvements in the in vitro antioxidant activity and in vivo anti-inflammatory efficacy were also obtained. Overall, these results supported that the Myr micelle ophthalmic solution could be a promising nanomedicine for ocular tissues.


Assuntos
Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Flavonoides/administração & dosagem , Flavonoides/química , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/química , Solubilidade/efeitos dos fármacos , Administração Oftálmica , Animais , Química Farmacêutica/métodos , Córnea/efeitos dos fármacos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Micelas , Permeabilidade/efeitos dos fármacos , Polietilenoglicóis/química , Polímeros/química , Polivinil/química , Coelhos
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