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1.
Orv Hetil ; 161(10): 363-373, 2020 Mar.
Artigo em Húngaro | MEDLINE | ID: mdl-32115992

RESUMO

Retrometabolic drug design combines the structure-activity and structure-metabolism relationships, allowing the effective separation of drug action and side effects. This combination results in significant improvement of the therapeutic index. The main aim is not only to study the metabolism but to build into the drug molecule the desired metabolic route, in addition to the therapeutic activity. There are two basically different approaches to achieve this aim. Both use designed-in metabolism. The 1. chemical drug-targeting systems (CDS) and 2. soft drug, both control the drug targeting and action by strategically designed metabolism. In the case of the soft drugs, we want to rely on hydrolytic enzymes, avoiding the oxidative processes. In the present work, we focus on the clinical successes of the soft drugs designed in our laboratories. In order to show the difference, we briefly present a brain-targeted delivery system, where the originally inactive molecular construct undergoes sequential metabolism to allow specific concentration of the active drug in the brain. Among the soft drugs first we present the highly successful soft corticosteroids. Loteprednol etabonate has been used worldwide for over twenty years, and its use is constantly growing. In addition to the dramatically improved therapeutic index, the specific, serious ophthalmic side effects (elevation of intraocular pressure; glaucoma and cataract formation) were completely eliminated. Similarly designed second generation of soft corticosteroids are also presented, where the soft pharmacophore is structurally unexpected. The most recent soft drug design involves anticholinergics. Sofpironium bromide, a highly effective molecule but without the typical anticholinergic side effects, was first developed to treat hyperhidrosis, an unmet need. Phase III clinical studies were successfully completed and its marketing approval is pending. Since the soft drug design principles, methods and rules are general and specific in nature, a computerized expert system was also developed. Orv Hetil. 2020; 161(10): 363-373.


Assuntos
Sistemas de Liberação de Medicamentos , Desenho de Drogas , Soluções Oftálmicas/farmacologia , Preparações Farmacêuticas/classificação , Corticosteroides , Olho , Glaucoma , Humanos , Soluções Oftálmicas/química
2.
Drug Discov Ther ; 14(1): 14-20, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32147626

RESUMO

We compared the pharmaceutical properties, such as surface tension, drop volume, nozzle inner diameter, and force to push the drug product out of the container (squeeze force), of purified sodium hyaluronate eye drops preparations of one brand-name (Hyalein) and 11 generic drugs used for treatment of keratoconjunctiva epithelial disorders, and examined product selection based on the needs of the patient. The surface tension of Nissin (51.0 dyn/cm) and Nitten (52.3 dyn/cm) was significantly lower than that of Hyalein (62.8 dyn/cm), whereas Nitten PF (69.5 dyn/cm) was significantly higher than Hyalein. The drop volume of Tearbalance (42.4 mg), Nissin (43.7 mg), and Nitten (42.7 mg) was significantly lower than that of Hyalein (50.4 mg). We compared the squeeze force using a wearable touch sensor (Haptic Skill Logger: HapLog®) and digital force gauge (DF). The squeeze force of HapLog® showed values of about 1.7- to 3.5-fold higher than that of DF. Moreover, the squeeze force of Eyecare (34.0 N), Kyorin (35.4 N), and Nitten PF (44.3 N) by HapLog® was significantly higher than that of Hyalein (10.5 N). In contrast, the squeeze force of Kyorin (20.8 N) and Nitten PF (25.0 N) by DF was significantly higher than that of Hyalein (12.2 N). Two questionnaire surveys on the feeling of instillation of eye drops revealed a strong negative correlation between feeling of use and squeeze force.


Assuntos
Avaliação de Medicamentos , Soluções Oftálmicas , Avaliação de Medicamentos/normas , Medicamentos Genéricos/normas , Humanos , Soluções Oftálmicas/normas , Satisfação do Paciente , Dispositivos Eletrônicos Vestíveis
3.
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
4.
Medicine (Baltimore) ; 99(7): e18618, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32049778

RESUMO

BACKGROUND: Allergic conjunctivitis (AC) is a multifactorial and common type of ocular surface disease that affects many people. The quality of life for AC patients can be significantly decreased caused by symptoms of ocular itching, swelling, redness, and tearing. Topical antihistaminics, mast cell stabilizers, non-steroidal anti-inflammatory drugs (NSAIDs), and steroids have been widely used to treat AC. Many clinical trials have indicated that olopatadine hydrochloride eye drops can provide quick relief of symptoms and signs. The purpose of this review is to evaluate systematically the effectiveness of olopatadine hydrochloride eye drops for treating AC. METHODS: A systematic review of all of the randomized controlled trials on the effectiveness and safety of olopatadine hydrochloride eye drops for AC will be conducted. We will search PubMed, Web of Science (WOS), EMBASE (OVID), the Cochrane Library, Google Scholar, China National Knowledge Infrastructure (CNKI), China Science and Technology Journal database (VIP), Wanfang Database, and CBM, from the database inception date to October 31, 2019. There are no language or publication status restrictions. Registers of clinical trials, potential gray literature, reference lists of studies, and conference abstracts will also be searched. Two reviewers will independently read the articles, extract the data information, and assess the quality of the studies. Data will be synthesized by a heterogeneity test. The primary outcomes include the main symptom and sign scores before and after treatment, the eye redness index, the presence of eosinophils in the conjunctival scraping. Quality of life, the total treatment efficacy, and safety will be evaluated as the secondary outcomes. RevMan V.5.3 software will be used for the meta-analysis. RESULTS: The study will provide an objective and normative systematic review to evaluate the effectiveness and safety of olopatadine hydrochloride eye drops for the treatment of AC. CONCLUSION: Our review will provide useful information to judge whether olopatadine hydrochloride eye drops is an effective intervention for patients with AC. ETHICS AND DISSEMINATION: It is not necessary to obtain ethical approval as participants are not involved patients. The protocol and results will be published in a peer-reviewed journal. The systematic review will also be disseminated electronically and in print to help guide health care practice and policy. PROSPERO REGISTRATION NUMBER: PROSPERO CRD42019132232.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Conjuntivite Alérgica/tratamento farmacológico , Cloridrato de Olopatadina/uso terapêutico , Anti-Inflamatórios não Esteroides/efeitos adversos , Humanos , Cloridrato de Olopatadina/efeitos adversos , Soluções Oftálmicas , Qualidade de Vida , Ensaios Clínicos Controlados Aleatórios como Assunto , Resultado do Tratamento
6.
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
7.
Expert Opin Pharmacother ; 21(1): 39-45, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31663782

RESUMO

Introduction: Reduction of intraocular pressure (IOP) is the only known modifiable risk factor for prevention and treatment of glaucoma. Rho-kinase (ROCK) inhibitors are a new class of glaucoma medications introduced recently with novel mechanisms of action and favorable safety profiles. Latanoprost, a common first line drug used for treatment of glaucoma, does not adequately control pressures in all cases. Addition of more than one anti-glaucoma medication affects patient compliance and adherence. Fixed-combination eye drops are combinations of two or more active drugs in a single dosage form, thus simplify dosing. New to this group is the fixed combination netarsudil- latanoprost (FCNL).Area covered: This review focuses on FCNL, its pharmacodynamics and pharmacokinetics. It also details the efficacy and safety of individual drugs compared to FCNL.Expert opinion: The combination of latanoprost and netarsudil is a potent medication and modulates all known targets for IOP reduction in a single drop and has been shown to be more effective than either drug alone. FCNL is an alternative for those with inadequately controlled IOP on a prostaglandin analog alone, as well as those for whom a simplified regimen is desirable, or those who are not good candidates for other classes of glaucoma medications.


Assuntos
Benzoatos/administração & dosagem , Glaucoma/tratamento farmacológico , Latanoprosta/administração & dosagem , Hipertensão Ocular/tratamento farmacológico , beta-Alanina/análogos & derivados , Anti-Hipertensivos/uso terapêutico , Combinação de Medicamentos , Feminino , Humanos , Pressão Intraocular/efeitos dos fármacos , Masculino , Soluções Oftálmicas , beta-Alanina/administração & dosagem
8.
Ophthalmic Res ; 63(1): 50-58, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31117087

RESUMO

PURPOSE: Ocular graft-versus-host disease (oGvHD) following allogeneic hematopoietic stem cell transplantation develops as severe dry eye disease (DED) and is initially treated with lubricants, although no clinical trials are available using artificial tears in oGvHD. This trial was set up to test perfluorohexyloctane (NovaTears®) as nonpreserved layer-forming agent for the treatment of DED in oGvHD. METHODS: 25 patients with severe DED due to oGvHD received 1 drop perfluorohexyloctane 4 times daily during a prospective, multicenter, observational 12-week study on top of established topical therapy. Clinical parameters included Schirmer test, tear film breakup time, corneal staining, meibum secretion and ocular surface disease index. Adverse events, visual acuity and intraocular pressure were key safety parameters. RESULTS: From 25 patients recruited, 23 presented for the second visit. Perfluorohexyloctane treatment did not lead to any changes in clinical or safety parameters but led to fast relief in symptoms in 57% of the patients. One adverse reaction occurred. CONCLUSIONS: This study showed no change in clinical signs in severe DED due to oGvHD, which was not unexpected due to the underlying pathomechanisms. However, the study showed improvement of symptoms in individual patients allowing application of perfluorohexyloctane as an additional symptomatic therapy in oGvHD.


Assuntos
Síndromes do Olho Seco/tratamento farmacológico , Fluorcarbonetos/uso terapêutico , Doença Enxerto-Hospedeiro/tratamento farmacológico , Soluções Oftálmicas/uso terapêutico , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos
9.
Eur J Ophthalmol ; 30(1): 94-103, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30585084

RESUMO

PURPOSE: To evaluate the efficacy and safety of plasma rich in growth factors eye drops for the treatment of corneal and ocular surface disorders in patients with graft versus host disease. METHODS: This retrospective and longitudinal study included graft versus host disease patients with ocular disorders. The resolution of corneal ulcers (area and density staining) was evaluated as primary outcome. Best corrected visual acuity, intraocular pressure, tear film breakup time, Schirmer test, ocular surface disease index, and visual analog score were evaluated as secondary outcomes. All variables were analyzed before and after plasma rich in growth factors treatment. The safety of plasma rich in growth factors treatment was also assessed. RESULTS: Twelve patients (23 eyes) with ocular graft versus host disease were evaluated. Statistically significant improvement in the area (75.7%) and density (73.3%) of the corneal staining, in best corrected visual acuity (74.7%), in ocular surface disease index scale (75.4%), visual analog score frequency (81.4%) and visual analog score severity (81.9%), and an increase of 3.8 s in tear film breakup time and 6 mm in Schirmer test was observed after plasma rich in growth factors treatment (p < 0.001). Some potential modifiers of the therapeutic effect were identified. All patients achieved corneal stability without perforation risk. No adverse events associated with the plasma rich in growth factors were observed. CONCLUSION: Immunosafe plasma rich in growth factors eye drops for the treatment of patients with ocular graft versus host disease could be safe and effective, showing a high rate of corneal ulcer resolution and dry eye disease control. Plasma rich in growth factors eye drops may help to maintain corneal stability and prevent it against higher ocular complications.


Assuntos
Síndromes do Olho Seco/terapia , Doença Enxerto-Hospedeiro/complicações , Peptídeos e Proteínas de Sinalização Intercelular/farmacologia , Plasma Rico em Plaquetas , Adulto , Idoso , Síndromes do Olho Seco/etiologia , Síndromes do Olho Seco/metabolismo , Feminino , Seguimentos , Doença Enxerto-Hospedeiro/terapia , Humanos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas/uso terapêutico , Estudos Retrospectivos , Lágrimas/metabolismo
11.
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
14.
Curr Opin Ophthalmol ; 31(1): 67-73, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31688226

RESUMO

PURPOSE OF REVIEW: Routine prophylaxis for adverse events following cataract surgery is evolving. Prior reliance on topical eyedrop instillation by patients is giving way to surgeon directed injections at the time of cataract surgery. The benefit of this new approach is assured delivery of drugs in standardized doses which should optimize the healing process and reduce the incidence of untoward events with higher confidence. RECENT FINDINGS: Adoption rates of intracameral antibiotic injection amongst European and American cataract surgeons is increasing. Techniques to inject periocular corticosteroid for routine inflammation prophylaxis are also in development. In combination with intraoperative pharmacologic dilation, a drop-free modality can be achieved. SUMMARY: Intraoperative injections offer the patient and surgeon assured drug delivery and hold promise to avoid the pitfalls of patient adherence, incorrect topical instillation, and topical drop-associated corneal issues.


Assuntos
Antibioticoprofilaxia , Extração de Catarata , Endoftalmite/prevenção & controle , Complicações Pós-Operatórias/prevenção & controle , Antibacterianos/uso terapêutico , Humanos , Soluções Oftálmicas/uso terapêutico
15.
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
17.
Expert Rev Clin Pharmacol ; 12(12): 1073-1079, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31842637

RESUMO

Introduction: Netarsudil and latanoprost ophthalmic solution (0.02%/0.005%) is indicated for intraocular pressure (IOP) lowering in open-angle glaucoma (OAG) or ocular hypertension (OHTN). The once-daily agent combines the mechanism of action for each of the individual components and provides a new avenue for long-term intraocular pressure control. This review aims to cover the agent's current efficacy and safety data and opine as to its role in glaucoma management.Areas covered: This article will cover Phase II-III clinical efficacy and safety data as well as basic science literature pertaining to the agent's mechanism of action and pharmacodynamics. In selecting articles for inclusion in this review, a literature search using the PubMed database was carried out. Cross-referencing was carried out where applicable. We did not use any date or language restrictions in electronic searches.Expert opinion: Netarsudil and latanoprost ophthalmic solution plays a pivotal role in management of individuals with OAG and OHTN. The agent may be used as first-line therapy to provide substantial IOP-lowering or when additional lowering is indicated and prostaglandins have provided insufficient IOP lowering. The once-daily dosing regimen decreases the risk of inadequate treatment due to nonadherence.


Assuntos
Benzoatos/administração & dosagem , Glaucoma de Ângulo Aberto/tratamento farmacológico , Latanoprosta/administração & dosagem , Hipertensão Ocular/tratamento farmacológico , beta-Alanina/análogos & derivados , Animais , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/efeitos adversos , Benzoatos/efeitos adversos , Combinação de Medicamentos , Humanos , Pressão Intraocular , Latanoprosta/efeitos adversos , Soluções Oftálmicas , beta-Alanina/administração & dosagem , beta-Alanina/efeitos adversos
18.
Vestn Oftalmol ; 135(5. Vyp. 2): 160-170, 2019.
Artigo em Russo | MEDLINE | ID: mdl-31691655

RESUMO

PURPOSE: To investigate the toxic effects of frequent instillations of anti-infective solutions (antibiotic eye drops - 0.3 and 1.4% tobramycin, 0.5% levofloxacin and 0.5% moxifloxacin; antiseptic eye drops - 0.05% pyloxidine and 0.025% chlorhexidine; antifungal drug - 2 mg/ml fluconazole solution) on ocular tissues. MATERIAL AND METHODS: The study was conducted on 21 Wistar rats (42 eyes) using method of semi-fine sections. RESULTS: The majority of antibiotics and antifungal agents do not cause toxic reactions in rats` eyes when instilled with frequent regimen with the exception of 'fortified' 1.4% tobramycin and pyloxidine solutions, which caused a decrease in corneal endothelial cells density and formation of fibrovascular tissue in the anterior chamber. CONCLUSION: Frequent instillations of antimicrobial drug solutions is a safe method for the treatment of purulent corneal ulcers and purulent keratitis. The exceptions were solutions of 'fortified' 1.4% tobramycin and piloxidine (vitabact).


Assuntos
Anti-Infecciosos/uso terapêutico , Infecções Oculares Bacterianas , Animais , Antibacterianos , Cefazolina , Células Endoteliais , Soluções Oftálmicas , Ratos , Ratos Wistar
19.
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
20.
Int J Mol Sci ; 20(20)2019 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-31614909

RESUMO

The use of eyewash solutions in Japan, especially in patients with allergic conjunctivitis and contact lens wearers, has been increasing. Our aim was to investigate how the use of preservative-free eyewash solution in healthy eyes for one month affects corneal safety and ocular surface mucin. We analyzed 42 eyes of 21 individuals (17 males, four females; mean age: 36.1 ± 7.4 years) without ocular allergies, dry eyes, or other ocular diseases through a prospective study. Eyes were randomized to a wash group (group one) and a nonwash follow up group (group two). We evaluated the dry eye-related quality-of-life score (DEQS), tear film breakup time (TBUT), fluorescein staining score, mRNA expression of MUC5AC and MUC16, MUC16 immunohistochemistry, and MUC5AC periodic acid Schiff (PAS) staining. There was a significant decrease in DEQS scores after one month of eyewash use (p < 0.05). There were no significant differences in other evaluation items that were analyzed (all p > 0.05). Furthermore, no significant differences were observed between group one and group two in all endpoints (all p > 0.05). The results suggest that one month use of a nonpreserved eyewash solution has no detrimental effects on the tear film and the ocular surface mucins.


Assuntos
Antígeno Ca-125/metabolismo , Túnica Conjuntiva/efeitos dos fármacos , Proteínas de Membrana/metabolismo , Mucina-5AC/metabolismo , Soluções Oftálmicas/efeitos adversos , Adulto , Túnica Conjuntiva/metabolismo , Córnea/metabolismo , Síndromes do Olho Seco/metabolismo , Feminino , Fluoresceína/metabolismo , Ácido Glicirrízico/farmacologia , Células Caliciformes/citologia , Células Caliciformes/metabolismo , Humanos , Japão , Masculino , Estudos Prospectivos , Lágrimas/metabolismo
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