scholarly journals Cyclosporine A eyedrops with self-nanoemulsifying drug delivery systems have improved physicochemical properties and efficacy against dry eye disease in a murine dry eye model

PLoS ONE ◽  
2019 ◽  
Vol 14 (11) ◽  
pp. e0224805 ◽  
Author(s):  
Seung Pil Bang ◽  
Chang Yeor Yeon ◽  
Nirpesh Adhikari ◽  
Sanjiv Neupane ◽  
Harim Kim ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Physicochemical Properties ◽  
Dry Eye ◽  
Cyclosporine A ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Dry Eye Disease ◽  
Eye Disease ◽  
Eye Model

scholarly journals A Comprehensive Review on Dry Eye Disease: Diagnosis, Medical Management, Recent Developments, and Future Challenges

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Suvarna P. Phadatare ◽  
Munira Momin ◽  
Premanand Nighojkar ◽  
Sonali Askarkar ◽  
Kamalinder K. Singh
Keyword(s):  
Drug Delivery ◽  
Dry Eye ◽  
Medical Management ◽  
Drug Delivery Systems ◽  
Disease Diagnosis ◽  
Delivery Systems ◽  
Dry Eye Disease ◽  
Eye Disease ◽  
Future Challenges ◽  
Recent Developments

Dry eye syndrome (DES) or keratoconjunctivitis sicca (KCS) is a common disorder of the tear film caused by decreased tear production or increased evaporation and manifests with a wide variety of signs and symptoms. The present review from interpretation of the literature gives detailed information on the prevalence, definition, causes, diagnostic tests, and medical management of dry eye disease. A number of systems contribute to the physiological integrity of the ocular surface and disruption of system may or may not produce symptoms. Therefore accurate diagnosis of dry eyes with no or minimal disruption of physiological function is necessary. The paper also discusses different colloidal drug delivery systems and current challenges in the development of topical ophthalmic drug delivery systems for treatment of KCS. Due to the wide prevalence and number of factors involved, newer, more sensitive diagnostic techniques and novel therapeutic agents have been developed to provide ocular delivery systems with high therapeutic efficacy. The aim of this review is to provide awareness among the patients, health care professionals, and researchers about diagnosis and treatment of KCS and recent developments and future challenges in management of dry eye disease.

scholarly journals The role of KPI-121 0.25% in the treatment of dry eye disease: penetrating the mucus barrier to treat periodic flares

2021 ◽  
Vol 13 ◽  
pp. 251584142110127
Author(s):  
Preeya K. Gupta ◽  
Nandini Venkateswaran
Keyword(s):  
Drug Delivery ◽  
Dry Eye ◽  
Ocular Surface ◽  
Dry Eye Disease ◽  
Eye Disease ◽  
Eye Drops ◽  
Short Term ◽  
Short Term Treatment ◽  
Loteprednol Etabonate ◽  
Mucus Barrier

The tear film, which includes mucins that adhere to foreign particles, rapidly clears allergens and pathogens from the ocular surface, protecting the underlying tissues. However, the tear film’s ability to efficiently remove foreign particles during blinking can also pose challenges for topical drug delivery, as traditional eye drops (solutions and suspensions) are cleared from the ocular surface before the drug can penetrate into the conjunctival and corneal epithelium. In the past 15 years, there has been an increase in the development of nanoparticles with specialized coatings that have reduced affinity to mucins and are small enough in size to pass through the mucus barrier. These mucus-penetrating particles (MPPs) have been shown to efficiently penetrate the mucus barrier and reach the ocular surface tissues. Dry eye disease (DED) is a common inflammatory ocular surface disorder that often presents with periodic flares (exacerbations). However, currently approved immunomodulatory treatments for DED are intended for long-term use. Thus, there is a need for effective short-term treatments that can address intermittent flares of DED. Loteprednol etabonate, an ocular corticosteroid, was engineered to break down rapidly after administration to the ocular surface tissues and thereby reduce risks associated with other topical steroids. KPI-121 is an ophthalmic suspension that uses the MPP technology to deliver loteprednol etabonate more efficiently to the ocular tissues, achieving in animal models a 3.6-fold greater penetration of loteprednol etabonate to the cornea than traditional loteprednol etabonate ophthalmic suspensions. In clinical trials, short-term treatment with KPI-121 0.25% significantly reduced signs and symptoms of DED compared with its vehicle (placebo). Recently approved KPI-121 0.25%, with its novel drug delivery design and ease of use, has the potential to effectively treat periodic flares of DED experienced by many patients.

scholarly journals One-Year Efficacy and Safety of 0.1% Cyclosporine a Cationic Emulsion in the Treatment of Severe Dry Eye Disease

2017 ◽  
Vol 27 (6) ◽  
pp. 678-685 ◽  
Author(s):  
Christophe Baudouin ◽  
Maite Sainz de la Maza ◽  
Mourad Amrane ◽  
Jean-Sébastien Garrigue ◽  
Dahlia Ismail ◽  
...  
Keyword(s):  
Dry Eye ◽  
Cyclosporine A ◽  
Ocular Surface ◽  
Dry Eye Disease ◽  
Eye Disease ◽  
Efficacy And Safety ◽  
Open Label ◽  
Once Daily ◽  
Surface Inflammation ◽  
Ocular Surface Inflammation

Purpose The SANSIKA study evaluated the efficacy/safety of 0.1% (1 mg/mL) cyclosporine A cationic emulsion (CsA CE) for treating dry eye disease (DED) with severe keratitis. The double-masked phase demonstrated that CsA CE was effective in reducing corneal damage and ocular surface inflammation, and was well-tolerated over 6 months. Here we report efficacy and safety findings of SANSIKA's open-label extension (OLE). Methods In this multicenter, double-masked, phase III study, patients with severe DED (corneal fluorescein staining [CFS] grade 4, modified Oxford scale) were randomized to once-daily CsA CE (Ikervis®) or its vehicle for 6 months, followed by 6-month open-label, once-daily CsA CE (CsA CE/CsA CE and vehicle/CsA CE groups). Results A total of 177 patients completed the OLE. Efficacy results reiterated the double-masked phase: CsA CE reduced CFS score and human leukocyte antigen-antigen D related expression, improved corneal clearing, and produced continuous improvements in global symptom scores (ocular surface disease index [OSDI], visual analogue scale). The CFS-OSDI response rates (≥2 CFS points, ≥30% OSDI improvement vs baseline) at 12 vs 6 months were 39.1% vs 28.6%, respectively, for CsA CE/CsA CE and 38.0% vs 23.1% for vehicle/CsA CE. Cyclosporine A CE's safety profile was similar to the initial 6 months. The most common treatment-related treatment-emergent adverse event was instillation site pain (7.8%, CsA CE/CsA CE group; 19.0%, vehicle/CsA CE group). No unexpected safety signals were observed; systemic CsA levels were undetectable/negligible in all patients except 2 previously treated with systemic CsA. Conclusions In this 12-month study, once-daily CsA CE was well-tolerated and showed reductions in ocular surface inflammation and improvements in signs/symptoms in DED patients with severe keratitis.

Author's Reply to: “Concerns Over: Efficacy and Safety of 0.1% Cyclosporine a Cationic Emulsion in the Treatment of Severe Dry Eye Disease”

2017 ◽  
Vol 27 (6) ◽  
pp. e194-e195
Author(s):  
Andrea Leonardi ◽  
Gysbert Van Setten ◽  
Mourad Amrane ◽  
Dahlia Ismail ◽  
Jean-Sebastien Garrigue ◽  
...  
Keyword(s):  
Dry Eye ◽  
Cyclosporine A ◽  
Dry Eye Disease ◽  
Eye Disease ◽  
Efficacy And Safety

scholarly journals Recent Advances in Phenylboronic Acid-Based Gels with Potential for Self-Regulated Drug Delivery

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1089 ◽  
Author(s):  
Chenyu Wang ◽  
Bozhong Lin ◽  
Haopeng Zhu ◽  
Fei Bi ◽  
Shanshan Xiao ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Physicochemical Properties ◽  
Boronic Acid ◽  
Drug Delivery Systems ◽  
Phenylboronic Acid ◽  
3D Structure ◽  
Three Dimensional ◽  
Drug Carriers ◽  
Delivery Systems ◽  
Diabetes Therapy

Glucose-sensitive drug platforms are highly attractive in the field of self-regulated drug delivery. Drug carriers based on boronic acid (BA), especially phenylboronic acid (PBA), have been designed for glucose-sensitive self-regulated insulin delivery. The PBA-functionalized gels have attracted more interest in recent years. The cross-linked three-dimensional (3D) structure endows the glucose-sensitive gels with great physicochemical properties. The PBA-based platforms with cross-linked structures have found promising applications in self-regulated drug delivery systems. This article summarizes some recent attempts at the developments of PBA-mediated glucose-sensitive gels for self-regulated drug delivery. The PBA-based glucose-sensitive gels, including hydrogels, microgels, and nanogels, are expected to significantly promote the development of smart self-regulated drug delivery systems for diabetes therapy.

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