scholarly journals Development of novel bioadhesive niosomal formulation for the transcorneal delivery of moxifloxacin hydrochloride in the treatment of corneal ulcer

2019 ◽  
Vol 10 (3) ◽  
pp. 1874-1882
Author(s):  
Manoj K ◽  
Suhail K
Keyword(s):  
Retention Time ◽  
Bacterial Infections ◽  
Contact Lenses ◽  
Corneal Ulcer ◽  
Ex Vivo ◽  
Eye Drops ◽  
Sustained Drug Release ◽  
Major Drawback ◽  
Duration Of Action

A corneal ulcer is an open sore or epithelial defect with an inflammation of the cornea of the eye. Most of the corneal ulcers are caused by bacterial infections and are common in people who wear contact lenses. Moxifloxacin eye drops are frequently used for the treatment of infectious ulcers. However such formulations have a major drawback, that is the short duration of action and usually, require 4-6 times installation daily. A bioadhesive polymer coated niosomal formulation of moxifloxacin was purposed to show a longer retention time on eyes and subsequent reduction in dosing frequency. Niosomes were prepared by solvent injection method using cholesterol and span 60. The coating of the niosomes was done using Carbopol 934or HPMC as a bioadhesive polymer. The mean particle size of bioadhesive niosomes found to be below 200nm. Optimization of the coating was based on in vitro diffusion studies, ex vivo transcorneal permeation studies and bioadhesion studies. The retention time of the formulation was determined by in vitro and ex vivo bioadhesion testing. The antimicrobial assay confirmed the potency of the formulation against the gram-negative organism. The current study revealed that bioadhesive niosomal formulations have longer corneal retention time and have sustained drug release for a period of 24 hours.

scholarly journals Extended levobunolol release from Eudragit nanoparticle-laden contact lenses for glaucoma therapy

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Navneet Kumar ◽  
Rohan Aggarwal ◽  
Meenakshi K. Chauhan
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Contact Lens ◽  
Contact Lenses ◽  
Ex Vivo ◽  
Eye Drops ◽  
Equilibrium Swelling ◽  
Drug Solution

Abstract Background Majorly, the reason for the permanent loss of vision is glaucoma. But the currently available common treatment methodologies such as eye drops have various disadvantages like patient incompliance due to repeated administration and poor (1–5%) bioavailability leading to poor efficiency. The objective of this research was to formulate Eudragit-based nanoparticles of levobunolol incorporated into a contact lens to obtain sustained ocular delivery of levobunolol at the therapeutics level. Eudragit nanoparticles of levobunolol were formulated by nanoprecipitation methodology utilizing different ratios of Eudragit S100 and polyvinyl alcohol. The prepared nanoparticles were evaluated and optimized by efficiency of entrapment, particle size, morphology of surface and zeta potential. The optimized nanoparticles were then entrapped into the matrix of the contact lens by the soaking method which were then characterized and compared for optical clarity study, equilibrium swelling study, shelf life and in vitro drug release in simulated tear fluid followed by ex vivo transcorneal permeation study. Results Formulation F3 was obtained as optimized nanoparticle formulation with 102.61 nm ± 3.92 of particle size, − 22.2 mV ± 2.76 of zeta potential and 86.995% ± 1.902 of efficiency of entrapment. The equilibrium swelling index and transmittance of nanoparticle incorporated into contact lenses showed better results when compared to drug solution-loaded lenses. In vitro release indicated more sustained drug profiles (84.33% ± 0.34 of drug release over a period of 12 days) as compared to drug solution-loaded lenses (89.282% ± 0.900 of drug release over a period of 3 days). Ex vivo transcorneal permeation studies showed more permeation (6.75% ± 0.170) through contact lenses as compared to marketed eye drops (3.03% ± 0.088). Conclusion This research demonstrates the remarkable results of drug-laden contact lenses to serve as a great medium for the continued delivery of ocular drugs without affecting the physical and optical characteristics of the lens content.

scholarly journals C5a and C5aR1 are key drivers of microvascular platelet aggregation in clinical entities spanning from aHUS to COVID-19

2021 ◽  
Author(s):  
Sistiana Aiello ◽  
Sara Gastoldi ◽  
Miriam Galbusera ◽  
Piero Luigi Ruggenenti ◽  
Valentina Portalupi ◽  
...  
Keyword(s):  
Endothelial Cells ◽  
Bacterial Infections ◽  
Viral Infections ◽  
Ex Vivo ◽  
Inflammatory Diseases ◽  
Thrombus Formation ◽  
Alternative Pathway ◽  
Atypical Hemolytic Uremic Syndrome ◽  
Uremic Syndrome

Unrestrained activation of the complement system till the terminal products, C5a and C5b-9, plays a pathogenetic role in acute and chronic inflammatory diseases. In endothelial cells, complement hyperactivation may translate into cell dysfunction, favoring thrombus formation. The aim of this study was to investigate the role of the C5a/C5aR1 axis as opposite to C5b-9 in inducing endothelial dysfunction and loss of anti-thrombogenic properties. In vitro and ex vivo assays with serum from patients with atypical hemolytic uremic syndrome (aHUS) -a prototype rare disease of complement-mediated microvascular thrombosis due to genetically determined alternative pathway dysregulation- and cultured microvascular endothelial cells, demonstrated that the C5a/C5aR1 axis is a key player of endothelial thromboresistance loss. C5a added to normal human serum, fully recapitulated the pro-thrombotic effects of aHUS serum. Mechanistic studies showed that C5a caused RalA-mediated exocytosis of vWF and P-selectin from Weibel-Palade bodies, which favored further vWF binding on the endothelium and platelet adhesion and aggregation. In patients with severe COVID-19 -who suffered from acute activation of complement triggered by SARS-CoV-2 infection- we found the same C5a-dependent pathogenic mechanisms. These results highlight C5a/C5aR1 as a common pro-thrombogenic effector spanning from genetic rare diseases to viral infections, and may have clinical implications. Selective C5a/C5aR1 blockade could have advantages over C5 inhibition, since the former preserves the formation of C5b-9 that is critical to control bacterial infections that often develop as comorbidities in severely ill patients. (Clinicaltrials.gov identifier NCT02464891)

scholarly journals Recent Advances in the Design of Topical Ophthalmic Delivery Systems in the Treatment of Ocular Surface Inflammation and Their Biopharmaceutical Evaluation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 570 ◽  
Author(s):  
Roseline Mazet ◽  
Josias B. G. Yaméogo ◽  
Denis Wouessidjewe ◽  
Luc Choisnard ◽  
Annabelle Gèze
Keyword(s):  
Ocular Surface ◽  
Ex Vivo ◽  
Immunosuppressive Agents ◽  
Delivery Systems ◽  
Ocular Inflammation ◽  
Limiting Factors ◽  
Common Symptom ◽  
Eye Drops ◽  
Colloidal Systems

Ocular inflammation is one of the most common symptom of eye disorders and diseases. The therapeutic management of this inflammation must be rapid and effective in order to avoid deleterious effects for the eye and the vision. Steroidal (SAID) and non-steroidal (NSAID) anti-inflammatory drugs and immunosuppressive agents have been shown to be effective in treating inflammation of the ocular surface of the eye by topical administration. However, it is well established that the anatomical and physiological ocular barriers are limiting factors for drug penetration. In addition, such drugs are generally characterized by a very low aqueous solubility, resulting in low bioavailability as only 1% to 5% of the applied drug permeates the cornea. The present review gives an updated insight on the conventional formulations used in the treatment of ocular inflammation, i.e., ointments, eye drops, solutions, suspensions, gels, and emulsions, based on the commercial products available on the US, European, and French markets. Additionally, sophisticated formulations and innovative ocular drug delivery systems will be discussed. Promising results are presented with micro- and nanoparticulated systems, or combined strategies with polymers and colloidal systems, which offer a synergy in bioavailability and sustained release. Finally, different tools allowing the physical characterization of all these delivery systems, as well as in vitro, ex vivo, and in vivo evaluations, will be considered with regards to the safety, the tolerance, and the efficiency of the drug products.

scholarly journals Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 682
Author(s):  
Eszter L. Kiss ◽  
Szilvia Berkó ◽  
Attila Gácsi ◽  
Anita Kovács ◽  
Gábor Katona ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Harmful Effect ◽  
Cell Junctions ◽  
Toxicity Tests ◽  
Eye Drops ◽  
Corneal Toxicity ◽  
Penetration Tests ◽  
Full Factorial

Generally, topically applied eye drops have low bioavailability due to short residence time and low penetration of the drug. The aim of the present study was to incorporate dexamethasone (DXM) into nano lipid carriers (NLC), which contain mucoadhesive polymer, in order to increase the bioavailability of the drug. A 23 factorial experimental design was applied, in which the three factors were the polymer, the DXM, and the emulsifier concentrations. The samples were analyzed for particle size, zeta potential, polydispersity index, and Span value. The significant factors were identified. The biocompatibility of the formulations was evaluated with human corneal toxicity tests and immunoassay analysis. The possible increase in bioavailability was analyzed by means of mucoadhesivity, in vitro drug diffusion, and different penetration tests, such as in vitro cornea PAMPA model, human corneal cell penetration, and ex vivo porcine corneal penetration using Raman mapping. The results indicated that DXM can be incorporated in stable mucoadhesive NLC systems, which are non-toxic and do not have any harmful effect on cell junctions. Mucoadhesive NLCs can create a depot on the surface of the cornea, which can predict improved bioavailability.

Biotribology measurement of in vitro and ex vivo contact lenses

2013 ◽  
Vol 36 ◽  
pp. e27 ◽  
Author(s):  
Aisling Mann ◽  
Amandeep Panaser ◽  
Brian Tighe
Keyword(s):  
Contact Lenses ◽  
Ex Vivo

scholarly journals Novel Contact Lenses Embedded with Drug-Loaded Zwitterionic Nanogels for Extended Ophthalmic Drug Delivery

Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2328
Author(s):  
Zhao Wang ◽  
Xinhua Li ◽  
Xiaojuan Zhang ◽  
Ruilong Sheng ◽  
Qing Lin ◽  
...  
Keyword(s):  
Drug Release ◽  
Contact Lenses ◽  
Eye Drops ◽  
Water Contact ◽  
In Vitro Drug Release ◽  
Molding Method ◽  
Ophthalmic Drug ◽  
One Step

Therapeutic ophthalmic contact lenses with prolonged drug release and improved bioavailability have been developed to circumvent tedious eye drop instillation. In this work, zwitterionic nanogels based on poly(sulfobetaine methacrylate) (PSBMA) were easily fabricated by one-step reflux-precipitation polymerization, with the advantages of being surfactant-free and morphology controlled. Then, the ophthalmic drug levofloxacin (LEV) was encapsulated into the nanogels. A set of contact lenses with varied nanogel-loading content was fabricated by the cast molding method, with the drug-loaded nanogels dispersed in pre-monomer solutions composed of 2-hydroxyethyl methacrylate (HEMA) and N-vinyl-2-pyrrolidone (NVP). The structure, surface morphology, water contact angle (WCA), equilibrium water content (EWC), transmittance, and mechanical properties of the contact lenses were subsequently investigated, and in vitro drug release and biocompatibility were further evaluated. As a result, the optimized contact lens with nanogel-loading content of 8 wt% could sustainably deliver LEV for ten days, with critical lens properties within the range of recommended values for commercial contact lenses. Moreover, cell viability assays revealed that the prepared contact lenses were cytocompatible, suggesting their significant potential as an alternative to traditional eye drops or ointment formulations for long-term oculopathy treatment.

scholarly journals Extended Release of Timolol from Ethyl Cellulose Microparticles Laden Hydrogel Contact Lenses

2015 ◽  
Vol 2 (1) ◽  
pp. 1-12 ◽  
Author(s):  
Furqan A. Maulvi ◽  
Tejal G. Soni ◽  
Dinesh O. Shah
Keyword(s):  
Physical Properties ◽  
Ethyl Cellulose ◽  
Contact Lenses ◽  
Drug Loading ◽  
Amorphous State ◽  
Eye Drops ◽  
Hydrogel Microparticles ◽  
Zero Order Kinetics ◽  
The Impact

Glaucoma is a second leading cause of blindness globally after cataract, which is managed through eye drops, which are highly inefficient due to a low bioavailability of less than 1-5%. Frequent administration of eye drops leads to incompliance in patients, so there is a great need for medical device such as contact lenses to treat glaucoma. The objective of research was to provide sustained ocular delivery of timolol via prototype poly (hydroxyethyl methacrylate) hydrogel contact lenses which may improve bioavailability due to increase in ocular residence time of drug. The present work was to encapsulate drug in ethylcellulose microparticles, and to entrap these microparticles in the hydrogel. Microparticles were prepared by spray drying method using different ratios of drug to ethylcellulose. The solid state characterization studies of drug loaded microparticles revealed the transformation of drug to an amorphous state. The hydrogels were characterized by studying their optical and physical properties to determine their suitability as extended wear contact lenses. Microparticles laden hydrogels were compared with direct drug loaded hydrogels. The study of microparticles laden hydrogels showed reduction in optical and physical properties and the impact was proportional to the amount of microparticles in hydrogels. The results suggest the application of optimization and nanotechnology. In vitro drug release study revealed that direct loading batch delivers drug for 22 hours with high drug loading of 150 µg, while microparticles laden hydrogel deliver drug up to 48 hours (zero order kinetics) with low drug loading of 50 µg. The hydrogels appeared safe in the cytotoxicity study. The study demonstrated the promising potential of loading the ethyl cellulose microparticles into hydrogels to serve as a good platform for sustained ophthalmic drug delivery.

scholarly journals Nanotechnology for Topical Drug Delivery to the Anterior Segment of the Eye

2021 ◽  
Vol 22 (22) ◽  
pp. 12368
Author(s):  
Alexander Vaneev ◽  
Victoria Tikhomirova ◽  
Natalia Chesnokova ◽  
Ekaterina Popova ◽  
Olga Beznos ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Anterior Segment ◽  
Drug Carriers ◽  
Ocular Tissue ◽  
Eye Drops ◽  
Topical Drug Delivery ◽  
Natural Polymers ◽  
Drug Bioavailability ◽  
Sustained Drug Release

Topical drug delivery is one of the most challenging aspects of eye therapy. Eye drops are the most prevalent drug form, especially for widely distributed anterior segment eye diseases (cataracts, glaucoma, dry eye syndrome, inflammatory diseases, etc.), because they are convenient and easy to apply by patients. However, conventional drug formulations are usually characterized by short retention time in the tear film, insufficient contact with epithelium, fast elimination, and difficulties in overcoming ocular tissue barriers. Not more than 5% of the total drug dose administered in eye drops reaches the interior ocular tissues. To overcome the ocular drug delivery barriers and improve drug bioavailability, various conventional and novel drug delivery systems have been developed. Among these, nanosize carriers are the most attractive. The review is focused on the different drug carriers, such as synthetic and natural polymers, as well as inorganic carriers, with special attention to nanoparticles and nanomicelles. Studies in vitro and in vivo have demonstrated that new formulations could help to improve the bioavailability of the drugs, provide sustained drug release, enhance and prolong their therapeutic action. Promising results were obtained with drug-loaded nanoparticles included in in situ gel.

Fabrication and Characterization of Ocular Phase Transition Systems for Blepharitis: A Novel Approach

2020 ◽  
Vol 10 (1) ◽  
pp. 24-37
Author(s):  
Deepali Verma ◽  
Shreya Kaul ◽  
Neha Jain ◽  
Upendra Nagaich
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Eye Drops ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Erythromycin Estolate

Introduction: In the present research, erythromycin estolate loaded in-situ gel was formulated and evaluated for blepharitis in order to improve its therapeutic efficacy, precorneal residence time of the system and to enhance the ocular bioavailability. Material and Methods: The developed formulation was characterized by several parameters viz. FTIR, clarity, pH, gelation temperature, rheological studies, drug content, in vitro drug release studies, transcorneal permeation studies, bioadhesion studies, isotonicity and stability studies. Results: The optimized formulation exhibited non-fickian release diffusion with a sustained release of drug 82.76 ± 0.94% up to 8h and drug content 93.64%. Isotonicity revealed that the formulation was isotonic in nature and there was no shrinkage and busting of cells. Bioadhesion study was performed to check the adherence of the prepared in situ gel to the corneal surface for 4h. Ex vivo transcorneal permeation was observed to be significantly higher when compared with market eye drops. Histopathological studies were conducted to confirm the presence of normal ocular surface tissues by maintaining their morphological structures without causing damage to the tissues. The formulation was nonirritant as confirmed by the HET-CAM test. Stability studies and accelerated stability studies were conducted for 13 weeks and 26 weeks respectively and formulations were analyzed for the visual appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release and results showed no change in the formulations. Conclusion: The formulation was therapeutically efficacious, sterile, stable and provided controlled release over a period of time. The developed system could be a viable alternative to conventional eye drops for treatment of various ocular diseases.

scholarly journals Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride

2007 ◽  
Vol 57 (1) ◽  
pp. 61-72 ◽  
Author(s):  
Vishnu Patel ◽  
Bhupendra Prajapati ◽  
Madhabhai Patel
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Stability Study ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
Propranolol Hydrochloride ◽  
Sustained Drug Release ◽  
Surface Ph

Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 ± 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.

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