Topical drug delivery to the posterior segment of the eye: The effect of benzalkonium chloride on topical dexamethasone penetration into the eye in vivo

2018 ◽  
Vol 48 ◽  
pp. 125-127 ◽  
Author(s):  
Sunna Johannsdottir ◽  
Phatsawee Jansook ◽  
Einar Stefansson ◽  
Iris Myrdal Kristinsdottir ◽  
Gudrun Marta Asgrimsdottir ◽  
...  
2011 ◽  
Vol 149 (2) ◽  
pp. 159-167 ◽  
Author(s):  
Priya Batheja ◽  
Larisa Sheihet ◽  
Joachim Kohn ◽  
Adam J. Singer ◽  
Bozena Michniak-Kohn

2020 ◽  
Vol 10 (5-s) ◽  
pp. 32-39
Author(s):  
Fatima Eram ◽  
, Vivek

Objectives: The purpose of this research was to develop the micro emulsion-based in situ gelling systems containing Ciprofloxacin for prophylaxis and treatment of the posterior segment diseases like endophthalmitis. Methods: Ciprofloxacin was encapsulated in small droplets owing to form microemulsion, and then the formed droplets were dispersed in a polymer solution that converted into a gel upon triggered by the electrolyte present in the tear fluid. Results: The formulation approach provides better absorption, penetration, retention, and improves the bioavailability of the drug. The average concentration reached into vitreous humor from topical microemulsion in situ gelling formulation was ~0.4 µg/ml, which is far more than the concentration required for therapeutic effect (i.e.  >0.047 µg/ml or >MIC90 for S. Epidermidis, a pathogen commonly responsible to cause endophthalmitis). Conclusion: Thus, novel micro emulsion-based in situ gelling formulation could be a potential drug delivery system for the treatment of posterior segment diseases like endophthalmitis. Keywords: Microemulsion, ciprofloxacin, endophthalmitis, ocular, infection, in situ


Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 134
Author(s):  
Marina Löscher ◽  
Chiara Seiz ◽  
José Hurst ◽  
Sven Schnichels

Topical drug delivery to the posterior segment of the eye is a very complex challenge. However, topical delivery is highly desired, to achieve an easy-to-use treatment option for retinal diseases. In this review, we focus on the drug characteristics that are relevant to succeed in this challenge. An overview on the ocular barriers that need to be overcome and some relevant animal models to study ocular pharmacokinetics are given. Furthermore, a summary of substances that were able to reach the posterior segment after eye drop application is provided, as well as an outline of investigated delivery systems to improve ocular drug delivery. Some promising results of substances delivered to the retina suggest that topical treatment of retinal diseases might be possible in the future, which warrants further research.


2018 ◽  
Vol 15 (7) ◽  
pp. 687-701 ◽  
Author(s):  
Yanyan Wang ◽  
Xiaoyue Xu ◽  
Yan Gu ◽  
Yanju Cheng ◽  
Feng Cao

2020 ◽  
Vol 3 (3) ◽  
pp. 1722-1729 ◽  
Author(s):  
Xingyu He ◽  
Zheng Yuan ◽  
Winston Kao ◽  
Daniel Miller ◽  
S. Kevin Li ◽  
...  

2015 ◽  
Vol 41 (5) ◽  
pp. 653-661 ◽  
Author(s):  
Yuko Shikamura ◽  
Yoshiko Yamazaki ◽  
Toru Matsunaga ◽  
Takao Sato ◽  
Akira Ohtori ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1685
Author(s):  
Ayah Mohammad Burhan ◽  
Butsabarat Klahan ◽  
Wayne Cummins ◽  
Vanessa Andrés-Guerrero ◽  
Mark E. Byrne ◽  
...  

Posterior segment eye diseases (PSEDs) including age macular degeneration (AMD) and diabetic retinopathy (DR) are amongst the major causes of irreversible blindness worldwide. Due to the numerous barriers encountered, highly invasive intravitreal (IVT) injections represent the primary route to deliver drugs to the posterior eye tissues. Thus, the potential of a more patient friendly topical route has been widely investigated. Mucoadhesive formulations can decrease precorneal clearance while prolonging precorneal residence. Thus, they are expected to enhance the chances of adherence to corneal and conjunctival surfaces and as such, enable increased delivery to the posterior eye segment. Among the mucoadhesive polymers available, chitosan is the most widely explored due to its outstanding mucoadhesive characteristics. In this review, the major PSEDs, their treatments, barriers to topical delivery, and routes of topical drug absorption to the posterior eye are presented. To enable the successful design of mucoadhesive ophthalmic drug delivery systems (DDSs), an overview of mucoadhesion, its theory, characterization, and considerations for ocular mucoadhesion is given. Furthermore, chitosan-based DDs that have been explored to promote topical drug delivery to the posterior eye segment are reviewed. Finally, challenges of successful preclinical to clinical translation of these DDSs for posterior eye drug delivery are discussed.


2021 ◽  
Vol 22 (18) ◽  
pp. 9743
Author(s):  
Eliana B. Souto ◽  
Ana S. Macedo ◽  
João Dias-Ferreira ◽  
Amanda Cano ◽  
Aleksandra Zielińska ◽  
...  

Administration of active pharmaceutical ingredients (APIs) through the skin, by means of topical drug delivery systems, is an advanced therapeutic approach. As the skin is the largest organ of the human body, primarily acting as a natural protective barrier against permeation of xenobiotics, specific strategies to overcome this barrier are needed. Liposomes are nanometric-sized delivery systems composed of phospholipids, which are key components of cell membranes, making liposomes well tolerated and devoid of toxicity. As their lipid compositions are similar to those of the skin, liposomes are used as topical, dermal, and transdermal delivery systems. However, permeation of the first generation of liposomes through the skin posed some limitations; thus, a second generation of liposomes has emerged, overcoming permeability problems. Various mechanisms of permeation/penetration of elastic/ultra-deformable liposomes into the skin have been proposed; however, debate continues on their extent/mechanisms of permeation/penetration. In vivo bioavailability of an API administered in the form of ultra-deformable liposomes is similar to the bioavailability achieved when the same API is administered in the form of a solution by subcutaneous or epi-cutaneous injection, which demonstrates their applicability in transdermal drug delivery.


2021 ◽  
Vol 11 (5-S) ◽  
pp. 176-187
Author(s):  
Sudip Das ◽  
Koushik Sen Gupta

The drug delivery within the stratum corneum of the skin prevails a challenging area for the pharmaceutical field, especially to the formulation scientists. Several investigations revealed that the lipid domain, which is the integral component of the transport barrier, must be breached if it is to be delivered transdermally at an appropriate rate. In particular, transdermal drug delivery has intrigued researchers with multiple suggestions because multiple dosing or insufficient drug delivery or characteristics of various drugs often results in low therapeutic effects. The application of permeation or penetration enhancers may prolong the number of drugs that can be offered topically. The application of any natural permeation enhancer is innoxious over the artificial permeation enhancers. The natural permeation enhancers are investigated, so notably include essential oils, terpenes, terpenoids, fatty acid esters, etc., have a certain effect in the transdermal drug delivery system. Despite decades of investigation on the natural chemical penetration enhancer, the researchers could not establish the effectiveness of natural penetration enhancers clinically due to the lack of in vivo models. Several factors, like solubility, solvent selection, experimental models, etc., has restricted the application and development of natural penetration enhancers in topical drug delivery systems, especially in the patches. Therefore, further investigation needs to do on skin irritation to decide natural penetration enhancers controlling optimum enhancement effects with minimal skin irritation. This review gives a comprehensive literature survey on naturally obtained chemical penetration enhancers and their future possibilities. Keywords: Topical Drug delivery system, Natural products, Penetration enhancer, Stratum corneum, In vivo models.


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