There are more than 100 recognized disorders of the eye. This makes the development of advanced ocular formulations an important topic in pharmaceutical science. One of the ways to improve drug delivery to the eye is the use of penetration enhancers. These are defined as compounds capable of enhancing drug permeability across ocular membranes. This review paper provides an overview of anatomical and physiological features of the eye and discusses some common ophthalmological conditions and permeability of ocular membranes. The review also presents the analysis of literature on the use of penetration-enhancing compounds (cyclodextrins, chelating agents, crown ethers, bile acids and bile salts, cell-penetrating peptides, and other amphiphilic compounds) in ocular drug delivery, describing their properties and modes of action.
Thermoresponsive polymers with the appropriate structure form physical networks upon changes in temperature, and they find utility in formulation science, tissue engineering, and drug delivery. Here, we report a cost-effective biocompatible alternative, namely OEGMA300 15 - b -BuMA 26 - b -DEGMA 13 , which forms gels at low concentrations (as low as 2% w/w); OEGMA300, BuMA, and DEGMA stand for oligo(ethylene glycol) methyl ether methacrylate (MM = 300 g mol –1 ), n -butyl methacrylate, and di(ethylene glycol) methyl ether methacrylate, respectively. This polymer is investigated in depth and is compared to its commercially available counterpart, Poloxamer P407 (Pluronic F127). To elucidate the differences in their macroscale gelling behavior, we investigate their nanoscale self-assembly by means of small-angle neutron scattering and simultaneously recording their rheological properties. Two different gelation mechanisms are revealed. The triblock copolymer inherently forms elongated micelles, whose length increases by temperature to form worm-like micelles, thus promoting gelation. In contrast, Pluronic F127’s micellization is temperature-driven, and its gelation is attributed to the close packing of the micelles. The gel structure is analyzed through cryogenic scanning and transmission electron microscopy. Ex vivo gelation study upon intracameral injections demonstrates excellent potential for its application to improve drug residence in the eye.
As drug delivery to the eye has evolved over the last decades, researchers have explored more effective treatments for ocular diseases. Despite this, delivering drugs to the cornea remains one of the most problematic issues in ophthalmology due to the poor permeability of the cornea and tear clearance mechanisms. In this study, four different types of polyaphron formulations are prepared with 10% poloxamer 188 (P188), 10% poly(2-ethyl-2-oxazoline), 1% polyquaternium 10, and 3% sodium carboxymethylcellulose solutions mixed with 1% Brij® L4 in a caprylic/capric triglycerides solution. Their physicochemical characteristics, rheological properties, and stability are assessed. Additionally, a polyaphron with 3% polyquaternium 10 was prepared for the assessment of ex vivo corneal retention along with four other polyaphrons. The best retention on the ex vivo cornea was displayed by the 3% polyquaternium 10-based formulation. The 10% poloxamer 188 along with 1% polyquaternium 10-based polyaphrons appeared to be the most stable among the four prepared formulations. A toxicological evaluation of these formulations was performed using a slug mucosal irritation test and bovine corneal opacity and permeability assay, with all four polyaphrons proving good biocompatibility with ocular tissues. The developed drug delivery systems demonstrated an excellent potential for ocular drug delivery.
Liposomes are promising spherical vesicles for topical drug delivery to the eye. Several types of vesicles were formulated in this study, including conventional, PEGylated, and maleimidedecorated PEGylated liposomes. The physicochemical characteristics of these liposomes, including their size, zeta potential, ciprofloxacin encapsulation efficiency, loading capacity, and release, were evaluated. The structure of these liposomes was examined using dynamic light scattering, transmission electron microscopy, and small angle neutron scattering. The ex vivo corneal and conjunctival retention of these liposomes were examined using the fluorescence flow-through method. Maleimidedecorated liposomes exhibited the best retention performance on bovine conjunctiva compared to other types of liposomes studied. Poor retention of all liposomal formulations was observed on bovine cornea.
The relevance of the study of this problem is due to the intensive implementation of new information technologies and various electronic courses that contribute to the introduction of digitalization in the educational system. According to the regulatory documents, the purpose of digitalization of the educational system is to ensure a broad access to information and digital resources, and the use of digital technologies in the educational process. In this regard, this article focuses on the identification and disclosure of the purpose and objectives of digitization in the education system, the implementation of the principle of organization of mastering of the optimally required knowledge, a particular algorithm, contributing to the development and transmission of knowledge by means of individual internal and external instruments of knowledge representing the cognitive organization of a personality. The leading method in the study of this problem is the interdisciplinary analysis of scientific literature, which allowed to reveal the essence of the digitalization of the educational process, optimization of the method of cognitive modeling in the educational process in order to develop internal instruments of knowledge of students; theoretical modeling, which allowed to structure the planning process of educational activities in higher education. The article reveals the changes determined by the new socio-cultural and economic situation of digital development, substantiates the new formats of collaboration and learning built around the student, requiring digital literacy teachers and responsibility of students for the quality of their education. The article is focused on the adaptation of teachers to the new conditions of professional activity in the field of education in the conditions of digitalization.
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