Stability testing of ophthalmic nanoemulsions under conditions of simulated tear turnover

Autor: Cepetić, Dorja
Přispěvatelé: Lovrić, Jasmina
Jazyk: chorvatština
Rok vydání: 2022
Předmět:
Popis: Bolest suhog oka jedan je od najčešćih razloga posjeta oftalmologu i pogađa milijune ljudi. Karakteriziraju ju kronična upala, hiperosmolalnost suznog filma i smanjena debljina lipidnog sloja suznog filma, što uzrokuje simptome poput pečenja, svrbeža, crvenila i suzenja oka. Prva linija liječenja bolesti suhog oka primjena je bezreceptnih kapi za oko. Zadnjih nekoliko desetljeća istražuju se kapi za oko u obliku nanoemulzija te je odobreno nekoliko lijekova u tom obliku za liječenje bolesti suhog oka. Nanoemulzije tipa U/V daju mogućnost uklapanja slabo topljivih djelatnih tvari te dulje zadržavanje na mjestu primjene, a nude i simptomatsko liječenje bez djelatne tvari, zahvaljujući sinergizmu korištenih pomoćnih tvari u vidu stabilizacije i nadoknade suznog filma. Složeni su farmaceutski oblici s nekoliko fizičko-kemijskih parametara (primjerice, veličina, raspodjela veličina i zeta-potencijal kapljica unutranje faze) koji utječu na njihovu in vivo učinkovitost. Postoji veliki interes za razvoj inovativnih i generičkih lijekova temeljenih na tehnologiji nanoemulzija, ali zbog složenosti nanoemulzija taj je razvoj vrlo izazovan. Trenutno ne postoje biorelevantne in vitro metode konstruirane na temelju ključnih fizioloških i anatomskih aspekata površine oka, a koje bi omogućile učinkovit razvoj oftalmičkih nanoemulzija. Cilj ovog diplomskog rada je ispitati stabilnost oftalmičke nanoemulzije u uvjetima simulirane izmjene suza. U tu svrhu pripravljene su jednostavne U/V nanoemulzije stabilizirane neionskom PAT te je određen utjecaj razrjeđenja vodom ili vanjskom fazom nanoemulzije na veličinu i raspodjelu veličina te zeta-potencijal kapljica nanoemulzije. Potom je određena stabilnost jednostavne nanoemulzije u uvjetima simulirane izmjene suza korištenjem umjetne suzne tekućine koja sadržava soli, ureu i glukozu. Tijekom 40 minuta ispitivanja u uvjetima kontinuiranog biorelevantnog razrjeđenja nanoemulzije stabilizirane neionskom površinski aktivnom tvari nije uočena značajnija promjena veličine i raspodjele veličina te zeta-potencijala kapljica unutarnje faze. Dry eye disease (DED) is one of the most common reasons for visiting an ophthalmologist and affects millions of people. It is characterized by chronic inflammation, hyperosmolarity of the tear film and reduced thickness of the lipid layer of the tear film, which causes symptoms such as burning, itching, redness and watering of the eye. The first line of treatment for DED is the use of over-the-counter (OTC) eye drops. For the last few decades, eye drops in the form of nanoemulsions have been researched, and several medicines in this form have been approved for treatment of DED. Oil-in-water (O/W) nanoemulsions provide the possibility of incorporating lipophilic drugs and prolonging their retention time at the site of application. Furthermore, they offer symptomatic treatment without the active substance, thanks to the synergism of the excipients, by stabilizing and replacing of the tear film. They are complex pharmaceutical forms with several physicochemical parameters (such as size, polydispersity index and zeta-potential of the internal phase droplets) which affect their in vivo efficiency. There is great interest in the development of innovative and generic drugs based on nanoemulsion technology, but due to the complexity of nanoemulsions, this development is very challenging. Currently, there are no biorelevant in vitro methods constructed on the basis of key physiological and anatomical aspects of the eye surface, which would enable the effective development of ophthalmic nanoemulsions. The aim of this thesis is to examine the stability of ophthalmic nanoemulsion under the conditions of simulated tear turnover. For this purpose, simple O/W nanoemulsions stabilized by non-ionic surfactant were prepared and the influence of dilution with water or the external phase of the nanoemulsion on the size and polydispersity index and zeta-potential of the nanoemulsion droplets was determined. Then, the stability of a simple nanoemulsion was determined under the conditions of simulated tear turnover using an artificial tear solution containing salts, urea and glucose. During 40 minutes of testing under conditions of continuous biorelevant dilution of the nanoemulsion stabilized with a nonionic surfactant, no significant change in the size, polydispersity index and zeta-potential of the internal phase droplets was observed.
Databáze: OpenAIRE
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