Title Određivanje mukoadhezivnih svojstva kationskih nanoemulzija
Title (english) Determination of mucoadhesive properties of cationic nanoemulsions
Author Marija Šare
Mentor Jasmina Lovrić (mentor)
Committee member Jasmina Lovrić (predsjednik povjerenstva)
Committee member Anita Hafner (član povjerenstva)
Committee member Dubravka Vitali Čepo (član povjerenstva)
Granter University of Zagreb Faculty of Pharmacy and Biochemistry (Department of pharmaceutical technology) Zagreb
Defense date and country 2019-09-25, Croatia
Scientific / art field, discipline and subdiscipline BIOMEDICINE AND HEALTHCARE Pharmacy Pharmacy
Abstract Topikalna primjena lijekova je najrašireniji i opće prihvaćen način liječenja velikog broja bolesti oka. Međutim, bioraspoloživost topikalnih oftalmičkih lijekova je mala zbog vrlo učinkovitih protektivnih mehanizama oka. Sve se više istažuje primjena nanoemulzija čije kapljice nanometarskih dimenzija omogućuju svladavanje ovih barijera. Poseban se naglasak stavlja na kationske nanoemulzije koje stupaju u interakciju s negativno nabijenom površinom oka i tako pospješuju apsorpciju lijeka. U sklopu ovog diplomskog rada istraživane su kationske nanoemulzije sa stearilaminom kao nositeljem pozitivnog naboja. Kako bi se odredila koncentracija stearilamina koja osigurava svojstva najpogodnija za oftalmičku primjenu ispitana su ključna fizičko-kemijska svojstva nanoemulzija koja utječu na njihov klinički učinak uključujući veličinu kapljica, indeks polidisperznosti, zeta-potencijal, pH, profil viskoznosti formulacije kao funkcije primijenjene sile smicanja te površinsku napetost.Utvrđeno je da sve nanoemulzije pokazuju karakteristike Newtonovskih sustava. Niska viskoznost nanoemulzija omogućavaju jednostavnu primjenu te točnost doziranje kapi za oko. Nanoemulzija s 0,05 % (m/m) stearilamina ima pH vrijednost najprikladniju za oftalmičku primjenu. Stearilamin smanjuje površinsku napetost nanoemulzije, a mjerenjem je utvrđeno da je 0,05 % (m/m) stearilamina u uzorku granična koncentracija koja neće uzrokovati nelagodu pri primjeni. Zeta-potencijal nanoemulzija raste proporcionalno s porastom koncentracije stearilamina. Nakon inkubacije s disperzijom mucina vrijednosti su se očekivano smanjile. Svi uzorci pokazuju prihvatljive veličine kapljica (⁓100 nm) i indekse polidisperznosti (PDI < 0,2). Zabilježen je porast veličine kapljica nanoemulzija koje sadrže stearilamin nakon inkubacije s disperzijom mucina, a promjene su najočitije kod uzoraka s 0,05 % (m/m) i 0,1 % (m/m) stearilamina pa su ti uzorci okarakterizirani kao najmukoadhezivniji. S obzirom na rezultate fizičko-kemijskih testova i testa mukoadhezivnosti, formulacija s 0,05 % (m/m) stearilamina se istaknula kao najoptimalnija za oftalmičku primjenu.
Abstract (english) Topical drug administration is the most widely used and commonly accepted treatment for many eye diseases. However, the bioavailability of topical ophthalmic drugs is low due to the highly effective protective mechanisms of the eye. As nanoemulsions can overcome these barriers, their application is increasingly being explored and particular emphasis is placed on cationic nanoemulsions that interact with the negatively charged surface of corneal epithelial cells and thus enhance drug absorption. As part of this thesis, cationic nanoemulsions with stearylamine as a positive charge carrier were examined. In order to determine the concentration of stearylamine that provides the properties most suitable for ophthalmic administration, the key physicochemical properties of nanoemulsions that affect their clinical performance including droplet size, polydispersity index, zeta potential, pH, formulation viscosity profile as a function of applied shear force, and surface tension were examined.It was found that all nanoemulsions show the characteristics of Newtonian systems. Low formulation viscosity enables dosing accuracy and ease of eye-drop administration. A nanoemulsion with 0.05 % (m/m) stearylamine has a pH value most suitable for ophthalmic administration. Stearylamine reduces the surface tension of the nanoemulsion, and by measurement it was found that 0.05 % stearylamine in the sample is a concentration limit that will not cause discomfort when applied. The zeta-potential of nanoemulsions increases in proportion with the increase of stearylamine concentration, and after incubation with the dispersion of mucin, values decreased. All samples show acceptable droplet sizes (⁓100 nm) and polydispersity indexes (PDI < 0.2). An increase in the size of stearylamine-containing nanoemulsions after incubation with mucin dispersion was observed. Changes were most evident in the 0.05 % (m/m) and 0.1 % (m/m) stearylamine samples so it was concluded that these samples have the strongest mucoadhesive properties. Considering the results of the physico-chemical and mucoadhesive tests, the formulation with 0.05 % (m/m) stearylamine stood out as the most optimal for ophthalmic use.
Keywords
nanoemulzije
oftalmička primjena
stearilamin
mukoadhezivnost
Keywords (english)
nanoemulsions
ophthalmic application
stearylamine
mucoadhesion
Language croatian
URN:NBN urn:nbn:hr:163:572173
Study programme Title: Pharmacy Study programme type: university Study level: integrated undergraduate and graduate Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
Type of resource Text
File origin Born digital
Access conditions Open access
Terms of use
Created on 2021-04-23 07:45:55