Razvoj oftalmičkih sekundarnih kationskih nanoemulzija za uklapanje slabo topljivih glukokortikoida

Autor: Pavić, Klara
Přispěvatelé: Lovrić, Jasmina
Jazyk: chorvatština
Rok vydání: 2022
Předmět:
Popis: Nanoemulzije se ističu kao inovativni farmaceutski oblik s velikim potencijalom u liječenju bolesti suhog oka. Prednosti nanoemulzija temelje se na njihovoj strukturi i sastavu koje imaju učinak nadomještanja i stabilizacije suznog filma te na mogućnosti uklapanja slabo topljivih gluokokoritikoida kao što je loteprednol etabonat, djelatna tvar nedavno odobrena u liječenju blagih do umjerenog oblika bolesti suhog oka. Poseban potencijal imaju kationske nanoemulzije, zbog dobrih svojstava širenja po površini oka pri primjeni te produljenom zadržavanju na površini oka. Cilj ovog diplomskog rada bio je razviti sekundarnu kationsku U/V nanoemulziju s kitozanom pogodnu za uklapanje loteprednol etabonata. Nanoemulzije U/V tipa izrađene su visokoenergetskom metodom mikrofluidizacije. Kao ulja faza odabran je Capryol 90 zbog dobre topljivosti loteprednol etabonata u toj uljnoj fazi. Razvoj nanoemulzije proveden je u tri faze, (i) probir vrste i udjela neionske površinski aktivne tvari, (ii) probir vrste i udjela anionske površinski aktivne tvari te (iii) probir udjela niskomolekulskog kitozana. U svih fazama razvoja provedena je fizičko-kemijska karakterizacija nanoemulzija u vidu određivanja veličine i raspodjele veličina kapljica disperzne faze te zeta-potencijala. Na temelju provedene fizičko-kemijske karakterizacije sekundarna kationska nanoemulzija s 0,05 % (m/m) kitozana, 5 % (m/m) Capryola® 90, 0,25% (m/m) makrogol 15 hidroksistearata i 0,1% (m/m) lecitina Lipoid S75 ističe se kao vodeća formulacija s najvećim potencijalom za uklapanje loteprednol etabonata. Nanoemulsions stand out as an innovative dosage form with great potential in the treatment of dry eye disease. The benefits of nanoemulsions are based on (i) their structure and composition, which have the effect of replacing and stabilizing the tear film; and (ii) the ability to incorporate poorly soluble glucocorticoids such as loteprednol etabonate, an active substance recently approved in the treatment of mild to moderate dry eye disease. Cationic nanoemulsions have a unique potential due to their good spreading properties on the eye surface and prolonged retention on the eye surface. The aim of this thesis was to develop a secondary cationic O/W nanoemulsion with chitosan suitable for the incorporation of loteprednol etabonate. O/W type nanoemulsions are prepared by microfluidization. Capryol® 90 was chosen as the oil phase due to the good solubility of loteprednol etabonate in this oil phase. The development of the nanoemulsion was carried out in three phases, (i) screening of the type and content of nonionic surfactants, (ii) screening of the type and content of anionic surfactants, and (iii) screening of the content of low molecular weight chitosan. In all phases of development, physicochemical characterization of nanoemulsions was performed in the terms of determining the size and size distribution of droplets of the dispersed phase and zeta potential. Based on the performed physicochemical characterization, the secondary cationic nanoemulsion with 0.05% (w/w) chitosan, 5% (w/w) Capryola® 90, 0.25% (w/w) macrogol 15 hydroxystearate and 0.1% (w/w) Lecithin Lipoid® S75 stands out as the leading formulation with the greatest potential for incorporation of loteprednol etabonate.
Databáze: OpenAIRE