In vitro ispitivanje oslobađanja azitromicina iz elastičnih liposoma

master's thesis

• Title (english): In vitro release test of azithromycin from the elastic liposomes
• Author: Matea Novosel
• Mentor: Željka Vanić (mentor)
• Committee member: Željka Vanić (predsjednik povjerenstva)
• Committee member: Mario Jug (član povjerenstva)
• Committee member: Lovorka Vujić (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of pharmaceutical technology); Zagreb
• Defense date and country: 2015-07-02, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Konvencionalni, deformabilni i propilenglikol liposomi s uklopljenim azitromicinom pripremljeni su metodom hidratacije suhog fosfolipidnog sloja, tzv. film metodom. Kako bi se postigla homogenost uzoraka i veličina vezikula optimalna za dermalnu primjenu, dobivene preparacije liposoma su ekstrudirane kroz polikarbonatne membrane veličine pora 400 nm i 100 nm. Nakon ekstruzije utvrđen je srednji promjer vezikula u rasponu rasponu od 113 nm do 140 nm i niski indeksi polidisperznosti (0,100 – 0,138). Svim je preparacijama određen zeta potencijali, a izmjerene negativne vrijednosti zeta potencijala za sve liposomske preparacije (od -36 mV do -45 mV) upućuju na formiranje fizički stabilnih liposomskih disperzija. In vitro ispitivanje oslobađanja azitromicina iz liposoma provedeno je na Franz difuzijskoj ćeliji tijekom 24 h, pri čemu je provedeno i ispitivanje oslobađanja lijeka iz kontrole (otopina lijeka). Sadržaj oslobođenog lijeka u sakupljenim uzorcima određen je kromatografski (HPLC). Dobiveni rezultati ukazuju na sporije oslobađanje azitromicina iz svih vrsta liposoma u usporedbi s kontrolom. Lijek se brže oslobađao iz elastičnih liposoma (deformabilni liposomi, propilenglikol liposomi) u odnosu na konvencionalne liposome, pri čemu je brzina oslobađanja bila najveća za deformabilne liposome. Može se zaključiti kako oslobađanje azitromicina iz fosfolipidnih vezikula ovisi o njihovim fizikalno-kemijskim svojstvima te o prisutnosti promotora penetracije ili rubnog aktivatora u sastavu. Elastični liposomi su se pokazali kao prikladni nosači azitromicina za dermalnu primjenu kojima bi se moglo postići produženo i kontrolirano oslobađanje.

Abstract (english)

Conventional, deformable and propylene glycol liposomes encapsulating azythromicin were prepared by the film hydration method. In order to obtain homogenous liposomal dispersions and optimize vesicle size for dermal application, liposomal preparations were extruded through polycarbonate membranes with pore size of 400 nm and 100 nm. Resulting vesicles were in the mean diameter range of 113 to 140 nm, with low values of polydispersity index measured (0,100 – 0,138). Negative values of zeta potential for all liposomal preparations (between -36 mV and -45 mV) indicated the formation of physically stable liposomal dispersions. In vitro release studies were performed during 24 h using Franz diffusion cell system. The release of azythromicin from different liposomes and control (azithromycin in 40% ethanol solution) was tested. The amount of the released azithromycin was determined cromatographically (HPLC). All of the liposomal formulations were characterized by the slower release rates and sustained release profiles as compared to the control (solution of the drug). Among the investigated liposomes, the release rates were higher for elastic vesicles (deformable and propylene glycol liposomes) than conventional liposome and the highest release rate was observed for deformable liposomes. It could be concluded that the azithromycin release from the phospholipid vesicles depends on their physicochemical properties and the presence of the penetration enhancer or edge activator in their composition. Elastic liposomes have been shown to be suitable as azithromycin carrier systems for dermal application which could possibly achieve prolonged and controlled release of the drug.

• Keywords: deformabilni liposomi; propilenglikol liposomi; azitromicin; dermalna primjena lijeka
• Keywords (english): deformable liposomes; propylene glycol liposomes; azythromicin; dermal application of drug
• Language: croatian
• URN:NBN: urn:nbn:hr:163:791334
• 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
• Created on: 2021-05-14 10:22:52