Naslov
Optimization of phospholipid vesicles for the treatment of sexually-transmitted bacterial infections

Autori
Amidžić Klarić, Daniela ; Rukavina, Zora ; Škalko-Basnet, Nataša ; Filipović-Grčić, Jelena ; Vanić, Željka

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
5th International Symposium Phospholipids in Pharmaceutical Research / - , 2017, 78-78

Skup
5th International Symposium Phospholipids in Pharmaceutical Research

Mjesto i datum
Heidelberg, Njemačka, 17.09.2017. - 18.09.2017

Vrsta sudjelovanja
Poster

Vrsta recenzije
Podatak o recenziji nije dostupan

Ključne riječi
Liposomes ; Bilayer elasticity ; In vitro drug release ; Propylene glycol ; Vaginal drug delivery

Sažetak
This study has focused on optimization of phospholipid-based vesicles for the vaginal treatment of recurrent bacterial infections. Different elastic and conventional liposomes entrapping azithromycin were prepared and characterized for size and surface properties, phospholipid bilayer elasticity/rigidity, encapsulation efficiency and release profile in conditions mimicking vaginal environment. Elastic propylene glycol-embedding liposomes were prepared by varying ratio of egg phosphatidylcholine (EPC), egg phosphatidylglycerol (EPG) and monoacyl phospholipid (LPC-80) [1]. Conventional liposomes with more rigid bilayers were prepared by proliposome method [2] using mixtures of EPC, EPG and hydrogenated phospholipid (SPC-3), while the ratio of azithromycin was kept constant for all the preparations. Physicochemical investigations of all azithromycin liposomes included size and surface charge assessments by dynamic light scattering, determination of bilayer elasticity [1] and in vitro stability/release in simulated vaginal conditions [2]. Regardless of the presence of LPC-80 or EPG, hydrodynamic diameters of all elastic propylene glycol-containing liposomes were of approx. 200 nm, while conventional liposomes were larger (240-420 nm), depending on the type and ratio of the phospholipids used. Zeta potentials of all the vesicles were in the range from -17 mV (elastic EPC/LPC-80 liposomes) up to -61 mV (conventional EPC/EPG/SPC-3 liposomes). Encapsulation of azithromycin into elastic liposomes was approx. 44%, while the lower values (31%) were obtained using rigid phospholipid bilayer constituents. Performed in vitro release studies demonstrated influence of pH, vaginal fluid components and lipid bilayer ingredients on the drug release profile. EPC/EPG/LPC-80 propylene glycol-embedding liposomes are considered as optimal elastic liposome formulation entrapping azithromycin for further investigations.

Izvorni jezik
Engleski

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