Naslov
Development and in vitro evaluation of a liposomal vaginal delivery system for acyclovir
(Development and in vitro evaluation of a liposomal vaginal delivety system for acyclovir)

Autori
Pavelić, Željka ; Škalko-Basnet, Nataša ; Filipović-Grčić, Jelena ; Martinac, Anita ; Jalšenjak, Ivan

Izvornik
Journal of Controlled Release (0168-3659) 106 (2005), 1-2; 34-43

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Liposomes; Acyclovir; Hydrogel; Stability; Vaginal application

Sažetak
Design of a liposomal delivery system for vaginal administration of acyclovir, able to provide sustained release and improved bioavailability of encapsulated drug for the local treatment of genital herpes was investigated. Acyclovir was encapsulated in liposomes prepared by polyol dilution method, whereby various phospholipid compositions were used: egg phosphatidylcholin (PC)/egg phosphatidylglycerol (PG) 9:1, egg phosphatidylcholine (PC) and egg phosphatidycholine (PC)/stearylamine (SA) 9:3. All liposome preparations were characterised and compared for particle size, polydispersity, encapsulation efficiency and tested for in vitro stability in different media chosen to simulate human vaginal conditions: buffer, pH 4.5 (corresponding to normal human vaginal pH), vaginal fluid stimulant (medium developed to mimic the fluid produced in vagina) without or with mucin. To be closer to in vivo application of liposomes and to achieve further improvement of their stability, liposomes were incorporated in vehicle suitable for vaginal self-administration. Bioadhesive hydrogel made from Carbopol 974P NF resin with adequate pH value and desirable viscosity was chosen as a vehicle for liposomes containing acyclovir. In vitro release studies of liposomes incorporated in gel proved their applicability as a novel vaginal delivery system in localised and sustained release of encapsulated acyclovir. Even after 24 h of incubation in vaginal fluid stimulant more than 35 % of originally encapsulated drug was retained in hydrogel.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

POVEZANOST RADA