Liposomal gels for vaginal drug delivery.
The aim of our study was to develop a liposomal drug carrier system, able to provide sustained and controlled release of appropriate drug for local vaginal therapy. To optimise the preparation of liposomes with regards to size and entrapment efficiency, liposomes containing calcein were prepared by five different methods. Two optimal liposomal preparations (proliposomes and polyol dilution liposomes) were tested for their in vitro stability in media that simulate human vaginal conditions (buffer, pH 4.5). To be closer to in vivo application of liposomes and to achieve further improvement of their stability, liposomes were incorporated in vehicles suitable for vaginal self-administration. Gels of polyacrylate were chosen as vehicles for liposomal preparations. Due to their hydrophilic nature and bioadhesive properties, it was possible to achieve an adequate pH value corresponding to physiological conditions as well as desirable viscosity. In vitro release studies of liposomes incorporated in these gels (Carbopol 974P NF or Carbopol 980 NF) confirmed their applicability as a novel drug carrier system in vaginal delivery. Regardless of the gel used, even 24 h after the incubation of liposomal gel in the buffer pH 4.5 more than 80% of the originally entrapped substance was still retained.
Pavelić
Z
Z
Department of Pharmaceutics, Faculty of Biochemistry, University of Zagreb, A. Kovacica 1, P.O. Box 156, 10000, Zagreb, Croatia. zelijka.pavelic@fbf.tel.hr
Skalko-Basnet
N
N
Schubert
R
R
D000180:Acrylic Resins; D000282:Administration, Intravaginal; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D005615:Freezing; D005782:Gels / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry*; D011145:Polyvinyls; D014783:Viscosity
D000180:Acrylic Resins; D004337:Drug Carriers; D005782:Gels; D008081:Liposomes; D011145:Polyvinyls; C006912:carboxypolymethylene