Deformable liposomes containing alkylcarbonates of γ-cyclodextrins for dermal applications |
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Authors: | D Chirio R Cavalli F Trotta M E Carlotti M Trotta |
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Institution: | (1) Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, via P. Giuria 9, 10125 Torino, Italy;(2) Dipartimento di Chimica Inorganica, Fisica e dei Materiali, Università degli Studi di Torino, via P. Giuria 7, 10125 Torino, Italy |
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Abstract: | Liposomes made with hydrogenated soya lecithin (HPC) mixed with dodecylcarbonate γ-cyclodextrin (C12CD) at 20:1, 10:1 and
5:1 w/w ratios were prepared by the solvent evaporation method. C12CD had emulsifying properties and the possibility of producing
deformable liposomes, as topical delivery system of progesterone (PG), was evaluated. Liposome size, deformability and drug
entrapment were determined and the interaction between C12CD and HPC was investigated using differential scanning calorimetry
(DSC). The size and the amount of PG loaded in the liposomes depended on the lipid:C12CD ratio: the smallest liposomes were
obtained using 20:1 ratio and the maximum drug entrapment at 5:1 ratio. DSC analysis suggested that C12CD interacted with
liposomes disrupting and fluidizing the lipid bilayer. PG transepidermal permeation through intact pig skin and PG skin uptake
from deformable liposomes were assessed and compared to the values obtained from aqueous suspension and conventional liposomes.
The PG permeations were negligible for all systems, while skin uptake increased for liposomes containing C12CD. This was attributed
to the deformability and to the increase in the drug entrapment efficiency of these liposomes. The use of C12CD in liposome
formulations can improve PG topical therapy. |
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Keywords: | Deformable liposomes Alkylcarbonate cyclodextrins Progesterone Skin uptake |
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