TI: Transdermal delivery of macromolecules using skin
electroporation.
AU: Lombry,-C; Dujardin,-N; Preat,-V
AD: Universite Catholique de Louvain, Ecole de Pharmacie, Unite
de Pharmacie Galenique, Industrielle et Officinale, Brussels, Belgium.
SO: Pharm-Res. 2000 Jan; 17(1): 32-7
JN: Pharmaceutical-research
PY: 2000
AB: PURPOSES: (1) To evaluate the feasibility of transdermal
delivery of macromolecules by skin electroporation. (2) To assess the influence
of the molecular weight of the permeant on transport and examine whether
there exists a "cut-off" value of molecular weight. (3) To localize the
transport pathways of the macromolecules in the skin. METHODS: FITC-dextran
(FD) of increasing molecular weight (4.4, 12 and 38 kDa) were used as model
macromolecules to study the extent of transport across hairless rats skin
in vitro and to localize their distribution in the skin by confocal scanning
laser microscopy. RESULTS: Electroporation enhanced the transport of the
macromolecules as compared to passive diffusion. The transdermal delivery
by skin electroporation of FITC and FD 4.4 was equivalent whereas transport
of higher molecular weight FD was lower but significant. FITC and FD 38
were observed in the epidermis both around and in the keratinocytes. CONCLUSIONS:
Transdermal and topical delivery of macromolecules of at least 40 kDa can
be achieved by skin electroporation.