期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 106, 期 -, 页码 294-301出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2017.06.025
关键词
Liposome; NSAID delivery; Iontophoresis; Transdermal drug delivery; Diclofenac sodium; Skin permeation
资金
- Academy of Finland [258114, 264988]
- Academy of Finland (AKA) [264988, 264988] Funding Source: Academy of Finland (AKA)
This study was aimed to evaluate the in vitro transdermal direct/pulsed current iontophoretic delivery of an amphiphilic model compound from various lipid vesicle-encapsulated formulations compared to free-drug formulation. Conventional, pegylated, ultradeformable liposomes (transfersomes) and ethosomes loaded with a negatively charged drug diclofenac sodium (DS) were prepared and characterized. All the liposomes possessed an average size of approximate to 100-150 nm and negative zeta potential. No changes in colloidal stability were detected after 8 h incubation of any vesicle formulation under constant or pulsed iontophoretic current. DS was released from all the liposome formulations with a similar, limited rate (approximate to 50% in 24 h), leading therefore to significantly lower transdermal fluxes across full-thickness porcine skin compared to the respective free drug formulation. From the tested lipid vesicle formulations, the transfersomes resulted in the highest passive flux and the ethosomes in the highest iontophoretic flux under direct constant current treatment. Higher negative surface charge of the vesicle led to better transport efficiency due to the higher mobility of the drug carrier under electric field. Pulsed current iontophoresis had no advantage over constant current treatment in combination with any type of lipid vesicular nanocarriers, in contrast to what has been described earlier with drug-loaded polymeric nano carriers.
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