Abstract:
PURPOSE:Iontophoresis was employed for enhancing the transdermal delivery of acyclovir through nude mouse skin in vitro, with the aim of understanding the mechanisms responsible for drug transport, in order to properly set the conditions of therapeutical application. METHODS:Experiments were done in horizontal diffusion cells, using as donor a saturated solution of acyclovir at two different pH values (3.0 and 7.4). Different electrical conditions (current density and polarity) were employed. RESULTS:At pH 3.0, acyclovir anodal transport was due to electrorepulsion, since acyclovir was 20% in the protonated form. In acyclovir anodal iontophoresis at pH 7.4 the main mechanism involved was electroosmosis, since the drug was substantially unionized and the negative charge of the skin at this pH caused the electroosmotic flow to be from anode to cathode. In the case of cathodal iontophoresis at pH 3.0, acyclovir transport was enhanced approx. seven times, due to the presence of an electroosmotic contribution caused by the reversal of the charge of the skin. At pH 7.4 during cathodal iontophoresis acyclovir transport was not enhanced because the electroosmotic flow was in the opposite direction, compared to drug electric transport, i.e. anode to cathode. The increased skin permeability caused by current application was demonstrated to be less important than electrorepulsion and electroosmosis. CONCLUSIONS:Anodal iontophoresis shows potential applicability for enhancing acyclovir transport to the skin, considering that both electric transport and electroosmosis can be used by appropriately setting the pH of the donor.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Volpato NM,Santi P,Colombo Pdoi
10.1023/a:1016284815501subject
Has Abstractpub_date
1995-11-01 00:00:00pages
1623-7issue
11eissn
0724-8741issn
1573-904Xjournal_volume
12pub_type
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更新日期:1993-04-01 00:00:00
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更新日期:1987-12-01 00:00:00
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更新日期:2003-06-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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更新日期:1995-04-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2016-08-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1024441702398
更新日期:2003-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2018-11-29 00:00:00
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pub_type: 杂志文章
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更新日期:2011-05-01 00:00:00