Abstract：
:We studied skin occlusion effects in vitro and in vivo on local and systemic delivery of ketoprofen across the organ, using the drug in a conventional non-occlusive topical gel (Togal Mobil-Gel), an occlusive tape (Mohrus), and the new targeted analgesic (Diractin), comprising ultradeformable, hydrophilic carriers in the form of a Transfersome vesicle. In vitro occluded skin permeability to ketoprofen from the tape (0.086cmh(-1)) marginally exceeds the value for the drug from carriers in a gel (0.058cmh(-1)), which resembles conventional gel on open excised skin (0.057cmh(-1)); smallness of occlusion-induced permeation enhancement ( approximately 1.5x) may be due to the high tested applied dose. In contrast, open skin permeability to the drug from the carriers in vitro is approximately 15xlower (0.004cmh(-1)). The benefit of ketoprofen association with the carriers for targeted transcutaneous delivery only shows-up in vivo after an non-occlusive epicutaneous application: the area under the curve (AUC) in peripheral deep muscle for the carrier-based gel then exceeds AUC for conventional gel approximately 35-fold. The AUC for occluded ultradeformable, hydrophilic carriers measured in living pigs is conversely approximately 10x lower, being 1.4-2.2x below that of the tape that is inferior to non-occluded carriers formulation (normalised cmax: approximately 200x). Occlusion thus disables ultradeformable, hydrophilic carriers by eliminating transcutaneous hydration gradient that normally drives the carriers across the skin. Compared with other non-steroidal anti-inflammatory agents (NSAIDs) for local usage, Diractin is thus evidently well differentiated and innovative.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Cevc G,Mazgareanu S,Rother M,Vierl Udoi
10.1016/j.ijpharm.2008.04.005subject
Has Abstractpub_date
2008-07-09 00:00:00pages
190-7issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(08)00279-2journal_volume
359pub_type
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abstract：:Chlorambucil (CHL) is a water-insoluble antineoplastic drug having a short elimination half-life. It suffers from remarkable differences in pharmacokinetics following oral administration. The current work aimed to assess safety and pharmacokinetics of CHL-loaded, lipoprotein-mimic, nanoparticles (NPs) following intrav...
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更新日期：2020-02-25 00:00:00
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更新日期：2016-03-16 00:00:00
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更新日期：2012-11-15 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2012-09-15 00:00:00
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更新日期：2017-05-15 00:00:00
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更新日期：2008-02-28 00:00:00
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pub_type： 杂志文章
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更新日期：2009-02-23 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：1999-11-15 00:00:00
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pub_type： 杂志文章
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更新日期：2002-03-20 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119080
更新日期：2020-03-15 00:00:00
abstract：:We prepared an injectable depot system for the long-term delivery of alendronate using a solid/water/oil/water multiple emulsion technique with poly(lactic-co-glycolic acid) as a carrier. The microparticles were spherical with smooth surfaces, ranging from 20 to 70 μm in size. The microspheres (ALD-HA-RG504H-MC70) wer...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.01.020
更新日期：2015-03-01 00:00:00
