Abstract：
:The objective was to quantify drug loss due to cold flow (CF) in marketed estradiol transdermal drug delivery systems (TDDS), and study its influence on the in vitro flux and drug transfer across contacting skin. TDDS samples (products-A and B) were induced with CF at 25 and 32°C/60% RH by applying 1-kg force for 72h. CF was measured as percent dimensional change and amount of drug loss/migration in CF region. In vitro drug permeation studies were conducted across human epidermis from TDDS excluding CF region, and CF region alone against control (without CF). In both products, significantly higher percentage of CF (dimensional change and drug migration) was observed at 32°C compared to 25°C. In vitro flux from both products excluding CF region either at 25 or 32°C was the same, but significantly lower compared to control. Drug transferred from CF region of product-A after 8h was the same at 25 and 32°C, but significantly higher in product-B. Flux from both products together with CF region at 32°C was significantly lower than that observed at 25°C. Results showed that excessive CF at storage (25°C) and clinical usage (32°C) conditions may have implications on product performance and safety of estradiol TDDS.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Krishnaiah YS,Yang Y,Hunt RL,Khan MAdoi
10.1016/j.ijpharm.2014.10.013subject
Has Abstractpub_date
2014-12-30 00:00:00pages
73-80issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(14)00736-4journal_volume
477pub_type
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