Evaluation of Pentravan^®, Pentravan^® Plus, Phytobase^®, Lipovan^® and Pluronic Lecithin Organogel for the transdermal administration of antiemetic drugs to treat chemotherapy-induced nausea and vomiting at the hospital

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• 作者：F. Bourdon^a ; ^b ; M. Lecoeur^a ; L. Leconte^a ; V. Ultré ; ^c ; M. Kouach^d ; P. Odou^a ; ^b ; C. Vaccher^a ; C. Foulon^a ; ^{catherine.foulon@univ-lille2.fr}
• 关键词：Apt ; aprepitant ; Dex ; dexamethasone ; MAPE ; mean absolute percentage error ; Ond ; ondansetron ; Pent ; Pentravan&reg ; Pent+ ; Pentravan&reg ; Plus ; Phyt ; Phytobase&reg ; Lipo ; Lipovan&reg ; PLO ; Pluronic Lecithin Organogel
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：30 December 2016
• 年：2016
• 卷：515
• 期：1-2
• 页码：774-787
• 全文大小：2939 K
• 卷排序：515

文摘

The objective of this study was to evaluate five commercial ready-to-use transdermal vehicles (Phytobase®, Lipovan®, Pentravan®, Pentravan® Plus and Pluronic Lecithin Organogel (PLO)), for the compounding of three antiemetic drugs (ondansetron, dexamethasone and aprepitant) and their administration in combination to treat chemotherapy-induced nausea and vomiting (CINV) at the hospital. Drugs were individually formulated in these vehicles and in mixture in Pentravan® Plus using different penetration enhancers. Quality control of the forms has demonstrated that formulation process was mastered and convenient for the hospital (time required: 20 min). Diffusion experiments through synthetic membranes and pig ear epidermis performed using Franz-type diffusion cells, have shown that the release and permeation process were greater for ondansetron than for dexamethasone and aprepitant, with a release step not limiting. As permeation of aprepitant was too low, it was discarded of the study. When ondansetron and dexamethasone were compounded in combination in Pentravan® Plus, the most efficient vehicle, a permeation decrease was observed. Finally, the use of tween 20 instead of EtOH as chemical enhancer has led to 2-fold factor increase in the flux of dexamethasone, resulting in fluxes convenient for transdermal administration of ondansetron to a child, but insufficient for an adult and for dexamethasone.