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.
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: 20min). 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.
Univ. Lille, EA GRITA-7365-Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France; CHU Lille, Pharmacy Institut, F-59000 Lille, France.
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Bourdon
Univ. Lille, EA GRITA-7365-Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France.
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Lecoeur
Univ. Lille, EA GRITA-7365-Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France.
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Leconte
Univ. Lille, NMR Plateform (LARMN), UFR Pharmacie, F-59000 Lille, France.
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Ultré
Univ Lille, Mass Spectrometry Plateform of the Faculty of Pharmacy, UFR Pharmacie, F-59000 Lille, France.
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Kouach
Univ. Lille, EA GRITA-7365-Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France; CHU Lille, Pharmacy Institut, F-59000 Lille, France.
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Odou
Univ. Lille, EA GRITA-7365-Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France.
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Vaccher
Univ. Lille, EA GRITA-7365-Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France. Electronic address: catherine.foulon@univ-lille2.fr.
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Foulon
D000279:Administration, Cutaneous; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000009:adverse effects*; D000077608:Aprepitant; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003907:Dexamethasone / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D006801:Humans; D054709:Lecithins / Q000737:chemistry*; D009025:Morpholines / Q000737:chemistry; D009325:Nausea / Q000139:chemically induced / Q000188:drug therapy*; D017294:Ondansetron / Q000737:chemistry; D014677:Pharmaceutical Vehicles / Q000737:chemistry*; D013552:Swine; D014839:Vomiting / Q000139:chemically induced / Q000188:drug therapy*
D000932:Antiemetics; D000970:Antineoplastic Agents; D004337:Drug Carriers; D054709:Lecithins; D009025:Morpholines; D014677:Pharmaceutical Vehicles; D000077608:Aprepitant; D017294:Ondansetron; D003907:Dexamethasone
Aprepitant; Dexamethasone; Franz-type diffusion cell; Kinetic; Ondansetron; Transdermal vehicle