Reformulating cyclosporine A (CsA): More than just a life cycle management strategy

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• 作者：Melissa Guada^a ; ^b ; ¹ ; Ana Beloqui^c ; ¹ ; M.N.V. Ravi Kumar^d ; Vé ; ronique Pré ; at^c ; Maria del Carmen Dios-Vié ; itez^a ; ^b ; Maria J. Blanco-Prieto^a ; ^b ; ^{mjblanco@unav.es" class="auth_mail" title="E-mail the corresponding author}
• 关键词：ASC ; adipose-derived stem cells ; AUC ; area under the curve ; Capmul MCM ; medium chain mono- and diglycerides ; Compritol® ; 888 ; glyceryl behenate ; Cremophor® ; EL ; ethoxylated castor oil ; Cremophor® ; RH ; polyoxyl 40 hydrogenated castor oil ; CsA ; cyclosporine A ; Cys-PEG-SA ; Thiolated polyethylene glicol monostearate ; DCM ; dichloromethane ; DCs ; dendritic cells ; DMAB ; N ; N-didodecyl-N ; N-dimethylammonium ; DSS ; dextran sodium sulfate ; Dynasan 110 ; tricaprin ; Dynasan 114 ; trimyristin ; Dynasan 116
• 刊名：Journal of Controlled Release
• 出版年：2016
• 出版时间：10 March 2016
• 年：2016
• 卷：225
• 期：Complete
• 页码：269-282
• 全文大小：970 K

文摘

Cyclosporine A (CsA) is a well-known immunosuppressive agent that gained considerable importance in transplant medicine in the late 1970s due to its selective and reversible inhibition of T-lymphocytes. While CsA has been widely used to prevent graft rejection in patients undergoing organ transplant it was also used to treat several systemic and local autoimmune disorders. Currently, the neuro- and cardio-protective effects of CsA (CiCloMulsion®; NeuroSTAT®) are being tested in phase II and III trials respectively and NeuroSTAT® received orphan drug status from US FDA and Europe in 2010. The reformulation strategies focused on developing Cremophor® EL free formulations and address variable bioavailability and toxicity issues of CsA. This review is an attempt to highlight the progress made so far and the room available for further improvements to realize the maximum benefits of CsA.