Elevating Bioavailability of Cyclosporine A via Encapsulation in Artificial Oil Bodies Stabilized by Caleosin

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• 作者：Miles C. M. Chen ; Jui-Ling Wang ; and Jason T. C. Tzen
• 刊名：Biotechnology Progress
• 出版年：2005
• 出版时间：August 2005
• 年：2005
• 卷：21
• 期：4
• 页码：1297 - 1301
• 全文大小：296K
• 年卷期：v.21,no.4(August 2005)
• ISSN：1520-6033

文摘

To elevate its bioavailability via oral administration, cyclosporine A (CsA), ahydrophobic drug, was either incorporated into olive oil directly or encapsulated inartificial oil bodies (AOBs) constituted with olive oil and phospholipid in the presenceor absence of recombinant caleosin purified from Escherichia coli. The bioavailabilitiesof CsA in these formulations were assessed in Wistar rats in comparison with thecommercial formulation, Sandimmun Neoral. Among these tests, CsA-loaded AOBsstabilized by the recombinant caleosin exhibited better bioavailability than thecommercial formulation and possessed the highest maximum whole blood concentration(C_max), 1247.4 ± 106.8 ng/mL, in the experimental animals 4.3 ± 0.7 h (t_max) after oraladministration. C_max and the area under the plasma concentration-time curve(AUC_0-24) were individually increased by 50.8% and 71.3% in the rats fed with caleosin-stabilized AOBs when compared with those fed with the reference Sandimmun Neoral.The results suggest that constitution of AOBs stabilized by caleosin may be a suitabletechnique to encapsulate hydrophobic drugs for oral administration.