Enhanced rectal absorption of insulin-loaded Pluronic® F-127 gels containing unsaturated fatty acids
Enhanced rectal absorption of insulin-loaded Pluronic® F-127 gels containing unsaturated fatty acids
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DOI：
10.1016/s0378-5173(99)00090-3
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发表时间：
1999-06-25
影响因子：
5.8
通讯作者：
Nagai, T
中科院分区：
文献类型：
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作者：
Barichello, JM;Morishita, M;Nagai, T
本研究的目的是制备并评估含有油酸 (18:1)、二十碳五烯酸 (20:5) 和二十二碳六烯酸 (22:6) 等不饱和脂肪酸的 Pluronic F-127 (PF127) 凝胶作为直肠胰岛素输送的潜在制剂。在正常大鼠中直肠施用各种制剂后检查胰岛素的降血糖作用。所有含有不同不饱和脂肪酸的PF127凝胶（胰岛素剂量，5U/kg）均显着增强直肠胰岛素吸收，并引起显着的低血糖。含有不饱和脂肪酸的 PF127 凝胶呈现出较低的 t(max) 平均值，表明直肠中胰岛素的吸收发生得非常快。含有油酸、二十碳五烯酸 (EPA) 和二十二碳六烯酸 (DHA) 等脂肪酸的 PF127 凝胶制剂的相对降血糖功效分别为 28.4 +/- 8.1、26.8 +/- 14.3 和 23.1 +/- 5.7%。该发现表明，含有不饱和脂肪酸的 20% PF127 凝胶是直肠胰岛素输送的潜在制剂。 (C) 1999 Elsevier Science B.V. 保留所有权利。
The objective of this study was to prepare and to evaluate Pluronic F-127 (PF127) gel containing unsaturated fatty acids such as oleic acid (18:1), eicosapentaenoic acid (20:5) and docosahexaenoic acid (22:6) as a potential formulation for rectal delivery of insulin. The hypoglycemic effect of insulin was examined following rectal administration of the various formulations in normal rats. Rectal insulin absorption was markedly enhanced, and marked hypoglycemia was induced by all PF127 gels (insulin dose, 5 U/kg) containing different unsaturated fatty acids. PF127 gels containing unsaturated fatty acids presented low t(max) mean values indicating that the absorption of insulin occurred very rapidly in the rectum. The relative hypoglycemic efficacy of PF127 gel formulations containing fatty acids such as oleic acid, eicosapentaenoic (EPA) and docosahexaenoic (DHA) were 28.4 +/- 8.1, 26.8 +/- 14.3 and 23.1 +/- 5.7%, respectively. The finding demonstrated that 20% PF127 gels containing unsaturated fatty acids are potential formulations for rectal delivery of insulin. (C) 1999 Elsevier Science B.V. All rights reserved.