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由海藻酸钠和麦芽糖制备的微针用于糖尿病大鼠的胰岛素经皮给药。

Microneedles fabricated from alginate and maltose for transdermal delivery of insulin on diabetic rats.

机构信息

Department of Polymer Materials, Zhejiang Sci-Tech University, Hangzhou 310018, China.

Department of Polymer Materials, Zhejiang Sci-Tech University, Hangzhou 310018, China; National Engineering Laboratory for Textile Fiber Materials and Processing Technology (Zhejiang), Hangzhou 310018, China; Key Laboratory of Advanced Textile Materials and Manufacturing Technology (ATMT), Ministry of Education, Hangzhou 310018, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2018 Apr 1;85:18-26. doi: 10.1016/j.msec.2017.12.006. Epub 2017 Dec 15.

Abstract

To reduce the inconvenient and painful of subcutaneous needle injection, the calcium ion cross-linked alginate/maltose (Ca/Alg-Mal) composite microneedles have been fabricated by a template method. The as-prepared microneedles exhibited strong mechanical properties with the highest failure force around 0.41N/needle. The biological activity and stability of loaded insulin in microneedles were investigated. Due to the good mechanical properties and excellent biocompatibility, the as-prepared microneedles have been applied for transdermal delivery of insulin on diabetic Sprague-Dawley (SD) rat models in vivo. After transdermal administration to the diabetic rats, the released insulin from biodegradable composite microneedles exhibit an obvious and effective hypoglycemic effect with relative pharmacological availability (RPA) and relative bioavailability (RBA) at 94.1±5.6% and 93.7±4.7% compared with that of subcutaneous injection route. This work suggests that as-prepared Ca/Alg-Mal microneedles can be used to encapsulate insulin and have a potential application in diabetes treatment via transdermal ingestion.

摘要

为了减少皮下注射带来的不便和痛苦,采用模板法制备了钙离子交联海藻酸盐/麦芽糖(Ca/Alg-Mal)复合微针。所制备的微针具有较强的机械性能,最高失效力约为 0.41N/针。研究了载胰岛素微针的生物活性和稳定性。由于良好的机械性能和优异的生物相容性,所制备的微针已应用于糖尿病 Sprague-Dawley(SD)大鼠模型的胰岛素经皮给药。经皮给予糖尿病大鼠后,可从可生物降解的复合微针中释放出具有明显和有效降血糖作用的胰岛素,其相对药效学(RPA)和相对生物利用度(RBA)分别为 94.1±5.6%和 93.7±4.7%,与皮下注射途径相当。这项工作表明,所制备的 Ca/Alg-Mal 微针可用于封装胰岛素,并有可能通过经皮摄入用于糖尿病治疗。

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