Department of Materials Engineering, Zhejiang Sci-Tech University, Hangzhou 310018, PR China.
Department of Materials Engineering, Zhejiang Sci-Tech University, Hangzhou 310018, PR China; National Engineering Laboratory for Textile Fiber Materials and Processing Technology (Zhejiang), Hangzhou 310018, PR China; Key Laboratory of Advanced Textile Materials and Manufacturing Technology (ATMT), Ministry of Education, Hangzhou 310018, PR China; Institute of Smart Fiber Materials, Zhejiang Sci-Tech University, Hangzhou 310018, PR China.
Mater Sci Eng C Mater Biol Appl. 2018 Sep 1;90:180-188. doi: 10.1016/j.msec.2018.04.055. Epub 2018 Apr 22.
Dissolving microneedles (MNs) display high efficiency, safety and painless in transdermal delivery for poorly permeable drugs. Here, a dissolving composite MNs prepared from insulin-loaded CaCO microparticles (INS-CaCO MPs) and poly(vinyl pyrrolidone) (PVP) as matrix were fabricated with two-step centrifuging and molding process to immobilize insulin in the MNs. The as-prepared INS-CaCO/PVP MNs exhibited remarkable mechanical strength and slower solubility properties when compared with pure PVP MNs. In vitro skin insertion capability was determined by staining with FITC-labeled insulin which was revealed after insertion, gradually diffusing from the puncture sites to deeper tissues. In vivo pharmacodynamic studies were then conducted to estimate the feasibility of the administration of insulin-loaded dissolving MNs on diabetic rats for glucose regulation. The relative pharmacological availability (RPA) and relative bioavailability (RBA) of insulin from MNs were 98.2 and 96.6%. Thus, this study suggests that the use of INS-CaCO/PVP MNs achieved both high efficiency and constant release of insulin in comparison with the traditional subcutaneous injection approach and presented a promising device to delivery insulin for diabetic therapy.
溶解微针（MNs）在经皮给药中对于难渗透的药物显示出高效、安全和无痛的特点。在这里，我们通过两步离心和成型工艺制备了一种由负载胰岛素的 CaCO 微粒（INS-CaCO MPs）和聚维酮（PVP）作为基质组成的溶解复合 MNs，以将胰岛素固定在 MNs 中。与纯 PVP MNs 相比，所制备的 INS-CaCO/PVP MNs 表现出显著的机械强度和较慢的溶解度特性。通过对 FITC 标记的胰岛素进行染色来确定体外皮肤插入能力，插入后，胰岛素逐渐从穿刺部位扩散到更深的组织。然后进行体内药效学研究，以评估负载胰岛素的溶解 MNs 在糖尿病大鼠中的给药用于葡萄糖调节的可行性。胰岛素从 MNs 的相对药效学利用率（RPA）和相对生物利用度（RBA）分别为 98.2%和 96.6%。因此，与传统的皮下注射方法相比，本研究表明使用 INS-CaCO/PVP MNs 可以实现胰岛素的高效和持续释放，并为糖尿病治疗提供了一种有前途的胰岛素输送装置。
