Diabetes, a metabolic disorder of glucose, is a serious chronic disease and an important public health problem. Insulin is one of the hormones for modulating blood glucose level and the products of which is indispensable for most diabetes patients. Introducing microneedles (MNs) to insulin delivery is promising to pave the way for modulating glucose level noninvasively of diabetes patients, as which born to be painless, easy to handle and no need of any power supply. In this work, we review the process of insulin delivery systems (IDSs) based on MN technology in terms of two categories: drug free MNs and drug loaded MNs. Drug free MNs include solid MNs (“poke and patch”), hollow MNs (“poke and flow”) and reservoir-based swelling MNs (“poke and swell R-type”), and drug loaded MNs include coated MNs (“coat and poke”), dissolving MNs (“poke and release”) and insulin incorporated swelling MNs (“poke and swell I-type”). Majority researches of MN-based IDSs have been conducted by using hollow MNs or dissolving MNs, and almost all clinical trials for MN-based IDSs have employed hollow MNs. “Poke and patch” approach dramatically increase skin permeability compared to traditional transdermal patch, but MNs fabricated from silicon or metal may leave sharp waste in the skin and cause a safety issue. “Poke and flow” approach, similar to transitional subcutaneous (SC) injection, is capable of producing faster insulin absorption and action than SC injection but may associate with blockage, leakage and low flow rate. Coated MNs are able of retaining the activity of drug, which loaded in a solid phase, for a long time, however have been relatively less studied for insulin application as the low drug dosing. “Poke and release” approach leaves no biohazardous sharp medical waste and is capable of rapid drug release. “Poke and swell R-type” can be seen as a combination of “poke and flow” and “poke and patch” approach, while “poke and swell I-type” is an approach between “coat and poke” and “poke and release” approach. Insulin MNs are promising for painless diabetes therapeutics, and additional efforts for addressing fundamental issues including the drug loading, the PK/PD profile, the storage and the safety of insulin MNs will accelerate the clinical transformation.

糖尿病是葡萄糖的代谢紊乱，是一种严重的慢性疾病，也是重要的公共卫生问题。胰岛素是调节血糖水平的激素之一，其产品对于大多数糖尿病患者都是必不可少的。将微针（MNs）引入胰岛素输送有望为无创调节糖尿病患者的葡萄糖水平铺平道路，因为糖尿病患者天生无痛，易于操作且无需任何电源。在这项工作中，我们从以下两个方面回顾了基于MN技术的胰岛素输送系统（IDS）的过程：无药物的MN和载药的MN。无毒品的MN包括固体MN（“戳和贴”），空心MN（“戳和流”）和基于储库的溶胀MN（“戳和溶胀R型”），载有药物的MN包括带涂层的MN（“包衣”然后戳”），溶解性MN（“戳和释放”）和胰岛素掺入的肿胀MN（“戳和溶胀I型”）。基于MN的IDS的大多数研究已经通过使用空心MN或溶解性MN进行，并且几乎所有针对基于MN的IDS的临床试验都采用了空心MN。与传统的透皮贴剂相比，“戳贴”方法显着提高了皮肤的渗透性，但是由硅或金属制成的MN可能会在皮肤上留下尖锐的废料并引起安全问题。类似于过渡皮下注射（SC）的“戳流”方法比SC注射能够产生更快的胰岛素吸收和作用，但可能与阻塞，泄漏和低流速相关。包覆的MN能够长时间保持固相负载的药物的活性，然而，由于胰岛素的低剂量使用，对胰岛素的研究相对较少。“戳和释放”方法不会留下任何对生物有害的尖锐医疗废物，并且能够快速释放药物。“ P肿R型”可以看作是“ p流”和“ p肿”方法的组合，而“ I肿I型”则是介于“ coat肿”和“ and肿”之间的方法。释放”的方法。胰岛素MNs有望用于无痛性糖尿病治疗，并且为解决基本问题（包括药物负载，PK / PD曲线，胰岛素MNs的储存和安全性）而付出的额外努力将加速临床转变。“ P肿R型”可以看作是“ p流”和“ p肿”方法的组合，而“ I肿I型”则是介于“ coat肿”和“ and肿”之间的方法。释放”的方法。胰岛素MNs有望用于无痛性糖尿病治疗，并且为解决基本问题（包括药物负载，PK / PD曲线，胰岛素MNs的储存和安全性）而付出的额外努力将加速临床转变。“ P肿R型”可以看作是“ p流”和“ p肿”方法的组合，而“ I肿I型”则是介于“ coat肿”和“ and肿”之间的方法。释放”的方法。胰岛素MNs有望用于无痛性糖尿病治疗，并且为解决基本问题（包括药物负载，PK / PD曲线，胰岛素MNs的储存和安全性）而付出的额外努力将加速临床转变。