PMID- 32969458 OWN - NLM STAT- MEDLINE DCOM- 20210428 LR - 20210428 IS - 2050-7518 (Electronic) IS - 2050-750X (Linking) VI - 8 IP - 40 DP - 2020 Oct 21 TI - Smart microneedle patches for rapid, and painless transdermal insulin delivery. PG - 9335-9342 LID - 10.1039/d0tb01822h [doi] AB - Insulin administration at mealtimes for the control of postprandial glucose is a major part of basal-bolus insulin therapy; however, painful subcutaneous (SC) injections lead to poor patient compliance. The microneedle (MN) patch, which allows painless transdermal drug delivery, is a promising substitute; however, it remains a big challenge to deliver insulin as rapidly as by SC injection. Here a novel MN patch is designed in which the MNs are coated with insulin/poly-l-glutamic acid (PGA) layer-by-layer (LBL) films at pH 3.0. This coating is pH-sensitive because the net charge of insulin turns from positive to negative when the pH increases from 3.0 to 7.4. As a result, when transferred to pH 7.4 media, e.g., when inserted into skin, the coating dissociates instantly and releases insulin rapidly. A brief epidermal application (<1 min) of the coated MNs is enough for complete film dissociation. More importantly, the coated MN patch exhibits a pharmacokinetic and a pharmacodynamic profile comparable to that of insulin administrated by SC injection, suggesting the coated MN patch can deliver insulin as rapidly as the SC injection. In addition, the patch exhibits excellent biocompatibility and storage stability. The new MN patch is expected to become a painless, convenient method for the control of postprandial glucose. FAU - Wang, Yuanpeng AU - Wang Y AUID- ORCID: 0000-0002-2724-8765 AD - Key Laboratory of Functional Polymer Materials and State Key Laboratory of Medicinal Chemical Biology, Institute of Polymer Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China. yingguan@nankai.edu.cn yongjunzhang@nankai.edu.cn. FAU - Wang, Haozheng AU - Wang H AUID- ORCID: 0000-0001-6373-8967 AD - Key Laboratory of Functional Polymer Materials and State Key Laboratory of Medicinal Chemical Biology, Institute of Polymer Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China. yingguan@nankai.edu.cn yongjunzhang@nankai.edu.cn. FAU - Zhu, X X AU - Zhu XX AUID- ORCID: 0000-0003-0828-299X AD - Departement de Chimie, Universite de Montreal, C.P. 6128, Succ. Centre-ville, Montreal, QC H3C 3J7, Canada. FAU - Guan, Ying AU - Guan Y AUID- ORCID: 0000-0002-2950-0100 AD - Key Laboratory of Functional Polymer Materials and State Key Laboratory of Medicinal Chemical Biology, Institute of Polymer Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China. yingguan@nankai.edu.cn yongjunzhang@nankai.edu.cn. FAU - Zhang, Yongjun AU - Zhang Y AUID- ORCID: 0000-0002-1079-4137 AD - Key Laboratory of Functional Polymer Materials and State Key Laboratory of Medicinal Chemical Biology, Institute of Polymer Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China. yingguan@nankai.edu.cn yongjunzhang@nankai.edu.cn. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - J Mater Chem B JT - Journal of materials chemistry. B JID - 101598493 RN - 0 (Insulin, Regular, Human) RN - 9011-14-7 (Polymethyl Methacrylate) SB - IM MH - Administration, Cutaneous MH - Animals MH - Diabetes Mellitus, Experimental/drug therapy MH - Drug Delivery Systems/instrumentation/*methods MH - Humans MH - Insulin, Regular, Human/*administration & dosage/therapeutic use MH - Male MH - Microinjections/instrumentation/*methods MH - *Needles MH - Polymethyl Methacrylate/chemistry/toxicity MH - Rats, Sprague-Dawley MH - Skin/metabolism MH - Swine EDAT- 2020/09/25 06:00 MHDA- 2021/04/29 06:00 CRDT- 2020/09/24 08:49 PHST- 2020/09/25 06:00 [pubmed] PHST- 2021/04/29 06:00 [medline] PHST- 2020/09/24 08:49 [entrez] AID - 10.1039/d0tb01822h [doi] PST - ppublish SO - J Mater Chem B. 2020 Oct 21;8(40):9335-9342. doi: 10.1039/d0tb01822h.