Delivery of salmon calcitonin using a microneedle patch.
Delivery of salmon calcitonin using a microneedle patch.
复制标题
使用微针斑块递送鲑鱼降钙素。
DOI：
10.1016/j.ijpharm.2011.11.046
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发表时间：
2012-02-28
影响因子：
5.8
通讯作者：
Prausnitz, Mark R.
中科院分区：
文献类型：
--
作者：
Tas, Cetin;Mansoor, Saffar;Kalluri, Haripriya;Zarnitsyn, Vladimir G.;Choi, Seong-O;Banga, Ajay K.;Prausnitz, Mark R.
肽和多肽具有重要的药理学性质，但由于与其递送相关的问题，仅有限数量的肽和多肽被用作治疗剂。这些药物中的大多数需要肠胃外递送系统，这引入了疼痛、可能的感染和进行注射所需的专业知识的问题。本研究的目的是开发一种含有微针（MN）的透皮贴剂，微针涂有肽类药物鲑鱼降钙素（sCT），作为传统皮下和鼻腔给药途径的替代方案。使用经验证的HPLC方法对微针上的涂层和干燥后的sCT进行定量分析。对无毛大鼠进行体内研究，并通过ELISA测定血清sCT水平。含海藻糖制剂包衣MN的AUC值（250 ± 83 ng/mL.min）与皮下注射（403 ± 253 ng/mL.min）相比无显著差异，但比鼻腔给药（18.4 ± 14.5 ng/mL.min）高约13倍。MN介导给药的Tmax（7.5 ± 5 min）值比皮下注射（15 min）短50%，可能是由于sCT快速溶解和被真皮毛细血管吸收。这些结果表明，随着涂层制剂的进一步优化，微针可以使sCT和其他肽的施用成为可能，而不需要皮下注射。
Peptides and polypeptides have important pharmacological properties but only a limited number have been exploited as therapeutics because of problems related to their delivery. Most of these drugs require a parenteral delivery system which introduces the problems of pain, possible infection, and expertise required to carry out an injection. The aim of this study was to develop a transdermal patch containing microneedles (MNs) coated with a peptide drug, salmon calcitonin (sCT), as an alternative to traditional subcutaneous and nasal delivery routes. Quantitative analysis of sCT after coating and drying onto microneedles was performed with a validated HPLC method. In vivo studies were carried out on hairless rats and serum levels of sCT were determined by ELISA. The AUC value of MNs coated with a trehalose-containing formulation (250 ± 83 ng/mL.min) was not significantly different as compared to subcutaneous injections (403 ± 253 ng/mL.min), but approximately 13 times higher than nasal administration (18.4 ± 14.5 ng/mL.min). Tmax (7.5 ± 5 min) values for MN mediated administration were 50% shorter than subcutaneous injections (15 min), possibly due to rapid sCT dissolution and absorption by dermal capillaries. These results suggest that with further optimization of coating formulations, microneedles may enable administration of sCT and other peptides without the need for hypodermic injections.
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DOI：
10.1086/649228
发表时间：
2010-01-15
期刊：
The Journal of infectious diseases
影响因子：
--
作者：
Kim YC;Quan FS;Yoo DG;Compans RW;Kang SM;Prausnitz MR
通讯作者：
Prausnitz MR
影响因子：
8.8
作者：
Lammert, AM;Schmidt, SJ;Day, GA
通讯作者：
Day, GA
影响因子：
3.7
作者：
Daddona, Peter E.;Matriano, James. A.;Maa, Yuh-Fun
通讯作者：
Maa, Yuh-Fun
影响因子：
3.7
作者：
Fernando GJ;Chen X;Prow TW;Crichton ML;Fairmaid EJ;Roberts MS;Frazer IH;Brown LE;Kendall MA
通讯作者：
Kendall MA
影响因子：
10.8
作者：
Cormier, M;Johnson, B;Daddona, P
通讯作者：
Daddona, P