Rapidly Dissolvable Microneedle Patches for Transdermal Delivery of Exenatide
详细信息 查看全文
- 作者：Zhuangzhi Zhu (1)
Huafei Luo (1)
Wangding Lu (1)
Hansen Luan (1)
Yubo Wu (1)
Jing Luo (1)
Youjie Wang (2)
Jiaxin Pi (1)
Chee Yen Lim (3)
Hao Wang (1) - 关键词：dissolving microneedles ; exenatide ; pharmacokinetics/pharmacodynamics ; transdermal delivery ; type 2 diabetes mellitus
- 刊名：Pharmaceutical Research
- 出版年：2014
- 出版时间：December 2014
- 年：2014
- 卷：31
- 期：12
- 页码：3348-3360
- 全文大小：1,300 KB
- 参考文献：1. DeFronzo RA. From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus. Diabetes. 2009;58(4):773-5. CrossRef
2. Association AD. Diagnosis and classification of diabetes mellitus. Diabetes Care. 2008;31(Supplement 1):S55-S60.
3. Eng J, Kleinman WA, Singh L, Singh G, Raufman JP. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Further evidence for an exendin receptor on dispersed acini from guinea pig pancreas. J Biol Chem. 1992;267(11):7402-.
4. Nielsen LL, Young AA, Parkes DG. Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes. Regul Peptides. 2004;117(2):77-8. CrossRef
5. Cai Y, Wei L, Ma L, Huang X, Tao A, Liu Z, / et al. Long-acting preparations of exenatide. Drug Des Dev Ther. 2013;7:963-0.
6. Gedulin BR, Smith PA, Jodka CM, Chen K, Bhavsar S, Nielsen LL, / et al. Pharmacokinetics and pharmacodynamics of exenatide following alternate routes of administration. Int J Pharm. 2008;356(1-):231-. CrossRef
7. Ahn S, Lee I-H, Lee E, Kim H, Kim Y-C, Jon S. Oral delivery of an anti-diabetic peptide drug via conjugation and complexation with low molecular weight chitosan. J Control Release. 2013;170(2):226-2. CrossRef
8. Nguyen H-N, Wey S-P, Juang J-H, Sonaje K, Ho Y-C, Chuang E-Y, / et al. The glucose-lowering potential of exendin-4 orally delivered via a pH-sensitive nanoparticle vehicle and effects on subsequent insulin secretion / in vivo. Biomaterials. 2011;32(10):2673-2. CrossRef
9. Lee J, Lee C, Kim TH, Lee ES, Shin BS, Chi S-C, / et al. Self-assembled glycol chitosan nanogels containing palmityl-acylated exendin-4 peptide as a long-acting anti-diabetic inhalation system. J Control Release. 2012;161(3):728-4. CrossRef
10. Lee C, Choi JS, Kim I, Oh KT, Lee ES, Park ES, / et al. Long-acting inhalable chitosan-coated poly(lactic-co-glycolic acid) nanoparticles containing hydrophobically modified exendin-4 for treating type 2 diabetes. Int J Nanomed. 2013;8:2975-3.
11. Hamman J, Enslin G, Kotzé A. Oral delivery of peptide drugs. BioDrugs. 2005;19(3):165-7. CrossRef
12. Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol. 2008;26(11):1261-. CrossRef
13. Hiraishi Y, Nakagawa T, Quan Y-S, Kamiyama F, Hirobe S, Okada N, / et al. Performance and characteristics evaluation of a sodium hyaluronate-based microneedle patch for a transcutaneous drug delivery system. Int J Pharm. 2013;441(1-):570-. CrossRef
14. Arora A, Prausnitz MR, Mitragotri S. Micro-scale devices for transdermal drug delivery. Int J Pharm. 2008;364(2):227-6. CrossRef
15. Gill HS, Denson DD, Burris BA, Prausnitz MR. Effect of microneedle design on pain in human volunteers. Clin J Pain. 2008;24(7):585-4. CrossRef
16. Kim YC, Park JH, Prausnitz MR. Microneedles for drug and vaccine delivery. Adv Drug Deliv Rev. 2012;64(14):1547-8. CrossRef
17. Van der Maaden K, Jiskoot W, Bouwstra J. Microneedle technologies for (trans) dermal drug and vaccine delivery. J Control Release. 2012;161(2):645-5. CrossRef
18. Lee JW, Park JH, Prausnitz MR. Dissolving microneedles for transdermal drug delivery. Biomaterials. 2008;29(13):2113-4. Luo (1)
Wangding Lu (1)
Hansen Luan (1)
Yubo Wu (1)
Jing Luo (1)
Youjie Wang (2)
Jiaxin Pi (1)
Chee Yen Lim (3)
Hao Wang (1)
1. National Pharmaceutical Engineering Research Center, China State Institute of Pharmaceutical Industry, 1111 Ha Lei Road, Shanghai, 201203, China
2. Engineering Research Center of Modern Preparation Technology of TCM, Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China
3. Micropoint Technologies Pte. Ltd., #02-10 CleanTech One, Singapore, 637141, Singapore - ISSN：1573-904X
文摘
Purpose To assess the feasibility of transdermal delivery of exenatide (EXT) using low-molecular-weight sodium hyaluronate (HA) dissolving microneedles (MNs) patches for type 2 diabetes mellitus therapy. Methods Micromold casting method was used to fabricate EXT-loaded dissolving MNs. The characteristics of prepared MNs including mechanical strength, in vitro/in vivo insertion capacity, dissolution profile and storage stability were then investigated. Finally, the in vivo pharmacokinetics and hypoglycemic effects were compared with traditional subcutaneous (SC) injection. Results EXT-loaded dissolving MNs made of HA possessed sufficient mechanical strength and the strength could be weakened as the water content increases. The EXT preserved its pharmacological activity during fabrication and one-month storage. With the aid of spring-operated applicator, dissolving MNs could be readily penetrated into the skin in vitro/in vivo, and then rapidly dissolved to release encapsulated drug within 2?min. Additionally, transepidermal water loss (TEWL) determinations showed that skin’s barrier properties disrupted by MNs recovered within 10-2?h. Transdermal pharmacokinetics and antidiabetic effects studies demonstrated that fabricated EXT MNs induced comparable efficacy to SC injection. Conclusions Our rapidly dissolving MNs patch appears to an excellent, painless alternative to conventional SC injection of EXT, and this minimally invasive device might also be suitable for other biotherapeutics.