Abstract��Transdermal drug delivery offers a number of advantages including improved patient compliance, sustained release, avoidance of gastric irritation, as well as elimination of pre-systemic first-pass effect. However, the skin barrier function limits the transdermal penetration of macromolecular drugs.Microneedle arrays can remarkably increase the skin permeability for drugs, especially macromolecular drugs, by forming microchannels in the skin. In recent years, the types and usages of microneedle have made great progress. This review focuses on remarking the wound repair and pharmacology evaluation, as well as introduces the microneedle percutaneous drug delivery system.
ARORA A, PRAUSNITZ M R, MITRAGOTRI S. Micro-scale devices for transdermal drug delivery[J]. Int J Pharm, 2008,364(2):227-236.
TUAN-MAHMOOD T M, MCCRUDDEN M T, TORRISI B M, et al. Microneedles for intradermal and transdermal drug delivery[J]. Eur J Pharm Sci, 2013,50(5):623-637.
BAL S M, DING Z, VAN RIET E, et al. Advances in transcutaneous vaccine delivery: do all ways lead to Rome?[J]. J Controlled Release, 2010,148(3):266-282.
HARDING C R. The stratum corneum: structure and function in health and disease[J]. Dermatologic Therapy, 2004,17(suppl 1):6-15.
MAIBACH H. Dermatological formulations: percutaneous absorption[J]. J Pharm Sci, 1984,73(4):573.
TAGAMI H, KOBAYASHI H, ZHEN X S, et al. Environmental effects on the functions of the stratum corneum[J]. J Invest Dermatol Symposium Proc, 2001,6(1):87-94.
MOORE T L, LUNT M, MCMANUS B, et al. Seventeen-point dermal ultrasound scoring system--a reliable measure of skin thickness in patients with systemic sclerosis[J]. Rheumatology, 2003,42(12):1559-1563.
ZHANG X J, HE C D, LU H G. Dermatovenereology(Ƥ���Բ�ѧ)[M]. Vol 7. Beijing: People's Medical Publishing House,2008:5.
CHEN J, CHEN Z P, QU M M. Application of microneedles in transdermal drug delivery[J]. Int J Pharm Res(����ҩѧ�о���־), 2011,38(2):142-147.
WIECHERS J W. The barrier function of the skin in relation to percutaneous absorption of drugs[J]. Pharm Weekblad Sci Ed, 1989,11(6):185-198.
EL-DOMYATI M, BARAKAT M, AWAD S, et al. Multiple microneedling sessions for minimally invasive facial rejuvenation: an objective assessment[J]. Int J Dermatol, 2015,54(12):1361-1369.
LI W Z, ZHANG H, HAN W X, et al. Study on the safety of solid microneedles for transdermal drug delivery[J]. Chin Pharm J(�й�ҩѧ��־), 2011,46(23):1818-1822.
BOS J D, MEINARDI M M. The 500 dalton rule for the skin penetration of chemical compounds and drugs[J]. Exper Dermatol, 2000,9(3):165-169.
HARVEY A J, KAESTNER S A, SUTTER D E, et al. Microneedle-based intradermal delivery enables rapid lymphatic uptake and distribution of protein drugs[J]. Pharm Res, 2011,28(1):107-116.
LIU S, JIN M N, QUAN Y S, et al. The development and characteristics of novel microneedle arrays fabricated from hyaluronic acid, and their application in the transdermal delivery of insulin[J]. J Controlled Release, 2012,161(3):933-941.
CHEN M C, LING M H, KUSUMA S J. Poly-gamma-glutamic acid microneedles with a supporting structure design as a potential tool for transdermal delivery of insulin[J]. Acta Biomater, 2015,24(15):106-116.
KIM M C, LEE J W, CHOI H J, et al. Microneedle patch delivery to the skin of virus-like particles containing heterologous M2e extracellular domains of influenza virus induces broad heterosubtypic cross-protection[J]. J Controlled Release, 2015,210(1):208-216.
HIROBE S, AZUKIZAWA H, HANAFUSA T, et al. Clinical study and stability assessment of a novel transcutaneous influenza vaccination using a dissolving microneedle patch[J]. Biomaterials, 2015,57(22):50-58.
DAUGIMONT L, BARON N, VANDERMEULEN G, et al. Hollow microneedle arrays for intradermal drug delivery and DNA electroporation[J]. J Membrane Biol, 2010,236(1):117-125.
DENG Y, CHEN J, ZHAO Y, et al. Transdermal delivery of siRNA through microneedle array[J]. Scientific Reports, 2016,6(1):21422.
YAN G, WARNER K S, ZHANG J, et al. Evaluation needle length and density of microneedle arrays in the pretreatment of skin for transdermal drug delivery[J]. Int J Pharm, 2010,391(1-2):7-12.
MILEWSKI M, PAUDEL K S, BROGDEN N K, et al. Microneedle-assisted percutaneous delivery of naltrexone hydrochloride in yucatan minipig: in vitro-in vivo correlation[J]. Molecular Pharm, 2013,10(10):3745-3757.
VERBAAN F J, BAL S M, VAN DEN BERG D J, et al. Assembled microneedle arrays enhance the transport of compounds varying over a large range of molecular weight across human dermatomed skin[J]. J Controlled Release, 2007,117(2):238-245.
HAQ M I, SMITH E, JOHN D N, et al. Clinical administration of microneedles: skin puncture, pain and sensation[J]. Biomed Microdevices, 2009,11(1):35-47.
KALLURI H, KOLLI C S, BANGA A K. Characterization of microchannels created by metal microneedles: formation and closure[J]. The AAPS J, 2011,13(3):473-481.
NAGUIB Y W, KUMAR A, CUI Z. The effect of microneedles on the skin permeability and antitumor activity of topical 5-fluorouracil[J]. Acta Pharm Sin B(ҩѧѧ��B), 2014,4(1):94-99.
WERMELING D P, BANKS S L, HUDSON D A, et al. Microneedles permit transdermal delivery of a skin-impermeant medication to humans[J]. Proc Nati Acad Sci, 2008,105(6):2058-2063.
BANKS S L, PAUDEL K S, BROGDEN N K, et al. Diclofenac enables prolonged delivery of naltrexone through microneedle-treated skin[J]. Pharm Res, 2011,28(5):1211-1219.
KUSAMORI K, KATSUMI H, SAKAI R, et al. Development of a drug-coated microneedle array and its application for transdermal delivery of interferon alpha[J]. Biofabrication, 2016,8(1):015006.
GUPTA J, PARK S S, BONDY B, et al. Infusion pressure and pain during microneedle injection into skin of human subjects[J]. Biomaterials, 2011,32(28):6823-6831.
GRISS P, STEMME G. Side-opened out-of-plane microneedles for microfluidic transdermal liquid transfer[J]. J Microelectromechanical Sys, 2003,12(3):296-301.
WANG P M, CORNWELL M, HILL J, et al. Precise microinjection into skin using hollow microneedles[J]. J Invest Dermatol, 2006,126(5):1080-1087.
KALLURI H, BANGA A K. Formation and closure of microchannels in skin following microporation[J]. Pharm Res, 2011,28(1):82-94.
KATSUMI H, LIU S, TANAKA Y, et al. Development of a novel self-dissolving microneedle array of alendronate, a nitrogen-containing bisphosphonate: evaluation of transdermal absorption, safety, and pharmacological effects after application in rats[J]. J Pharm Sci, 2012,101(9):3230-3238.
DANGOL M, YANG H, LI C G, et al. Innovative polymeric system (IPS) for solvent-free lipophilic drug transdermal delivery via dissolving microneedles[J]. J Controlled Release, 2016,223(1):118-125.