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[1]陈健敏,蔡小真,朱丹虹,等.益母草碱可溶性微针的制备与初步研究[J].天津医科大学学报,2023,29(05):547-553.
　CHEN Jian-min,CAI Xiao-zhen,ZHU Dan-hong,et al.Preparation and preliminary study of leonurine dissolving microneedles[J].Journal of Tianjin Medical University,2023,29(05):547-553.
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益母草碱可溶性微针的制备与初步研究(PDF)
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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:
29卷
期数:
2023年05期
页码:
547-553
栏目:
药学
出版日期:
2023-09-20

文章信息/Info

Title:
Preparation and preliminary study of leonurine dissolving microneedles
文章编号:
1006-8147（2023）05-0547-07
作者:
陈健敏1; 2; 3; 蔡小真1; 2; 朱丹虹1; 2; 李金兰1; 2; 陈科元3
（1.莆田学院药学与医学技术学院，莆田 351100 ；2.药物分析与检验医学福建省高校重点实验室，莆田 351100；3.中药质量研究国家重点实验室，澳门科技大学，澳门 999078）
Author(s):
CHEN Jian-min1; 2; 3;  CAI Xiao-zhen1; 2;  ZHU Dan-hong1; 2;  LI Jin-lan1; 2; CHEN Ke-yuan3
（1.School of Pharmacy and Medical Technology， Putian University， Putian 351100， China；2.Key Laboratory of Pharmaceutical Analysis and Laboratory Medicine， Fujian Province University， Putian 351100，China；3.State Key Laboratory of Quality Research in Chinese Medicines，Macao University of Science and Technology， Macao 999078， China）
关键词:
益母草碱; 可溶性微针; 经皮给药; 皮肤吸收率
Keywords:
leonurine; dissolving microneedles; transdermal drug delivery; skin absorption rate
分类号:
R9
DOI:
-
文献标志码:
A
摘要:
目的：采用经皮给药方式而避免首过效应，研制益母草碱可溶性微针。方法：制备含益母草碱的普通可溶性微针（CDMNs)和针体载药微针（TDMNs)，测试力学强度并评价穿刺性能，研究微针的体外溶出和在模拟皮肤中的药物释放行为，进而考察微针在体内的溶解行为和经皮给药释放规律，最后对微针的皮肤安全性进行评价。结果： TDMNs和CDMNs的针形均完整饱满，并实现药物剂量和药物分布可控；每根针体承受0.14 N的压力，有足够强度刺入皮肤；CDMNs中药物的体外溶出高于TDMNs，然而在模拟皮肤中的药物释放率却低于TDMNs；微针能提高益母草碱的皮肤吸收，其中TDMNs的吸收率达到约63%，是CDMNs的2倍左右；微针作用后的皮肤在5～6 h后完全愈合，而且未发现明显的红肿现象。结论：建立了益母草碱可溶性微针给药体系，为其经皮给药制剂的研发提供理论基础和数据支撑。
Abstract:
Objective： To develop the leonurine dissolving microneedles by transdermal administration to avoid the first pass effect. Methods：Common dissolving microneedles（CDMNs) and tip loaded dissolving microneedles（TDMNs) were prepared， the mechanical strength and puncture performance were tested. And then the in vitro dissolution of microneedles and the drug release behavior in simulated skin were studied. After that， the dissolution behavior in vivo and the rule of drug release by transdermal administration of microneedles were investigated. Finally， the skin safety of microneedles was evaluated. Results：The needle shapes of TDMNs and CDMNs were complete and plump， and the drug dosage and drug distribution were controllable. Each needle body bears a pressure of 0.14 N and has enough strength to penetrate the skin. The drug dissolution rate in vitro of CDMNs was higher than that of TDMNs， but the drug release rate in simulated skin was lower than that of TDMNs. Microneedles can improve the skin absorption of leonurine， among which the absorption rate of TDMNs is about 63%， about twice that of CDMNs. The skin treated with microneedles healed completely 5-6 hours later， and no obvious redness or swelling were found. Conclusion：The dissolving microneedles drug delivery system of leonurine has been established， which provides theoretical basis and data support for the research and development of its transdermal drug delivery preparation.

参考文献/References:

[1] MIYAKE S，OGO A，KUBOTA H，et al.β-Hydroxy-β-methylbutyrate suppresses NF-?资B activation and IL-6 production in TE-1 cancer cells[J]. In Vivo，2019，33（2）：353-358.
[2] LIU X，PAN L，GONG Q，et al. Leonurine（SCM-198） improves cardiac recovery in rat during chronic infarction[J]. Eur J Pharmacol，2010，649（1/3）：236-241.
[3] GUSTAFSON D L，DUVAL D L，REGAN D P，et al. Canine sarcomas as a surrogate for the human disease[J]. Pharmacol Ther，2018， 188：80-96.
[4] LEE H，SONG C，BAIK S，et al. Device-assisted transdermal drug delivery[J]. Adv Drug Deliv Rev，2018，127：35-45.
[5] JEONG W Y，KWON M，CHOI H E，et al. Recent advances in transdermal drug delivery systems：a review[J]. Biomater Res，2021，25（1）：24.
[6] ZHOU X，HAO Y，YUAN L，et al. Nano-formulations for transdermal drug delivery：a review[J]. Chinese Chem Lett，2018，29（12）：1713-1724.
[7] 包玉胜. 透皮给药系统的研究进展[J]. 山东化工，2014，43（6）：4-7.
[8] 伍兰萼，章青青，郭倩，等. 益母草碱抑制人脑血管外膜成纤维细胞增殖并促进细胞凋亡的机制研究[J]. 河北医药，2022，44（6）：4-9.
[9] WAGHULE T，SINGHVI G，DUBEY S K，et al. Microneedles：a smart approach and increasing potential for transdermal drug delivery system[J]. Biomed Pharmacother，2019，109：1249-1258.
[10] 陈欢欢，宋信莉，汪云霞，等. 可溶性微针在经皮给药系统中的研究进展[J]. 广东化工，2021，48（16）：2-5.
[11] KIM H S，SUN X，LEE JH，et al. Advanced drug delivery systems and artificial skin grafts for skin wound healing[J]. Adv Drug DelivRev，2019，146：209-239.
[12] MOORE L E，VUCEN S，MOORE A C. Trends in drug- and vaccine-based dissolvable microneedle materials and methods of fabrication[J]. Eur J Pharm Biopharm，2022，173：54-72.
[13] KUCHTA K，ORTWEIN J，BRIEL D，et al. Leonurine in leonurus and leonotis drugs? Detection and quantitative determination by a newly developed HPLC method[J]. Planta Med，2010，76（12）：541.
[14] CHEN J，HUANG W，HUANG Z，et al. Fabrication of tip-dissolving microneedles for transdermal drug delivery of meloxicam[J]. AAPS Pharm Sci Tech，2018，19（3）：1141-1151.
[15] CHEN J，LIU X，LIU S，et al. Fabrication and characterization of dissolving microneedles for transdermal drug delivery of allopurinol[J]. Drug Dev Ind Pharm，2021，47（10）：1578-1586.
[16] CHEN J，WANG M，RAN M，et al. Fabrication and Evaluation of Glabridin Tip-loaded Dissolving Microneedles[J]. Curr Drug Deliv，2021，18（10）：1585-1594.
[17] 陈健敏，刘欣莹，刘思弯，等. 包覆涂层的可溶性微针的制备及性能测试[J]. 安徽大学学报：自然科学版，2021，45（6）：90-98.
[18] LARRA?譙ETA E，STEWART S，FALLOWS S J，et al. A facile system to evaluate in vitro drug release from dissolving microneedle arrays[J]. IntJPharm，2016，497（1/2）：62-69.
[19] ZHU D D，CHEN B Z，HE M C，et al. Structural optimization of rapidly separating microneedles for efficient drug delivery[J]. J Ind Eng Chem，2017，51：178-184.
[20] CHA K J，KIM T，PARK S J，et al. Simple and cost-effective fabrication of solid biodegradable polymer microneedle arrays with adjustable aspect ratio for transdermal drug delivery using acupuncture microneedles[J]. J Micromech Microeng，2014，24（11）：115015.
[21] 张远杏，武凤兰，李玉珍. 莫索尼定贴片的制备及体外释放、透皮吸收研究[J]. 沈阳药科大学学报，2001，18（4）：3.
[22] SUGURO R，CHEN S，YANG D，et al. Anti-hypercholesterolemic effects and a good safety profile of SCM-198 in animals：from ApoE knockout mice to rhesus monkeys[J]. Frontpharmacol，2018，9：1468.
[23] ONO A，AZUKIZAWA H，ITO S，et al. Development of novel double-decker microneedle patches for transcutaneous vaccine delivery[J]. Int J Pharm，2017，532（1）：374-383.
[24] ZHU D D，ZHANG X P，ZHANG B L，et al. Safety assessment of microneedle technology for transdermal drug delivery：a review[J].Adv Ther，2020，3（8）：2000033.
[25] LING M H，CHEN M C. Dissolving polymer microneedle patches for rapid and efficient transdermal delivery of insulin to diabetic rats[J]. Acta Biomater，2013，9（11）：8952-8961.

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备注/Memo

备注/Memo:
基金项目 国家自然科学基金资助项目（82001926）；莆田市科技局科研创新专项（2021ZP01）；大学生创新创业训练计划（S202211498003，S202211498004，S202111498016，S202111498016）
作者简介 陈健敏（1985-），男，教授，博士，研究方向：微针经皮给药研究；E-mail：chenjianmin1985@sina. com。
更新日期/Last Update: 2023-09-25