防脱生发活性物共输送纳米脂质体的制备及功效评价

doi:10.3969/j.issn.1001-1803.2020.06.007

日用化学工业 ›› 2020, Vol. 50 ›› Issue (6): 396-401.doi: 10.3969/j.issn.1001-1803.2020.06.007

防脱生发活性物共输送纳米脂质体的制备及功效评价

王志鹏¹,沈慧慧²,罗丹²,陈丹²,盛剑勇^1,³,刘卫^1,³()

^1. 华中科技大学生命科学与技术学院,湖北武汉 430074
^2. 武汉百思凯瑞生物科技有限公司,湖北武汉 430075
^3. 华中科技大学国家纳米药物工程技术研究中心,湖北武汉 430075

收稿日期:2019-10-24 修回日期:2020-05-27 出版日期:2020-06-22 发布日期:2020-06-22
通讯作者: 刘卫
作者简介:王志鹏（1994-）,男,山西太原人,硕士研究生,电话：18552862305,E-mail：brockwangno1@163.com。

Preparation and efficacy evaluation of nanoliposomes for co-delivery of anti-alopecia agents

WANG Zhi-peng¹,SHEN Hui-hui²,LUO Dan²,CHEN Dan²,SHENG Jian-yong^1,³,LIU Wei^1,³()

^1. College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, Hubei 430074, China
^2. Wuhan Bestcarrier Biotechnology Co., Ltd., Wuhan, Hubei 430075, China
^3. National Engineering Research Center for Nanomedicine, Huazhong University of Science and Technology, Wuhan, Hubei 430075, China

Received:2019-10-24 Revised:2020-05-27 Online:2020-06-22 Published:2020-06-22
Contact: Wei LIU

摘要/Abstract

摘要：

采用高压均质技术制备了载有二氨基嘧啶氧化物（Kopexil）和吡咯烷基二氨基嘧啶氧化物（Kopyrrol）这两种防脱生发活性物的共输送纳米脂质体（Kopexil/Kopyrrol-LPs）,其平均粒径为（81.2±1.3） nm,多分散系数PDI为0.104±0.006,Zeta电位为（-15.6±0.6） mV。纳米脂质体中Kopexil的载药量和包封率分别为22.1%和93.8%,Kopyrrol的载药量和包封率分别为11.0%和94.6%。采用Franz扩散池法研究Kopexil/Kopyrrol-LPs的体外释放和透皮特性,结果表明,纳米脂质体中Kopexil和Kopyrrol呈明显的缓释行为,其Kopexil的皮肤累积渗透量和滞留量分别为95.66和7.23 μg/cm ²,Kopyrrol的皮肤累积渗透量和滞留量分别为40.48和6.07 μg/cm ²。Kopexil/Kopyrrol-LPs中Kopexil和Kopyrrol的24 h皮肤滞留量分别较游离活性物提升约1.8和2.2倍。比较连续给药21天后雄激素脱发模型小鼠背部毛发生长情况以及皮肤组织切片,结果显示Kopexil/Kopyrrol-LPs组小鼠生发速度以及毛囊数量均显著高于游离活性物组。

关键词: 防脱生发, 共输送, 纳米脂质体, 雄激素脱发, 功效评价

Abstract:

The co-delivery nanoliposomes （Kopexil/Kopyrrol-LPs） containing two kinds of anti-alopecia agents （Kopexil and Kopyrrol） were prepared by high pressure homogenization technology. The mean particle size of the Kopexil/Kopyrrol-LPs was （81.2±1.3） nm, the PDI was 0.104±0.006, and the Zeta potential was （-15.6±0.6） mV. The drug loading efficiency and encapsulation efficiency of Kopexil in the nanoliposomes were 22.1% and 93.8%, respectively, and those of Kopyrrol were 11.0% and 94.6%, respectively. The in vitro release profiles and transdermal efficiency of the two agents in the Kopexil/Kopyrrol-LPs were studied by Franz diffusion cell method. Sustained release of the two agents from the Kopexil/Kopyrrol-LPs were demonstrated. The cumulative skin penetration and retention of Kopexil were 95.66 and 7.23 μg/cm ², respectively, and those of Kopyrrol were 40.48 and 6.07 μg/cm ², respectively. The 24 h skin retentions of Kopexil and Kopyrrol in Kopexil/Kopyrrol-LPs were approximately 1.8 and 2.2 times higher than that of free active agents, respectively. After 21 days of continuous administration of the Kopexil/Kopyrrol-LPs in the back skin of androgenetic alopecia murine models, the speed of hair growth and the number of hair follicles in the Kopexil/Kopyrrol-LPs group were significantly higher than those in the free active agents group, based on the hair growth and tissue section of the treated skin.

Key words: anti-alopecia, co-delivery, nanoliposomes, androgenetic alopecia, efficacy evaluation

中图分类号:

TQ658

王志鹏,沈慧慧,罗丹,陈丹,盛剑勇,刘卫. 防脱生发活性物共输送纳米脂质体的制备及功效评价[J]. 日用化学工业, 2020, 50(6): 396-401.

WANG Zhi-peng,SHEN Hui-hui,LUO Dan,CHEN Dan,SHENG Jian-yong,LIU Wei. Preparation and efficacy evaluation of nanoliposomes for co-delivery of anti-alopecia agents[J]. China Surfactant Detergent & Cosmetics, 2020, 50(6): 396-401.

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参考文献 15

[1]	An Jingying, Lv Xinxiang, Zhuo Na. Advances in the pathogenesis of androgenetic alopecia[J]. World Latest Medicine Information, 2018,18(68) : 52-53.
[2]	Bazzano G S. Substituted pyrimidine oxides useful for hair growth: EP0187854A1 [P]. 1986-07-23.
[3]	Bazzano G S. N, N-substituted amines and use thereof in hair growth promotion: US5137888A [P]. 1992-08-11.
[4]	Harisha S, Kiran V, Ranganathan K R, et al. Clinical trials of water based composition of active hair growth stimulants in the treatment of alopecia[J]. European Journal of Biomedical and Pharmaceutical Sciences, 2014,1(3) : 284-305.
[5]	Mahe Y F, Buan B, Bernard B A, et al. A minoxidil-related compound lacking a C6 substitution still exhibits strong anti-lysyl hydroxylase activity in vitro[J]. Skin Pharmacology and Physiology, 2009,9(3) : 177-183.
[6]	Shu Chentan, Xia Qin, Xue Jin, et al. Liposomes as vehicles for lutein: preparation, stability, liposomal membrane dynamics, and structure[J]. Journal of Agricultural and Food Chemistry, 2013,61(34) : 8175-8184.
[7]	Qi Rong, He Ruirui, Li Boyu, et al. Advances in transdermal drug delivery system[J]. Journal of External Therapy of TCM, 2007 (1) : 3-6.
[8]	Fakhravar Z, Ebrahimnejad P, Daraee H, et al. Nanoliposomes: synjournal methods and applications in cosmetics[J]. Journal of Cosmetic and Laser Therapy, 2015,18(3) : 1-31. doi: 10.3109/14764172.2016.1151264
[9]	Chen Dan, Shi Congjiao, Xu Qi, et al. Research progress on nanocarriers of skin functional ingredients[J]. Herald of Medicine, 2018,320(6) : 40-45.
[10]	Shen Huihui, Wen Qing, Guo Saihong, et al. Preparation and efficacy evaluation of pleiotropic moisturizing co-delivery nanoemulsion[J]. Detergent & Cosmetics, 2019,42(4) : 41-45.
[11]	Rouzi B, Tosi G, Forni F, et al. Ketorolac tromethamine liposomes: encapsulation and release studies[J]. Liposome Res., 2005,15:175-185.
[12]	Rahman H S, Rasedee A, How C W, et al. Zerumbone-loaded nanostructured lipid carriers: preparation, characterization, and antileukemic effect[J]. International Journal of Nanomedicine, 2013: 2969-2781.
[13]	Gao Heyi, Huang Jiancong, Lei Dengfeng, et al. Study on preperation and efficacy evaluation of herbal compound material for promoting hair growth[J]. China Surfactant Detergent & Cosmetics, 2018 (9) : 521-526.
[14]	Zhang L. The study of isatis indigotica fort treat animal model of androgenetic alopecia[D]. Lanzhou: Lanzhou University, 2016.
[15]	Bernárdez C, Molina-Ruiz A M, Requena L. Histologic features of alopecias-part I: nonscarring alopecias[J]. Actas Dermo-Sifiliográficas (English Edition) , 2015,106(3) : 158-167.

组别	t₁/d	t₂/d
Kopexil/Kopyrrol	11.75±3.30	6.00±1.41
Kopexil/Kopyrrol-LPs	8.00±1.41^*	4.00±1.15

组别	真皮厚度/μm	毛囊总数/个
正常组	364.7±23.3	95.6±14.0
Model	272.3± 6.7	21.3±14.3
Blank-LPs	276.7± 6.4	25.4± 4.0
Kopexil/Kopyrrol	278.5± 6.0	93.7±13.3^*
Kopexil/Kopyrrol-LPs	285.4±12.8	119.4±24.7^*Δ

防脱生发活性物共输送纳米脂质体的制备及功效评价

Preparation and efficacy evaluation of nanoliposomes for co-delivery of anti-alopecia agents

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