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

Abstract

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

CLC Number:

TQ658

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.

Figures/Tables 7

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References 15

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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

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

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