Effects of microneedle-roller insertion times on skin permeation characteristics,drug distribution and skin irritation

ZHANG Juanjuan; FU Xiang; ZHU Quangang; ZHANG Lichao

doi:10.3969/j.issn.1006-0111.2019.05.006

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Objective To study the effects of microneedle-roller insertion times on skin permeation. Methods Tretinoin was used as model drug.The in vitro transdermal characteristics in nude mice were studied with Franz diffusion cell and the tissue homogenization method.The drug distribution in nude mice skin was investigated by methylene blue staining and confocal lasers scanning microscope.The skin irritation was evaluated by trans-epidermal water-loss (TEWL) measurement and laser Doppler flowmetry. Results Within the microneedle roller insertion times 1,3,5,8,and 10,the better penetration effect and drug accumulation in skin were achieved with the increment of insertion times.However,there was no significant difference in the skin accumulation between 8 and 10 times of the insertion(P>0.05).The results from methylene blue staining and microscope confocal lasers scanning indicated that the uniformity of needle hole distribution was increased with the increased insertion times.However,some needle hole overlap and skin damages were observed from methylene blue staining when insertion times were more than five.The in vivo drug absorption study indicated that the drug accumulation was inhomogeneous in nude mice skin after one treatment.It was significantly improved after three treatments.The results from TEWL measurements suggested that the recovery time of skin barrier function was 24 hours if insertion was less than five times and 36 hours if more than eight times.The results of laser Doppler flowmetry indicated that the recovery time of skin barrier function was 1 hour if insertion times were less than five,and 2 hours if more than eight times. Conclusion The optimal microneedle insertion time was five times,which could ensure the safety and effectiveness of the skin permeation study in nude mice.

Effects of microneedle-roller insertion times on skin permeation characteristics,drug distribution and skin irritation

1. Department of Pharmacy, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai 200071, China;Department of Pharmacy, Shanghai Pudong New District Xinchang Community Health Service Center, Shanghai 201314, China

2. Department of Pharmacy, Shanghai KongJiang Hospital, Shanghai 200093, China

3. Department of Pharmacy, Shanghai Dermatology Hospital, Shanghai 200443, China

4. Department of Pharmacy, Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai 200071, China

Received Date: 2019-03-03

Rev Recd Date: 2019-04-28

Key words:

Abstract: Objective To study the effects of microneedle-roller insertion times on skin permeation. Methods Tretinoin was used as model drug.The in vitro transdermal characteristics in nude mice were studied with Franz diffusion cell and the tissue homogenization method.The drug distribution in nude mice skin was investigated by methylene blue staining and confocal lasers scanning microscope.The skin irritation was evaluated by trans-epidermal water-loss (TEWL) measurement and laser Doppler flowmetry. Results Within the microneedle roller insertion times 1,3,5,8,and 10,the better penetration effect and drug accumulation in skin were achieved with the increment of insertion times.However,there was no significant difference in the skin accumulation between 8 and 10 times of the insertion(P>0.05).The results from methylene blue staining and microscope confocal lasers scanning indicated that the uniformity of needle hole distribution was increased with the increased insertion times.However,some needle hole overlap and skin damages were observed from methylene blue staining when insertion times were more than five.The in vivo drug absorption study indicated that the drug accumulation was inhomogeneous in nude mice skin after one treatment.It was significantly improved after three treatments.The results from TEWL measurements suggested that the recovery time of skin barrier function was 24 hours if insertion was less than five times and 36 hours if more than eight times.The results of laser Doppler flowmetry indicated that the recovery time of skin barrier function was 1 hour if insertion times were less than five,and 2 hours if more than eight times. Conclusion The optimal microneedle insertion time was five times,which could ensure the safety and effectiveness of the skin permeation study in nude mice.

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Reference (11)

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Effects of microneedle-roller insertion times on skin permeation characteristics,drug distribution and skin irritation

doi: 10.3969/j.issn.1006-0111.2019.05.006

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