Comparative Study on Transdermal Absorption of Bulleyaconitine A in Four Skin Barrier Models of Rabbits

Peipei ZHANG; Jiali CUI; Hongbin LIU; Dangzhu TANG; Yan YANG; Deguang Li

doi:10.12259/j.issn.2095-610X.S20240404

Volume 45 Issue 4

Apr. 2024

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Peipei ZHANG, Jiali CUI, Hongbin LIU, Dangzhu TANG, Yan YANG, Deguang Li. Comparative Study on Transdermal Absorption of Bulleyaconitine A in Four Skin Barrier Models of Rabbits[J]. Journal of Kunming Medical University, 2024, 45(4): 26-34. doi: 10.12259/j.issn.2095-610X.S20240404

Citation:

Peipei ZHANG, Jiali CUI, Hongbin LIU, Dangzhu TANG, Yan YANG, Deguang Li. Comparative Study on Transdermal Absorption of Bulleyaconitine A in Four Skin Barrier Models of Rabbits[J]. Journal of Kunming Medical University, 2024, 45(4): 26-34. doi: 10.12259/j.issn.2095-610X.S20240404

Citation:

Peipei ZHANG, Jiali CUI, Hongbin LIU, Dangzhu TANG, Yan YANG, Deguang Li. Comparative Study on Transdermal Absorption of Bulleyaconitine A in Four Skin Barrier Models of Rabbits[J]. Journal of Kunming Medical University, 2024, 45(4): 26-34. doi: 10.12259/j.issn.2095-610X.S20240404

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Comparative Study on Transdermal Absorption of Bulleyaconitine A in Four Skin Barrier Models of Rabbits

doi: 10.12259/j.issn.2095-610X.S20240404

1.
School of Pharmacy，Kunming Health Vocational College，Kunming Yunnan 650500
2.
Innovation and R & D Center/Drug Safety Evaluation Center，Yunnan Bai Yao Group Kunming Yunnan 650111
3.
Dept. of Orthopaedics，Kunming Municipal Hospital of Traditional Chinese Medicine，Kunming Yunnan 650051，China

Received Date: 2023-10-06
Available Online: 2024-04-28
Publish Date: 2024-04-29

Abstract

Abstract

Objective To compare the transdermal absorption of Bulleyaconitine A on normal rabbit intact skin, normal rabbit damaged skin, pathological damaged normal skin, and pathological damaged injured skin barrier models in vivo. Methods The rabbit model of pathological injury was obtained by intramuscular injection of 50% glycerol. The damaged skin was prepared by gently rubbing the skin surface with a wooden stick wrapped in No. 1 sandpaper until it turned light red. Four skin barrier models were topically treated with Bulleyaconitine A gel. Blood samples were collected at various time points after drug administration for normal skin （1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 8 h, 10 h） and damaged skin （1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 8 h, 10 h, 12 h, 24 h, 36 h）. HPLC-MS/MS was used to detect drug concentrations in rabbit models at different time points after Carbenoxolone administration. Drug pharmacokinetic parameters were calculated using DAS 3.2.0, and inter-group pharmacokinetic parameters were statistically analyzed using SPSS 23.0. Results The trends of three pharmacokinetic parameters, AUC（0-t）, AUC（0-∞）, and Cmax, in four skin barrier models of rabbits are consistent. They are as follows in size order: intact skin of normal rabbits > damaged skin from pathological injury > intact skin from pathological injury > intact skin of normal rabbits. Different external skin environments have a significant impact on the permeability of Bulleyaconitine A absorption. The permeability of damaged skin is significantly higher than that of normal skin （P < 0.05）. Pure pathological damage （internal injury）, with consistent skin conditions, shows no significant impact on the absorption and elimination of Chuanwu （P > 0.05）. Compared to intact skin of normal rabbits, damaged skin from simulated external trauma, and damaged skin from internal and external trauma, the absorption of Bulleyaconitine A significantly increases and the elimination capacity significantly decreases （P < 0.05）. Conclusion The barrier function of the stratum corneum is the main limiting factor for Bulleyaconitine A transdermal absorption. Bulleconitine A may accumulate in the body under the condition of trauma or internal or external injuries, which may affect drug safety. When conducting experiments on transdermal drug delivery formulations, it is advisable to simultaneously compare normal skin with damaged skin caused by simulated trauma or pathological damage from internal and external injuries. Studying the transdermal absorption under conditions simulating clinical muscle and skin injuries from internal and external trauma will help in a more comprehensive and accurate evaluation of the efficacy, pharmacokinetics, and toxicological properties of transdermal drug delivery formulations.
- Bulleyaconitine A,
- Normal skin,
- Damaged skin,
- Pathological injury,
- HPLC-MS/MS

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