Optical Coherence Tomography and Microdialysis for Microneedle-Mediated Penetration Enhancement Study of Paeoniflorin-Loaded Ethosomes.

IF 2.8 4区 医学 Q2 DERMATOLOGY Skin Pharmacology and Physiology Pub Date : 2021-01-01 Epub Date: 2021-05-06 DOI:10.1159/000514321
Jiayi Huang, Yahua Cui, Yanling Yang, Huahua Li, Yi Zhang, Haiju Yang, Shouying Du, Jie Bai
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引用次数: 5

Abstract

Background: To understand the cumulative effect of topical formulations after medication, evaluate the therapeutic effect of microneedle-assisted (MN-assisted) paeoniflorin-loaded ethosomes (TGP-E), and explore the potential for deep penetration of drugs, this paper uses microdialysis to systematically study the percutaneous pharmacokinetics of TGP-E.

Methods: First, optical coherence tomography (OCT) was used to study the effectiveness of microneedle puncture. Second, a microdialysis method and a UPLC-MS method for determining the amount of paeoniflorin (Pae) in dialysate were established. Finally, the transdermal pharmacokinetics of TGP-E was studied using in vivo microdialysis in rats under the above MN-assisted conditions.

Results: The optimal MN-assisted conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N, and an action time of 3 min. The pharmacokinetic results demonstrated that the maximum drug concentration (Cmax) and the area under the curve (AUC) of the TGP-E gel were higher than the TGP-saline solution gel, and the mean retention time was lower. These indicated that microneedle can promote the entry of the ethosomes into the skin for in vivo experiments and greatly improve the possibility of deep penetration of the water-soluble Pae.

Conclusion: Therefore, the microneedle-ethosomes delivery system is a more ideal means for promoting the deep penetration of Pae. These findings may provide a reference for the combination of multiple penetration-enhancement ways to promote drug absorption, and also provide a new insight to realize the development of novel, safe, and more effective dosage forms and administration routes of drugs.

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光学相干断层扫描和微透析微针介导的芍药苷运载体穿透增强研究。
背景:为了解外用制剂给药后的累积效应,评价微针辅助(mn辅助)芍药苷负载体(TGP-E)的治疗效果,探索药物的深度渗透潜力,本文采用微透析方法系统研究TGP-E的经皮药代动力学。方法:首先,利用光学相干断层扫描(OCT)研究微针穿刺的有效性。其次,建立了透析液中芍药苷(Pae)含量的微透析法和超高效液相色谱-质谱法。最后,在上述mn辅助条件下,采用体内微透析法研究TGP-E的透皮药代动力学。结果:在微针长度为500 μm、压力为3 N、作用时间为3 min的条件下,获得了最佳的mn辅助条件。药代动力学结果表明,TGP-E凝胶的最大药物浓度(Cmax)和曲线下面积(AUC)均高于tgp -生理盐水凝胶,平均滞留时间较低。这表明微针可以促进溶酶体进入皮肤进行体内实验,大大提高了水溶性Pae深入渗透的可能性。结论:微针-溶酶体递送系统是一种较理想的促进Pae深度渗透的手段。本研究结果可为多种渗透增强方法联合应用促进药物吸收提供参考,并为开发新型、安全、有效的药物剂型和给药途径提供新的思路。
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来源期刊
Skin Pharmacology and Physiology
Skin Pharmacology and Physiology 医学-皮肤病学
CiteScore
5.20
自引率
7.40%
发文量
23
审稿时长
>12 weeks
期刊介绍: In the past decade research into skin pharmacology has rapidly developed with new and promising drugs and therapeutic concepts being introduced regularly. Recently, the use of nanoparticles for drug delivery in dermatology and cosmetology has become a topic of intensive research, yielding remarkable and in part surprising results. Another topic of current research is the use of tissue tolerable plasma in wound treatment. Stimulating not only wound healing processes but also the penetration of topically applied substances into the skin, this novel technique is expected to deliver very interesting results.
期刊最新文献
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