Drug Delivery and Translational Research
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2023
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IF 5.4
Nan Longyi,Song Haoyuan,Wang Haijun,Mi Ru,Wang Xiaoxu,Fang Liang
The aim of this study was to design a tulobuterol (TUL) patch with good penetration behavior and mechanical properties. Particular attention was paid to the effect of transdermal permeation enhancers on the release process of metal ligand-based acrylic pressure-sensitive adhesive (AA-NAT/Fe 3+ ). The type and dosage of the enhancers were screened by in vitro transdermal penetration in rat skin. The optimized formulation was evaluated in a pharmacokinetic study in rats. Furthermore, the molecular mechanism by which Azone (AZ) improves the release rate of TUL from AA-NAT/Fe 3+ was investigated by FT-IR, shear strength test, rheological study, and molecular simulation. As a result, the optimized formula using AA-NAT/Fe 3+ showed better mechanical properties compared to commercial products. Meanwhile, the AUC 0-t and C max of the optimized patch were 1045 ± 89 ng/mL·h and 106.8 ± 28.5 ng/mL, respectively, which were not significantly different from those of the commercial product. In addition, AZ increased the mobility of the pressure-sensitive adhesive (PSA) rather than decreasing the drug-PSA interaction, which was the main factor in enhancing TUL release from the patch. In conclusion, a TUL transdermal drug delivery patch was successfully developed using metal-coordinated PSA, and a reference was provided for the design of metal-coordinated acrylic PSA for transdermal patch delivery applications. Graphical Abstract
研究领域:
药学
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2020
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IF 2.734
Jing Yuan,Jieyu Wu,Tianxiang Yin
Ionic liquids have recently been found to be effective ingredient in formulation of transdermal drug delivery system . In this work, we synthesized two cholinium-animo acid based ionic liquids CHAAILs, cholinium glycinate [Ch][Gly] and cholinium analinate [Ch][Ala], and investigated their ability to enhance the solubility and permeation of model drug ibuprofen . The solubility measurements showed that slight amount of CHAAILs can significantly increase the solubility of ibuprofen. Besides, the effective enhancement of permeation of ibuprofen across polyethersulfone (PES) membrane was clearly presented at low concentration (0.8 wt%) of CHAAILs. It is more valuable that the addition of CHAAILs brings little cytotoxicity. Therefore, [Ch][Gly] and [Ch][Ala] can be served as green and effective constituents in transdermal drug delivery system.
研究领域:
药剂学
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药物递送系统
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分子药理学
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生物药剂学
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药物代谢
✓ 已验证
DOI
高影响因子
Materialia
·
2025
·
IF 2.9
Bo Yang,Shuang Liang,Hongtao Han,Yuesheng Majia,Jiaheng Zhang,Gang Zhao,Chengyu Wu
To address the challenge of poor intradermal penetration of hyaluronic acid (HA), researchers applied deep eutectic solvent (DES) technology within a drug delivery system. In this study, supramolecular HA nanoparticles (Supra HA) were successfully prepared by combining HA and decanoic acid-menthol deep eutectic solvent (DAM-DES). The resulting Supra HA nanoparticles exhibited an average particle size of 124 nm and a zeta potential of -35 mV. The intradermal penetration efficacy of Supra HA was 2.26 times greater than that of GTCC HA. Furthermore, Supra HA significantly increased type I collagen synthesis in fibroblasts by 54.0 % and reduced MMP-1 secretion by 57.4 %, demonstrating anti-wrinkle and skin-tightening effects. Under identical conditions, Supra HA enhanced the synthesis of the FLG gene and AQP3 protein in keratinocytes by 55 % and 227.4 %, respectively, indicating skin barrier repair and moisturizing effects. Human clinical trials demonstrated that 28-day application of Supra HA significantly enhanced skin hydration (13.3 % increace), with concurrent improvements in skin elasticity (21.3 % increase), firmness (21.9 % elevation), and wrinkle reduction (20.1 % decrease in count and 23.3 % reduction in area). Collectively, these findings indicate that the utilization of deep eutectic solvents in hyaluronic acid delivery systems facilitates transdermal permeation, thereby contributing to sustained moisturization and anti-aging efficacy.
研究领域:
药物递送系统
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纳米技术
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皮肤科学
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化妆品科学
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生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
International Journal of Pharmaceutics-X
·
2019
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IF 0
Xiao-Qian Niu,Dan-Ping Zhang,Qiong Bian,Xing-Fu Feng,Hao Li,Yue-Feng Rao,Yong-Mei Shen,Fu-Neng Geng,An-Ran Yuan,Xiao-Ying Ying,Jian-Qing Gao
Ethosomes are widely used to promote transdermal permeation of both lipophilic and hydrophilic drugs, but the mechanism of interaction between the ethosomes and the skin remains unclear. In this work, it was exploded with several technologies and facilities. Firstly, physical techniques such as attenuated total reflectance fourier-transform infrared and laser confocal Raman were used and the results indicated that the phospholipids configuration of stratum corneum changes from steady state to unstable state with the treatment of ethosomes. Differential scanning calorimetry reflected the thermodynamics change in stratum corneum after treatment with ethosomes. The results revealed that the skin of Bama mini-pigs, which is similar to human skin, treated by ethosomes had a relatively low T m and enthalpy. Scanning electron microscopy and transmission electron microscopy showed that the microstructure and ultrastructure of stratum corneum was not damaged by ethosomes treatment. Furthermore, confocal laser scanning microscopy revealed that lipid labeled ethosomes could penetrate the skin via stratum corneum mainly through intercellular route, while during the process of penetration, phospholipids were retained in the upper epidermis. Cell experiments confirmed that ethosomes were distributed mainly on the cell membrane. Further study showed that only the drug-loaded ethosomes increased the amount of permeated drug. The current study, for the first time, elucidated the mechanistic behavior of ethosomes in transdermal application from molecular configuration, thermodynamic properties, ultrastructure, fluorescent labeling and cellular study. It is anticipated that the approaches and results described in the present study will benefit for better design of drug-loaded ethosomes.
研究领域:
药剂学
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生物物理学
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皮肤病学
✓ 已验证
产品关联
DOI
PubMed
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2020
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IF 4.845
Danping Zhang,Qiong Bian,Junjun Li,Qiaoling Huang,Jianqing Gao
Topical administration is a promising clinical strategy to avoid serious gastrointestinal adverse reactions of loxoprofen sodium (LOX), a new non-steroidal anti-inflammatory drug. Small molecule organic acids had been reported with the ability of promoting transdermal rate of several drugs. In this article, the effect of small molecule organic acids on the transdermal delivery of LOX was studied, and the possible mechanism was also explored by Fourier infrared spectroscopy , differential scanning calorimetry , tape stripping, etc. The results showed that lactic acid and fumaric acid could significantly increase the penetration rate of LOX and reduce time lag even without the help of acidic environment. The preliminary mechanism investigation inferred that fumaric acid could increase LOX’s distribution in stratum corneum and might change its complexation state, but had little effect on the drug structure and skin’s lipids and proteins configuration. The topical LOX gel using fumaric acid as penetration enhancer had higher transdermal rate, significant anti-inflammatory effect and no obvious skin irritation . This study proved the promising application of small molecule organic acids in transdermal enhancing and provided a potential strategy for transdermal delivery of LOX combined with fumaric acid.
研究领域:
药剂学
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药理学
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药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
Nature Communications
·
2022
·Vol. 13
·期 1
·1-13
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IF 17.694
Yang Yuan,Luo Ruizeng,Chao Shengyu,Xue Jiangtao,Jiang Dongjie,Feng Yun Hao,Guo Xin Dong,Luo Dan,Zhang Jiaping,Li Zhou,Wang Zhong Lin
Epidermal growth factor is an excellent drug for promoting wound healing; however, its conventional administration strategies are associated with pharmacodynamic challenges, such as low transdermal permeability, reduction, and receptor desensitization. Here, we develop a microneedle-based self-powered transcutaneous electrical stimulation system (mn-STESS) by integrating a sliding free-standing triboelectric nanogenerator with a microneedle patch to achieve improved epidermal growth factor pharmacodynamics. We show that the mn-STESS facilitates drug penetration and utilization by using microneedles to pierce the stratum corneum. More importantly, we find that it converts the mechanical energy of finger sliding into electricity and mediates transcutaneous electrical stimulation through microneedles. We demonstrate that the electrical stimulation applied by mn-STESS acts as an “adjuvant” that suppresses the reduction of epidermal growth factor by glutathione and upregulates its receptor expression in keratinocyte cells, successfully compensating for receptor desensitization. Collectively, this work highlights the promise of self-powered electrical adjuvants in improving drug pharmacodynamics, creating combinatorial therapeutic strategies for traditional drugs.
研究领域:
药学
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生物医学工程
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材料科学
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药物递送系统
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伤口愈合
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）