Current Drug Delivery
·
2021
·Vol. 18
·期 10
·1585-1594
·
IF 2.565
Chen Jianmin,Wang Meixia,Ran Mengnan,Liu Xinying,Liu Siwan,Ruan Zhipeng,Jin Nan
Background: The clinical application of glabridin in treating skin diseases has been constrained by the limitations of its poor chemical stability and low skin permeability. Objective: Here, we describe Tip-loading Dissolving Microneedles (TDMNs) encapsulating drugs only in the
tips of needles for glabridin delivery with improved stability and skin permeability. Methods: The TDMNs fabricated by solvent casting technique had sufficient mechanical strength to penetrate through the excised rat's skin without fracture. Drug delivery efficiency and drug residual
in the skin of TDMNs were 63.16% and 49.28%, respectively. Glabridin encapsulated in the tips of TDMNs was effectively delivered into the abdominal skin of rat, and the in vivo delivery efficiency was inversely proportional to the drug doses. Results: Transepidermal Water Loss (TEWL)
significantly increased to 34.80 g/m2·h after the application of TDMNs and returned to normal levels (11.31 g/m2·h) after 8 h, indicating that the TDMNs were well tolerated. The stability of glabridin at room temperature was appreciably improved when loaded in TDMNs. Conclusion:
These results suggest that intradermal delivery of glabridin by TDMNs is a safe and efficient alternative to currently available routes of administration.
研究领域:
药剂学
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皮肤科学
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生物医学工程
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DOI
PubMed
高影响因子
MOLECULES
·
2023
·Vol. 29
·期 1
·66
·
IF 4.6
Meng Zhang,Xue Zhuang,Siqi Li,Yansong Wang,Xiangyu Zhang,Jinlian Li,Dongmei Wu
Binary ethosome vesicles have been developed as flexible lipid vesicles for the enhanced physicochemical stability and skin delivery of drugs. This work aimed to prepare phloretin-loaded propylene glycol ethosomes (PHL-PGEs) to improve their stability, skin permeability and antioxidant activity. PHL-PGEs were prepared via the ethanol injection method and optimized using different weight ratios of ethanol to propylene glycol (PG). When the ethanol/PG mass ratio changed from 10:0 to 0:10, the encapsulation efficiency and stability of ethosomes increased. At a PHL concentration of 1mg/mL, the EE% was 89.42 ± 2.42 and the DL% was 4.21 ± 0.04, which exhibited their highest values. The encapsulation of the PHL in the PHL-PGEs was strengthened via XRD analysis and FTIR analysis. The results of the in vitro percutaneous permeability test demonstrated that the combined use of ethanol and PG exhibited a notable enhancement in skin permeability, and the skin retention of PHL-PGEs was 1.06 times that of PHL-ethosomes (PHL-Es) and 2.24 times that of the PHL solution. An in vitro antioxidant activity study indicated that solubility and antioxidant activity was potentiated via the nanoencapsulation of phloretin. Therefore, these results confirm the potential of this nanocarrier to enhance physicochemical stability, skin permeability and antioxidant activity.Keywords:binary ethosomes;propylene glycol;skin permeability;antioxidant activity
研究领域:
药剂学
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皮肤科学
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生物化学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2017
·
IF 3.649
Hanqing Zhao,Chao Liu,Peng Quan,Xiaocao Wan,Meiyue Shen,Liang Fang
Though ion-pair strategy has been widely used in transdermal drug delivery system , knowledge about the molecular mechanisms involved in the skin permeation processes of ion-pair complexes is still limited. In the present study, a homologous series of fatty acids were chosen to form model ion-pair complexes with bisoprolol (BSP) to rule out the influence of functional groups on polar surface area, stability and other physicochemical properties of ion-pair complexes. The ion-pair complexes were characterized by FTIR , thermal analysis, and 1 H NMR. The skin permeability of BSP as well as its ion-pair complexes was investigated by in vitro skin permeation experiments then visualized by CLSM . The skin permeability coefficient ( k p ) of BSP ion-pair complex was negatively related to its n -octanol/water apparent partition coefficient ( P’ o/w ) in the hydrophobic vehicle caprylic/capric triglyceride , (log k p = −1.657 − 1.229 log P’ o/w ), suggesting that the instability of ion-pair complexes due to their dissociation in the viable epidermis (VED) played an important role in controlling the skin permeability of BSP, which was further proved by 1 H NMR and molecular docking. These findings broadened our understanding about the molecular mechanisms involved in the skin permeation processes of ion-pair complexes.
研究领域:
药剂学
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皮肤科学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2024
·
IF 3.6
Siqi Li,Di Wang,Meng Zhang,Ying Yang,Xiangyu Zhang,Jinlian Li,Dongmei Wu
Biocompatible fatty acids are natural biological materials which exhibit widespread biomedical applications. Nevertheless, their application in vesicle forms is hampered by strong pH sensitivity and poor stability to changes in ionic strength, temperature, and storage. In the investigation, the incorporation of alkyl glycoside (APG), a surfactant with non-ionic properties, into the oleic acid (OA) vesicles was undertaken as a means to address this issue. The newly formed OA/APG composite vesicles form in a pH range of between 5.4 and 7.4, which is close to the pH range of the physiological environment. The stability studies results showed that the OA/APG composite vesicles have excellent stability in terms of ionic strengths, temperature and storage. The formation of NAR-loaded OA/APG composite vesicles was demonstrated through FT-IR, DSC and XRD. In vitro topical delivery and skin retention studies confirmed that the composite vesicles improve skin permeation rate and have better skin permeation behavior. Antioxidant activity experiments confirmed that the antioxidant effect composite vesicles were significantly increased as compared to the naringenin (NAR). This finding has theoretical implications for the use of drug-loaded fatty acid vesicles in cosmetics industries and topical delivery systems.
研究领域:
化妆品科学
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药剂学
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生物材料科学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2024
·
IF 5.3
Xinyu Fan,Ying Yang,Yuxi Gong,Yuqi Zhan,Xiangyu Zhang,Shi Zhou,Dongmei Wu
Based on the inherent alkaline adaptability of fatty acid vesicles (FAVs) when in contact with the human body, along with the very narrow pH window for the formation and application of FAVs, which is far from the physiological pH range, this study successfully prepared a composite vesicle of non-ionic surfactant Tween60 (TW60) with nonanoic acid (NA) to migrate and expand the pH window. Acid-base titration confirmed that adding varying proportions of TW60 to sodium nonanoate (SN) solutions expanded the pH window from 6.6–7.5 to 1.28–6.52, widening it by 5.24, as determined by conductivity and turbidity. Studies under different conditions such as ionic strength, temperature, and storage time indicated that NA/TW60-FAV exhibited excellent stability. At a myricetin (MYR) concentration of 1 mg/mL and a pH of 6, encapsulation efficiency (EE) was 93.03 ± 0.03 %, and the drug loading capacity (DLC) was 8.65 ± 0.02 %, reaching the highest values. In vitro release and skin permeation results indicated that compared to free MYR solution (1 mg/mL), the skin permeability of the MYR-loaded composite vesicles (NA/TW60/MYR-FAV) was 1.64 times that of the MYR solution, significantly increasing skin absorption and retention, with a pronounced sustained release effect. The antioxidant activity experiments confirmed a significant enhancement in its ability to scavenge DPPH, ferric ions, and hydroxyl radicals (OH). The antibacterial experiments showed that NA/TW60/MYR-FAV had significant inhibitory effects against Escherichia coli ( E. coli ) and Staphylococcus aureus ( S. aureus ), indicating potential applications in cosmetics. In summary, the pH range of the blank composite vesicles (NA/TW60-FAV) aligns with the requirements for human skin adaptation, significantly enhancing the intrinsic value of the loaded substance. This indicates that it is a reliable and stable vesicle carrier, offering preliminary evidence for further research and application in the cosmetics industry.
研究领域:
化妆品科学
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药剂学
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生物医学工程
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产品关联
DOI
高影响因子
COLLOID AND POLYMER SCIENCE
·
2018
·Vol. 296
·期 3
·471-481
·
IF 1.967
Han Lidong,Yang Rong,Yuan Shengxiao,Ding Shuang,Wu Ziheng,Wu Zhenghong,Qi Xiaole
Multiple emulsions are potential transdermal drug carriers for their remarkable ability to enhance skin permeability, but their intrinsic thermodynamically instability always limits further application. Here, we developed freeze-thawing water-in-oil-in-water multiple emulsion transdermal drug delivery system, which could accomplish solid-liquid transition in freeze-thawing cycles and keep stable under hypothermic storage (4 °C). In this study, freeze-thawing multiple emulsions were prepared by a two-step emulsification method with isopropyl palmitate as the oil phase, which could freeze at 4 °C to gain solid multiple emulsions and regain intact liquid emulsions at a shell temperature (32 °C) upon application on the skin. In vitro skin permeation studies on excised mice skin showed that the cumulative permeation percentages of diclofenac sodium from freeze-thawing multiple emulsions, multiple emulsions, and cream (Dakangfen®) were 41.22 ± 4.27, 36.63 ± 4.71, and 23.96 ± 3.49% separately. Moreover, pharmacokinetic experiments in rabbits indicated that the AUC 0 − t (area under the curve) of freeze-thawing multiple emulsions (30.872 ± 3.989 μg/mL h) and multiple emulsions (27.337 ± 2.804 μg/mL h) were significantly higher than those of the controlled cream (14.981 ± 1.331 μg/mL h) ( p < 0.05). These results suggested that freeze-thawing multiple emulsions could be a promising substitute of traditional multiple emulsions for transdermal drug delivery.
研究领域:
药剂学
·
药物递送系统
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产品关联
DOI
高影响因子
Pharmaceutics
·
2023
·Vol. 15
·期 7
·2007
·
IF 5.4
Mengzhen Xing,Yuning Ma,Xiaocen Wei,Chen Chen,Xueli Peng,Yuxia Ma,Bingwen Liang,Yunhua Gao,Jibiao Wu
Poor transdermal permeability limits the possibility of most drug delivery through the skin. Auxiliary permeable microneedles (AP-MNs) with a three-dimensional network structure can effectively break the skin stratum corneum barrier and assist in the transdermal delivery of active ingredients. Herein, we propose a simple method for preparing AP-MNs using polyvinyl alcohol and Eudragit NM30D for the first time. To optimize the formulation of microneedles, the characteristics of swelling properties, skin insertion, solution viscosity, and needle integrity were systematically examined. Additionally, the morphology, mechanical strength, formation mechanism, skin permeability, swelling performance, biocompatibility, and in vitro transdermal drug delivery of AP-MNs were evaluated. The results indicated that the microneedles exhibited excellent mechanical-strength and hydrogel-forming properties after swelling. Further, it proved that a continuous and unblockable network channel was created based on physical entanglement and encapsulation of two materials. The 24 h cumulative permeation of acidic and alkaline model drugs, azelaic acid and matrine, were 51.73 ± 2.61% and 54.02 ± 2.85%, respectively, significantly enhancing the transdermal permeability of the two drugs. In summary, the novel auxiliary permeable microneedles prepared through a simple blending route of two materials was a promising and valuable way to improve drug permeation efficiency.Keywords:auxiliary permeation microneedles;polyvinyl alcohol;Eudragit NM30D;skin permeability;transdermal drug delivery
研究领域:
药剂学
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药物递送系统
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
MICROSYSTEM TECHNOLOGIES-MICRO-AND NANOSYSTEMS-INFORMATION STORAGE AND PROCESSING SYSTEMS
·
2024
·
IF 1.6
Zhang Xiaoning,Han Qingxin,Hu Xiaoqing,Zhang Lei,Kang Xiaoya,Li Ming,Gao Qiang,Liu Fengyi,Sun Jingyao,Zhu Jingxian,Zhuang Jian
This article proposes a new process for fabricating a polymer microneedles (MNs) patch integrated with an LED light source (LED-HEMA/MN, LH-MN) using ultraviolet (UV) curing technology. Hydroxyethyl methacrylate (HEMA) is used as the base material, with a focus on studying the active integrated fabrication process of the MNs patch. The study also investigates the morphology, size, mechanical properties, ex vivo skin penetration performance, operating temperature, and performance optimization of the LH-MN. The experimental results show that the LH-MN fabricated using the optimal process has a good appearance, high molding rate, short production cycle, and excellent mechanical properties. It can effectively penetrate the skin without the risk of thermal injury. In addition, the MNs patch (LED-HEMA/HEA-MN, LHH-MN) prepared by optimizing and modifying with hydroxyethyl acrylate (HEA) possesses good flexibility and mechanical properties. It can adapt to different shapes and locations of the affected area, greatly enhancing the practicality of the MNs.
研究领域:
生物医学工程
·
材料科学
·
医学
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产品关联
DOI
高影响因子
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
·
2021
·
IF 5.051
Hao He,Huifang Li,Toyosi Akanji,Shengli Niu,Zhujun Luo,Dongli Li,Navindra P. Seeram,Panpan Wu,Hang Ma
Oleanolic acid (OA) is a natural cosmeceutical compound with various skin beneficial activities including inhibitory effect on hyaluronidase but the anti-hyaluronidase activity and mechanisms of action of its synthetic analogues remain unclear. Herein, a series of OA derivatives were synthesised and evaluated for their inhibitory effects on hyaluronidase. Compared to OA, an induction of fluorinated (6c) and chlorinated (6g) indole moieties led to enhanced anti-hyaluronidase activity (IC50 = 80.3 vs. 9.97 and 9.57 µg/mL, respectively). Furthermore, spectroscopic and computational studies revealed that 6c and 6g can bind to hyaluronidase protein and alter its secondary structure leading to reduced enzyme activity. In addition, OA indole derivatives showed feasible skin permeability in a slightly acidic environment (pH = 6.5) and 6c exerted skin protective effect by reducing cellular reactive oxygen species in human skin keratinocytes. Findings from the current study support that OA indole derivatives are potential cosmeceuticals with anti-hyaluronidase activity.
研究领域:
化妆品科学
·
药物化学
·
生物化学
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DOI
PubMed
高影响因子
Journal of Materials Chemistry B
·
2019
·Vol. 7
·期 47
·7515-7524
·
IF 5.047
Ya Gao,Mengmeng Hou,Ruihao Yang,Lei Zhang,Zhigang Xu,Yuejun Kang,Peng Xue
Microneedles are primarily designed for enhancing transdermal drug delivery in a minimally invasive manner. In particular, coated microneedles have attracted increasing attention due to the resulting mode of rapid and highly efficient drug administration. In this study, we developed a novel gelatin/sucrose film-coated poly(ethylene glycol)diacrylate (PEGDA) microneedle patch, which can effectively improve the skin permeability of therapeutic drugs and realize convenient and efficient drug administration. A simple and reliable technique was proposed to produce uniform film coatings on microneedles at room temperature. After introducing a prepolymer solution into the mold cavity, a film-coated microneedle patch was fabricated via a photo-induced polymerization process. Four categories of molecular models, including rhodamine B (RhB), bovine serum albumin (BSA), doxorubicin (DOX) and indocyanine green (ICG), were encapsulated into the gelatin/sucrose film to evaluate their transdermal delivery and therapeutic effects both in vitro and in vivo. The presented methodology represents a facile technique for rapid formation of film-coated microneedles for efficient transdermal delivery of small molecular drugs and large proteins.
研究领域:
生物医学工程
·
药物递送系统
·
材料科学
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产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2023
·
IF 9.5
Yuqin Zhang,Shuqing Gong,Lin Liu,Huan Shen,Ergang Liu,Li Pan,Nan Gao,Rongli Chen,Yongzhuo Huang
Psoriasis is a chronic inflammatory skin disease that is difficult to treat. Quercetin (QT) is a dietary flavonoid known for its anti-inflammatory effects and safe use in humans. However, the topical application of quercetin for psoriasis treatment presents a significant challenge due to its poor water solubility and low stability in semisolid preparations, where it tends to recrystallize. This work presents a novel liposome-in-gel formulation for the quercetin-based topical treatment of psoriasis. The quercetin-loading liposomes are stabilized by hydroxypropyl-β-cyclodextrin (HPCD), which interacts with phospholipids via hydrogen bonding to form a layer of an HPCD coating on the liposome interface, thus resulting in improved stability. Various analytical techniques, such as FTIR spectroscopy, Raman spectroscopy, and TEM, were used to characterize the molecular coordination patterns between cyclodextrin and liposomes. The results demonstrated that HPCD assisted the liposomes in interfacing with the matrix lipids and keratins of the stratum corneum, thereby enhancing skin permeability and promoting drug penetration and retention in the skin. The in vivo results showed that the topical QT HPCD-liposome-in-gel improved the treatment efficacy of psoriatic plaque compared to free QT. It alleviated the symptoms of skin thickening and downregulated proinflammatory cytokines, including TNF-α, IL-17A, and IL-1β. The results suggested that the HPCD-coordinated liposome-in-gel system could be a stable carrier for topical QT therapy with good potential in psoriasis treatment.
研究领域:
药剂学
·
皮肤病学
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药物递送系统
·
药物化学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2024
·
IF 4.4
Zhenchao Ma,Yingrong Chen,Kaixian Tang,Hongxia Yang,Mengli Tian,Xiaoyuan Xi,Shuwen Han,Shuixin Yang,Lixin Ru,Xiang Yu
PEGylated superoxide dismutase (PEG-SOD) is commonly used as a cytoprotective agent in radiotherapy. However, its effectiveness in preventing radiation dermatitis is limited owing to its poor skin permeability. To address this issue, a PEG-SOD-loaded dissolving microneedle (PSMN) patch was developed to effectively prevent radiation dermatitis. Initially, PSMN patches were fabricated using a template mold method with polyvinylpyrrolidone K90 as the matrix material. PSMNs exhibited a conical shape with adequate mechanical strength to penetrate the stratum corneum. More than 90 % of PEG-SOD was released from the PSMN patches within 30 min. Notably, the PSMN patches showed a significantly higher drug skin permeation than the PEG-SOD solutions, with a 500-fold increase. In silico simulations and experiments on skin pharmacokinetics confirmed that PSMN patches enhanced drug permeation and skin absorption, in contrast to PEG-SOD solutions. More importantly, PSMN patches efficiently mitigated ionizing radiation-induced skin damage, accelerated the healing process of radiation-affected skin tissues, and exhibited highly effective radioprotective activity for DNA in the skin tissue. Therefore, PSMN patches are promising topical remedy for the prevention of radiation dermatitis.
研究领域:
药学
·
放射肿瘤学
·
生物医学工程
·
皮肤科
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）