INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
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IF 8.5
Bin Li,Xiaojuan Li,Shuying Li,Chen Chen,Ting Xiao,Yuehong Xu
Psoriasis is a chronic and incurable inflammatory skin disease usually requiring long-term disease management. Natural phytochemical resveratrol (RES) has been known for high efficiency and low toxicity, exhibiting good anti-psoriasis potential. However, its biological activity is limited by poor solubility, chemical instability, and insufficient skin retention. Herein, we developed an adhesive eutectogel loaded with RES constructed through electrostatic and hydrogen bonding cross-linking between cyclodextrin-levulinic acid supramolecular deep eutectic solvent (DES) and chitosan (CS). A series of characterizations combined with molecular dynamics simulations demonstrated that such DES not only significantly increased the solubility and stability of RES, but also acted as the cross-linker and plasticizer in eutectogel preparation. When applied to the skin surface, the eutectogel formed a soft film in situ that established tight contact with the skin, thereby enhancing RES sustained penetration into the skin. In an imiquimod-induced psoriasis-like mice model, the eutectogel effectively alleviated psoriasis symptoms, inhibited the excessive proliferation of keratinocytes, and regulated the expression of IL-23/IL-17 axis-related factors, whose therapeutic effect was better than that of commercially available calcipotriol ointment. Overall, The DES-strengthened eutectogel offers a promising topical drug delivery platform for psoriasis treatment and expands the applications of green polysaccharide medical materials.
研究领域:
药剂学
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皮肤科
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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
CHEMICAL ENGINEERING JOURNAL
·
2021
·
IF 13.273
Yiru Gao,Yanan Hao,Wenxin Zhang,Yanan Wei,Yang Shu,Jianhua Wang
Phototherapy still lacks effectiveness in treating tissue infections due to poor penetration depth of light and laser-induced non-specific thermal diffusion. Microwave thermal therapy (MWTT) is advantageous as characterized by strong tissue penetration, and higher heating rate. In addition, transdermal delivery of drugs helps in the treatment of tissue infections. Herein, we present an all-in-one MW-therapeutic hydrogel for eradicating bacterial infections with transdermal drug delivery. A microwave-responsive ionic liquid (IL), i.e., vinylbenzyl trimethylammonium chloride (VBTMACl), and a transdermal-enhancer IL, i.e., [2-(methacryloyloxy)ethyl] trimethylammonium chloride (ChMACl), are copolymerized with acrylic acid (AA) to form the hydrogel VACPHs. Polyvinylpyrrolidone (PVP) is incorporated with VACPHs to improve their mechanical stability. The model drug levofloxacin (LEVO) is subsequently loaded into the hydrogel, and the VACPHs-LEVO shows strong antibacterial effect. It is attributed to the efficient microwaveocaloric therapy of VBTMACl and enhanced transdermal antibiotic delivery by ChMACl. The drug delivery hydrogel developed in this research exhibits excellent performance for the treatment of deep tissue infections.
研究领域:
生物医学工程
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药剂学
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治疗学
✓ 已验证
产品关联
DOI
高影响因子
Current Drug Delivery
·
2024
·Vol. 22
·期 4
·479-491
·
IF 2.8
Teng Guo,Chenming Zhang,Yuling Chen,Yihan Wu,Zhenda Liu,Yongtai Zhang,Nianping Feng
BackgroundAdding a suitable surfactant can enhance the transdermal permeability of transethosomes while also leveraging its functionality as a functional material. In this study, transethosomes were prepared using D-α-tocopherol acid polyethylene glycol succinate (TPGS) as edge activators for transdermal delivery of curcumin (Cur).MethodsThe TPGS-mediated curcumin-loaded transethosomes (Cur@TES) were prepared and formulated optimally, and the optimized formulations were characterized for their morphology, particle size, entrapment efficiency (EE) and drug loading (DL). The stability and deformability of Cur@TES were investigated, while the transdermal delivery of Cur@TES was investigated through in vitro transdermal assays and fluorescence imaging. A mouse ear swelling model was performed to determine the anti-inflammatory effect of Cur@TES.ResultsCur@TES appeared round or elliptical in shape. The particle size, EE and DL for the optimized formulation were observed as 131.2 ± 7.2 nm, 97.68 ± 2.26%, and 6.58 ± 0.62%, respectively. X-ray diffraction analysis confirmed the formation of disordered structures in the inner core of the vesicles. Moreover, Cur@TES system demonstrated better stability and deformability compared to the curcumin-loaded ethosomes (Cur@ES). In vitro transdermal experiments demonstrated that Cur@TES significantly increased the amount of drug retained in the skin (P<0.05). Fluorescence imaging confirmed that the skin distribution was distinctly enhanced with the delivery by TPGS mediated transethosomes. In addition, Cur@TES showed a significant inhibitory effect on Inflammatory swelling in the mouse ear-swelling model.ConclusionTPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.
研究领域:
药剂学
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生物医学工程
✓ 已验证
DOI
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
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2020
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IF 2.997
Ting Zhong,Jiuheng Ruan,Chao Liu,Peng Quan,Liang Fang
The objective of this work was to develop a drug-in-adhesive (DIA) patch of TIZ by employing ion-pair and permeation enhancer to increase drug-polymer miscibility and drug release. Special attention was paid on the regulation effect of permeation enhancer on ion-pair status in pressure sensitive adhesives (PSA). Formulation factors including TIZ-fatty acids ion-pair, drug loading and permeation enhancer were investigated by ex-vivo transdermal experiments. Optimized patch was evaluated by pharmacokinetics study. The better polarity similarity and strong hydrogen bonding interactions between TIZ-caproic acid ion-pair (TIZ-C6) and PSA was confirmed by polarity determination, FT-IR, TOPEM of MDSC and theoretical calculation, which determined enhanced miscibility of ion-pair and PSA. The permeation enhancer affected status of ion-pair in PSA by regulating polarity similarity and interaction between ion-pair and PSA, resulting in increased drug-PSA miscibility and drug release, which was characterized by FT-IR, polarity determination, thermal analysis and molecular dynamics simulation. The optimized patch showed high drug-polymer miscibility and drug skin permeability with AUC 0-t of 14641.12 ± 854.45 h ng/mL and C max of 834.55 ± 155.68 ng/mL, which was significantly higher than the control group. In conclusion, DIA patch of TIZ was prepared and it supplied a reference for design of DIA patches with TIZ.
研究领域:
药学
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药剂学
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药物递送系统
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药代动力学
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材料科学
✓ 已验证
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2024
·
IF 4.5
Qi Zong,Guozhen Wang,Zijie Zhao,Wenzhuo Li,Xiaonan Hou,Mengfei Yao,Duo Tang,Chao Sheng,Zijia Liu,Yuchen Zheng,Zhixiang Zhou,Xiaofei Zhang,Xiao Li
Hypocrellin A (HA) is an efficient photosensitizer for photodynamic therapy in recent years. In order to improve the delivery of this photosensitizer, dissolving HA microneedles were established. Firstly, dissolving microneedles were prepared from HA by a two-step solvent casting method. Then, the dissolving HA microneedle were characterized by stereomicroscope, laser confocal microscope, scanning electron microscope, differential scanning calorimeter (DSC), X-ray diffractometer (XRD) and fourier infrared spectrometer (FTIR). Finally, the transdermal cumulative penetration experiments were conducted. The results showed that the dissolving HA microneedle has a conical shape with an average height of 650 μm. The mechanical strength endure a force of 44.78 N, resulting in 0.20 N per needle. The in vitro transdermal experiment showed that the dissolving HA microneedle almost completely dissolved in 5 minutes after insertion into the mouse skin. The depth of drug penetration through the skin can reach 601.36 μm. Moreover, the dissolving HA microneedle significantly improved the cumulative transdermal penetration efficiency of the photosensitizer through the skin. Therefore, the present study successfully established a dissolving microneedle of HA, which can quickly dissolve and significantly improve the transdermal delivery efficiency of HA.
研究领域:
药剂学
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生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
DRUG DELIVERY
·
2019
·
IF 3.829
Yujia Zhang,Nan Zhang,Hui Song,He Li,Jin Wen,Xiaochuan Tan,Wensheng Zheng
Gout is a kind of joint disease characterized by the accumulation of monosodium urate (MSU) crystals in the joint and its surrounding tissue, causing persistent hyperuricemia. Colchicine is the first choice of treatment for acute gout attacks. Due to strong toxicity of colchicines oral tablets, there are high fluctuations of blood drug concentration and serious irritation of gastrointestinal tract, and hence a transdermal preparation can help to slow down the blood drug concentration, reduce the frequency of drug taking, and improve the patients' compliance of the drug. The ethosome is a lipid carrier with high concentration of ethanol and has been proved to promote the penetration of drugs into the skin. Borneol (BO) is an excellent penetration enhancer in Chinese medicine, which can promote the entry of drugs into the skin. This paper prepared the borneol-physically-modified colchicine ethosome (COL-bpES) and used the prepared borneol-dioleoyl phosphoethanloamine (BO-DOPE) to prepare borneol-chemically-modified colchicine ethosome (COL-bcES). Compared to the free colchicine aqueous solution (free COL) and normal colchicine ethosome (COL-ES), the borneol-modified colchicine ethosome (COL-bES) demonstrated better drug penetration effect, while the particle size of the COL-bcES was lower than that of the COL-bpES. Toxicity, in vitro diffusion, pharmacokinetics and pharmacodynamics are superior to those of COL-bpES, providing a better delivery system for the treatment of small molecule inflammatory drugs.
研究领域:
药剂学
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2023
·
IF 5
Ying Sun,Yongxiang Zhang,Xiaxia Liu,Yan Tingting,Liyan Shen,Dan Ye,Xia Kong,Yonghui Su,Qingping Tian
Transfersomes is one of the most effective nanotechnology-based formulation for transdermal delivery of minoxidil (MXD), however the potential use was limited by its low drug content ( DC ) and entrapment efficiency ( EE ). In this study, efforts have been made to improve DC and EE of MXD in transfersomes for effective topical treatment of alopecia . By dissolving both MXD and edge activator (Tween 80) in aqueous phase than either or both of them co-dissolving in organic solvent with lipids (phospholipid and cholesterol with mass ratio of 5:1), the DC and EE of MXD transfersomes prepared by thin film hydration method were significantly increased. The optimized transfersomes (MT) and its gel (MT gel ) with mass ratio of drug, Tween 80 and lipids 3:1:18 have a spherical morphology without aggregation, and a particle size of not more than 100 nm. The differential scanning calorimetry measurements revealed that the drug in MT was in the non-crystalline state. MT and MT gel exhibited better in vitro transdermal penetration ability and hair of C57BL/6 mice growth-promoting capacity than commercial formulations. MT gel has non-irritation and is better than MT in skin adhesion, stability, potential for skin storage and hair growth promotion ability, which could endow it to be a promising strategy for topical treatment of alopecia.
研究领域:
药剂学
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纳米技术
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皮肤科学
✓ 已验证
产品关联
DOI
高影响因子
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2019
·
IF 2.367
Xiaoqin Chu,Xingqi Wang,Chunling Tian,Liu Liu,Mengqiu Xia,Jianqin Jiang,Shuangying Gui
The goal of this paper was to develop and evaluate dual component-loaded with the hydrophilic sinomenine hydrochloride (SH) and lipophilic cinnamaldehyde (CA) cubic liquid crystal gels for transdermal delivery. The gels was prepared with a vortex method using phytantriol/water (70:30, w/w) and characterized by polarized light microscopy, small-angle X-ray scattering and rheology. The inner structure of the gels were Pn3m cubic phase and exhibited a pseudoplastic fluid behavior. Furthermore, the in vitro release profile showed that the release behavior of the two drugs from cubic liquid crystal gels conformed to Higuchi equation and were dominated by Fick’s diffusion (n < 0.45). The ex vivo penetration experiment indicated that dual components-loaded liquid crystal gels can enhance and extend the skin permeation of these two drugs, especially the ratio of SH to CA is 1: 0.5. Finally, transdermal mechanisms were evaluated using laser scanning confocal microscopy and attenuated total reflectance-fourier transform infrared, hinting that hydrophilic and lipophilic drugs weaken each other’s transdermal velocity at the initial stage of penetration. In short, the dual drug-loaded liquid crystal gels was a promising strategy for transdermal applications in treatment of chronic disease.
研究领域:
药剂学
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药物递送系统
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材料科学
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生物物理学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Peng Xu,Kun Xu,Jiayin Li,Aoxue Liu,Wei Xiao,Lin Sun
Psoriasis, a prevalent immunoinflammatory skin condition, is characterized by abnormal skin thickening, which complicates traditional topical drug delivery and hinders drug penetration. Our goal is to enhance the efficacy of psoriasis treatment by developing a transdermal drug formulation. Microneedles (MNs) can improve treatment outcomes by increasing the absorption of topical medications through skin penetration. Curcumin (Cur), a natural anti-inflammatory, antioxidant, and immunomodulatory small molecule with water-insoluble properties, shows promise for psoriasis relief. In this research, three Cur nano-formulations (NFs) were screened and prepared using antisolvent and ethanol injection methods, with one being dispersed into hyaluronic acid (HA) dissolving MNs. A transdermal nano-MNs delivery system was constructed using a double-layer centrifugation technique. This co-delivery system overcame Cur’s solubility issues, poor absorption, and instability, allowing targeted and efficient delivery of Cur-NFs to the skin without being hindered by the skin barrier. In vitro studies demonstrated that Cur-NF dissolving MNs possess adequate mechanical properties for skin implantation, exhibit rapid dissolution, and achieve an effective drug release rate of 73 % within 6 h. Pharmacodynamic evaluations demonstrated that the MNs system effectively ameliorated key psoriatic skin manifestations. Notably, MNs treatment significantly reduced the Psoriasis Area and Severity Index (PASI) score from 12.0 ± 0.0 (model group) to 4.7 ± 0.5 ( p < 0.05), alongside a marked suppression of pro-inflammatory cytokines, including TNF-α, IL-17, IL-22, and IL-23, compared to untreated psoriatic controls. Therefore, the composite dissolving MNs delivery system loaded with Cur-NFs represents a promising approach for psoriasis treatment.
研究领域:
药剂学
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皮肤病学
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纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2025
·
IF 5.6
Yao-Yao Wei,Yang Zhang,Xue Lu,Jie Zhou,Huang-Wei Cheng,Yuan-Yuan Liu,Hua Zhang,Wen Chen
Gout is a disease caused by the deposition of sodium urate (MSU) crystals in the joints and tissues. Colchicine (COL) has become the first-line drug for the treatment of acute gout due to its low price and efficacy. However, colchicine is highly cytotoxic and oral administration is prone to cause severe adverse effects on the gastrointestinal tract, liver and kidney. Therefore, this study aimed to develop a novel dermal delivery formulation for addressing the safety concerns of this drug. The researchers used ethosomes encapsulation technology to improve the skin permeability of COL. In addition, in order to improve the performance of the ethosomes, it was screened and determined that the addition of 1.0–1.5 mg of ceramide III (Cer3) per mL of ethosomes as a modifier could significantly enhance the stability of the ethosomes, Cer3/COL-ethosomes (CCE) were successfully constructed. The CCE was then mixed with a cataplasm matrix to produce a colchicine-carrying CCE cataplasm, which demonstrated the superimposed effect of the advantages of the two dosage forms, the ethosomes and the cataplasm. Compared with the traditional delivery method of COL, this topical formulation is an attractive alternative for the treatment of gout as it can achieve effective blood levels without causing fluctuations in blood levels, and has good efficacy and higher safety profile.
研究领域:
药剂学
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生物医学
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皮肤病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Lujie Zhang,Qinghua Song,Peijing Yang,Zhanqiang Liu
Microneedle (MN) technology is a promising minimally invasive tool for interstitial skin fluid (ISF) extraction. Hydrogel MN patches enable efficient ISF extraction. However, the traditional polydimethylsiloxane (PDMS) photopolymerization method has limitations in morphology control, accuracy, and susceptibility to process parameter interference, affecting MN strength and functional consistency. To address these challenges, we propose a composite hydrogel MN patch based on Digital Light Processing (DLP) 3D bioprinting of hyaluronic acid methacryloyl (HAMA)/gelatin methacryloyl (GelMA) for high-efficiency ISF transdermal extraction. The structure and performance of the MNs were improved by optimizing the bio-ink ratio and printing parameters. Adjusting the ratio of GelMA and HAMA improved the cross-linking structure, optimizing the mechanical properties and swelling performance of the composite hydrogel. Optimizing the light intensity and exposure time ensured consistent MN morphology, resulting in well-defined and evenly distributed needle tips. Controlled UV exposure avoided defects such as uneven cross-linking or brittleness. The results showed that when the HAMA-to-GelMA ratio was 8:2, the light intensity was 9 mW/cm 2 , and the exposure time was 6 s, the MN patches demonstrated excellent microstructures and mechanical properties, with each MN enduring over 1.28 N and achieving a swelling rate above 1200 %. In vitro experiments verified effective penetration and ISF extraction, obtaining 8.5 mg of PBS in 1 min and successfully quantifying glucose concentration. In summary, this study establishes a robust MN patch with superior swelling performance and enhanced ISF extraction efficiency and provides a promising platform for minimally invasive diagnosis and real-time health monitoring.
研究领域:
生物医学工程
·
材料科学
·
药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2018
·
IF 3.466
Jun Wan,Sheng-mei Wang,Zhi-ping Gui,Zhuan-zhuan Yang,Qian-qian Shan,Xiao-qin Chu,Shuang-ying Gui,Ye Yang
The purpose of this study was examined the feasibility of using phytantriol-based cubic and hexagonal liquid crystal preparation for the percutaneous administration of trans ‑cinnamaldehyde (TCA). TCA-loaded lyotropic liquid crystal formulations were prepared and characterized, their skin permeability in vitro and in vivo was evaluated. Preliminary pharmacodynamics were also investigated in adjuvant arthritics (AA) rats. The formulations were identified respectively as cubic and hexagonal structure. The in vitro permeability study exhibited that both cubic and hexagonal liquid crystal improved the cumulative permeation quantity and permeation rates of TCA compared with home-made gel. The results of an in vivo transdermal permeability experiment showed that the area under the curve [AUC (0–∞) ] of the hexagonal and cubic liquid crystal was 1.62 and 1.53 times higher than that of the gel group, respectively. Preliminary pharmacodynamics studies indicated that the group of high-dose TCA-loaded (200 mg·kg −1 ) hexagonal liquid crystal was shown to inhibit the paw swelling of AA rats, improve synovial hyperplasia and inflammatory cell infiltration, and down-regulate the levels of serum interleukin (IL)‑1β and tumor necrosis factor (TNF)‑α. Furthermore, there was no significant difference in the anti-inflammatory effects of TCA-loaded hexagonal liquid crystal and the commercially available product Voltaren® emulgel®. Thus, hexagonal liquid crystal was considered as an effective delivery system for TCA.
研究领域:
药剂学
·
生物医学工程
·
药物递送系统
✓ 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）