INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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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
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2024
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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
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产品关联
DOI
高影响因子
DRUG DELIVERY
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2019
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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
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2023
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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
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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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
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2025
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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
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产品关联
DOI
PubMed
高影响因子
Applied Materials Today
·
2025
·
IF 6.9
Huixian Xu,Rui Ye,Ye Zhong,Wanling Chen,Jichuan Zhang,Zhenyuan Wang,Le Du,Fan Hu,Chengyu Wu,Jiaheng Zhang
Although retinol and its derivatives are effective anti-aging substances, they can induce “retinoid dermatitis.” To solve this problem, a novel 4-t-butylcyclohexanol α-lipoic acid ionic liquid (BLA-IL) was prepared and confirmed. Retinol can be directly dissolved into BLA-IL, encapsulated into nanoparticles (NPs) and form retinoid-loaded ionic liquid NPs. In-vivo and ex-vivo studies investigated the developed formulation's safety, transdermal enhancement, and efficacy. Safety assessments revealed that BLA-IL-mediated TRPV1 antagonism was achieved. In particular, IL-NPs increase the amount of retinoid in the skin by 4.3 times compared to the free retinoid and 27 % more than NPs. Based on in vivo and in vitro experiments, BLA-IL synergistically doubled the effect of fibroblast COL-I synthesis, with upregulation to 756.9 %, simultaneously enhancing COL-I, COL3A1, and Elna gene expression and inhibiting MMP-1, reactive oxygen species, and neutrophil aggregation. Clinically, retinoid-loaded IL-NPs significantly improved wrinkles, R2, collagen intensity, ITA°, and l -value compared to free retinoid in volunteers. In conclusion, this study displayed that BLA-IL NPs could promote transdermal delivery and achieve synergistic anti-aging efficacy. It could be a promising technology combining IL and nano-technology in the pharmaceutic and cosmetic transdermal areas.
研究领域:
药剂学
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皮肤科学
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生物材料
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化妆品科学
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产品关联
DOI
高影响因子
Frontiers in Bioengineering and Biotechnology
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2025
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IF 4.8
Xiuli Cheng,Xiangyu Zhou,Wenping Wang,Jing Chen,Yikun Cao,Jia Wen,Jin Hu
Sophora alopecuroides L. empyreumatic oil (SoA oil) exhibits therapeutic potential for psoriasis and eczema but suffers from poor skin permeability and formulation challenges. To overcome these limitations, a nanoemulsion (NE) gel was developed. The NE was optimized using pseudo-ternary phase diagrams and characterized for droplet size, polydispersity index (PDI), zeta potential, and rheological properties. Skin permeability and retention were assessed in vitro using Franz diffusion cells, with oxymatrine quantified by HPLC. In vivo skin irritation was tested on rabbit dorsal skin, and anti-biofilm activity was evaluated against Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus (MRSA). A final concentration of 5% SoA oil in the NE formulation was used for subsequent studies. The optimized SoA oil NE (the NE) had a mean droplet size of 53.27 nm, PDI of 0.236, and zeta potential of −38.13 mV. Adding 2% carbomer 940 (CP940) to the gel enhanced viscoelasticity. The NE showed superior skin permeability and higher cutaneous retention of oxymatrine. SoA oil caused moderate irritation to the skin of rabbits, while the other two formulations did not. The NE demonstrated enhanced biofilm inhibition against S. aureus at 0.09766 mg/mL, with an 8.9% rate surpassing SoA oil (2.0%) and SoA oil NE gel (the gel, 4.0%). At 12.50 mg/mL, the NE and the gel achieved slightly higher inhibition rates (81.7% and 82.1%, respectively) than SoA oil (78.3%). Notably, the NE showed significantly greater anti-biofilm effects against MRSA within the concentration range from 0.09766 to 3.12 mg/mL (P < 0.001). In mature biofilm clearance against S. aureus, the NE demonstrated a clearance rate of 4.9% at 0.09766 mg/mL, while SoA oil and the NE gel achieved clearance rates of 2.3% and 0.8%, respectively. At a higher concentration of 12.50 mg/mL, the clearance rate for the NE increased to 38.1%, significantly outperforming SoA oil (29.1%) and the NE gel (36.4%). Against MRSA, the NE and the gel displayed significantly improved clearance at 12.50 mg/mL (42.7% and 43.9%, respectively) compared to SoA oil (31.9%) (P < 0.0001). These findings highlight the potential of nanotechnology-driven delivery systems to improve the clinical application of herbal extracts for treating biofilm-associated dermatological infections.
研究领域:
药剂学
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皮肤病学
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微生物学
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产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2020
·
IF 5.115
Yun-Chun Zhao,Hai-Li Zheng,Xiao-Rong Wang,Xiao-Ling Zheng,Yue Chen,Wei-Dong Fei,Yong-Quan Zheng,Wen-Xi Wang,Cai-Hong Zheng
Background Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N′,N′-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed.Materials and Methods DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments.Results In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100–120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX.Conclusion These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.
研究领域:
药剂学
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皮肤病学
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生物材料
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2022
·
IF 5.062
Tingting Kang,Jinyi Zhao,Long Lin,Long Zhu,Zewei Zhao,Yao Huang,Xiaolong Gao,Jian Zhuang,Jingyao Sun,Daming Wu
The transdermal delivery effect of polymeric microneedles can be significantly improved with the aids of synergetic vibration. The finite element simulation software ANSYS was used to explore the skin puncturing results of microneedles under different vibration frequencies. The dynamic mechanical properties of polymeric microneedles and human skin were also investigated. Meanwhile, puncturing experiments were also performed under different vibration frequencies on abdomen of female mice using polymeric microneedles with different lengths. The results showed that the peak value of maximum equivalent stress and the plastic deformation of skin were the smallest at the vibrative frequency of 200 Hz. The maximum equivalent stresses presented 20%–50% decreases during the second puncturing cycle. Moreover, the puncturing result of longer microneedles (550 μm) is much better than that of shorter ones (350 μm) under the same vibration frequency. The average bottom diameter and penetration depth of the microchannel obtained under the conditions of 200 Hz vibration and 550 μm height microneedles were 671.03 and 367.55 μm, respectively. These results provided an experimental basis to verify the effectiveness of mechanical vibration for skin puncturing.
研究领域:
生物医学工程
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药剂学
✓ 已验证
产品关联
DOI
高影响因子
International Journal of Nanomedicine
·
2022
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IF 7.033
Jiangxiu Niu,Ming Yuan,Zhaowei Zhang,Liye Wang,Yanli Fan,Xianghui Liu,Xianming Liu,Huiyuan Ya,Yansong Zhang,Yang Xu
Background The poor skin permeation and deposition of topical therapeutic drugs is a major issue in topical drug delivery, improving this issue is conducive to improving the topical therapeutic effect of drugs. Methods In this study, octadecylamine modified hyaluronic acid (OHA) copolymer was synthesized by amide reaction technique to prepare curcumin (CUR)-loaded micelles (CUR-M) for topical transdermal administration. CUR-M was successfully prepared by dialysis, and the formulation was evaluated for particle size, zeta potential, surface morphology, entrapment effciency (EE%), drug loading (DL), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and the in vitro drug release. Additionally, in vitro skin permeation and retention, in vivo topical analgesic and anti-inflammatory activity, and skin irritation were assessed. Results The mean drug loading (DL), drug entrapment efficiency (EE), hydrodynamic diameter and zeta potential of CUR-M were 8.26%, 90.86%, 165.64 nm and −26.85 mV, respectively. CUR-M was characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR), it was found that there was an interaction between CUR and OHA, and CUR existed in CUR-M in an amorphous form. CUR-M exhibited sustained release in 48 h and good stability at 4 °C for 21days. CUR-M could significantly increase the skin penetration and retention of CUR and had better analgesic and anti-inflammatory activities in vivo when compared with CUR solution. Hematoxylin-eosin staining results revealed that the transdermal penetration mechanism of CUR-M might be related to the hydration of stratum corneum by HA. In addition, CUR-M showed no skin irritation to mouse skin. Conclusion CUR-M might be a promising and safe drug delivery system for the treatment of topical diseases.
研究领域:
药剂学
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皮肤科学
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生物材料
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产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2022
·
IF 6.819
Ming Yuan,Jiangxiu Niu,Qinghan Xiao,Huiyuan Ya,Yansong Zhang,Yanli Fan,Lingmei Li,Xueke Li
Hyaluronic acid (HA), as a hygroscopic and biocompatible molecule, has displayed unique permeation enhancement in transdermal delivery systems. Hence, indomethacin (IND) was encapsulated in HA-modified transfersomes (IND-HTs) to enhance transdermal IND delivery to reduce adverse effects in this study. The physiochemical properties of IND-HTs were characterized. Results showed that the prepared IND-HTs were spherical and revealed good entrapment efficiency (87.88 ± 2.03%), with a nanometric particle size (221.8 ± 93.34 nm). Then, IND-HTs were further incorporated into a carbopol 940 hydrogel (IND-HTs/Gel) to prolong retention capacity on the skin. The in vitro release and skin permeation experiments of IND-HTs/Gel were carried out with the Franz diffusion cells. It was found that IND-HTs/Gel exhibited sustained drug release, as well as superior drug permeation and flux across the skin. Confocal laser scanning microscopy showed improved penetration of HTs/Gel with a wider distribution and higher fluorescence intensity. The hematoxylin–eosin stained showed that HA improved the transdermal effect by changing the microstructure of skin layers and decreasing skin barrier function. In addition, IND-HTs/Gel showed significant analgesic activity in hot plate test and no potentially hazardous skin irritation. This study indicated that the developed IND-HTs/Gel could be a promising alternative to conventional oral delivery of IND by topical administration.
研究领域:
药剂学
·
皮肤科学
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生物材料
✓ 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）