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
·
生物医学工程
✓ 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
·
生物医学
·
皮肤病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PLoS One
·
2016
·Vol. 11
·期 7
·e0159967
·
IF 3.057
Zhenwei Yu,Hongyan Lv,Gang Han,Ke Ma
The aim of this study was to develop ethosomes loaded with cryptotanshinone (CPT) and formulate them as a topical gel for the treatment of acne. Ethosomes were prepared and evaluated for vesicle size, CPT loading and encapsulation efficiency. Optimized ethosomes were formulated as Carbomer 974 gels and compared with conventional hydroethanolic gels for transdermal permeation and skin deposition in vitro . The anti-acne activity and skin irritation of the gel was investigated in rabbits. Optimized ethosomes had an average vesicle size of 69.1 ± 1.9 nm with CPT loading and encapsulation efficiency of 0.445 ± 0.007 mg/mL and 40.31 ± 0.67%, respectively. The transdermal flux and skin deposition of the optimized ethosomal gel were 2.5- and 2.1-times those of conventional gels. The ethosomal gel revealed better anti-acne effect with only slight skin irritation. This study demonstrates that ethosomal formulation is an effective dermal delivery system for CPT, and that CPT ethosomal gels are promising future acne treatments.
研究领域:
药剂学
·
皮肤病学
·
纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2012
·Vol. 13
·期 2
·485-492
·
IF 1.432
Shi Jun,Wang Yiming,Luo Guoan
In the present study, we have investigated transdermal administration of ligustrazine phosphate (LP), as an antioxidant, for the treatment of Alzheimer’s disease (AD). The LP transdermal ethosomal system was designed and characterized. Franz-type diffusion cells and confocal laser scanning microscopy were used for the in vitro permeation studies. Furthermore, the effect of LP transdermal ethosomal system on AD was evaluated in the scopolamine-induced amnesia rats by evaluating the behavioral performance in the Morris water maze test. The activities of the antioxidant enzymes and the levels of the lipid peroxidation product malondialdehyde (MDA) in the brain of rats were also determined. The results showed that both the penetration ability and the drug deposition in skin of the LP ethosomal system were significantly higher than the aqueous one. The LP transdermal ethosomal system could recover the activities of the antioxidant enzymes and the levels of MDA in the brain of the amnesic rats to the similar status of the normal rats, which was also indirectly reflected by the improvement in the behavioral performance. In conclusion, LP might offer a potential alternative therapeutic drug in the fight against AD, and ethosomes could be vesicles of choice for transdermal delivery of LP.
研究领域:
药理学
·
神经科学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2016
·
IF 3.994
Yibang Zhang,Weibeng Ng,Xue Feng,Fangying Cao,Huaxi Xu
Nanoscale delivery systems have been widely investigated to overcome the penetration barrier of stratum corneum for effective transcutaneous application. The aim of this study is the development of effective vesicular formulations of ovalbumin and saponin which are able to promote penetration through the skin layers. Three kinds of vesicular formulations have been investigated as carriers, including liposomes , transfersomes and ethosomes, in which cholesterol and/or cationic lipid stearylamine are incorporated. The impact of membrane composition variations on the protein entrapment has been evaluated for each vesicle type. Formulations were characterized for particle size, polydispersity and encapsulation efficiency. The best formulations for each type of vesicle were subjected to in vivo transdermal immunization in mice. Among the three kinds of vesicular carrier, ethosomal nano carrier not only showed the best stability over a two months’ storage, but also enabled the highest increase in the titer of serum antibody. In this regard, cationic nano-ethosomes can be considered as a promising vesicular carrier for transdermal vaccines. Meanwhile, we have developed a simple method to determine encapsulation efficiency of vesicular systems, which has potential application as a high throughput screening for vesicular formulations.
研究领域:
药剂学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Silicon
·
2018
·Vol. 11
·期 1
·287-292
·
IF 1.246
Kang Zhen-Wei,Gao Zhan-Chen,Lv Su-Fang,Zhang Fei-Bao,Jiang Jian-Xiong
Palladium nanocatalysts supported on commercial fumed silica were synthesized via a convenient liquid method without any external reductant or surfactants. The catalysts were characterized by inductively coupled plasma-mass spectrometry, X-ray powder diffraction and the transmission electron microscope analysis. Then it was applied for Suzuki-Miyaura cross-coupling reactions. It was found that a number of aryl halides were efficiently catalyzed using these catalysts in aqueous-ethanol under relatively mild condition within 0.5h. Further study showed that the catalyst could be recycled up to 10 times without loss of activity.
Palladium nanocatalysts supported on commercial fumed silica were synthesized and applied for Suzuki-Miyaura cross-coupling reactions. A number of aryl halides were efficiently catalyzed using these catalysts in aqueous-ethanol under relatively mild condition within 0.5h. Further study showed that the catalyst could be recycled up to 10 times without loss of activity.
研究领域:
催化化学
·
材料科学
·
绿色化学
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产品关联
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2018
·
IF 8.097
Zheng Zhang,Ying Liu,Yunsheng Chen,Lexiang Li,Ping Lan,Dannong He,Jie Song,Yixin Zhang
5-Aminolevulinic acid (ALA)-loaded nanoethosome (ALA-ES) gels are successfully prepared to realize a transdermal delivery of ALA, and they provide a feasible approach for the photodynamic therapy (PDT) of hypertrophic scars (HS). Herein, the morphological and physicochemical features indicate that ALA-ES is stable in gel matrix. In vitro transdermal penetration studies suggest ALA-ES gels can overcome the compact dermal barrier and deliver more ALA into human HS tissue. In vivo delivery studies further reveal that ALA-ES gels can penetrate into rabbit HS tissue to facilitate ALA accumulating in hypertrophic scar fibroblast (HSF) and converting into protoporphyrin IX in the cytoplasm. Utilizing transmission electron microscopy, the visual in vivo penetration process indicates ALA-ES penetrate into HS tissue utilizing its deformable membrane, enters HSF by a pinocytotic-like mechanism, and then releases ALA in the cytoplasm. Subsequently, PDT efficacy is assessed using rabbit HS models. The morphological and histological analysis reveal that ALA-ES gels can improve HS by promoting HSF apoptosis, remodelling collagen fibers and increasing MMP3 expression. The results demonstrate that ALA-ES gels are suitable in clinical treatment of HS and make a substantial progress within the field.
研究领域:
药剂学
·
医学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2024
·
IF 4.9
Miaomiao Zi,Jiming Ke,Suping Jiang,Xinge Cui,Jing Zhang,Shujie Yuan,Shan Huang,Jie Wang,Huanhuan Liu,Jiwen Zhang,Can Peng
Colchicine (COL) is the primary medication for treating an acute gout attack, however, it has a narrow therapeutic index and can cause mild to severe gastrointestinal side effects when administered orally. To address this, transethosomes (TEs) were developed as a transdermal drug delivery vehicle for COL in order to promote permeability. Studies have shown that TEs can disrupt the multilamellar and organized lipid domains of the skin, alter the structure of keratin, and increase the fluidity of the stratum corneum (SC), which facilitates the penetration of COL into the deeper layers of the skin. Additionally, ethanol has been found to play a role in the infiltration process, but is not the sole driving force. Results have demonstrated that COL-TEs have higher transdermal efficiency, increased drug permeability, longer skin retention time, and better biocompatibility than the COL water solution and the 40% ethanol COL-solution. Furthermore, the drug was found to effectively reduce inflammatory cytokine levels, thus providing the expected therapeutic effects.
研究领域:
药剂学
·
药物递送系统
·
药理学
·
炎症
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2024
·Vol. 22
·期 1
·1-21
·
IF 10.6
Wang Pengyu,Hong Shihao,Cao Can,Guo Shijie,Wang Chen,Chen Xi,Wang Xinnan,Song Ping,Li Ning,Xu Ruodan
Psoriasis is a chronic, relapsing, and refractory immune-mediated skin disease with the etiology and pharmaceutical targets remaining unsatisfactorily addressed. Topical herbal-derived compounds, such as tryptanthrin (Tryp), have been considered as an alternative therapy for psoriasis due to their lower costs and fewer side effects compared to other therapies. However, the effectiveness of topically administered drugs is substantially limited by the thickened pathological skin barrier and the low bioavailability of drugs in the deeper layers of the lesion. Ethosomes, being a novel phospholipid-based vesicle system with high content of ethanol, have been implicated in enhancing topical drug absorption and restoring psoriatic lesions. In this study, taking advantages of ethosomes as a soft and malleable drug carrier, we constructed the Tryp-loaded ethosome (Tryp-ES) through a one-step microfluidics-based technique. The optimal formulation of Tryp-ES was achieved by adding amino-acid-derived surfactant sodium lauroyl glutamate, and Tryp-ES exhibited homogeneous particle size and favorable stability at room temperature. In vitro evaluations showed that Tryp of Tryp-ES could be easily internalized into cells and accumulated in cell nuclei, hence inhibited the abnormally proliferated keratinocytes by inducing apoptosis. In vivo and in vitro assessment using psoritic skin of mice revealed that Tryp-ES had preferred skin retention and permeation of loaded drugs within the initial 1 h of topical administration, which could be attributed to transient disintegrations of cell membranes by ethosomes, thus improved cellular fluidity and permeability. Notably, a synergistic effect of ethosomes and Tryp was found in psoriatic mice. Tryp-ES-treated mice showed substantially ameliorated symptoms of psoriasis and reduced pathological alterations due to hyperplasia, inflammation and angiogenesis, without detectable local or systemic toxicities. Interestingly, lipidomics analysis confirmed that the supplementation of phospholipids, as in the form of ethosome vehicles, was an alterantive strategy to relieve psoriatic pathologies. Taken together, this study provides a novel impact for ethosomal topical delivery of Tryp and underlines their potential as an effective therapy for the management of psoriasis.
研究领域:
药学
·
皮肤病学
·
纳米技术
·
药理学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Nanoscale
·
2017
·Vol. 9
·期 19
·6362-6369
·
IF 7.367
Xue Wang,Libo Zhou,Yunling Liu,Shengyan Yin,Zhen-An Qiao,Qisheng Huo
Transformation from single-mesoporous to dual-mesoporous structured organosilica nanoparticles can be achieved by simply varying the volume fraction of ethanol in the synthesis system, using lauryl sulfonate betaine and sodium dodecyl sulfonate as dual-templates. Core–shell structured dual-mesoporous organosilica nanoparticles possess smaller mesopores (4.0 nm) in the shell and flower-like larger mesopores (46 nm) in the core. Owing to the unique mesostructure, dual-mesoporous organosilica nanoparticles show a high loading capacity and a slow release rate for cargo molecules. The large mesopores on the inside can provide a large storage space for the guest molecules and the small mesopores in the outer shell act as a natural valve, slowing the release. In addition, both single-mesoporous and dual-mesoporous organosilica nanoparticles, exhibit low cell toxicity and excellent cell permeability.
研究领域:
纳米医学
·
药物递送系统
·
生物材料学
·
纳米生物技术
·
药剂学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Aqin Yan,Rui Ruan,Xiaolei Zhu,Wei Qiang,Yeneng Guan,Qi Yu,Hongmei Sun,Mingxing Liu,Hongda Zhu
The most prevalent kind of hair loss is androgenic alopecia (AGA), which is characterized by hair follicle miniaturization and microenvironment dysfunction. Although topical Minoxidil (MXD) was considered to be a safe and effective treatment for AGA, excess reactive oxygen species (ROS) and lower sulfotransferase activity in the hair follicular microenvironment led to an unsatisfactory treatment of AGA. Here, we developed the ethosome (MTE) load of minoxidil and tocopherol acetate to improve the therapeutic effect of MXD on androgenic alopecia. It could regulate the microenvironment around hair follicles, promote the telogen-to-anagen transition of hair follicles, and boost hair regeneration, thus achieving a synergistic effect of 1 + 1 > 2. The results proved that MTE showed excellent stability, biosafety, and good dermal and follicular permeability in vitro . The hair regeneration ability of AGA model mice showed that the co-delivery ethosome might regulate the microenvironment around the hair follicles and improve hair regeneration in comparison to the commercial minoxidil tincture alone. As a result, the strategy provided a promising new strategy for the treatment of AGA.
研究领域:
药学
·
皮肤科
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2022
·
IF 5.062
Di Jiang,Yuxin Jiang,Kaili Wang,Zhe Wang,Yifei Pei,Jinglei Wu,Chuanglong He,Xiumei Mo,Hongsheng Wang
This study aimed to develop a strategy combining binary ethsomes (BES) and microneedles (MNs) to improve the bioavailability of drugs that are poorly bioavailable by oral administration, such as carvedilol (CL). The formula of BES was optimized by Box-Benhnken Designes from four aspects: particle size, zeta potential , encapsulation efficiency and cumulative release in vitro. The optimized BES was then mixed with polyvinylpyrrolidone and sprayed onto the silk fibroin matrix by electrospray to obtain transdermal drug delivery patches (TDDP). In vitro skin penetration test showed that, TDDP has much better transdermal drug release performance compared with free drugs, and MNs-assisted TDDP (MNs-TDDP) can deliver more drugs to the receiving chamber. In vivo studies indicate that MNs-TDDP can significantly reduce the fluctuation of CL concentration in plasma and increase serum level of NO , thereby lower blood pressure for a longer time. These results suggest that the bioavailability of CL can be greatly improved via administration of MNs-TDDP, compared with the oral route. Considering its advantages of non-invasiveness, convenience and good biosafety, MNs-TDDP has a promising prospect in improving the bioavailability of drugs for treating chronic diseases such as hypertension.
研究领域:
药剂学
·
药物递送系统
·
透皮给药
·
高血压治疗
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）