Journal of Oleo Science
·
2013
·
IF 1.242
Xin Liu,Teng Chen,Xuesong Liu,Yong Chen,Longhu Wang
The present study investigated the feasibility of ostrich oil utilizing as a promising vehicle for improved skin permeation of sinomenine with reference to vaseline matrix containing different content of chemical enhancers. The fatty acid composition of ostrich oil was analyzed by GC-MS. Penetration enhancing potential of ostrich oil on permeation of sinomenine across rat abdominal skin in vitro was studied using an automatic diffusion cell apparatus. The content of sinomenine percutaneous absorbed was determined by HPLC. Various parameters viz. steady-state skin flux (Jss), permeability coefficient (kP), cumulative amount of sinomenine (Q) and enhancement ratios (ER) were calculated from the permeation data. Fick’s law of diffusion and Scheuplein kinetic were used to evaluate the transdermal absorbent enhancement of ostrich oil to sinomenine. Ostrich oil showed significant penetration effect on sinomenine compared with vaseline matrix containing different content of chemical enhancers, the density sequence as follow: 2% Azone > ostrich oil > 1% Azone plus 1% propylene glycol > 1% Azone > 3% Azone > 1% propylene glycol. The percutaneous endosmic rate constant (Jss) and permeability coefficient (kP) of sinomenine in ostrich oil through rat skin were 10.01 μg/cm2/h and 0.087, respectively. Ostrich oil produced stronger enhancement (ER = 24.31) with greater cumulative amount of drug permeated (255.53 μg/cm2) up to 24 h and caused no skin irritation. The drug release of sinomenine was coincided with Fick’s equation. In summary, ostrich oil containing fatty acids is proposed as a promising adjuvant for use in cosmetics and pharmaceuticals for improved permeation of drug.
研究领域:
药剂学
·
皮肤科学
✓ 已验证
DOI
高影响因子
JOURNAL OF MEMBRANE SCIENCE
·
2023
·
IF 9.5
Liu-Kun Wu,Zhen-Liang Xu,Min Tong,En-Chao Li,Yong-Jian Tang
In recent years, the incorporation of nanoparticles in nanofiltration membranes has received extensive attention as a practical approach to improve membrane performance. However, previous studies attributed the enhancement of TFN membrane performance primarily to the advanced properties of nanoparticles and the structural impact on the polyamide layer, while ignoring the influence and contribution of the substrate. This study provides compelling evidence that the effect on the substrate of blending nanoparticles contributes to the enhancement of membrane permeability. We quantified the changes in permeation resistance composition of the TFC and TFN membranes before and after heat treatment by a resistance-in-series model, combined with the addition of polyvinylpyrrolidone. After incorporation of ZIF-8, the permeation resistance of substrate decreased from 0.177 h bar m −1 to 0.0313 h bar m −1 after heat curing, while that of PA layer decreased from 0.1375 h bar m −1 to 0.0972 h bar m −1 . In addition, we removed the PA layer of TFC and TFN membranes by acid hydrolysis. The results indicated that the PWP of TFN membrane were continuously greater than that of the TFC membrane, which supports our conclusion that nanoparticles impacted the shrinkage of substrate during heat curing. The current study provides a novel mechanistic understanding of the improvement of TFN membrane performance by nanoparticles.
研究领域:
材料科学
·
环境工程
✓ 已验证
产品关联
DOI
高影响因子
ACS Sustainable Chemistry & Engineering
·
2022
·
IF 9.224
Zhuo Li,Yaqian He,Chunhui Li,Yuchu He,Xuwu Zhang,Song Ni,Desong Wang,Dawei Gao
The high interstitial fluid pressure at the tumor tissue is a key factor that hinders the deep penetration of nanomedicines into the tumor and affects the therapeutic effect. Herein, we designed a CaO2-based Ru nanozyme to efficiently consume the tumor interstitial fluid and enhance deep tumor penetration as well as treatment. CaO2/Ru-PDA-HA (CRPH) reached tumors via hyaluronic acid (HA)-mediated tumor targeting. Under 808 nm laser irradiation, CRPH pyrolyzed and released CaO2 and Ru, and then CaO2 would consume H2O to produce O2 and H2O2 for reducing the tumor interstitial fluid volume to promote the tumor penetration of medicines. Meanwhile, Ru nanoparticles with good peroxidase activity can decompose H2O2 to generate cytotoxic •OH. Therefore, photothermal and ROS synergistic therapy damaged deep tumor stem cells. The results showed that the relative tumor interstitial pressure was reduced to 56.34%, and the tumor inhibition rate was 99.67%. The design provides a synergetic hydrodynamic therapy strategy for enhancing the deep penetration of nanomedicines and boosting the antitumor effect.
研究领域:
肿瘤学
·
纳米医学
·
生物材料
✓ 已验证
产品关联
DOI
高影响因子
Scientific Reports
·
2016
·Vol. 6
·期 1
·1-11
·
IF 5.228
Zhao Qingliang,Dai Cuixia,Fan Shanhui,Lv Jing,Nie Liming
Salicylic acid (SA) has been frequently used as a facial chemical peeling agent (FCPA) in various cosmetics for facial rejuvenation and dermatological treatments in the clinic. However, there is a tradeoff between therapeutic effectiveness and possible adverse effects caused by this agent for cosmetologists. To optimize the cosmetic efficacy with minimal concentration, we proposed a chemical permeation enhancer (CPE) azone to synergistically work with SA on human skin in vivo . The optical properties of human skin after being treated with SA alone and SA combined with azone (SA@azone) were successively investigated by diffuse reflectance spectroscopy (DRS) and optical coherence tomography (OCT). Our results revealed that as the SA concentration increased, the light reflectance decreased and the absorption increased. We also found that SA@azone exhibited a synergistic effect on enhancing light penetration and OCT imaging depth. We demonstrated that the combination of DRS and OCT techniques could be used as a noninvasive, rapid and accurate measurement method to monitor the subtle changes of skin tissue after treatment with FCPA and CPE. The approach will greatly benefit the development of clinical cosmetic surgery, dermatosis diagnosis and therapeutic effect inspection in related biomedical studies.
研究领域:
皮肤病学
·
生物医学工程
·
化妆品科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL RESEARCH
·
2014
·Vol. 31
·期 8
·1907-1918
·
IF 3.952
Chen Yang,Cun Dongmei,Quan Peng,Liu Xiaochang,Guo Wenjia,Peng Lihua,Fang Liang
Purpose Saturated long-chain esters of isopulegol were synthesized and their activities as permeation enhancers for transdermal delivery of amlodipine and flurbiprofen were investigated, in contrast to the saturated fatty acids and isopulegol, as well as their physical mixtures. Methods
In vitro permeation experiments, confocal laser scanning microscopy (CLSM) and attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy were introduced to investigate the regulation of enhancers in the skin permeability and biophysical properties. With in vitro cytotoxicity test and in vivo erythema model, the skin irritation of enhancers was evaluated. Results The esters significantly increased the permeation of amlodipine and flurbiprofen, whereas saturated fatty acids and isopulegol had no such effect and even decreased the drug permeation when they were used alone or in combination. These results were supported by CLSM and ATR-FTIR studies, which revealed that only the esters could decrease the order of the alkyl chains in the skin lipids. Additionally, almost no skin irritation and cytotoxicity were observed for these esters. Conclusions Saturated long-chain esters of isopulegol are shown to be suitable permeation enhancers for transdermal drug delivery. Covalent attachment of isopulegol and saturated fatty acids might represent a promising strategy to design novel and potent permeation enhancers.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2023
·Vol. 24
·期 7
·1-12
·
IF 3.3
Lv Jianhua,Wu Pan,Fang Yaru,Zhang Wenchang,Liu Dongwen,Wu Mi,Shang Lei,Li Huaiguo,Zhao Yan
By selecting L-arginine as the hydrogen bond acceptor (HBA) and 2-hydroxypropyl-β-cyclodextrin (2HPβCD) as the hydrogen bond donor (HBD), deep eutectic solvents (DESs) with various water content were prepared at the 4:1 mass ratio of L-arginine to 2HPβCD with 40 to 60% of water, and were studied for its application in transdermal drug delivery system (TDDS). The hydrogen bond networks and internal chemistry structures of the DESs were measured by attenuated total reflection Fourier transform infrared (ATR-FTIR) and 1 H-nuclear magnetic resonance spectroscopy ( 1 H-NMR), which demonstrated the successful synthesis of DESs. The viscosity of DES was decreased from 10,324.9 to 3219.6 mPa s, while glass transition temperature (Tg) of the DESs was increased from − 60.8 to − 51.4 °C, as the added water was increased from 45 to 60%. The solubility of ibuprofen, norfloxacin, and nateglinide in DES with 45% of water were increased by 79.3, 44.1, and 3.2 times higher than that in water, respectively. The vitro study of transdermal absorption of lidocaine in DESs showed that the cumulative amounts of lidocaine reached 252.4 µg/cm 2 , 226.1 µg/cm 2 , and 286.1 µg/cm 2 at 8 h for DESs with 45%, 50%, and 60% of water, respectively. The permeation mechanism of DES with lower content of water (45%) was mainly by changing the fluidization of lipids, while changing the secondary structure of keratin in stratum corneum (SC) at higher water content (50% and 60%). These nonirritant and viscous fluid like DESs with good drug solubility and permeation enhancing effects have broad application prospect in the field of drug solubilization and transdermal drug delivery system. Graphical Abstract
研究领域:
药剂学
·
药物递送系统
·
药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2018
·
IF 8.097
Jianming Liang,Caifang Gao,Ying Zhu,Chengli Ling,Qi Wang,Yongzhuo Huang,Jing Qin,Jue Wang,Weigen Lu,Jianxin Wang
The unsatisfactory therapeutic outcome for glioma is mainly due to the poor blood–brain barrier (BBB) permeability and inefficient accumulation in the glioma area of chemotherapeutic agents. The existing drug delivery strategies can increase drug transport to the brain but are restricted by side effects and/or poor delivery efficiency. In this study, potent brain penetration enhancers were screened from the active components of aromatic resuscitation drugs used in traditional Chinese medicine. A novel glioma-targeting system based on enhancer-modified albumin nanoparticles was developed to safely and efficiently deliver drugs to the glioma regions in the brain. The nanoparticles improved the transport of nanoparticles across brain capillary endothelial cell (BCEC) monolayer by increasing endocytosis in endothelial cells and causing BBB disruption. In vivo imaging studies demonstrated that the systems could enter the brain and subsequently accumulate in glioma cells with a much higher targeting efficiency than that of transferrin-modified albumin nanoparticles. Of note, the nanoparticles could be captured and penetrate through endothelial cells fenestrae in pineal gland, which is suggestive of an effective way to deliver a nanosystem to the brain by bypassing the BBB. The nanoparticles showed good biocompatibility and negligible cytotoxicity. The results reveal an efficient and safe strategy for brain drug delivery in glioma therapy.
研究领域:
神经科学
·
药理学
·
纳米技术
·
中医药
·
癌症治疗
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2021
·Vol. 22
·期 5
·1-14
·
IF 3.246
Luo Zheng,Liu Chao,Quan Peng,Zhang Yimeng,Fang Liang
Chemical penetration enhancers (CPEs) are commonly added into transdermal patches to impart improved skin permeation of drug. However, significant unexplained variability in drug release kinetics in transdermal patches is possible as a result of the addition of CPEs; investigations into the underlying mechanisms are still limited. In the present study, a diverse set of CPEs was employed to draw broad conclusions. Solubility parameters of CPEs and acrylate pressure-sensitive adhesive were calculated by molecular dynamics simulation and Fedors group contribution method to evaluate drug-adhesive miscibility. CPE-adhesive interaction was characterized by FT-IR study, 13 C NMR spectroscopy, and molecular docking simulation. Results showed that release enhancement ratio ( ER R ) of CPEs for zolmitriptan was rank ordered as isopropyl myristate > azone > Plurol Oleique ® CC497 > Span ® 80 > N -methylpyrrolidone > Transcutol ® P. It was found that solubility parameter difference (Δ δ ) between CPE and adhesive was negatively related with ER R . It was proved that hydrogen bonding between CPE and adhesive would increase drug release rate, but only if the CPE showed good miscibility with adhesive. CPE like isopropyl myristate, which had good miscibility with adhesive, could decrease drug-adhesive interaction leading to the release of drug from adhesive.
研究领域:
药剂学
·
药学化学
·
生物物理学
·
材料科学
✓ 已验证
DOI
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2020
·
IF 7.727
Degong Yang,Chao Liu,Peng Quan,Liang Fang
The present study was to systematically evaluate the enhancement action efficacy and sites of chemical permeation enhancer (CPEs), which provided references for the reasonable application of CPEs and the formula optimization of transdermal patch . Enhancement action efficacy was characterized using an indicator of comprehensive enhancement effect ( ER com ). In addition, enhancement action sites were evaluated using a novel enhancement action parameter ( β R/P ), which was derived from the release enhancement effect ( ER release ) and skin permeation enhancement effect ( ER permeation ) using seven CPEs with different physicochemical properties. Then the molecular mechanism was revealed by quantitative structure−activity relationship. Hydrophilic CPEs obtained highest ER release indicated that its enhancement action site was polymer matrix according to β R/ P value (>1), due to CPEs formed the strongest hydrogen bonds with polymer, thereby undermined drug-polymer interaction according to the results of FT-IR, MDSC and molecular docking. CPEs with high log P , molecular weight and polarizability showed highest ER permeation , which indicated that its enhancement action site was skin according to its β R/ P value <1, due to it interacted with skin lipid strongly and obtained the lowest diffusion rate in skin. Thus, it increased the disruption level of highly ordered arrangement of intercellular lipid bilayers , which was characterized by ATR-FTIR, Raman, confocal laser scanning microscopy and molecular dynamics simulation. In conclusion, physicochemical properties of CPEs determined its enhancement action efficacy and sites in transdermal drug delivery process, which permitted rational selection of CPEs and the development of safer and more efficacious transdermal patch.
研究领域:
药剂学
·
药物递送系统
·
药学化学
·
分子生物学
·
生物物理学
✓ 已验证
DOI
高影响因子
ADVANCED FUNCTIONAL MATERIALS
·
2019
·Vol. 29
·期 19
·1900004
·
IF 15.621
Jinrong Peng,Qian Yang,Yao Xiao,Kun Shi,Qingya Liu,Ying Hao,Fan Yang,Ruxia Han,Zhiyong Qian
Nanomedicine constructed by therapeutics has unique and irreplaceable advantages in biomedical applications, especially in drug delivery for cancer therapy. The strategy, however, used to construct the therapeutics-based nanomedicines with tumor microenvironmental factor responsiveness is still sophisticated. In this study, an easy-operating procedure is used to construct a therapeutics-based nanosystem with active tumor-targeting, enhanced penetration, and stimuli-responsive drug release behavior as well as programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) blockading mediated immunomodulation to enhance tumor immunotherapy. The matrix metalloproteinase-2 responsive peptide with the existence of Lyp-1 sequence contributes to the success of active tumor-targeting and the enhancement of the penetration of the nanoparticles in tumor tissue. The obtained nanosystem strikingly inhibits the primary tumor growth in the first 24 h (more than 97.5% of tumor cells are inhibited), and total inhibition can be achieved with the combination of photothermal therapy. IR820, which is served as the carrier for the therapeutics, is used as a photosensitizer for photothermal therapy. The progress and aggression of distal tumor has further been alleviated by a d -peptide which is an antagonist for PD-1/PD-L1 blockage. Therefore, a therapeutics-constructed multifunctional nanosystem is provided to realize a combinational therapeutic strategy to enhance the therapeutic outcome.
研究领域:
癌症治疗
·
纳米医学
·
药学
·
免疫治疗
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
BIOMATERIALS
·
2022
·
IF 15.304
Guangzhi Li,Tao Tao,Dashi Deng,Shaohua Zhang,Yu Chao,Yizhi Dai,Yuqing Li,Ran Tao,Simin Yuan,Zhuang Liu,Song Wu
Intravesical instillation of chemotherapeutics or immune-stimulating agents could reduce the recurrence rate of non-muscle-invasive bladder cancer (NMIBC) after transurethral resection of the bladder tumors. Its efficacy, however, remains to be improved due to the bladder epithelial barrier. Although certain transmucosal delivery carriers are able to enhance the transepithelial penetration of intravesical agents, they could hardly differentiate carcinoma and adjacent normal tissues of the bladder wall. Here, we reported polyethylene glycol (PEG) & glutaraldehyde co-modified fluorinated chitosan (PGFCS) as a collagen-targeted transepithelial penetration enhancer, which could create a tumor-targeted adhesive interface by the aldehyde-selective reaction with collagen amines enriched in the tumor, thus opening the transepithelial-delivery barrier at the tumor site though the fluorinated-chitosan-mediated tight junction regulation. Interestingly, with the help of PGFCS pre-treatment, intravesical instillation of chemotherapeutics pirabucin (THP) combined with immune stimulating agent interleukin-12 could trigger potent antitumor chemoimmunotherapeutic responses in destructing orthotopic bladder tumors and inhibiting cancer recurrence. Our work presents a unique type of tumor-specific transepithelial penetration enhancer, which shows great potential for safe and effective intravesical instillation of NMIBC.
研究领域:
肿瘤学
·
药学
·
生物医学工程
·
免疫疗法
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Theranostics
·
2021
·
IF 11.556
Yan Li,Weihong Ji,Huan Peng,Ruichen Zhao,Tianlu Zhang,Zhiguo Lu,Jun Yang,Ruiyuan Liu,Xin Zhang
Insulin, a peptide hormone, is one of the most common and effective antidiabetic drugs. Although oral administration is considered to be the most convenient and safe choice for patients, the oral bioavailability of insulin is very low due to the poor oral absorption into blood circulation. Intestinal epithelium is a major barrier for the oral absorption of insulin. Therefore, it is vital to develop intestinal permeation enhancer to increase the antidiabetic efficacy of insulin after oral administration. Methods: Charge-switchable zwitterionic polycarboxybetaine (PCB) was used to load insulin to form PCB/insulin (PCB/INS) particles through the electrostatic interaction between positively charged PCB in pH 5.0 and negatively charged insulin in 0.01 M NaOH. The opening effect of PCB/INS particles on intestinal epithelium was evaluated by detecting the changes of claudin-4 (CLDN4) protein and transepithelial electrical resistance (TEER) after incubation or removal. The mechanism was further elucidated based on the results of Western blot and fluorescence images. The PCB/INS particles were then used for type 1 diabetes mellitus therapy after oral administration. Results: PCB could load insulin with the loading efficiency above 86% at weight ratio of 8:1. PCB/INS particles achieved sustained release of insulin at pH 7.4 due to their charge-switchable ability. Surprisingly, PCB/INS particles induced the open of the tight junctions of intestinal epithelium in endocytosis-mediated lysosomal degradation pathway, which resulted in increased intestinal permeability of insulin. Additionally, the opening effect of PCB/INS particles was reversible, and the decreased expression of CLDN4 protein and TEER values were gradually recovered after particles removal. In streptozotocin-induced type 1 diabetic rats, oral administration of PCB/INS particles with diameter sub-200 nm, especially in capsules, significantly enhanced the bioavailability of insulin and achieved longer duration of hypoglycemic effect than the subcutaneously injected insulin. Importantly, there was no endotoxin and pathological change during treatment, indicating that PCB/INS particles were safe enough for in vivo application. Conclusion: These findings indicate that this system can provide a platform for oral insulin and other protein drugs delivery.
研究领域:
药学科学
·
药物递送系统
·
生物药剂学
·
药理学
·
糖尿病研究
✓ 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）