Asian Journal of Pharmaceutical Sciences
·
2021
·
IF 6.598
Anpu Yang,Yanan Sun,Bochen Lyu,Binlong Chen,Zhipu Fan,Minghui Li,Yao Zhao,Jijun Fu,Bing He,Hua Zhang,Xueqing Wang,Wenbing Dai,Qiang Zhang
Photothermal (PTT) and photodynamic (PDT) combined therapy has been hindered to clinical translation, due to the lack of available biomaterials, difficult designs of functions, and complex chemical synthetic or preparation procedures. To actualize a high-efficiency combination therapy for cancer via a feasible approach, three readily available materials are simply associated together in one-pot, namely the single-walled carbon nanohorns (SWCNH), zinc phthalocyanine (ZnPc), and surfactant TPGS. The established nanodispersion is recorded as PCT. The association of SWCNH/ZnPc/TPGS was confirmed by energy dispersive spectrum, Raman spectrum and thermogravimetric analysis. Under lighting, PCT induced a temperature rising up to about 60 °C due to the presence of SWCNH, production a 7-folds of singlet oxygen level elevation because of ZnPc, which destroyed almost all 4T1 tumor cells in vitro . The photothermal effect of PCT depended on both laser intensity and nanodispersion concentration in a linear and nonlinear manner, respectively. After a single peritumoral injection in mice and laser treatment, PCT exhibited the highest tumor temperature rise (to 65 °C) among all test groups, completely destroyed primary tumor without obvious toxicity, and inhibited distant site tumor. Generally, this study demonstrated the high potential of PCT nanodispersion in tumor combined therapy.
研究领域:
纳米技术
·
癌症研究
·
治疗学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Pharmaceuticals
·
2025
·Vol. 18
·期 9
·1383
·
IF 4.8
Hongtao Han,Dan Hu,Yaoming Deng,Jiayi Song,Yuyang Sheng,Jingxin Liu,Chengyu Wu,Bin Zeng
Background:Skin whitening agents often face challenges such as poor stability and low permeability. To overcome these issues, a novel 4-butylresorcinol (4-BR)/D-a- Tocopherol Polyethylene Glycol Succinate (TPGS) deep eutectic solvent (DES) system was developed, which can self-assemble into carrier-free nanoparticles (NPs).Methods: The 4-BR/TPGS DES was synthesized and characterized by theoretical calculations, DSC, FTIR, 1H-NMR, and 2D NMR to confirm its successful formation.Results: The self-assembled 4-BR/TPGS DES NPs showed a 3.46-fold increase in skin permeability, a 1.53-fold improvement in 4-BR stability, a 1.55-fold increase in melanin inhibition in B16 cells, and a 2.16-fold higher melanin suppression in zebrafish compared with traditional 4-BR oil-based formulations. These results indicated the excellent whitening efficacy and transdermal delivery potential of this formulation.Conclusions: The combination of TPGS-based DES and self-assembly technology represents a revolutionary approach for advanced transdermal delivery and the development of skin care products.
研究领域:
药用纳米技术
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透皮药物递送
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美容药剂学
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皮肤病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2020
·
IF 4.902
Xiaojing Xia,Jin Tao,Zhuwa Ji,Chencheng Long,Ying Hu,Zhiying Zhao
The aim of this work is to apply Solutol® HS15 and TPGS to prepare self-assembled micelles loading with ginsenoside Rh2 to increase the solubility of ginsenoside Rh2, hence, improving the antitumor efficacy. Ginsenoside Rh2-mixed micelles (Rh2-M) were prepared by thin film dispersion method. The optimal Rh2-M was characterized by particle size, morphology, and drug encapsulation efficiency. The enhancement of in vivo anti-tumor efficacy of Rh2-M was evaluated by nude mice bearing tumor model. The solubility of Rh2 in self-assembled micelles was increased approximately 150-folds compared to free Rh2. In vitro results demonstrated that the particle size of Rh2-M is 74.72 ± 2.63 nm(PDI = 0.147 ± 0.15), and the morphology of Rh2-M is spherical or spheroid, and the EE% and LE% are 95.27 ± 1.26% and 7.68 ± 1.34%, respectively. The results of in vitro cell uptake and in vivo imaging showed that Rh2-M could not only increase the cell uptake of drugs, but also transport drug to tumor sites, prolonging the retention time. In vitro cytotoxicity and in vivo antitumor results showed that the anti-tumor effect of Rh2 can be effectively improved by Rh2-M. Therefore, Solutol® HS15 and TPGS could be used to entrapping Rh2 into micelles, enhancing solubility and antitumor efficacy.
研究领域:
药学
·
肿瘤学
·
纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2019
·
IF 8.456
Yi Zhang,Qiaoqiao Zhou,Shuxin Jia,Kunpeng Lin,Guangfang Fan,Jintao Yuan,Shuling Yu,Jiahua Shi
A kind of specific cyclodextrin polyrotaxanes (PRs) drug delivery system was developed for an effective drug delivery and enhancing antitumor effect. In this work, we prepared the PR by using α-CD derivatives and dicarboxyl-PEG (Mn = 4200) self-assembling and end-capping with β-CD derivatives. Then, we chose d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) with an antitumor effect to modify the PR. The modified PRs have a certain anticancer effect and can assist the anticancer drug to treat cancer. The 10-hydroxycamptothecin (HCPT) was combined to the specific PRs by covalent bonds to prepare drug-loaded specificity PRs (PR-TPGS-HCPT). The enhanced antitumor activities of PR-TPGS-HCPT were studied by in vitro and in vivo experiments, and the experiment results proved that the TPGS could effectively assist the drug to treat cancer and prolong the lifetime of the tumor-bearing mice. Therefore, this research provides a promising drug-loaded material for the cancer treatment and the specific water-soluble PRs will have potential applications in the biomedical field.
研究领域:
药学
·
生物医学工程
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2025
·
IF 9.8
Yitong Wang,Keyu Qiu,Ruizi Zhou,Shuxian Bai,Chao Ai,Yanan Zhao,Jesus Simal-Gandara,Hui Teng,Lei Chen
Naringin (NRG), despite their demonstrated health benefits as natural bioactive compounds, are hampered by intrinsic hydrophobicity, which consequently impedes processability in aqueous systems and severely constrains oral bioavailability. The aim of this study was to form different type nanoparticles by Zein, TPGS and NRG, nanoparticles were obtained by the anti-solvent method, and to analyze the internal interaction forces, stability and antioxidative. The sequence of the antisolvents used becomes the primary factor influencing the properties of the nanoparticles. Nanoparticles were characterized by multimodal analysis, as spectroscopy, molecular docking, SEM, XRD, FTIR, TGA, and ITC. NRG is stabilized within the Zein matrix through hydrogen bonding involving Gln residues and hydroxyl or carbonyl groups, coupled with hydrophobic sequestration of its aglycone moiety in Pro-rich nonpolar cavities. The encapsulation efficiency of NRG increased up to 72.71 % at ( Z -N)-T, which is the highest stability among different types of nanoparticles. The nanoparticles average size below 105 nm, and the zeta potential is 25.48 mV, and also exhibits significant antioxidant activity. This study architected Zein-based nanoparticles to methodically assess the interaction force and stability, pioneering a formulation approach for engineered carriers in food and drug delivery matrices.
研究领域:
纳米技术
·
药物递送
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食品科学
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药物制剂
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胶体与界面化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2019
·
IF 3.845
Li Hong,Yan Liping,Tang Edith K.Y.,Zhang Zhen,Chen Wei,Liu Guohao,Mo Jingxin
Curcumin (CCM) has many potential uses in anticancer chemotherapy, but its low water solubility poses a major problem, preventing its translation into clinical use. TPGS is a water-soluble derivative of vitamin E that acts as a surfactant with the ability to form micellar nanoparticles in water. More importantly, TPGS acts as a potent antioxidant that can neutralize intracellular reactive oxygen species (ROS). In this study, we solubilized CCM with TPGS using thin-film rehydration to prepare aqueous formulations containing CCM at clinically relevant concentrations. We found that the minimal TPGS:CCM ratio for producing nanoparticles was 5:1 (w/w): at or above this ratio, stable nanoparticles formed with an average particle diameter of 12 nm. CCM was released from TPGS/CCM micelles in simulated colonic and gastric fluids. These TPGS/CCM nanoparticles were shown to decrease intracellular ROS levels and apoptosis and inhibited migration of HT-29 human colon cancer cells more potently than free CCM. Pharmacokinetic analysis showed TPGS/CCM to be more bioavailable than free CCM after oral administration to rats. Our results suggest that TPGS/CCM may increase therapeutic efficacy of CCM against colon cancer and merits further investigation in a clinical setting.
研究领域:
药学
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纳米技术
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癌症研究
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Siyuan Xu,Xinya Huang,Yanyan Wang,Jianping Liu,Wenli Zhang
Recombinant high-density lipoprotein (rHDL) as anti-atherosclerosis (AS) vehicle has unique advantages including multiple anti-atherogenic functions and homing features to plaques. However, rHDL may be converted into dysfunctional forms due to complex treatment during preparation. Herein, oxidation-induced dysfunction of non-split HDL and rHDL was initially investigated. It was found that although both non-split HDL and rHDL showed oxidative dysfunction behavior, non-split HDL demonstrated superior oxidation defense compared to rHDL due to its intact composition and avoidance of overprocessing such as split and recombination. Unfortunately, in vivo oxidative stress could compromise the functionality of HDL. Therefore, surface engineering of non-split HDL and rHDL with cascade antioxidant enzyme analogues Ebselen and mitochondrial-targeted TPGS-Tempo was conducted to construct a dual-line defense HDL nano system ( i.e. , T@E-HDLs/rHDL), aiming to restore plaque redox balance and preserving the physiological function of HDL. Results indicated that both T@E-HDLs and rHDLs performed without distinction and exhibited greater resistance to oxidative stress damage as well as better functions than unmodified HDLs in macrophage foam cells. Overall, the modification of dual antioxidants strategy bridges the gap between non-split HDL and rHDL, and provides a promising resolution for the dilemmas of oxidative stress in plaques and HDL self dysfunction.
研究领域:
心血管科学
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药学
·
生物技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2024
·
IF 5.4
Huan Sun,Shen Yan,Chaojie Wu,Jingye Ma,Kangwei Lu,Xi Cheng,Wenqi Yan,Shengyu Zhang,Xiao Dong Chen,Winston Duo Wu
Active pharmaceutical ingredient (API) embedded dry powder for inhalation (AeDPI) shows higher drug loading and delivery dose for directly treating various lung infections. Inspired by the dandelion, we propose a novel kind of AeDPI microparticle structure fabricated by spray freeze drying technology, which would potentially enhance the alveoli deposition efficiency. When inhaling, such microparticles are expected to be easily broken-up into fragments containing API that acts as ‘seed’ and could be delivered to alveoli aided by the low density ‘pappus’ composed of excipient. Herein, itraconazole (ITZ), a first-line drug for treating pulmonary aspergillosis, was selected as model API. TPGS, an amphiphilic surfactant, was used to achieve stable primary ITZ nanocrystal (INc) suspensions for spray freeze drying. A series of microparticles were prepared, and the dandelion-like structure was successfully achieved. The effects of feed liquid compositions and freezing parameters on the microparticle size, morphology, surface energy, crystal properties and in vitro aerosol performance were systematically investigated. The optimal sample (SF (-50) D-INc 7 Leu 3 -2) in one-way experiment showed the highest fine particle fraction of ~ 68.96% and extra fine particle fraction of ~ 36.87%, equivalently ~ 4.60 mg and ~ 2.46 mg could reach the lung and alveoli, respectively, when inhaling 10 mg dry powders. The response surface methodology (RSM) analysis provided the optimized design space for fabricating microparticles with higher deep lung deposition performance. This study demonstrates the advantages of AeDPI microparticle with dandelion-like structure on promoting the delivery efficiency of high-dose drug to the deep lung.
研究领域:
药学
·
生物医学工程
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材料科学
·
呼吸医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2015
·
IF 6.723
Ning Han,Qinfu Zhao,Long Wan,Ying Wang,Yikun Gao,Pu Wang,Zhanyou Wang,Jinghai Zhang,Tongying Jiang,Siling Wang
Multidrug resistance (MDR) is known to be a great obstruction to successful chemotherapy, and considerable efforts have been devoted to reverse MDR including designing various functional drug delivery systems. In this study, hybrid lipid-capped mesoporous silica nanoparticles (LTMSNs), aimed toward achieving stimuli-responsive drug release to circumvent MDR, were specially designated for drug delivery. After modifying MSNs with hydrophobic chains through disulfide bond on the surface, lipid molecules composing polymer d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) with molar ratio of 5:1 were subsequently added to self-assemble into a surrounded lipid layer via hydrophobic interaction acting as smart valves to block the pore channels of carrier. The obtained LTMSNs had a narrow size distribution of ca. 190 nm and can be stably dispersed in body fluids, which may ensure a long circulating time and ideal enhanced permeability and retention effect. Doxorubicin (DOX) was chosen as a model drug to be encapsulated into LTMSNs. Results showed that this hybrid lipid-capped mesoporous silica drug delivery system can achieve redox and pH-responsive release of DOX, thereby avoiding the premature leakage of drug before reaching the specific site and releasing DOX within the cancerous cells. Owing to the presence of TPGS-containing lipid layer, LTMSNs–DOX exhibited higher uptake efficiency, cytotoxicity, and increased intracellular accumulation in resistant MCF-7/Adr cells compared with DOX solution, proving to be a promising vehicle to realize intracellular drug release and inhibit drug efflux.
研究领域:
纳米医学
·
药物递送系统
·
癌症治疗
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Nanoscale
·
2017
·Vol. 9
·期 25
·8781-8790
·
IF 7.367
Yuxin Xing,Jixi Zhang,Feng Chen,Junjie Liu,Kaiyong Cai
Theranostic agents for combined chemo-photothermal therapy have attracted intensive interest in the treatment of multi-drug resistance (MDR) in cancer therapy. However, the development of simple theranostic agents as dual hosts for both heat and a high payload of chemotherapeutic agents remains a big challenge. Herein, mesoporous polydopamine nanoparticles (MPDA) were successfully developed with properties of a high payload of DOX (up to 2000 μg mg−1) and the drug efflux inhibitor TPGS (D-α-tocopheryl polyethylene glycol 1000 succinate), as well as strong near-infrared absorption. Particularly, DOX and TPGS were sequentially loaded in the pore space and on the external particle surface of MPDA via π–π stacking and hydrophobic interactions, resulting in a MPDA–DOX@TPGS complex. The DOX release observably relies on the pH value and glutathione (GSH). Furthermore, it is possible to accelerate the rate of drug release by NIR irradiation. Importantly, the MPDA–DOX@TPGS complex was found to escape from endosomes after cellular uptake and release the loaded drugs into the cytosol. By TPGS mediated MDR reversal, the delivered DOX induced significant cytotoxicity to MCF-7/ADR cells. Besides, MPDA can absorb the NIR light and convert it into fatal heat to kill the cancer cells. As a consequence, the combined therapy in our system yields a synergistic effect with high therapeutic efficacy.
研究领域:
癌症治疗
·
纳米医学
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2017
·
IF 7.504
Ye Zhang,Congjun Zhang,Jing Chen,Li Liu,Mengyue Hu,Jun Li,Hong Bi
Multidrug resistance (MDR) has been recognized as a major obstacle to successful chemotherapy for cancer in the clinic. In recent years, more and more nanoscaled drug delivery systems (DDS) are constructed to modulate drug efflux protein (P-gp) and deliver chemotherapeutic drugs for overcoming MDR. Among them, d-α-tocopheryl polyethylene glycol succinate (TPGS) has been widely used as a drug carrier due to its capability of inhibiting overexpression of P-gp and good amphiphilicity favorable for improving permeation and long-circulation property of DDS. In the present work, a novel kind of mitochondria-targeting nanomicelles-based DDS is developed to integrate chemotherapeutics delivery with fluorescence imaging functionalities on a comprehensive nanoplatform. The mitochondria-targeting nanomicelles are prepared by self-assembly of triphenylphosphine (TPP)-modified TPGS and fluorescent carbon quantum dots (CQDs) in an n-hexane/H2O mixed solution, named CQDs-TPGS-TPP. Notably, although the drug loading content of doxorubicin (DOX) in the as-prepared nanomicelles is as low as 3.4%, the calculated resistant index (RI) is greatly decreased from 66.23 of free DOX to 7.16 of DOX-loaded nanomicelles while treating both parental MCF-7 cells and drug-resistant MCF-7/ADR cells. Compared with free DOX, the penetration efficiency of DOX-loaded nanomicelles in three-dimensional multicellular spheroids (MCs) of MCF-7/ADR is obviously increased. Moreover, the released DOX from the nanomicelles can cause much more damage to cells of drug-resistant MCs. These results demonstrate that our constructed mitochondria-targeting nanomicelles-based DDS have potential application in overcoming MDR of cancer cells as well as their MCs that mimic in vivo tumor tissues. The MDR-reversal mechanism of the DOX-loaded CQDs-TPGS-TPP nanomicelles is also discussed.
研究领域:
药学
·
纳米技术
·
癌症研究
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Biomaterials Science & Engineering
·
2018
·
IF 4.432
Zhaoxu Meng,Liping Zhang,Zhonggui He,He Lian
The integration of noninvasive photodynamic therapy (PDT) and imaging in the gastrointestinal tract is extremely challenging because of the limited light penetration in traditional PDT, and physiological barriers such as inorganic salts and mucous layers. Herein, d-α-tocopherol polyethylene glycol 1000 succinate-succinic acid-mercapto-ethylamine (TPGS-SH) was used to functionalize upconverting nanoparticles (UCNPs) and endow the modified UCNPs@TPGS-SH nanoparticles with excellent hydrophilic properties, biocompatibility, gastrointestinal stability and mucus penetration. After loading the photosensitizer zinc phthalocyanine (ZnPC) onto UCNPs@TPGS-SH, the resulting nanosystem ZnPC-UCNPs@TPGS-SH converted near-infrared light (NIR) to visible light, which activated ZnPC to generate singlet oxygen that showed a strong killing effect in Caco-2 cells. In-situ mucosal penetration assay showed that ZnPC-UCNPs@TPGS-SH accumulated more in the enterocytes of duodenum, jejunum and ileum, and less in the mucosal layer compared to ZnPC-UCNPs@TPGS. Moreover, cellular uptake and in situ tracing experiments confirmed that the florescent light emitted by UCNPs upon upconversion of deep penetrating NIR light could also serve as an imaging probe. These findings demonstrate the promising potential of this theranostic nanosystem for simultaneous deep penetrating biological tracing and PDT in gastrointestinal cancer.
研究领域:
纳米技术
·
生物医学工程
·
癌症研究
·
药学科学
✓ 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）