Heliyon
·
2022
·
IF 3.776
Onyinyechi Lydia Ugorji,Ogochukwu Ngozi Chidimma Umeh,Chukwuma Obumneme Agubata,Dickson Adah,Nicholas Chinedu Obitte,Amarauche Chukwu
The formulation of niosomes is influenced by a number of variables, and these variables may eventually affect the formulation’s outcome. One of the elements that can influence the physico-chemical properties of niosomes is the method used in preparation of the formulation. In this study, we established if various methods of preparation have any impact on the prepared vesicles when loaded with 5-fluorouracil. Thereafter, a real-time cell assay (an in vitro cytotoxicity test) against HCT-116 colon cancer cell lines was done on an optimised batch. 5-fluorouracil loaded niosomes were prepared with either Tween 60 or Span 60 by four different methods - namely thin film hydration (TFH), reverse phase evaporation (RPE), evaporation/sonication (EVP/SON), and the ethanol injection method (EIM). In vitro evaluations were done on the formulations, and these included particle size analysis, entrapment efficiency, scanning electron microscopy (SEM), photomicrography, drug release, polydispersity index, and Fourier transform infrared spectroscopy (FTIR). The effects of the preparation method and type of non-ionic surfactants on encapsulation efficiency, particle size, and in vitro drug release of the niosomes at pH 7.4 were evaluated. An in vitro cytotoxicity test (real time cell assay (RTCA)) against HCT-116 cells was carried out using the optimised formulation. Results showed physically stable formulations. The TFH method produced the smallest particle sizes (187 nm and 482 nm), while the EVP/SON method produced the largest particle sizes (4476 nm and 9111 nm). The Tween-based niosomes prepared by TFH or RPE had higher drug entrapment. The FTIR studies of niosomal formulations showed broad peaks at wavenumbers above 3000 cm −1 , indicating strong hydrogen bonds. The RTCA showed 5-fluorouracil-loaded niosomes caused more sustained cell death compared to the pure drug and blank niosomes. The methods of preparation affected the particle size, polydispersity index, entrapment efficiency, and the physical stability of the vesicles. The thin film hydration method was more robust in the entrapped 5-fluorouracil and showed lower particle sizes when compared to all the other methods. RTCA showed sustained cell death in real time.
研究领域:
药剂学
·
肿瘤学
·
药物递送系统
·
细胞生物学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
Food Bioscience
·
2023
·
IF 5.2
Man Ding,Xuechen Zhang,Jiangying Shi,Kaili Cui,Ruipeng Yang,Fengming Liu,Shuhua Shan,Ghani Israr,Zhuoyu Li
Colorectal cancer (CRC) is one of the most common malignant tumors worldwide, occurring in the colon or rectum portion. Quinoa is a dicotyledonous plant, and the quinoa bran is the outer seed coat of quinoa. Functional molecules in plants play an important role in the treatment and alleviation of chronic diseases. In this study, quinoa bran was used as the raw material. The active components with an anti-colorectal cancer effect were extracted by acetone and separated with an AB-8 macroporous resin column, which was further identified as terpenoids by liquid-mass spectrometry (LMS), named Quinoa bran terpenoids (QBT). The yield of quinoa bran terpenoids was 0.77%. Moreover, the results showed that QBT significantly inhibited the proliferation of colorectal cancer cells DLD-1 and HCT-8 with a concentration gradient dependent manner. Respectively, the IC 50 values of DLD-1 and HCT-8 cells were 0.42 ± 0.02 and 0.54 ± 0.05 mg/mL. Further studies showed that QBT upregulated apoptosis-related proteins such as activated-caspase-3, 8, and 9. In addition, QBT decreased mitochondrial membrane potential , promoted the expression of the pro-apoptotic protein Bax, and inhibited the anti-apoptotic protein Bcl-2. The experiments showed that QBT significantly repressed the growth of tumors in nude mice . In conclusion, these results indicated that QBT largely inhibits the development of colorectal cancer to large extent through upregulation of caspase-3, 8, and 9 and reduction of mitochondrial membrane potential, and has great potential for anti-tumor progression.
研究领域:
肿瘤学
·
药理学
·
植物科学
✓ 已验证
产品关联
DOI
高影响因子
STARCH-STARKE
·
2017
·
IF 1.837
Dan-Ting Yin,Xin-Huai Zhao
The aim of this study was to assess the potential impact of 10 exogenous strains on acid production of maize resistant starch (RS) and xylo-oligosaccharides (XOS) during in vitro fermentation and on anti-colon cancer activities of fermentation products. Maize RS and XOS were fermented in vitro by the fecal extract from healthy adults in the absence and presence of one exogenous strain culture. Fermentation products were measured for their acetate, propionate, butyrate, and lactate contents, and growth inhibition on human colon carcinoma (HCT-116) cells. These strains in general conferred fermentation products with increased acetate, propionate, and butyrate contents, enhanced lactate conversion, and different growth inhibition on HCT-116 cells. Correlation analysis results demonstrated that butyrate and lactate contents of fermentation products made respective positive and negative contribution to the measured growth inhibition ( p < 0.05); however, acetate and propionate contents made an insignificant contribution to the measured growth inhibition ( p > 0.05). These results were mostly consistent with those from confirmation trials using standard acid solutions for the cells. It is highlighted that these strains had beneficial intervention in colonic fermentation of maize RS and XOS and anti-cancer activities of fermentation products, rendering lower lactate and higher butyrate contents and especially higher anti-colon cancer activities.
研究领域:
营养学
·
微生物学
·
癌症研究
·
食品科学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
·
2021
·Vol. 40
·期 1
·1-16
·
IF 11.161
Ye Lili,Chen Yaoming,Mao Jizong,Lei Xiaotian,Yang Qian,Cui Chunhui
Background The exploitation of novel nanomaterials combining diagnostic and therapeutic functionalities within one single nanoplatform is challenging for tumor theranostics. Methods We synthesized dendrimer-modified gold nanorods for combinational gene therapy and photothermal therapy (PTT) of colon cancer. Poly(amidoamine) dendrimers (PAMAM, G3) grafted gold nanorods were modified with GX1 peptide (a cyclic 7-mer peptide, CGNSNPKSC). The obtained Au NR@PAMAM-GX1 are proposed as a gene delivery vector to gene (FAM172A, regulates the proliferation and apoptosis of colon cancer cells) for the combination of photothermal therapy (PTT) and gene therapy of Colon cancer cells (HCT-8 cells). In addition, the CT imaging function of Au NR can provide imaging evidence for the diagnosis of colon cancer. Results The results display that Au NR@PAMAM-GX1 can specifically deliver FAM172A to cancer cells with excellent transfection efficiency. The HCT-8 cells treated with the Au NR@PAMAM-GX1/FAM172A under laser irradiation have a viability of 20.45%, which is much lower than the survival rate of other single-mode PTT treatment or single-mode gene therapy. Furthermore, animal experiment results confirm that Au NR@PAMAM-GX1/FAM172A complexes can achieve tumor thermal imaging, targeted CT imaging, PTT and gene therapy after tail vein injection. Conclusion Our findings demonstrate that the synthesized Au NR@PAMAM-GX1 offer a facile platform to exert antitumor and improve the diagnostic level of tumor.
研究领域:
纳米技术
·
癌症治疗
·
生物医学工程
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Shu-Fang Li,Teng-Gen Hu,Hong Wu
A colon-targeted delivery system that can efficiently deliver and release quercetin is essential to improve its bioavailability. We previously found that hydrophobic ethyl cellulose (EC) nanofibers could efficiently deliver quercetin to colon, but the release of quercetin was limited. To address this problem, hydrophilic gelatin (GN) was used as a regulator, and quercetin-loaded nanofibers with different mass ratios of EC to GN (3:1, 1:1, 1:2, 1:3) were fabricated by electrospinning. All nanofibers had a cylindrical morphology and high encapsulation efficiency (over 94 %), and there existed molecular interactions among quercetin, EC, and GN. The high GN content reduced the thermal stability of nanofibers but increased their surface wettability. Besides, these nanofibers had good stability in acidic and aqueous foods. Importantly, the release of quercetin in the simulated gastrointestinal fluid was <3 %. The addition of GN was beneficial to the release of quercetin in colon, and nanofibers with EC to GN being 1:3 had a more preferable release performance. The anticancer activity of nanofibers against HCT-116 cells was proved by inhibiting cell viability through the induction of apoptosis. Therefore, these nanofibers are potential carriers for efficient colon-targeted delivery of bioactive compounds in the food industry.
研究领域:
药学
·
生物医学工程
·
材料科学
·
癌症研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Heliyon
·
2024
·
IF 3.4
Onyinyechi Lydia Ugorji,Ikechukwu Virgilius Onyishi,Amarauche Chukwu,Anthony Amaechi Attama
5-flourouracil (5-FU) is typically modulated with leucovorin (LEU) in clinical practice to improve clinical efficacy and patient survival rates. However, this combination has undesirable side effects and makes 5-FU more toxic. Hence, integrating a vesicular system (proniosomes) with another delivery vehicle may improve drug targeting, while resolving the aforementioned drawbacks. This study aimed to engineer 5-FU/LEU proniosomes for possible delivery to the colon. The modified slurry approach was used to create drug-loaded proniosomes (150 mg/9 g of carrier) using both water-soluble (dextrin (DEX) and lactose (LAC)) and insoluble (Neusilin FH 2 (NEU)) carriers. The powdered formulations were filled into Eudragit S100 (10 %)-coated capsules or Eudragit FS 30D capsules for enteric- or colon-specific delivery. In vitro evaluations (flow properties, powder X-ray diffractometry (XRD) analysis, particle size analysis, entrapment efficiency, drug release, scanning electron microscopy (SEM), polydispersity index, Fourier transform infrared spectroscopy (FTIR), and stability studies) were performed on the formulations. An in vitro cytotoxicity test [real-time cell assay (RTCA)] against HCT-116 colon cancer cell lines was performed using the optimized formulation. In vitro evaluations showed that the nanoparticles had good physicochemical properties. RTCA studies showed sustained cell death with the formulations compared to the pure drug and placebo. The sequential drug release of the colon-targeted capsules containing 5-FU and LEU- loaded proniosomes showed negligible drug release in SGF (pH 1.2) and phosphate buffer solution (pH 6.8) (approximately 11 %) but profound drug release (>80 %) at pH 7.4. Drug-loaded proniosomes engineered for colon targeting (Eudragit S100 (10 %) capsules or Eudragit FS 30D capsules) showed good colon-specific targeting and favorable in vitro cytotoxicity profiles.
研究领域:
药剂学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Nano Materials
·
2024
·
IF 5.3
Yuchen Feng,Siyi Lu,Qi Zhao,Tianyang Sun,Yuxi Shi,Guanyue Gao,Hao Wang,Jinfang Zhi
Carbon-based nanomaterials are viewed as preferred candidates as photothermal agents in tumor photothermal therapy due to their tailored structure and excellent biocompatibility. Herein, onion-like carbon (OLC) with controlled sp2/sp3-hybridized carbon ratios was explored as an effective photothermal reagent. The OLC was synthesized through thermal annealing of nanodiamonds, with an increase of the sp2 carbon content as the annealing temperature increased. The obtained OLC demonstrated high photothermal efficiency under 808 nm laser irradiation with a maximum value of 74.36% at an annealing temperature of 1400 °C. We suggest that a well-regulated amount of sp2 carbon in the OLC provided an abundance of conjugated π bonds, leading to enhanced light absorption and electron–phonon coupling. In addition, the OLC was conjugated with polyethylene glycol (PEG) and fluorescent molecules (FITC) to visualize the cellular uptake in HCT 116. In vivo tests demonstrated that the OLC-PEG-FITC exhibited good biocompatibility and achieved photothermal killing of cancer cells upon near-infrared laser irradiation. After treatment with the OLC-based photothermal agent, tumor tissues in tumor-bearing mice were effectively ablated. Taken together, these findings confirm the potential of the developed OLC as a photothermal agent for tumor therapy.
研究领域:
纳米技术
·
生物医学工程
·
材料科学
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Shu-Fang Li,Teng-Gen Hu,Yuan-Bao Jin,Hong Wu
In this study, the feasibility of shellac nanofibers as carrier system for colonic delivery of quercetin was evaluated. Firstly, the nanofibers without and with different amounts (2.5 %, 5.0 %, and 7.5 %) of quercetin were fabricated using pure shellac as a carrier by electrospinning. The morphology of nanofibers was bead-shape confirmed by SEM. FTIR, XRD, and DSC analysis showed that quercetin was encapsulated into shellac nanofibers, forming an amorphous complex. The molecular docking simulation indicated quercetin bound well to shellac through hydrogen bonding and van der Waals forces. These nanofibers had higher thermal stability than pure quercetin, and their surface wettability exhibited a pH-responsive behavior. The loading capacity of quercetin varied from 2.25 % to 6.84 % with the increased amount of quercetin, and it affected the stability of nanofibers in food simulants by measuring the release profiles of quercetin. The shellac nanofibers had high gastrointestinal stability, with a minimum quercetin release of 16.87 % in simulated digestive fluids, while the remaining quercetin was delivered to the colon and was released gradually. Moreover, the nanofibers exerted enhanced anticancer activity against HCT-116 cells by arresting cell cycle in G0/G1 phase and inducing cell apoptosis. Overall, shellac nanofibers are promising materials for colon-targeted delivery of active compounds.
研究领域:
药学
·
纳米技术
·
药物递送系统
·
癌症研究
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2025
·
IF 4.5
Zhen Zhang,Hongbo Wang,Zhijun Zhang,Yaoyao Zhang,Huajing Sun,Xi Chen,Jiayu Gu,Yanling Gong
Small interfering RNA (siRNA)-based therapy, which silences disease-associated genes, has emerged as a potential therapeutic strategy for various disorders, including cancer. Lipid nanoparticles (LNPs) have become a leading platform for efficient siRNA delivery. SOX9, a family member of SRY-related high-mobility-group box (SOX) transcription factors, plays an important role in the pathogenesis and progression of colorectal cancer (CRC). Here, we developed cRGDfK peptide-modificed LNPs (R-LNPs) composed of DLin-MC3-DMA, DMG-PEG, DSPC, DSPE-PEG-cRGDfK, and cholesterol for the targeted delivery of SOX9 siRNA (siSOX9) in CRC treatment. The formulation, delivery, and antitumor effect on CRC in vitro and in vivo were explored. The optimized R-LNPs exhibited favorable physicochemical properties including a uniform particle size (159.6 ± 0.93 nm), low polydispersity index (PDI = 0.207 ± 0.016), near-neutral zeta potential (2.74 ± 0.35 mV), and high encapsulated efficiency (90.71 ± 1.63%). Additionally, R-LNPs demonstrated sustained and controlled in vitro release and good serum stability. The prepared R-LNPs were efficiently uptaken by HCT-116 via clathrin, lipid rafts, and caveolae dependent endocytosis and macropinocytosis. Subsequently, R-LNPs were colocalized with lysosomes before escaping into the cytoplasm, ensuring effective siRNA release. In vivo distribution studies confirmed tumor-specific accumulation for R-LNPs in HCT-116 xenograft models. Functionally, R-LNPs loading siSOX9 inhibited the proliferation, migration, and invasion of HCT-116 cells and Caco-2 cells (P < 0.05 or 0.01) and inhibited tumor growth and proliferation in tumor-bearing mice (P < 0.05 or 0.01). The antitumor effects were attributed to the silence of SOX9, which subsequently downregulated key oncogenic mediators, including β-catenin, cyclin D1, and c-Myc (P < 0.05 or 0.01). Furthermore, R-LNPs demonstrated favorable safety in in vivo application. In conclusion, our cRGDfK-modified LNPs loading siSOX9 represent a promising targeted therapeutic strategy for CRC, offering both efficacy and biocompatibility.
研究领域:
药剂学
·
肿瘤学
·
纳米技术
·
分子生物学
·
药物递送
·
生物技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2016
·
IF 7.145
Lisi Xie,Yan Tan,Zhiyong Wang,Hong Liu,Na Zhang,Chao Zou,Xin Liu,Gang Liu,Jian Lu,Hairong Zheng
RNA interference (RNAi) therapy is a promising treatment for various diseases. However, its application is still restricted by the lack of efficient and safe delivery systems. A novel siRNA delivery vehicle based on ε-caprolactone-modified polyethylenimine (PEI-CL) is presented here. The PEI-CL macromolecules with different grafting degrees were synthesized via a simple ring-opening reaction. This macromolecule strongly protects the siRNA from degradation in serum and promotes the cellular uptake and endosomal escape detected via chemical exchange saturation transfer magnetic resonance analysis and fluorescence imaging. The in vivo measurement was performed with HCT-116 colon tumor xenograft that stably expressed luciferase. The data showed that the PEI-CL/siRNA nanocomplexes elicited strong RNAi response. More interestingly, enhanced gene transfection efficiency was achieved by simultaneous cotransfection with siRNA and DNA plasmid via this novel nanosystem. Overall, our study suggests the PEI-CL macromolecule with great promise for siRNA delivery.
研究领域:
药学
·
生物技术
·
纳米技术
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2019
·
IF 3.973
Mei Shao,Cong Chang,Zuhao Liu,Kai Chen,Yimin Zhou,Guohua Zheng,Zhijun Huang,Haixing Xu,Peihu Xu,Bo Lu
A nanocarrier system of methoxypolyethylene glycol amine (mPEG-NH 2 ) functionalized polydopamine (PDA) coated hollow mesoporous silica nanoparticles (HMSNs-PDA-PEG) was developed with pH-responsive, which combined doxorubicin hydrochloride (DOX) and quercetin (QUR) to reverse multidrug resistance (MDR) and improved anticancer effects on taxol (TAX) and DOX double resistant human colorectal cancer cell line HCT-8 (HCT-8/TAX cells). Well-dispersed nanoparticles (HMSNs-PDA-PEG) were prepared with a dimension of around 170 nm. The surface morphology and chemical properties of HMSNs-PDA-PEG were also successfully characterized by transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS), thermal gravimetric analysis (TGA), X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) method, Fourier transform infrared spectroscopy (FT-IR) and dynamic light scattering (DLS). Drug release experiments results indicated that DOX and QUR (QD) loaded nanoparticles (HMSNs-PDA-PEG@QD) had similar release kinetic profiles of each drug, which all exhibited highly sensitive to pH value due to the surface PDA coating. Additionally, the HCT-8 cells or HCT-8/TAX cells were employed to assess the cellular uptake and cytotoxicity of various drug-free or drug-loaded HMSNs samples. Meanwhile, a series of biological evaluations demonstrated that the HMSNs-PDA-PEG@QD exhibited remarkable ability to overcome MDR compared with free DOX and HMSNs-PDA-PEG@DOX. Taken together, these results revealed that HMSNs-PDA-PEG@QD was suitable as a prospective and efficient drug delivery nanosystem for overcoming multidrug resistance.
研究领域:
纳米技术
·
药学
·
癌症研究
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
PROCESS BIOCHEMISTRY
·
2022
·
IF 4.885
Yanyan Qian,Li Wang,Zhiqiang Zhang,Xinxin Li,Chaofei Niu,Xiao Li,Erjuan Ning,Bingji Ma
The crude heteropolysaccharides from four forms of Rehmannia glutinosa were extracted by boiling water, then purified and named FRP, DRP, HRP and NRP, respectively. The physicochemical properties, blood-enriching and immunomodulatory activities of the heteropolysaccharides were analyzed. Mg, Ca and K were the dominant metal elements in all four fractions; galactose and galacturonic acid were the predominant monosaccharides . All fractions had good thermal stabilities . The bioactive tests showed that the levels of HCT and HGB in all four groups were significantly higher than that in the model group. In addition, FRP, DRP, HRP and NRP can significantly stimulate mRNA levels of tumor necrosis factor- α (TNF- α ), interleukin-6 (IL-6), interleukin-4 (IL-4), and interleukin-10 (IL-10). The immunomodulatory activities of HRP and NRP were better than that of DRP and FRP, while immunomodulatory activities of HRP were better than that of NRP. The results demonstrated that the heteropolysaccharides from different R. glutinosa products can improve blood-enriching activities and immunomodulatory activities. These results provide experimental evidence to justify further research of heteropolysaccharides from R. glutinosa in pharmaceuticals and functional foods.
研究领域:
药理学
·
免疫学
·
生物化学
✓ 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）