scholarly journals Synthesis, Characterization of Nano-β-Tricalcium Phosphate and the Inhibition on Hepatocellular Carcinoma Cells

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Langlang Liu ◽  
Yanzeng Wu ◽  
Chao Xu ◽  
Suchun Yu ◽  
Xiaopei Wu ◽  
...  

It is difficult to synthesize nano-β-tricalcium phosphate (nano-β-TCP) owing to special crystal habit. The aim of this work was to synthesize nano-β-TCP using ethanol-water system and characterize it by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), Malvern laser particle size analyzer, and transmission electron microscope (TEM). In addition, the inhibitory effect of nano-β-TCP on human hepatocellular carcinoma (HepG2) cells was also investigated using MTT assay, lactate dehydrogenase (LDH) leakage test, and 4′-6-diamidino-2-phenylindole (DAPI) staining. The results showed that negatively charged rod-like nano-β-TCP with about 55 nm in diameter and 120 nm in length was synthesized, and the average particle size of nano-β-TCP was 72.7 nm. The cell viability revealed that nano-β-TCP caused reduced cell viability of HepG2 cells in a time- and dose-dependent manner. These findings presented here may provide valuable reference data to guide the design of nano-β-TCP-based anticancer drug carrier and therapeutic systems in the future.

2021 ◽  
Vol 21 (2) ◽  
pp. 977-986
Author(s):  
Zhongxing Shi ◽  
Jinping Li ◽  
Hongwei Liang ◽  
Hongbo Hu ◽  
Huijie Jiang

Poly[lactic-co-glycolic] acid (PLGA) targeting nanoparticles AFP/PLGA/Dt386, loaded with Dt386 plasmid of diphtheria toxin gene, modified by Alpha fetoprotein (AFP) monoclonal antibody, is prepared. Its physical and chemical properties and its effect on HepG2 cells are studied. Firstly, Dt386 expression plasmid pET11a/Dt386 is constructed and PLGA nanoparticles are prepared by emulsion solvent evaporation (ESE). Scanning electron microscope (SEM) is used to observe its morphology. Laser Particle Sizer is used to measure the particle size. In addition, the encapsulation efficiency, drug loading and in vitro release rate of PLGA nanoparticles are measured. Carboxy fluorescein and rhodamine fluorescein are used to double label IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanospheres, respectively, the entry of nanospheres into HepG2 cells are observed at 3 h and 12 h. The effect of AFP/PLGA/Dt386 nanospheres on the migration of HepG2 cells is examined by wounding healing assay. Transwell chamber experiment is used to detect the effect of AFP/PLGA/Dt386 nanospheres on the invasion of HepG2 cells. MTT method is utilized to determine the inhibitory activity of nanoparticles on HepG2 cell proliferation. After treated with IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanoparticles for 48 hours, flow cytometry is used to detect the apoptosis rate and cell cycle of HepG2 cells in each group. The results show that the prepared nanospheres have regular morphology, flat surface, average particle size of 265.72±12.46 nm, zeta potential of −18.15 mV. The average entrapment efficiency and drug loading are 78.48±1.71% and 3.16±0.35%, respectively. The nanoparticles release slowly and stably in vitro. At the 10th day, the release rate reaches 75.13%. PLGA nanospheres can effectively protect DNA from nuclease degradation. The results show that AFP/PLGA/Dt386 nanospheres have biological targeting effect and can be enriched in cells. AFP/PLGA/Dt386 nanoparticles can significantly inhibit the migration, invasion and proliferation of HepG2 cells, and promote apoptosis.


Crystals ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 295 ◽  
Author(s):  
Tímea Tari ◽  
Piroska Szabó-Révész ◽  
Zoltán Aigner

The therapeutic usage of cilostazol is limited owing to its poor aqueous solubility and oral bioavailability. Our aim was to produce cilostazol crystals with small average particle size; besides suitable roundness, narrow particle size distribution and stable polymorphic form to increase its dissolution rate and improve processability. Different conventional crystallization methods with or without sonication were compared with impinging jet crystallization combined with cooling, and the optimization of the various parameters was also implemented. The effects of post-mixing time and temperature difference were studied by means of a full factorial design. The physical properties of powder particles were characterized by, i.a., XRPD, DSC and SEM. The dissolution rate and the contact angle of solid surfaces were also determined to elucidate the relationship between wettability and dissolution. It was observed that impinging jet crystallization combined with cooling is a very effective and reproducible method for reducing the particle size of cilostazol. This method resulted in significantly smaller particle size (d(0.5) = 3–5 μm) and more uniform crystals compared to the original ground material (d(0.5) = 24 μm) or the conventional methods (d(0.5) = 8–14 μm), and it also resulted in a stable polymorphic form and enhanced the dissolution rate.


2019 ◽  
Vol 8 (4) ◽  
pp. 111 ◽  
Author(s):  
Razakou Maman ◽  
Jianmei Yu

This study investigated the effect of particle size and chemical composition of grape seed flour (GSF) on the physical, chemical and sensory quality of cookies. Results indicate that the chemical composition of GSF varied significantly with particle sizes and smaller particle fraction had higher ash, fat, protein and extractible polyphenol contents but lower dietary fiber. Inclusion of 2.5-10% GSF in the cookie formula enhanced darkening, increased thickness and hardness, increased polyphenol and dietary fiber contents in dose-dependent manner, but reduced diameter and consumer acceptability of cookies to various degrees. The impacts of GSF on the cookie quality and sensory properties were strongly associated with the inclusion level and particle size of GSF. Higher GSF (5%) inclusion and smaller GSF particle size (104 µm) resulted in lower consumer acceptability. To minimize the undesirable effect of GSF on cookie quality, up to 5% of GSF with average particle size 209 µm is recommended.


2022 ◽  
Vol 18 ◽  
Author(s):  
Vivian Cordeiro Rodrigues ◽  
William Queiroz Felippe ◽  
Carla Marins Goulart ◽  
Aurea Echevarria ◽  
Ana Paula Pereira da Silva

Background: Chalcones are open-chain flavonoids especially attractive to medicinal chemistry due to their easy synthesis and the possibility of structural modifications. Objective: Evaluate the in vitro anticancer activity of a series of hybrids chalcones-thiosemicarbazones against the human hepatocellular carcinoma cell line, HepG2. Methods: Seven hybrid chalcones-thiosemicarbazones (CTs), 3-(4’-X-phenyl)-1-phenylprop-2-en-1-one thiosemicarbazone, where X=H (CT-H), CH3 (CT-CH3), NO2 (CT-NO2), Cl (CT-Cl), CN (CT-CN), F (CT-F) and Br (CT-Br), were synthesized and their effects on cells viability and mitochondrial oxygen consumption were accessed. Results: Incubation with CTs caused a decrease in HepG2 cells viability in a time-concentration-dependent manner. The most effective compounds in inhibiting cell viability, after 24 hours of treatment, were CT-Cl and CT-CH3 (IC50 20.9 and 23.63 μM, respectively). In addition, using 10 M and only 1 hour of pre-incubation, CT-CH3 caused a reduction in basal respiration (-37%), oxygen consumption coupled with ATP synthesis (-60%) and maximum oxygen consumption (-54%). These alterations in respiratory parameters may be involved with the inhibitory effects of CT-CH3, since significant changes in oxygen consumption rates were observed in a condition that anticipates more significant losses of cell viability. The ADME parameters and the no violation of Lipinski Rule of Five showed that all compounds are safe. Conclusion: These results may contribute to the knowledge about the effects of CTs on these cells and the development of new treatments against HCCs.


2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Hongjun Liu ◽  
Yiru Wang ◽  
Bing Chen ◽  
Xia Shen ◽  
Wenxian Li

Lidocaine displays antitumor activity by inducing apoptosis and suppressing tumor growth in human hepatocellular carcinoma (HepG2) cells in vitro. However, the molecular mechanism underlying lidocaine-mediated antitumor activity is unclear. In this study, HepG2 cells were treated with lidocaine, and cell proliferation and colony-forming ability were assessed. The expression level of cytoplasmic polyadenylation element binding protein 3 (CPEB3) was detected by real-time quantitative PCR and western blot. Lidocaine treatment resulted in decreased HepG2 cell viability and colony formation in a dose-dependent manner. In hepatocellular carcinoma patient samples, CPEB3 was downregulated and was associated with poor prognosis and high-grade malignancy. Additionally, CPEB3 was a critical mediator of lidocaine-induced repression of HepG2 cell proliferation. These results demonstrated that lidocaine decreased cell viability and colony-forming ability of HepG2 cells by upregulating CPEB3 expression.


1970 ◽  
Vol 26 (1) ◽  
pp. 16 ◽  
Author(s):  
S Balasubramanian ◽  
Rajkumar Rajkumar ◽  
K K Singh

Experiment to identify ambient grinding conditions and energy consumed was conducted for fenugreek. Fenugreek seeds at three moisture content (5.1%, 11.5% and 17.3%, d.b.) were ground using a micro pulverizer hammer mill with different grinding screen openings (0.5, 1.0 and 1.5 mm) and feed rate (8, 16 and 24 kg h-1) at 3000 rpm. Physical properties of fenugreek seeds were also determined. Specific energy consumptions were found to decrease from 204.67 to 23.09 kJ kg-1 for increasing levels of feed rate and grinder screen openings. On the other hand specific energy consumption increased with increasing moisture content. The highest specific energy consumption was recorded for 17.3% moisture content and 8 kg h-1 feed rate with 0.5 mm screen opening. Average particle size decreased from 1.06 to 0.39 mm with increase of moisture content and grinder screen opening. It has been observed that the average particle size was minimum at 0.5 mm screen opening and 8 kg h-1 feed rate at lower moisture content. Bond’s work index and Kick’s constant were found to increase from 8.97 to 950.92 kWh kg-1 and 0.932 to 78.851 kWh kg-1 with the increase of moisture content, feed rate and grinder screen opening, respectively. Size reduction ratio and grinding effectiveness of fenugreek seed were found to decrease from 4.11 to 1.61 and 0.0118 to 0.0018 with the increase of moisture content, feed rate and grinder screen opening, respectively. The loose and compact bulk densities varied from 219.2 to 719.4 kg m-3 and 137.3 to 736.2 kg m-3, respectively.  


2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.


2020 ◽  
Vol 17 ◽  
Author(s):  
Mohammad Hossain Shariare ◽  
Tonmoy Kumar Mondal ◽  
Hani Alothaid ◽  
Md. Didaruzzaman Sohel ◽  
MD Wadud ◽  
...  

Aim: EPAS (evaporative precipitation into aqueous solution) was used in the current studies to prepare azithromycin nanosuspensions and investigate the physicochemical characteristics for the nanosuspension batches with the aim of enhancing the dissolution rate of the nanopreparation to improve bioavailability. Methods: EPAS method used in this study for preparing azithromycin nanosuspension was achieved through developing an in-house instrumentation method. Particle size distribution was measured using Zetasizer Nano S without sample dilution. Dissolved azithromycin nanosuspensions were also compared with raw azithromycin powder and commercially available products. Total drug content of nanosuspension batches were measured using an Ultra-Performance Liquid Chromatography (UPLC) system with Photodiode Array (PDA) detector while residual solvent was measured using gas chromatography (GC). Results: The average particle size of azithromycin nanosuspension was 447.2 nm and total drug content was measured to be 97.81% upon recovery. Dissolution study data showed significant increase in dissolution rate for nanosuspension batch when compared to raw azithromycin and commercial version (microsuspension). The residual solvent found for azithromycin nanosuspension is 0.000098023 mg/ mL or 98.023 ppb. Conclusion: EPAS was successfully used to prepare azithromycin nanoparticles that exhibited significantly enhanced dissolution rate. Further studies are required to scale up the process and determine long term stability of the nanoparticles.


Materials ◽  
2021 ◽  
Vol 14 (8) ◽  
pp. 2003
Author(s):  
Wei Xu ◽  
Jintao Wei ◽  
Zhengxiong Chen ◽  
Feng Wang ◽  
Jian Zhao

The type and fineness of a filler significantly affect the performance of an asphalt mixture. There is a lack of specific research on the effects of filler fineness and dust from aggregates on the properties of epoxy asphalt (EA) mixtures. The effects of aggregate dust and mineral powder on the properties of an EA mixture were evaluated. These filler were tested to determine their fineness, specific surface area and mineral composition. The effects of these fillers on the EA mastic sample and mixture were evaluated. The morphology of the EA mastic samples was analyzed using scanning electron microscopy (SEM). The effects of the fillers on the Marshall stability, tensile strength and fatigue performance of the EA mixture were evaluated. The dust from the aggregates exhibited an even particle size distribution, and its average particle size was approximately 20% of that of the mineral powder. The SEM microanalysis showed that the EA mastic sample containing relatively fine dust formed a tight and dense interfacial bonding structure with the aggregate. The EA mixture sample containing filler composed of dust from aggregate had a significantly higher strength and longer fatigue life than that of the EA sample containing filler composed of mineral powder.


2021 ◽  
Vol 13 (15) ◽  
pp. 8122
Author(s):  
Shijie Tian ◽  
Weiqiang Tan ◽  
Xinyuan Wang ◽  
Tingting Li ◽  
Fanhao Song ◽  
...  

Surface activity of humic acid (HA) and its six sub-fractions isolated from forest soil were characterized by surface tension measurements, dynamic light scattering, and laser doppler electrophoresis. The surface tension of HA and its sub-fractions reduced from 72.4 mN·m−1 to 36.8 mN·m−1 in exponential model with the increasing concentration from 0 to 2000 mg·L−1. The critical micelle concentration (CMC) and Z-average particle size ranged from 216–1024 mg·L−1 and 108.2–186.9 nm for HA and its sub-fractions, respectively. The CMC have related with alkyl C, O-alkyl C, aromatic C, and carbonyl C (p < 0.05), respectively, and could be predicted with the multiple linear regression equation of CMC, CMC = 18896 − 6.9 × C-296 × alkyl C-331 × aromatic C-17019 × H/C + 4054 × HB/HI (p < 0.05). The maximum particle size was 5000 nm after filtered by a membrane with pore size of 450 nm, indicating HA and its sub-fractions could progressed self-assembly at pH 6.86. The aggregate sizes of number-base particle size distributions were mainly in six clusters including 2 ± 1 nm, 5 ± 2 nm, 10 ± 3 nm, 21 ± 8 nm, 40 ± 10 nm, and >50 nm analyzed by Gaussian model that maybe due to the inconsistency of the components and structures of the HA sub-fractions, requiring further study. It is significance to explore the surface activity of HA and its sub-fractions, which is helpful to clarify the environmental behavior of HA.


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