In vitro antitumor efficacy of berberine: solid lipid nanoparticles against human HepG2, Huh7 and EC9706 cancer cell lines

2016 ◽  
Author(s):  
Xiang-Ping Meng ◽  
Xiao Wang ◽  
Huai-ling Wang ◽  
Tong-sheng Chen ◽  
Yi-fei Wang ◽  
...  
Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 131
Author(s):  
Hamdan N. Alajami ◽  
Ehab A. Fouad ◽  
Abdelkader E. Ashour ◽  
Ashok Kumar ◽  
Alaa Eldeen B. Yassin

This work aimed to optimize a celecoxib (CXB)-loaded solid lipid nanoparticles (SLN) colon delivery system for the enhancement of anticancer activity. An ultrasonic melt-emulsification method was employed in this work for the preparation of SLN. The physical attributes were characterized for their particle sizes, charges, morphology, and entrapment efficiency (%EE), in addition to DSC and FTIR. The in vitro drug release profiles were evaluated, and the anticancer activity was examined utilizing an MTT assay in three cancer cell lines: the colon cancer HT29, medulloblastoma Daoy, and hepatocellular carcinoma HepG2 cells. All of the prepared SLN formulations had nanoscale particle sizes ranging from 238 nm to 757 nm. High zeta-potential values (mv) within −30 s mv were reported. The %EE was in the range 86.76–96.6%. The amorphous nature of the SLN-entrapped CXB was confirmed from SLN DSC thermograms. The in vitro release profile revealed a slow constant rate of release with no burst release, which is unusual for SLN. Both the F9 and F14 demonstrated almost complete CXB release within 24 h, with only 25% completed within the first 5 h. F9 caused a significant percentage of cell death in the three cancer cell lines tested after 24 h of incubation and maintained this effect for 72 h. The prepared CXB-loaded SLN exhibited unique properties such as slow release with no burst and a high %EE. The anticancer activity of one formulation was extremely significant in all tested cancer cell lines at all incubation times, which is very promising.


2019 ◽  
Vol 9 (20) ◽  
pp. 4438 ◽  
Author(s):  
Amélia Silva ◽  
Carlos Martins-Gomes ◽  
Tiago Coutinho ◽  
Joana Fangueiro ◽  
Elena Sanchez-Lopez ◽  
...  

The surface properties of nanoparticles have decisive influence on their interaction with biological barriers (i.e., living cells), being the concentration and type of surfactant factors to have into account. As a result of different molecular structure, charge, and degree of lipophilicity, different surfactants may interact differently with the cell membrane exhibiting different degrees of cytotoxicity. In this work, the cytotoxicity of two cationic solid lipid nanoparticles (SLNs), differing in the cationic lipids used as surfactants CTAB (cetyltrimethylammonium bromide) or DDAB (dimethyldioctadecylammonium bromide), referred as CTAB-SLNs and DDAB-SLNs, respectively, was assessed against five different human cell lines (Caco-2, HepG2, MCF-7, SV-80, and Y-79). Results showed that the cationic lipids used in SLN production highly influenced the cytotoxic profile of the particles, with CTAB-SLNs being highly cytotoxic even at low concentrations (IC50 < 10 µg/mL, expressed as CTAB amount). DDAB-SLNs produced much lower cytotoxicity, even at longer exposure time (IC50 from 284.06 ± 17.01 µg/mL (SV-80) to 869.88 ± 62.45 µg/mL (MCF-7), at 48 h). To the best of our knowledge, this is the first report that compares the cytotoxic profile of CTAB-SLNs and DDAB-SLNs based on the concentration and time of exposure, using different cell lines. In conclusion, the choice of the right surfactant for biological applications influences the biocompatibility of the nanoparticles. Regardless the type of drug delivery system, not only the cytotoxicity of the drug-loaded nanoparticles should be assessed, but also the blank (non-loaded) nanoparticles as their surface properties play a decisive role both in vitro and in vivo.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Rita R. Lala ◽  
Amol S. Shinde

Abstract Background The main objective of the present study was to formulate, optimize and characterize solid lipid nanoparticles (SLNs) loaded with Atorvastatin Calcium (ATS) and Vinpocetine (VIN) as a potential drug delivery system to improve its solubility and assess its anti-tumor activity on cell lines. The SLNs were formulated by emulsification with high speed homogenization followed by probe sonication. Central composite design was selected for optimization. Drug: lipid ratio, surfactant: co-surfactant ratio and homogenization speed were considered critical process parameters (CPP) to study the effects on critical quality attributes (CQA) of SLNs i.e. particle size, percent entrapment efficiency (% EE) and percent drug loading (% DL). Results The optimized (F3) SLNs formulations were characterized by transmission electron microscopy (TEM), X- ray diffraction (X-RD), in vitro drug release by dialysis bag method and stability studies. In vitro cell line studies were performed on HepG2, MCF 7 and melanoma B16 F10 cell line. The optimized F3 formulation showed a particle size of 323 ± 6 nm, poly dispersity index (PDI) 0.333 ± 0.02, Zeta potential (ZP) − 30.4 ± 0.66 emv with % EE 64.69 ± 1.1; 65.98 ± 0.91 of ATS and VIN respectively. In vitro release (F3) of ATS and VIN in PBS pH 7.4 was found to be 89.45% and 91.86%, respectively, up to 24 h. Conclusions In vitro cell line study demonstrated that SLNs enhanced the anti-cancer activity of ATS, VIN on all the stated cell lines when compared with free drugs. Combination index (CI) for HEPG2 was 0.8, which signified synergistic effect. The results exhibited that SLNs is effective, stable and had enhanced activity against HepG2, MCF 7 and melanoma B16 F10 cell lines.


2020 ◽  
Vol 233 ◽  
pp. 105003
Author(s):  
Mohammed Muqtader Ahmed ◽  
Farhat Fatima ◽  
Md. Khalid Anwer ◽  
Mohammed F. Aldawsari ◽  
Yasser Saud M. Alsaidan ◽  
...  

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