Preparation and In Vitro Cellular Uptake Assessment of Multifunctional Rubik-Like Magnetic Nano-Assemblies

2019 ◽  
Vol 19 (6) ◽  
pp. 3301-3309
Author(s):  
Xiawen Zheng ◽  
Yuejian Chen ◽  
Zhiming Wang ◽  
Lina Song ◽  
Yu Zhang ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Folic Acid ◽  
Cellular Uptake ◽  
Hela Cells ◽  
Drug Loading ◽  
Superparamagnetic Iron Oxide ◽  
Drug Carriers ◽  
High Drug ◽  
High Drug Loading

Through self-assembly of nanoparticles into high-order and stable structures of cubic clusters, high drug-loading rubik-like magnetic nano-assemblies (MNAs), possessing folic acid targeting and strong magnetism-enhanced cellular uptake capabilities, were built. In this study, the core of the cubic drug assemblies consisted of four monodisperse superparamagnetic iron oxide nanoparticles coated with layers of oleic acid (Fe3O4@OA), simultaneously encapsulating fluorescein, and Paclitaxol (Flu-MNAs and PTX-MNAs) for imaging and therapeutic applications. To enable preferential tumor cellular uptake by the nanocarriers, the outermost layer of Fe3O4 was functionalized with the new dual-oleic acid-polyethylene glycol-folic acid polymer (FA-PEG-Lys-OA2) as a “shell.” The drug carriers exhibited excellent stability and biocompatibility, and showed high drug loading and excellent magnetic response In Vitro. Furthermore, preliminary evaluations of the drug carriers with Hela cells showed effective cellular targeting capability. In addition, the cubic assemblies enhanced anticancer efficiency for Hela cells compared to bare drugs. Especially, the applied external magnetic field further improved the uptake of the vectors, and thereby enhanced the inhibitory effect. In brief, all these results suggested that cubic assemblies could serve as potential strategies for targeted anticancer therapies.

Nanoscale covalent organic frameworks as smart carriers for drug delivery

2016 ◽  
Vol 52 (22) ◽  
pp. 4128-4131 ◽  
Author(s):  
Linyi Bai ◽  
Soo Zeng Fiona Phua ◽  
Wei Qi Lim ◽  
Avijit Jana ◽  
Zhong Luo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Loading ◽  
Drug Carriers ◽  
Loading Capacity ◽  
Covalent Organic Frameworks ◽  
High Drug ◽  
Good Biocompatibility ◽  
High Drug Loading

Two nanoscale covalent organic frameworks as drug carriers with good biocompatibility were developed, showing high drug loading capacity and sustained release in vitro.

scholarly journals Photosensitive Supramolecular Micelle-Mediated Cellular Uptake of Anticancer Drugs Enhances the Efficiency of Chemotherapy

2020 ◽  
Vol 21 (13) ◽  
pp. 4677 ◽  
Author(s):  
Yihalem Abebe Alemayehu ◽  
Wen-Lu Fan ◽  
Fasih Bintang Ilhami ◽  
Chih-Wei Chiu ◽  
Duu-Jong Lee ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Anticancer Drugs ◽  
Cellular Uptake ◽  
Self Assembly ◽  
Apoptotic Cell ◽  
Drug Loading ◽  
Stimuli Responsive ◽  
High Drug ◽  
High Drug Loading

The development of stimuli-responsive supramolecular micelles with high drug-loading contents that specifically induce significant levels of apoptosis in cancer cells remains challenging. Herein, we report photosensitive uracil-functionalized supramolecular micelles that spontaneously form via self-assembly in aqueous solution, exhibit sensitive photo-responsive behavior, and effectively encapsulate anticancer drugs at high drug-loading contents. Cellular uptake analysis and double-staining flow cytometric assays confirmed the presence of photo-dimerized uracil groups within the irradiated micelles remarkably enhanced endocytic uptake of the micelles by cancer cells and subsequently led to higher levels of apoptotic cell death, and thus improved the therapeutic effect in vitro. Thus, photo-dimerized uracil-functionalized supramolecular micelles may potentially represent an intelligent nanovehicle to improve the safety, efficacy, and applicability of cancer chemotherapy, and could also enable the development of nucleobase-based supramolecular micelles for multifunctional biomaterials and novel biomedical applications.

Doxorubicin-loaded Fe3O4-ZIF-8 nano-composites for hepatocellular carcinoma therapy

2019 ◽  
Vol 33 (10) ◽  
pp. 1373-1381 ◽  
Author(s):  
Chong Cheng ◽  
Cheng Li ◽  
Xulong Zhu ◽  
Wei Han ◽  
Jianhui Li ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Hepatocellular Carcinoma ◽  
Cellular Uptake ◽  
Laser Scanning ◽  
Drug Loading ◽  
Confocal Laser Scanning Microscope ◽  
Confocal Laser ◽  
Nano Composites ◽  
High Drug ◽  
High Drug Loading

Hepatocellular carcinoma (HCC) is one of the most common and malignant cancers and has no effective therapeutic approaches. Chemotherapeutic drug doxorubicin (DOX) is widely used for HCC therapy, but its application is limited by the clinical toxicity. In the present study, an Fe3O4-ZIF-8 magnetic nano-composite was fabricated and used for DOX delivery for HCC therapy. The morphology, structure and property of Fe3O4-ZIF-8 nano-composites were evaluated by scanning electron microscopy, transmission electron microscopy and N2 adsorption-desorption isotherms studies. The drug release from DOX@Fe3O4-ZIF-8 was measured in pH 7.4 phosphate-buffered saline. The cellular uptake ability of DOX@Fe3O4-ZIF-8 into hepatocarcinoma cell line (MHCC97H) was visualized with a confocal laser scanning microscope. The effects of Fe3O4-ZIF-8, DOX and DOX@Fe3O4-ZIF-8 against MHCC97H cells were evaluated by CCK-8 assay and flow cytometry assay. Fe3O4-ZIF-8 nano-composites were synthesized and used as a nano-carrier for the delivery of DOX. Because of high drug loading property of ZIF-8, 1 mg Fe3O4-ZIF-8 nano-composites loaded 120 μg DOX when DOX@Fe3O4-ZIF-8 was synthesized in 30 mg/mL DOX solution. The cumulative DOX release curve showed a slow and sustained release pattern over time. The results of CCK-8 assay showed that Fe3O4-ZIF-8 was nontoxic to MHCC97H cells, and DOX@Fe3O4-ZIF-8 presented effective inhibiting effect on cell viability of MHCC97H cells. Cellular uptake assay showed that DOX@Fe3O4-ZIF-8 accumulated in both cytoplasm and nuclei. Moreover, because of valid drug accumulation, DOX@Fe3O4-ZIF-8 exhibited a good inducing effect on cell apoptosis of MHCC97H cells. In conclusion, based on the nontoxic and high drug loading capability of Fe3O4-ZIF-8, DOX@Fe3O4-ZIF-8 presented enhanced effects on HCC cells compared to free DOX, indicating its potential for the chemotherapy of HCC.

scholarly journals A Micellar Mitotane Formulation with High Drug Loading and Solubility: Physico-Chemical Characterization and Cytotoxicity Studies in 2D and 3D in Vitro Tumor Models.

2019 ◽  
Author(s):  
Malik Salman Haider ◽  
Jochen Schreiner ◽  
Sabine Kendl ◽  
Matthias Kroiß ◽  
Robert Luxenhofer
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Plasma Concentrations ◽  
Ethanol Solution ◽  
Comparable Efficacy ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Cytotoxicity Studies ◽  
High Drug Loading

Adrenocortical carcinoma (ACC) is a rare tumor and prognosis is overall poor but heterogeneous. Mitotane (MT) has been used for treatment of ACC for decades, either alone or in combination with cytotoxic chemotherapy. Even at doses up to 6 g per day, more than half of the patients do not achieve targeted plasma concentration (14-20 mg/L) even after many months of treatment which is caused by low water solubility and unfavorable pharmacokinetic properties such as poor bioavailability and high volume of distribution of MT. The clinical need and previously reported extraordinary high drug loading of poly(2-methyl-2-oxazoline)-block-poly(2-butyl-2-oxazoline)-block-poly(2-methyl-2-oxazoline) (A-pBuOx-A) based micelles for paclitaxel (PTX), led us to develop MT loaded micelles which may enable an injectable formulation. We successfully solubilized up to 6 g/L of MT in an aqueous formulation. The MT loaded nanoformulations were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and powder X-ray<br> <p>diffraction (XRD), confirmed the amorphous nature of drug in the formulations. The polymer itself did not show cytotoxicity in adrenal and liver cell lines. By using the ACC model cell line NCI-H295 both in monolayers and tumor cell spheroids, we demonstrated micellar MT to exhibit comparable efficacy to its ethanol solution. We postulate that this formulation would be suitable for i.v. application and more rapid attainment of therapeutic plasma concentrations. In conclusion, we consider our micellar formulation a promising tool to alleviate major drawbacks of current MT treatment while retaining bioactivity towards ACC in vitro.</p>

scholarly journals Zirconium-Porphyrin PCN-222: pH-responsive Controlled Anticancer Drug Oridonin

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Xin Leng ◽  
Hongliang Huang ◽  
Wenping Wang ◽  
Na Sai ◽  
Longtai You ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hepg2 Cells ◽  
Drug Loading ◽  
Annexin V ◽  
Controlled Drug Release ◽  
Dapi Staining ◽  
High Drug ◽  
High Drug Loading

Drug delivery carriers with a high drug loading capacity and biocompatibility, especially for controlled drug release, are urgently needed due to the side effects and frequent dose in the traditional therapeutic method. Guided by nanomaterials, we have successfully synthesized zirconium-based metal−organic frameworks, Zr-TCPP (TCPP: tetrakis (4-carboxyphenyl) porphyrin), namely, PCN-222, which is synthesized by solvothermal method. And it has been designed as a drug delivery system (DDS) with a high drug loading of 38.77 wt%. In our work, PCN-222 has achieved pH-sensitive drug release and showed comprehensive SEM, TEM, PXRD, DSC, FTIR, and N2 adsorption-desorption. The low cytotoxicity and good biocompatibility of PCN-222 were certificated by the in vitro results from an MTT assay, DAPI staining, and Annexin V/PI double-staining even cultivated L02 cells and HepG2 cells for 48h. Furthermore, Oridonin, a commonly used cancer chemotherapy drug, is adsorbed into PCN-222 via the solvent diffusion technique. Based on an analysis of the Oridonin release profile, results suggest that it can last for more than 7 days in vitro. And cumulative release rate of Ori at the 7 d was about 86.29% and 63.23% in PBS (pH 5.5 and pH 7.2, respectively) at 37°C. HepG2 cells were chosen to research the cytotoxicity of PCN-222@Ori and free Oridonin. The results demonstrated that the PCN-222@Ori nanocarrier shows higher cytotoxicity in HepG2 cells compared to Oridonin.

Core–shell noble-metal@zeolitic-imidazolate-framework nanocarriers with high cancer treatment efficiency in vitro

2019 ◽  
Vol 7 (7) ◽  
pp. 1050-1055 ◽  
Author(s):  
Liangcan He ◽  
Kanglei Pang ◽  
Wenwen Liu ◽  
Yue Tian ◽  
Lin Chang ◽  
...  
Keyword(s):  
Drug Release ◽  
Cancer Treatment ◽  
Drug Loading ◽  
Controlled Drug Release ◽  
Core Shell ◽  
Treatment Efficiency ◽  
Zeolitic Imidazolate Framework ◽  
High Drug ◽  
High Drug Loading

Core–shell Au@zeolitic-imidazolate-framework nanocarriers with high drug-loading, controlled drug release properties, and high cancer treatment efficiency.

Preparation and Characterization of Hydroxycamptothecin-Loaded Poly(D,L-lactic acid) Nanoparticles with High Drug Loading Capacity

2012 ◽  
Vol 531 ◽  
pp. 503-506
Author(s):  
Zhen Qing Hou ◽  
Shui Fan Zhou ◽  
Fei Cui ◽  
Yi Xiao Hang ◽  
Yun Feng Yi
Keyword(s):  
Drug Release ◽  
Orthogonal Design ◽  
Drug Loading ◽  
Influential Factors ◽  
Prolonged Release ◽  
Loading Capacity ◽  
Sustained Drug Release ◽  
High Drug ◽  
High Drug Loading

Hydroxycamptothecin (HCPT) loaded PLA nanoparticles were prepared by a facile dialysis method. Three main influential factors, PLA concentration, ratio of HCPT to PLA (wt/wt), dialysis bags with different molecule weight cutoff, were evaluated using an orthogonal design, gave the nanoparticles with an average diameter of approximately 226.8 nm and fine drug loading content (5.16%, w/w). The in vitro drug release studies exhibited a slow and prolonged release profile over 30 days. It is concluded that the new method to prepare HCPT-PLA nanoparticles resulted in improved formulation characteristics including small size, high drug loading capacity, and long sustained drug release.

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