Poly(2-methyl-2-oxazoline) conjugates with doxorubicin: From synthesis of high drug loading water-soluble constructs to in vitro anti-cancer properties

2020 ◽  
Vol 326 ◽  
pp. 53-62
Author(s):  
Ondrej Sedlacek ◽  
Alexandra Van Driessche ◽  
Annemiek Uvyn ◽  
Bruno G. De Geest ◽  
Richard Hoogenboom
Keyword(s):  
Drug Loading ◽  
Water Soluble ◽  
High Drug ◽  
Anti Cancer ◽  
High Drug Loading

Co-delivery of dual chemo-drugs with precisely controlled, high drug loading polymeric micelles for synergistic anti-cancer therapy

2020 ◽  
Vol 8 (3) ◽  
pp. 949-959 ◽  
Author(s):  
Yuchen Wu ◽  
Shixian Lv ◽  
Yongjuan Li ◽  
Hua He ◽  
Yong Ji ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
High Drug ◽  
Delivery Strategy ◽  
Anti Cancer ◽  
High Drug Loading

The introduction of donor-receptor coordination between micelles and drug payloads provides a precise co-delivery strategy for two different chemo-drugs with high drug loading and ROS responsiveness.

Water soluble multiarm-polyethylene glycol–betulinic acid prodrugs: design, synthesis, and in vivo effectiveness

2014 ◽  
Vol 5 (19) ◽  
pp. 5775-5783 ◽  
Author(s):  
Lin Dai ◽  
Dan Li ◽  
Jing Cheng ◽  
Jing Liu ◽  
Li-Hong Deng ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Betulinic Acid ◽  
Water Solubility ◽  
Drug Loading ◽  
Water Soluble ◽  
Loading Capacity ◽  
Design Synthesis ◽  
High Drug ◽  
High Drug Loading

Multiarm-polyethylene glycol–betulinic acid prodrugs were prepared by using multiarm-polyethylene glycol linkers and betulinic acid, which exhibited high drug loading capacity, good water solubility, and excellent anticancer activity.

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>

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.

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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