scholarly journals Light-Responsive Micelles Loaded With Doxorubicin for Osteosarcoma Suppression

2021 ◽  
Vol 12 ◽  
Author(s):  
Jiayi Chen ◽  
Chenhong Qian ◽  
Peng Ren ◽  
Han Yu ◽  
Xiangjia Kong ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Blood Circulation ◽  
Tumor Targeting ◽  
Polymeric Micelles ◽  
Polymeric Nanoparticles ◽  
Amide Bond ◽  
Significant Damage ◽  
Stimulus Responsive ◽  
Significant Factors

The enhancement of tumor targeting and cellular uptake of drugs are significant factors in maximizing anticancer therapy and minimizing the side effects of chemotherapeutic drugs. A key challenge remains to explore stimulus-responsive polymeric nanoparticles to achieve efficient drug delivery. In this study, doxorubicin conjugated polymer (Poly-Dox) with light-responsiveness was synthesized, which can self-assemble to form polymeric micelles (Poly-Dox-M) in water. As an inert structure, the polyethylene glycol (PEG) can shield the adsorption of protein and avoid becoming a protein crown in the blood circulation, improving the tumor targeting of drugs and reducing the cardiotoxicity of doxorubicin (Dox). Besides, after ultraviolet irradiation, the amide bond connecting Dox with PEG can be broken, which induced the responsive detachment of PEG and enhanced cellular uptake of Dox. Notably, the results of immunohistochemistry in vivo showed that Poly-Dox-M had no significant damage to normal organs. Meanwhile, they showed efficient tumor-suppressive effects. This nano-delivery system with the light-responsive feature might hold great promises for the targeted therapy for osteosarcoma.

Radioisotope Co-57 incorporated layered double hydroxide nanoparticles as a cancer imaging agent

RSC Advances ◽  
2016 ◽  
Vol 6 (54) ◽  
pp. 48415-48419 ◽  
Author(s):  
Tae-Hyun Kim ◽  
Jun Young Lee ◽  
Min-Kyu Kim ◽  
Jeong Hoon Park ◽  
Jae-Min Oh
Keyword(s):  
Layered Double Hydroxide ◽  
Cellular Uptake ◽  
Tumor Targeting ◽  
Cancer Imaging ◽  
Imaging Agent ◽  
Isomorphous Substitution ◽  
Double Hydroxide ◽  
Layered Double Hydroxide Nanoparticles

Radioisotope Co-57 substituted LDH were successfully prepared by isomorphous substitution and showed high in vitro cellular uptake and tumor targeting in vivo biodistribution.

Topotecan–tamoxifen duple PLGA polymeric nanoparticles: Investigation of in vitro, in vivo and cellular uptake potential

2014 ◽  
Vol 473 (1-2) ◽  
pp. 384-394 ◽  
Author(s):  
Tahir Khuroo ◽  
Devina Verma ◽  
Sushama Talegaonkar ◽  
Santwana Padhi ◽  
Amulya K. Panda ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Polymeric Nanoparticles

scholarly journals Ligand-Clustered “Patchy” Nanoparticles for Modulated Cellular Uptake and In Vivo Tumor Targeting

2010 ◽  
Vol 49 (40) ◽  
pp. 7266-7270 ◽  
Author(s):  
Zhiyong Poon ◽  
Shujun Chen ◽  
Amanda C. Engler ◽  
Hyung-il Lee ◽  
Evrim Atas ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Tumor Targeting ◽  
Patchy Nanoparticles

scholarly journals Improved Tumor-Targeting with Peptidomimetic Analogs of Minigastrin 177Lu-PP-F11N

Cancers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 2629
Author(s):  
Nathalie M. Grob ◽  
Roger Schibli ◽  
Martin Béhé ◽  
Thomas L. Mindt
Keyword(s):  
Tumor Targeting ◽  
Amide Bond ◽  
Amide Bonds ◽  
Structural Modifications ◽  
The Past ◽  
Cell Internalization ◽  
Biodistribution Studies ◽  
Metabolic Degradation

The cholecystokinin-2 receptor (CCK2R) is an attractive target in nuclear medicine due to its overexpression by different tumors. Several radiolabeled peptidic ligands targeting the CCK2R have been investigated in the past; however, their low stability against proteases can limit their uptake in tumors and metastases. Substitution of single or multiple amide bonds with metabolically stable 1,4-disubstituted 1,2,3-triazoles as amide bond bioisosteres proved a promising strategy for improving the tumor-targeting properties of a truncated analog of minigastrin. In this study, we applied the previously studied structural modifications to improve the pharmacokinetic and pharmacodynamic properties of PP-F11N, a minigastrin analog currently in clinical trials. Novel minigastrins (NMGs) as analogs of PP-F11N with one or two amide bonds substituted by 1,2,3-triazoles were synthesized, radiolabeled with 177Lu3+, and subjected to full evaluation in vitro (cell internalization, receptor affinity, stability in blood plasma) and in vivo (stability, biodistribution, SPECT/CT imaging). NMGs with triazoles inserted between the amino acids DGlu10-Ala11 and/or Tyr12-Gly13 showed a significantly increased cellular uptake and affinity toward the CCK2R in vitro. Resistance against the metabolic degradation of the NMGs was comparable to those of the clinical candidate PP-F11N. Imaging by SPECT/CT and biodistribution studies demonstrated a higher uptake in CCK2R-positive tumors but also in the CCK2R-positive stomach. The peptidomimetic compounds showed a slow tumor washout and high tumor-to-kidney ratios. The structural modifications led to the identification of analogs with promising properties for progression to clinical applications in the diagnosis and therapy of CCK2R-positive neoplasms.

Fabrication of RGD-conjugated Gd(OH)3:Eu nanorods with enhancement of magnetic resonance, luminescence imaging and in vivo tumor targeting

2016 ◽  
Vol 45 (36) ◽  
pp. 14063-14070 ◽  
Author(s):  
Bianyun Cai ◽  
Zhongbing Huang ◽  
Zhi Wu ◽  
Lei Wang ◽  
Guangfu Yin ◽  
...  
Keyword(s):  
Magnetic Resonance ◽  
Hydrothermal Method ◽  
Blood Circulation ◽  
Tumor Targeting ◽  
Circulation Time ◽  
Luminescence Imaging

RGD-linked Gd(OH)3:Eu NRs with long blood circulation time were fabricated via a hydrothermal method, PEGylation and thiolation conjugation, and these NRs could enhance in vivo MR and luminescence imagings of gliomas by a good targeting of gliomas.

scholarly journals Nanoformulations of α-Mangostin for Cancer Drug Delivery System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 1993
Author(s):  
Lisna Meylina ◽  
Muchtaridi Muchtaridi ◽  
I Made Joni ◽  
Ahmed Fouad Abdelwahab Mohammed ◽  
Nasrul Wathoni
Keyword(s):  
Drug Delivery ◽  
Cellular Uptake ◽  
Polymeric Nanoparticles ◽  
Cancer Drug ◽  
Garcinia Mangostana ◽  
Active Constituent ◽  
Anticancer Efficacy ◽  
Anticancer Properties ◽  
Cancer Drug Delivery

Natural compounds are emerging as effective agents for the treatment of malignant diseases. The active constituent of α-mangostin from the pericarp of Garcinia mangostana L. has earned significant interest as a plant base compound with anticancer properties. Despite α-mangostin’s superior properties as an anticancer agent, its applications are limited due to its poor solubility and physicochemical stability, rapid systemic clearance, and low cellular uptake. Our review aimed to summarize and discuss the nanoparticle formulations of α-mangostin for cancer drug delivery systems from published papers recorded in Scopus, PubMed, and Google Scholar. We investigated various types of α-mangostin nanoformulations to improve its anticancer efficacy by improving bioavailability, cellular uptake, and localization to specific areas These nanoformulations include nanofibers, lipid carrier nanostructures, solid lipid nanoparticles, polymeric nanoparticles, nanomicelles, liposomes, and gold nanoparticles. Notably, polymeric nanoparticles and nanomicelles can increase the accumulation of α-mangostin into tumors and inhibit tumor growth in vivo. In addition, polymeric nanoparticles with the addition of target ligands can increase the cellular uptake of α-mangostin. In conclusion, nanoformulations of α-mangostin are a promising tool to enhance the cellular uptake, accumulation in cancer cells, and the efficacy of α-mangostin as a candidate for anticancer drugs.

Co-delivery of doxorubicin and curcumin by polymeric micelles for improving antitumor efficacy on breast carcinoma

RSC Advances ◽  
2014 ◽  
Vol 4 (87) ◽  
pp. 46737-46750 ◽  
Author(s):  
Lu Sun ◽  
Xiaohui Deng ◽  
Xi Yang ◽  
Zhaojun Li ◽  
Zhihan Wang ◽  
...  
Keyword(s):  
Breast Carcinoma ◽  
Cellular Uptake ◽  
Polymeric Micelles ◽  
Antitumor Efficacy

Polymeric micelles co-delivered hydrophilic doxorubicin and hydrophobic curcumin improved cytotoxicity, apoptosis, and cellular uptakein vitroand enhanced antitumor and anti-metastasis activityin vivoon breast carcinoma.

Biodegradable Polymeric Nanoparticles for Tumor-Selective Tamoxifen Delivery: In Vitro and in Vivo Studies

2004 ◽  
Vol 845 ◽  
Author(s):  
Dinesh B. Shenoy ◽  
Jugminder S. Chawla ◽  
Mansoor M. Amiji
Keyword(s):  
Cellular Uptake ◽  
Polymeric Nanoparticles ◽  
Therapeutic Benefit ◽  
In Vivo Studies ◽  
Tumor Mass ◽  
Biodistribution Studies ◽  
Poly Ethylene ◽  
Surface Modified

1. ABSTRACT: This study was performed to evaluate the in-vitro and in-vivo tumor-cellular uptake and biodistribution pattern of tamoxifen when administered intravenously as a simple solution and upon encapsulation into biodegradable, surface-modified poly(ε-caprolactone) (PCL) nanoparticles. PCL (MW ∼ 15, 000) nanoparticles were prepared by the solvent displacement method and characterized for particle size/charge and surface morphology (by scanning electron microscopy). We investigated the nanoparticle-surface modification potential of the hydrophilic stabilizer (Pluronic® F-68 and F-108) employed during the preparation by electron spectroscopy for chemical analysis (ESCA). Quantitative in-vitro cellular uptake of tritiated (3H) tamoxifen in solution form and as nanoparticulate formulation was assessed in MCF-7 breast cancer cells. In-vivo biodistribution studies for the same formulations were carried out in Nu/Nu mice bearing MDA-MB-231 human breast carcinoma xenograft. Spherical nanoparticles having positive zeta potential (∼25 mV) were obtained in the size range of 200-300 nm. Pluronics (both F-68 and F-108), the triblock copolymers of poly(ethylene oxide) (PEO) and poly(propylene oxide) induced surface hydrophilization of the nanoparticles via adsorption as evident by ESCA. Nanoparticulate formulations of tamoxifen achieved higher intracellular concentrations when exposed at therapeutic concentrations to tumor cells in-vitro compared to solutions. The in-vivo biodistribution studies carried out in nude mice bearing experimental breast tumor suggested increased tumor concentrations for the drug administered as nanoparticulate formulations besides longer retention times within tumor mass. This type of delivery system is expected to provide better therapeutic benefit by dual means: preferential concentration within the tumor mass via enhanced permeation and retention pathway, and; subsequent controlled release, thus maintaining the local drug concentration for longer periods of time to achieve maximal cell-kill.

scholarly journals Ligand-Clustered “Patchy” Nanoparticles for Modulated Cellular Uptake and In Vivo Tumor Targeting

2010 ◽  
Vol 122 (40) ◽  
pp. 7424-7428 ◽  
Author(s):  
Zhiyong Poon ◽  
Shujun Chen ◽  
Amanda C. Engler ◽  
Hyung-il Lee ◽  
Evrim Atas ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Tumor Targeting ◽  
Patchy Nanoparticles

scholarly journals Tumor-Acidity Responsive Polymeric Nanoparticles for Targeting Delivery of Angiogenesis Inhibitor for Enhanced Antitumor Efficacy With Decreased Toxicity

2021 ◽  
Vol 9 ◽  
Author(s):  
Xiufeng Cong ◽  
Jun Chen ◽  
Ran Xu
Keyword(s):  
Tumor Targeting ◽  
Polymeric Nanoparticles ◽  
Angiogenesis Inhibitor ◽  
Pharmacokinetic Property ◽  
Tumor Acidity ◽  
Targeting Delivery ◽  
Targeting Ability ◽  
Anti Tumor Activity ◽  
Tumor Growth Suppression

Various nanocarriers with tumor targeting ability and improved pharmacokinetic property have been extensively utilized to reduce the toxicity of existing clinical chemotherapeutics. Herein, we showed that by encapsulating angiogenesis inhibitor anlotinib into polymeric nanoparticles, we could significantly decrease its in vivo toxicity. The introduction of pH-responsiveness into the nanocarrier further enhanced its anti-tumor activity. Systemic administration of the anlotinib-loaded nanocarrier into mice bearing A549 and 4T1 subcutaneous tumor received a higher tumor growth suppression and metastasis inhibition without detectable side effects. This strategy offers a promising option to improve the patient compliance of anlotinib.

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