Cyclic RGD targeting nanoparticles with pH sensitive polymer–drug conjugates for effective treatment of melanoma

RSC Advances ◽  
2014 ◽  
Vol 4 (98) ◽  
pp. 55187-55194 ◽  
Author(s):  
Xingang Guan ◽  
Xiuli Hu ◽  
Shi Liu ◽  
Yubin Huang ◽  
Xiabin Jing ◽  
...  
Keyword(s):  
Effective Treatment ◽  
Ph Sensitive ◽  
Drug Conjugates ◽  
Ph Sensitive Polymer ◽  
Polymer Drug Conjugates

Cyclic RGD targeting polymeric nanomedicines prepared from pH sensitive polymer–drug conjugates for effective treatment of melanoma.

scholarly journals Polymer Nanomedicines with Ph-Sensitive Release of Dexamethasone for the Localized Treatment of Inflammation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 700
Author(s):  
Alena Libánská ◽  
Eva Randárová ◽  
Franck Lager ◽  
Gilles Renault ◽  
Daniel Scherman ◽  
...  
Keyword(s):  
Near Infrared ◽  
Therapeutic Potential ◽  
Joint Inflammation ◽  
Ph Sensitive ◽  
Current Therapy ◽  
Polymer Conjugates ◽  
Drug Conjugates ◽  
Anti Inflammatory ◽  
Polymer Drug Conjugates

Polymer-drug conjugates have several advantages in controlled drug delivery to inflammation as they can accumulate and release the drug in inflamed tissues or cells, which could circumvent the shortcomings of current therapy. To improve the therapeutic potential of polymer-drug conjugates in joint inflammation, we synthesized polymer conjugates based on N-(2-hydroxypropyl) methacrylamide) copolymers labeled with a near-infrared fluorescent dye and covalently linked to the anti-inflammatory drug dexamethasone (DEX). The drug was bound to the polymer via a spacer enabling pH-sensitive drug release in conditions mimicking the environment inside inflammation-related cells. An in vivo murine model of adjuvant-induced arthritis was used to confirm the accumulation of polymer conjugates in arthritic joints, which occurred rapidly after conjugate application and remained until the end of the experiment. Several tested dosage schemes of polymer DEX-OPB conjugate showed superior anti-inflammatory efficacy. The highest therapeutic effect was obtained by repeated i.p. application of polymer conjugate (3 × 1 mg/kg of DEX eq.), which led to a reduction in the severity of inflammation in the ankle by more than 90%, compared to 40% in mice treated with free DEX.

pH-Sensitive brush polymer-drug conjugates by ring-opening metathesis copolymerization

2011 ◽  
Vol 47 (15) ◽  
pp. 4493 ◽  
Author(s):  
Jiong Zou ◽  
Goran Jafr ◽  
Efrosyni Themistou ◽  
Yoonsing Yap ◽  
Zachary A. P. Wintrob ◽  
...  
Keyword(s):  
Ring Opening ◽  
Ph Sensitive ◽  
Drug Conjugates ◽  
Brush Polymer ◽  
Polymer Drug Conjugates

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

scholarly journals Folic Acid-Targeted Paclitaxel-Polymer Conjugates Exert Selective Cytotoxicity and Modulate Invasiveness of Colon Cancer Cells

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 929
Author(s):  
Antonella Grigoletto ◽  
Gabriele Martinez ◽  
Daniela Gabbia ◽  
Tommaso Tedeschini ◽  
Michela Scaffidi ◽  
...  
Keyword(s):  
Folic Acid ◽  
Cancer Cells ◽  
Pharmacokinetic Profile ◽  
Strong Impact ◽  
Passive Targeting ◽  
Drug Conjugates ◽  
Tumor Delivery ◽  
The Right ◽  
Polymer Drug Conjugates ◽  
Ht 29

Although selective tumor delivery of anticancer drugs has been sought by exploiting either passive targeting or by ligand-mediated targeting, a selective anticancer therapy remains an unmet medical need. Despite the advances which have been achieved by nanomedicines, nanosystems such as polymer-drug conjugates still miss the goal of clinical efficacy. In this study, we demonstrated that polymer-drug conjugates require a thoroughly chemical design and the right targeting agent/polymer ratio to be selective and effective towards cancer cells. In particular, two PEG conjugates carrying paclitaxel and targeted with different folic acid (FA)/PEG ratios (one or three) were investigated. The cytotoxicity study in positive (HT-29) and negative (HCT-15) FA receptor (FR)-cell lines demonstrated that the conjugates with one or three FAs were 4- or 28-fold more active in HT-29 cells, respectively. The higher activity of the 3-FA conjugate was confirmed by its strong impact on cell cycle arrest. Furthermore, FA targeting had a clear effect on migration and invasiveness of HT-29 cells, which were significantly reduced by both conjugates. Interestingly, the 3-FA conjugate showed also an improved pharmacokinetic profile in mice. The results of this study indicate that thorough investigations are needed to optimize and tune drug delivery and achieve the desired selectivity and activity towards cancer cells.

Long-Circulating and Passively Tumor-Targeted Polymer-Drug Conjugates Improve the Efficacy and Reduce the Toxicity of Radiochemotherapy

2010 ◽  
Vol 12 (9) ◽  
pp. B413-B421 ◽  
Author(s):  
Twan Lammers ◽  
Vladimir Subr ◽  
Karel Ulbrich ◽  
Peter Peschke ◽  
Peter E. Huber ◽  
...  
Keyword(s):  
Drug Conjugates ◽  
Polymer Drug Conjugates
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