Prodrug-based intracellular delivery of anticancer agents

Bildstein, Lucien; Dubernet, Catherine; Couvreur, Patrick

doi:10.1016/j.addr.2010.12.005

Cited by 281 publications

(199 citation statements)

References 136 publications

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“…Its inertness and biocompatibility justify the use of squalene derivatives (6) (18) with the inclusion of an alternative linker [40][41][42]. In this study, the squalene moiety and the active compound were connected by a disulfide-containing linker able to guarantee the drug release inside the cell.…”

Section: Squalenementioning

confidence: 99%

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Self-assembly drug conjugates for anticancer treatment

Fumagalli

Marucci

Christodoulou

et al. 2016

Drug Discovery Today

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Please cite this article as: Fumagalli, G., Marucci, C., Christodoulou, M.S., Stella, B., Dosio, F., Passarella, D.,Self-assembly drug conjugates for anticancer treatment, Drug Discovery Today (2016), http://dx.doi.org/10.1016/j.drudis. 2016.06.018 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. A c c e p t e d M a n u s c r i p t Keywords: Self-assembly; drug conjugate; nanoparticle. Self-assembly drug conjugates for anticancer treatmentTeaser: In this review we summarize the recent advances in nanoparticles obtained by self-assembly drug conjugates, a useful tool to improve drug delivery of anticancer compounds. Page 4 of 25A c c e p t e d M a n u s c r i p tSelf-assembly drug conjugate preparation is a promising approach to improve activity and penetration through physiological barriers of potent small molecules, as well as to reduce any side effects. Drug conjugates can self-assemble in water to form nanoparticles (NPs) that offer several advantages because: (i) they are easy to obtain; (ii) they can reach high local drug concentration in tumor tissues; and (iii) they can reduce the side effects of drugs. All these factors improve drug pharmacokinetic properties. Here, we have reviewed the scope of nanotechnology-based self-assembly drug delivery approaches focusing on prodrugs able to form NPs by self-assembly; we have also summarized the current perspective and challenges facing the successful treatment of cancer.

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Section: Squalenementioning

confidence: 99%

“…In recent years, the use of drug conjugates to obtain NPs has gained considerable attention [4][5][6]. These conjugates are usually obtained by a covalent coupling of the drug to biocompatible lipid moieties and the resulting molecules are able to form NPs by selfassembly.…”

mentioning

confidence: 99%

Self-assembly drug conjugates for anticancer treatment

Fumagalli

Marucci

Christodoulou

et al. 2016

Drug Discovery Today

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“…The potential of polymeric micelles to deliver anticancer drugs has been suggested in various preclinical and clinical studies. NK012, a poly(ethylene glycol)‐poly(glutamic acid) (PEG‐PGlu)‐based micelle formulation carrying an irinotecan active metabolite (SN‐38), has shown significant antitumor activity with no toxicity in several orthotopic tumor models by enhancing distribution and prolonging release of SN‐38 91. This candidate has entered phase II trials in patients with TNBC 91.…”

Section: Tnbc: Strategies For Diagnosis and Treatmentmentioning

confidence: 99%

“…NK012, a poly(ethylene glycol)‐poly(glutamic acid) (PEG‐PGlu)‐based micelle formulation carrying an irinotecan active metabolite (SN‐38), has shown significant antitumor activity with no toxicity in several orthotopic tumor models by enhancing distribution and prolonging release of SN‐38 91. This candidate has entered phase II trials in patients with TNBC 91. Styrene‐co‐maleic acid (SMA)‐based micelles have also been used to deliver RL71—a hydrophobic second generation curcumin derivative with poor bioavailability—in various TNBC cell lines 92.…”

Section: Tnbc: Strategies For Diagnosis and Treatmentmentioning

confidence: 99%

Triple Negative Breast Cancer: Nanosolutions for a Big Challenge

2015

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Triple negative breast cancer (TNBC) is a particular immunopathological subtype of breast cancer that lacks expression of estrogen and progesterone receptors (ER/PR) and amplification of the human epidermal growth factor receptor 2 (HER2) gene. Characterized by aggressive and metastatic phenotypes and high rates of relapse, TNBC is the only breast cancer subgroup still lacking effective therapeutic options, thus presenting the worst prognosis. The development of targeted therapies, as well as early diagnosis methods, is vital to ensure an adequate and timely therapeutic intervention in patients with TNBC. This review intends to discuss potentially emerging approaches for the diagnosis and treatment of TNBC patients, with a special focus on nano‐based solutions that actively target these particular tumors.

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“…The majority of polymer drug carriers have no active but passive targeting characteristic. For example, CPT-loaded NPs with polyethylene glycol shells can stay in circulation for a long time (Bildstein et al, 2011;Luo & Jiang, 2012), thereby allowing the prolonged exposure of tumor cells to antitumor drugs. The drugs subsequently reach the target site during passive targeting through the enhanced permeability and retention effect.…”

Section: Introductionmentioning

confidence: 99%

Preparation of camptothecin-loaded targeting nanoparticles and their antitumor effects on hepatocellular carcinoma cell line H22

Yang

Yan

et al. 2014

Drug Delivery

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Camptothecin (CPT) is an effective anticancer agent against various cancers but the clinical application is limited because of its poor water solubility, low bioavailability and severe toxic side effects. The aim of the present study was to evaluate the feasibility of using targeted NPs as a high-performance CPT delivery system that targets liver cancer cells through intravenous (i.v.) administration route. CPT was incorporated into biotin-F127-PLA or F127-PLA polymeric nanoparticles (NPs) by a dialysis method. The preparation of the targeting NPs was performed by conjugating biotin-F127-PLA NPs with anti-3A5 antibody. The antitumor effect of the CPTloaded nanoparticles against H22 cells in vitro was determined using an MTT assay. Tissue distribution and tumor inhibition in vivo were also evaluated. Survivin mRNA expression was assessed by real-time polymerase chain reaction. Results showed that the targeted CPT NPs exhibited regular spherical shapes with a mean diameter of approximately 180 nm. In vitro release of the targeted CPT NPs exhibited an initial burst (40%) within 12 h, followed by a slow release. Cytotoxicity test against H22 cells indicated that the targeted CPT NPs exerted significant antitumor effects. Compared with free CPT and non-targeted CPT NPs, the targeted CPT NPs showed superior inhibition ratio against tumor in vivo, which may be associated with reduced survivin mRNA expression. The results suggested that the new targeted CPT NPs may be a promising injectable delivery system for cancer therapy.

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Prodrug-based intracellular delivery of anticancer agents

Cited by 281 publications

References 136 publications

Self-assembly drug conjugates for anticancer treatment

Self-assembly drug conjugates for anticancer treatment

Triple Negative Breast Cancer: Nanosolutions for a Big Challenge

Preparation of camptothecin-loaded targeting nanoparticles and their antitumor effects on hepatocellular carcinoma cell line H22

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