camptothecin/kaaries

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Human and murine macrophages mediate activation of MEN 4901/T-0128: a new promising camptothecin analogue-polysaccharide conjugate.

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MEN 4901/T-0128 is a new cytotoxic prodrug constituted by the camptothecin analogue T-2513 bound to carboxymethyl dextran through a triglycine linker. MEN 4901/T-0128 was designed to target the active camptothecin at the tumour site. MEN 4901/T-0128 is weakly cytotoxic in vitro and thus T-2513 must

Synthesis, optimization, and characterization of camptothecin-loaded acetalated dextran porous microparticles for pulmonary delivery.

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We propose the use of a new biopolymer, acetalated dextran (Ac-DEX), to synthesize porous microparticles for pulmonary drug delivery. Ac-DEX is derived from the polysaccharide dextran and, unlike polyesters, has tunable degradation from days to months and pH neutral degradation products. Ac-DEX

Human topoisomerase I inhibition: docking camptothecin and derivatives into a structure-based active site model.

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Human topoisomerase I (top1) is an important target for anti-cancer drugs, which include camptothecin (CPT) and its derivatives. To elucidate top1 inhibition in vitro, we made a series of duplex DNA substrates containing a deoxyadenosine stereospecifically modified by a covalent adduct of

Amorphous solid dispersion studies of camptothecin-cyclodextrin inclusion complexes in PEG 6000.

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Abstract: The present work focused on the solubility enhancement of the poorly water-soluble anti-cancer agent camptothecin which, in its natural state, presents poor solubility inducing lack of activity with a marked toxicity. A new approach is adopted by using a ternary system including

Drug product development and pharmacological evaluation of a sparingly soluble novel camptothecin analog for peroral administration.

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This work focused on the developmental aspects, pharmacokinetic evaluation, and pharmacological assessment of a drug inclusion complex for a novel camptothecin analog (CA) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). Camptothecins analog belong to topoisomerase-I inhibitor class of compounds with

Modulation of photophysics and pKa shift of the anti-cancer drug camptothecin in the nanocavities of supramolecular hosts.

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This article reports the pK(a) shift of an anti-cancer drug, 20(S)-camptothecin (CPT), upon encapsulation into the nanocavity of a cucurbit[7]uril (CB7) macrocycle. Steady-state, time-resolved fluorescence and electrospray ionisation mass spectrometry (ESI-MS) studies provide evidence for the

Molecular Insight into the Interaction between Camptothecin and Acyclic Cucurbit[4]urils as Efficient Nanocontainers in Comparison with Cucurbit[7]uril: Molecular Docking and Molecular Dynamics Simulation.

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Cucurbit[n]urils (CB[n], n = 5, 6, 7, 8, 10, 14) and their derivatives due to the hydrophobic cavities and polar carbonyl portals have been considerably explored for their potential uses as drug delivery systems. It is important to understand how these macrocyclic compounds interact with guests.

Efficient intracellular delivery of camptothecin by silica/titania hollow nanoparticles.

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Silica/titania hollow nanoparticles (HNPs) with 50 nm were fabricated by using the dissolution and redeposition method and modified with anti-[human epidermal growth factor receptor 2] monoclonal antibody (herceptin), and their application as camptothecin (CPT) delivery agents to human breast cancer

Hollow nanosphere fabricated from β-cyclodextrin-grafted α,β-poly(aspartic acid) as the carrier of camptothecin.

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This research is aimed to develop a kind of hollow nanosphere based on β-cyclodextrin-grafted α, β-poly(aspartic acid) (β-CD-graft-PAsp) as drug carrier to enhance the stability of camptothecin (CPT) in aqueous media. Firstly, mono(6-(2-aminoethyl) amino-6-deoxy)-β-cyclodextrin (β-CDen) was

Prevention of K-Ras- and Pten-mediated intravaginal tumors by treatment with camptothecin-loaded PLGA nanoparticles.

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Primary squamous cell carcinoma of the vagina is an uncommon disease that often exhibits few symptoms before reaching an advanced stage. Topical intravaginal therapies for resolving precancerous and cancerous vaginal lesions have the potential to be non-invasive and safer alternatives to existing

Preparation of camptothecin-loaded PCEC microspheres for the treatment of colorectal peritoneal carcinomatosis and tumor growth in mice.

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The aim of this study was to prepare PCL-PEG-PCL (PCEC) microspheres to protect camptothecin from hydrolysis, to extend its release time and to enhance its treatment efficacy on colorectal peritoneal carcinomatosis and tumor growth in mice. Camptothecin (CPT)-loaded PCL-PEG-PCL (PCEC) microspheres

Codelivery of doxorubicin and camptothecin by dual-responsive unimolecular micelle-based β-cyclodextrin for enhanced chemotherapy.

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Tumor microenvironment (TME)-induced drug delivery technology is a promising strategy for improving low drug accumulation efficiency, short blood circulation and weak therapeutic effect. In this work, a dual-responsive (reduction- and pH-responsive) polyprodrug nanoreactor based on β-cyclodextrin

Successful local regional therapy with topotecan of intraperitoneally growing human ovarian carcinoma xenografts.

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The therapeutic effects of intraperitoneal topotecan, a water-soluble camptothecin analogue, were investigated in two models of human ovarian carcinoma xenografted intraperitoneally into nude mice: the IGROV-1 tumour, which originated from an untreated patient, and the A2780 tumour, selected for

Phase I and pharmacologic study of i.p. 9-aminocamptothecin given as six fractions over 14 days.

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We sought to define the tolerance of 9-amino-20(S)-camptothecin (9-AC) when given by the i.p. route to patients with cancer in the peritoneal cavity consisting of nodules that did not exceed 1 cm in maximum diameter. 9-AC was given in six fractions over 12 days, at doses ranging from 1.25 to 13.5

Synthesis, topoisomerase I inhibitory and cytotoxic activities of chromone derivatives.

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A series of chromone derivatives were designed as potential topoisomerase I (Top I) inhibitors based on the docking simulation study. Sixteen synthesized compounds were evaluated for Top I inhibitory activity and some compounds were further tested for in vitro cytotoxic activity. The most potent

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