- Conjugation of Paclitaxel to Hybrid Peptide Carrier and Biological Evaluation in Jurkat and A549 Cancer Cell Lines
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Paclitaxel (PTX) is one of the most potent cancer drugs; however, its low solubility and strong systemic side effects limit its clinical applications. To overcome these issues, new drug formulations and chemical modifications have been proposed. In this s
- Ayalew, Luladey,Acuna, Jessica,Urfano, Selina F.,Morfin, Cristobal,Sablan, Anthony,Oh, Myungeun,Gamboa, Alicia,Slowinska, Katarzyna
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- Simple weak-acid derivatives of paclitaxel for remote loading into liposomes and improved therapeutic effects
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Liposomes are among the most successful nanocarriers; several products have been marketed, all of which were prepared by active loading methods. However, poorly water-soluble drugs without ionizable groups are usually incorporated into the lipid bi-layer
- Chi, Dongxu,He, Zhonggui,Li, Jinbo,Lin, Guimei,Liu, Dan,Su, Yujiao,Wang, Jiamei,Wang, Xue,Wang, Yingli,Wang, Yongjun,Yu, Jiang,Zhou, Shuang
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- Multicomponent Conjugates of Anticancer Drugs and Monoclonal Antibody with PAMAM Dendrimers to Increase Efficacy of HER-2 Positive Breast Cancer Therapy
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Purpose: Conjugation of nanocarriers with antibodies that bind to specific membrane receptors that are overexpressed in cancer cells enables targeted delivery. In the present study, we developed and synthesised two PAMAM dendrimer-trastuzumab conjugates t
- Marcinkowska, Monika,Stanczyk, Maciej,Janaszewska, Anna,Sobierajska, Ewelina,Chworos, Arkadiusz,Klajnert-Maculewicz, Barbara
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- Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant-taxoid conjugates as novel cytotoxic agents
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Various dietary antioxidants, including vitamins, flavonoids, curcumin, and a coumarin, were conjugated with paclitaxel (1) through an ester linkage. The newly synthesized compounds were evaluated for cytotoxic activity against several human tumor cell lines as well as the corresponding normal cell lines. Interestingly, most tested conjugates selectively inhibited the growth of 1A9 (ovarian) and KB (nasopharyngeal) tumor cells without activity against other cell lines. Particularly, conjugates 16 and 20 were highly active against 1A9 (ED50 value of 0.005 μg/mL) as well as KB (ED50 values of 0.005 and 0.14 μg/mL, respectively) cells. Compound 22b, the glycinate ester salt of vitamin E conjugated with 1, appears to be a promising lead for further development as a clinical trial candidate as it exhibited strong inhibitory activity against Panc-1 (pancreatic cancer) with less effect on the related E6E7 (normal) cell line.
- Nakagawa-Goto, Kyoko,Yamada, Koji,Nakamura, Seikou,Chen, Tzu-Hsuan,Chiang, Po-Cheng,Bastow, Kenneth F.,Wang, Shao-Chun,Spohn, Bill,Hung, Mien-Chie,Lee, Fang-Yu,Lee, Fang-Chen,Lee, Kuo-Hsiung
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- Nitrogen-doped Carbon Nanodots for bioimaging and delivery of paclitaxel
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Carbon nanodots (CNDs) hold great potential in imaging and drug delivery applications. In this study, nitrogen-doped CNDs (NCNDs) were coupled to the anticancer agent paclitaxel (PTX) through a labile ester bond. NCNDs showed excellent cell viability and
- Gomez, I. Jennifer,Arnaiz, Blanca,Cacioppo, Michele,Arcudi, Francesca,Prato, Maurizio
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- Synthesis and biological evaluation of paclitaxel and vorinostat co-prodrugs for overcoming drug resistance in cancer therapy in vitro
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Paclitaxel (PTX) is the first-line treatment drug for breast cancer. However, drug resistance after a course of treatment and low selectivity restricted its clinical utility sometimes. In this study, we successfully bound PTX and vorinostat (SAHA) to form
- Liu, Shuangxi,Zhang, Kaili,Zhu, Qiwen,Shen, Qianqian,Zhang, Qiumeng,Yu, Jiahui,Chen, Yi,Lu, Wei
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- Conjugation of paclitaxel on adeno-associated virus (AAV) nanoparticles for co-delivery of genes and drugs
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We have investigated the use of adeno-associated virus (AAV) nanoparticles as platforms for the co-delivery of genes and drugs to cancer cells. With its regular geometry, nanoscale dimensions, lack of pathogenicity, and high infection efficiency in a wide
- Wei, Fang,McConnell, Kellie I.,Yu, Tse-Kuan,Suh, Junghae
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- Preparation and characterization of novel poly(ethylene glycol) paclitaxel derivatives
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Paclitaxel has been found to be very effective against several human cancers; one of the major problems with its use is its poor solubility, which makes necessary its solubilization with excipients that can determine allergic reactions often severe. The a
- Arpicco, Silvia,Stella, Barbara,Schiavon, Oddone,Milla, Paola,Zonari, Daniele,Cattel, Luigi
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- Photoacoustic Imaging Quantifies Drug Release from Nanocarriers via Redox Chemistry of Dye-Labeled Cargo
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We report a new approach to monitor drug release from nanocarriers via a paclitaxel–methylene blue conjugate (PTX-MB) with redox activity. This construct is in a photoacoustically silent reduced state inside poly(lactic-co-glycolic acid) (PLGA) nanopartic
- Chen, Fang,Jeevarathinam, Ananthakrishnan Soundaram,Jokerst, Jesse V.,Lemaster, Jeanne E.,Zhao, Eric
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- Delivery platform for hydrophobic drugs: Prodrug approach combined with self-assembled multilayers
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We report the design of a platform for the delivery of hydrophobic drugs via a macromolecular prodrug approach combined with LbL-assembled polyelectrolyte multilayers. A hyaluronan ester prodrug of the chemotherapeutic drug paclitaxel has been synthesized
- Thierry, Benjamin,Kujawa, Piotr,Tkaczyk, Cathy,Winnik, Francoise M.,Bilodeau, Luc,Tabrizian, Maryam
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- Cancer nanomedicines stabilized by π-π stacking between heterodimeric prodrugs enable exceptionally high drug loading capacity and safer delivery of drug combinations
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Abstract Combination therapy using distinct mode-of-action drugs has sparked a rapidly growing interest because this paradigm holds promise for improving the therapeutic efficacy of anticancer therapy. However, the current drug combination therapy refers
- Wang, Hangxiang,Chen, Jianmei,Xu, Chang,Shi, Linlin,Tayier, Munire,Zhou, Jiahui,Zhang, Jun,Wu, Jiaping,Ye, Zhijian,Fang, Tao,Han, Weidong
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- Nitrogen-doped carbon nanodots for bioimaging and delivery of paclitaxel
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Carbon nanodots (CNDs) hold great potential in imaging and drug delivery applications. In this study, nitrogen-doped CNDs (NCNDs) were coupled to the anticancer agent paclitaxel (PTX) through a labile ester bond. NCNDs showed excellent cell viability and
- Gomez, I. Jennifer,Arnaiz, Blanca,Cacioppo, Michele,Arcudi, Francesca,Prato, Maurizio
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- Self-assembly of oxidation-responsive polyethylene glycol-paclitaxel prodrug for cancer chemotherapy
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Amphiphilic drug conjugates can self-assemble into nanovehicles for cancer drug delivery, but the key is to design stable yet intracellular labile drug linkers for drug retention during blood circulation but fast intracellular drug release. The conjugatio
- Dong, Chengyuan,Liu, Fusheng,Shen, Youqing,Xiang, Jiajia,Zhou, Quan,Zhou, Zhuxian
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- Superior antitumor effect of self-assembly supramolecular paclitaxel nanoparticles
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Paclitaxel (Ptx), a microtubule depolymerization inhibitor, is one of the first-line regimens in lung cancer chemotherapy. However, the poor solubility of Ptx, as well as hypersensitivity of the solvent Cremphor EL, severely limits its clinical applicatio
- Ding, Dan,Li, Jun,Li, Xiaolin,Xu, Huae,Yu, Na,Zhang, Yuan
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- Kinetic control over supramolecular hydrogelation and anticancer properties of taxol
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We reported a kinetic control over supramolecular hydrogelation and more importantly over the anticancer properties of taxol.
- Zhang, Xiaoli,Wang, Youzhi,Hua, Yongquan,Duan, Jinyou,Chen, Minsheng,Wang, Ling,Yang, Zhimou
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- Conjugated chitosan as a novel platform for oral delivery of paclitaxel
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A new platform for oral delivery of paclitaxel (PTX) was developed through chemical conjugation of PTX to a low molecular weight chitosan (LMWC). The LMWC-PTX conjugate contained ~12 wt % PTX and showed greatly enhanced water solubility (> 1 mg/mL) as com
- Lee, Eunhye,Lee, Jinju,Lee, In-Hyun,Yu, Mikyung,Kim, Hyungjun,Chae, Su Young,Jon, Sangyong
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- Far-Red Light-Activatable Prodrug of Paclitaxel for the Combined Effects of Photodynamic Therapy and Site-Specific Paclitaxel Chemotherapy
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Paclitaxel (PTX) is one of the most useful chemotherapeutic agents approved for several cancers, including ovarian, breast, pancreatic, and nonsmall cell lung cancer. However, it causes systemic side effects when administered parenterally. Photodynamic therapy (PDT) is a new strategy for treating local cancers using light and photosensitizer. Unfortunately, PDT is often followed by recurrence due to incomplete ablation of tumors. To overcome these problems, we prepared the far-red light-activatable prodrug of PTX by conjugating photosensitizer via singlet oxygen-cleavable aminoacrylate linker. Tubulin polymerization enhancement and cytotoxicity of prodrugs were dramatically reduced. However, once illuminated with far-red light, the prodrug effectively killed SKOV-3 ovarian cancer cells through the combined effects of PDT and locally released PTX. Ours is the first PTX prodrug that can be activated by singlet oxygen using tissue penetrable and clinically useful far-red light, which kills the cancer cells through the combined effects of PDT and site-specific PTX chemotherapy.
- Thapa, Pritam,Li, Mengjie,Bio, Moses,Rajaputra, Pallavi,Nkepang, Gregory,Sun, Yajing,Woo, Sukyung,You, Youngjae
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- Somatostatin receptor-mediated specific delivery of paclitaxel prodrugs for efficient cancer therapy
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In this study, a novel PTX prodrug, octreotide(Phe)-polyethene glycol-paclitaxel [OCT(Phe)-PEG-PTX], was successfully synthesized and used for targeted cancer therapy. A nontargeting conjugate, mPEG-PTX, was also synthesized and used as a control. Chemica
- Huo, Meirong,Zhu, Qinnv,Wu, Qu,Yin, Tingjie,Wang, Lei,Yin, Lifang,Zhou, Jianping
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- Polymeric micelles with water-insoluble drug as hydrophobic moiety for drug delivery
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The hydrophobic block of polymeric micelles formed by amphiphilic copolymers has no direct therapeutical effect, and the metabolites of these hydrophobic segments might lead to some unexpected side effects. Here the hydrophobic core of polymeric micelles
- Li, Guolin,Liu, Jinyao,Pang, Yan,Wang, Ruibin,Mao, Limin,Yan, Deyue,Zhu, Xinyuan,Sun, Jian
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- Drug-initiated, controlled ring-opening polymerization for the synthesis of polymer-drug conjugates
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Paclitaxel, a polyol chemotherapeutic agent, was covalently conjugated through its 2′-OH to polylactide with 100% regioselectivity via controlled polymerization of lactide mediated by paclitaxel/(BDI-II)ZnN(TMS)2 (BDI-II = 2-((2,6-diisopropylph
- Tong, Rong,Cheng, Jianjun
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- Conjugation of paclitaxel to C-6 hexanediamine-modified hyaluronic acid for targeted drug delivery to enhance antitumor efficacy
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Polymer-based paclitaxel (PTX) conjugates have demonstrated application potentials to improve the water solubility and enhance the efficiency of drug delivery. In this study, a novel HA-based drug conjugate, HA-6-PTX, was designed and successfully synthes
- Chen, Yangjian,Peng, Fujun,Song, Xiaoda,Wu, Jicheng,Yao, Wenbin,Gao, Xiangdong
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- Tumor-targeted polymeric nanostructured lipid carriers with precise ratiometric control over dual-drug loading for combination therapy in non-small-cell lung cancer
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Gemcitabine (GEM) and paclitaxel (PTX) are effective combination anticancer agents against non-small-cell lung cancer (NSCLC). At the present time, a main challenge of combination treatment is the precision of control that will maximize the combined effec
- Liang, Yan,Tian, Baocheng,Zhang, Jing,Li, Keke,Wang, Lele,Han, Jingtian,Wu, Zimei
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- Stepwise orthogonal click chemistry toward fabrication of paclitaxel/galactose functionalized fluorescent nanoparticles for hepg2 cell targeting and delivery
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In this report, we used stepwise orthogonal click chemistry (SOCC) involving strain-promoted azide-alkyne cycloaddition (SPAAC) and microwave-assisted Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) to assemble an anticancer drug (paclitaxel, PTX) and
- Lai, Chian-Hui,Chang, Tsung-Che,Chuang, Yung-Jen,Tzou, Der-Lii,Lin, Chun-Cheng
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- Design of a paclitaxel prodrug conjugate for active targeting of an enzyme upregulated in breast cancer cells
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Breast cancer is the second most common cause of cancer-related deaths in women. Chemotherapy is an important treatment modality, and paclitaxel (PTX) is often the first-line therapy for its metastatic form. The two most notable limitations related to PTX
- Satsangi, Arpan,Roy, Sudipa S.,Satsangi, Rajiv K.,Vadlamudi, Ratna K.,Ong, Joo L.
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- Synthesis and evaluation of water-soluble poly(vinyl alcohol)-paclitaxel conjugate as a macromolecular prodrug
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Paclitaxel (PTX) is an antitumor agent for the treatment of various human cancers. Cremophor EL and ethanol are used to formulate PTX in commercial injection solutions, because of its poor solubility in water. However, these agents cause severe allergic r
- Kakinoki, Atsufumi,Kaneo, Yoshiharu,Tanaka, Tetsuro,Hosokawa, Yoshitsugu
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- Biotin functionalized PEGylated poly(amidoamine) dendrimer conjugate for active targeting of paclitaxel in cancer
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In the current study, we employed poly(amidoamine) (PAMAM) dendrimers of generation 4 (G4) to deliver paclitaxel (PTX), a poorly soluble anti-cancer agent precisely to cancer cells via its conjugation on dendrimer surface. Further, G4 PAMAM has been PEGyl
- Rompicharla, Sri Vishnu Kiran,Kumari, Preeti,Bhatt, Himanshu,Ghosh, Balaram,Biswas, Swati
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- Design, synthesis and applications of hyaluronic acid-paclitaxel bioconjugates
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Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatment of breast and ovarian cancer, suffers from significant disadvantages such as low solubility, certain toxicity and specific drug-resistance of some tumor cells. To overcome thes
- Leonelli, Francesca,La Bella, Angela,Migneco, Luisa Maria,Bettolo, Rinaldo Marini
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- Preparation and in vitro evaluation of amphiphilic paclitaxel small molecule prodrugs and enhancement of oral absorption
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A series of novel amphiphilic paclitaxel (PTX) small molecule prodrugs, PTX-succinic anhydride-cystamine (PTX-Cys), PTX-dithiodipropionic anhydride (PTX-SS-COOH) and PTX-succinic anhydride-cystamine-valine (PTX-SS-Val) were designed, synthesized and evaluated against cancer cell lines. Compared with paclitaxel, these prodrugs contained water-soluble groups such as amino, carboxyl and amino acid, which improved the aqueous solubility of the prodrugs. More importantly, the valine was introduced in PTX-SS-Val molecule and made the molecule conform to the structural characteristics of intestinal oligopeptide transporter PEPT1 substrate. Thus the oral bioavailability of prodrug could be improved because of the mediation of PEPT1 transporter. These small molecule paclitaxel prodrugs could self-assemble into nanoparticles in aqueous solution, which effectively improved the solubility of paclitaxel, and had certain stability in pH 6.5, pH 7.4 buffer solutions and simulated gastrointestinal fluids. Some of these prodrugs, especially for PTX-Cys and PTX-SS-Val, exhibited nearly equal or slightly better anticancer activity when compared to paclitaxel. Further studies on PTX-Cys and PTX-SS-Val showed that both had good intestinal absorption in the rat single-pass intestinal perfusion (SPIP) experiments. Oral pharmacokinetic experiments showed that PTX-SS-Val could effectively improve the oral bioavailability of PTX.
- Li, Lingbing,Li, Yuanyuan,Xu, Wei,Yang, Min,Zhao, Yanli
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- Self-assembled nanoparticles from hyaluronic acid-paclitaxel prodrugs for direct cytosolic delivery and enhanced antitumor activity
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A prodrug-based nanosystem obtained by formulating prodrug and nanotechnology into a system is one of the most promising strategies to enhance drug delivery for disease treatment. Herein, we report a new nanosystem based on HA-PTX conjugates (HA-PTX Ns),
- Xu, Chaoran,He, Wei,Lv, Yaqi,Qin, Chao,Shen, Lingjia,Yin, Lifang
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- A novel multifunctional nanoparticles formed by molecular recognition between AS1411 aptamer and redox-responsive paclitaxel-nucleoside analogue prodrug for combination treatment of β-lapachone and paclitaxel
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Despite its high antitumor activity, the clinical application of chemotherapy is greatly impeded by lacking of specific accumulation and poor solubility. To address the above challenges, we designed a AS1411 aptamer modified nanoparticles based on molecular recognition of nucleobases. Firstly, a redox sensitive Paclitaxel-SS-Zidovudine (PZ) prodrug was synthesized. Then PZ/β-lapachone/AS1411/DSPE-PEG nanoparticles were prepared and AS1411 aptamer was connected through molecular recognition between the nucleoside analogue Zidovudine (ZDV) and the thymine on aptamer. DSPE-PEG (DP) was incorporated into nanoparticles to prolong the residence time of nanoparticles in the blood circulation. Furthermore, to realize the combination treatment, β-lapachone (LAP) has been incorporated into nanoparticles with high drug loading efficiency through the interaction of π-π stacking force and H-bonding between LAP and Paclitaxel (PTX). LAP can generate abundant exogenous reactive oxygen species (ROS) via the bioactivation of NAD(P)H: quinone oxidoreductase-1 (NQO1). Moreover, the connection of Zidovudine (ZDV) and AS1411 through molecular recognition of nucleobases further optimized the nanoparticles with high affinity to nucleolin which overexpressed on tumor cell membrane, thereby inducing the specific accumulation of nanoparticles in tumor sites. In vivo and in vitro studies showed that the obtained nanoparticles of PZ/LAP/AS1411/DP exhibited better tumor growth inhibition and lower systemic side effects. Herein, we have rationally conducted a novel self-codelivery system for effectively synergistic antitumor treatment.
- Chen, Xuling,Fan, Xiaohui,Ji, Jianbo,Li, Lingbing,Xu, Wei,Zhou, Ke
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- Fluorescence opening type diarylethene fluorescent probe, and preparation method and application thereof
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The invention provides a fluorescence opening type diarylethene fluorescent probe, and a preparation method and application thereof. The fluorescence opening type diarylethene fluorescent probe has a structure as shown in a formula I, the probe is compose
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Paragraph 0075; 0101-0103
(2021/07/28)
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- LHRH-PACLITAXEL CONJUGATES AND METHODS OF USE
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Aspects of the disclosure relate to compositions comprising Luteinizing Hormone Releasing Hormone (LHRH) or an analog of LHRH conjugated to paclitaxel, and methods of treatment of cancer, for example, triple negative breast cancer, using such compositions
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Paragraph 0129
(2021/05/07)
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- Reduction-Sensitive Dextran-Paclitaxel Polymer-Drug Conjugate: Synthesis, Self-Assembly into Nanoparticles, and in Vitro Anticancer Efficacy
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Delivery systems that can encapsulate a precise amount of drug and offer a spatiotemporally controlled drug release are being actively sought for safe yet effective cancer therapy. Compared to polymer nanoparticle (NP)-based delivery systems that rely on
- Kanwal, Sidra,Naveed, Muhammad,Arshad, Ali,Arshad, Azka,Firdous, Farhat,Faisal, Amir,Yameen, Basit
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p. 2516 - 2529
(2021/11/24)
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- A new NT4 peptide-based drug delivery system for cancer treatment
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The development of selective tumor targeting agents to deliver multiple units of chemotherapy drugs to cancer tissue would improve treatment efficacy and greatly advance progress in cancer therapy. Here we report a new drug delivery system based on a tetr
- Bracci, Luisa,Brunetti, Jlenia,Cipriani, Giulia,Depau, Lorenzo,Falciani, Chiara,Fragai, Marco,Menichetti, Stefano,Piantini, Sara,Pini, Alessandro,Scali, Silvia
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- Paclitaxel weakly acidic derivative active medicine carrier liposome and preparation method and application thereof
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The invention belongs to the field of liposome drug delivery, and relates to a paclitaxel weakly acidic derivative active medicine carrier liposome and a preparation method and application thereof. The paclitaxel weakly acidic derivative is provided, and
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Paragraph 0043-0046
(2020/05/01)
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- Water-soluble anti-tumor compounds
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The invention relates to a water-soluble antitumor compound represented by the formula (I), and further relates to a preparation method of the compound and an application of the compound in preparation of antitumor drugs. Stable prodrug with a good water
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Paragraph 0139-0143
(2019/05/04)
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- BIGUANIDINE DERIVATIVES OF THERAPEUTIC AGENTS AND METHODS OF PREPARATION AND USE THEREOF
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The invention includes biguanidine derivatives of therapeutic agents of Formula IA or Formula IB including pharmaceutically acceptable, prodrugs, metabolites and isomers thereof. The invention also provides methods of preparation and use of these compound
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Page/Page column 250-251
(2019/04/09)
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- Micro-molecule modified taxane water soluble prodrug and pharmaceutical applications thereof
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The invention belongs to the field of biomedicine, and relates to a micro-molecule modified taxane water soluble prodrug and pharmaceutical applications thereof. The invention provides a micro-molecule modified taxane water soluble prodrug represented by
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Paragraph 0034; 0035; 0036; 0037-0039
(2019/03/26)
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- Multi-arm type PEG paclitaxel derivative and preparation thereof
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According to a preparation method of a multi-arm PEG paclitaxel derivative, by utilizing the nontoxicity and easy-to-combination characteristics of multi-arm PEG, four-arm PEG, six-arm PEG and eight-arm PEG are connected with paclitaxel by virtue of a hyd
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Paragraph 0028-0030; 0033; 0038; 0043; 0048; 0053; 0058
(2018/12/02)
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- Co-prodrug of vorinostat and paclitaxel as well as preparation method and application thereof
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The invention discloses a co-prodrug of vorinostat and paclitaxel as well as a preparation method and application thereof, wherein the co-prodrug is coated with vorinostat and paclitaxel at the same time and has the structure of the formula I; the prepara
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Paragraph 0062; 0063; 0064; 0065
(2018/09/08)
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- Anti-tumor medicine conjugate, preparation method, preparation and application
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The invention discloses an anti-tumor medicine conjugate, a preparation method, nano-micelle preparation thereof and application. The structural formula of the conjugate provided by the invention is represented by the formula (I), and the conjugate is for
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Paragraph 0060; 0061; 0062; 0063; 0064; 0065
(2017/06/10)
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- Targeted polymeric conjugates and uses thereof
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Polymeric conjugates comprising a polymeric backbone having attached thereto a bone targeting moiety and a therapeutically active agent, wherein the bone targeting moiety is attached to one end of the polymeric backbone via a branching unit such that a mo
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Page/Page column 45
(2016/04/05)
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- Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity
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Novel water-soluble paclitaxel prodrugs were designed and synthesized by introducing morpholino groups through different linkers. These derivatives showed 400–20,000-times greater water solubility than paclitaxel as well as comparable activity in MCF-7 an
- Feng, Siliang,Chen, Kuncheng,Wang, Chenhong,Jiang, Xifeng,Dong, Huajin,Gong, Zehui,Liu, Keliang
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p. 3598 - 3602
(2016/07/21)
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- PRODRUG COMPOSITIONS, PRODRUG NANOPARTICLES, AND METHODS OF USE THEREOF
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The present invention encompasses prodrug compositions, nanoparticles comprising one or more prodrugs, and methods of use thereof.
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Paragraph 0017; 0113
(2016/10/17)
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- HYDROGELATORS COMPRISING D-AMINO ACIDS
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Described herein are compounds comprising an oligopeptide and a non-steroidal antiinflammatory agent. The compounds self-assemble into supramolecular hydrogels and can be used as topical treatments for inflammatory conditions, such as osteoarthritis. Also
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Page/Page column 57
(2014/05/24)
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- Dephosphorylation of d -peptide derivatives to form biofunctional, supramolecular nanofibers/hydrogels and their potential applications for intracellular imaging and intratumoral chemotherapy
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d-Peptides, as the enantiomers of the naturally occurring l-peptides, usually resist endogenous proteases and are presumably insensitive to most enzymes. But, it is unclear whether or how a phosphatase catalyzes the dephosphorylation from d-peptides. In t
- Li, Jiayang,Gao, Yuan,Kuang, Yi,Shi, Junfeng,Du, Xuewen,Zhou, Jie,Wang, Huaimin,Yang, Zhimou,Xu, Bing
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supporting information
p. 9907 - 9914
(2013/07/26)
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- Design, synthesis, and biological evaluation of novel cRGD-paclitaxel conjugates for integrin-assisted drug delivery
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The efficacy of taxane-based antitumor therapy is limited by several drawbacks which result in a poor therapeutic index. Thus, the development of approaches that favor selective delivery of taxane drugs (e.g., paclitaxel, PTX) to the disease area represen
- Pilkington-Miksa, Michael,Arosio, Daniela,Battistini, Lucia,Belvisi, Laura,De Matteo, Marilenia,Vasile, Francesca,Burreddu, Paola,Carta, Paola,Rassu, Gloria,Perego, Paola,Carenini, Nives,Zunino, Franco,De Cesare, Michelandrea,Castiglioni, Vittoria,Scanziani, Eugenio,Scolastico, Carlo,Casiraghi, Giovanni,Zanardi, Franca,Manzoni, Leonardo
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experimental part
p. 1610 - 1622
(2012/10/08)
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- Synthesis and biological evaluation (in Vitro and in Vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrin αvβ3
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A small library of integrin ligand-paclitaxel conjugates 10-13 was synthesized with the aim of using the tumor-homing cyclo[DKP-RGD] peptidomimetics for site-directed delivery of the cytotoxic drug. All the paclitaxel-RGD constructs 10-13 inhibited biotinylated vitronectin binding to the purified αVβ3 integrin receptor at low nanomolar concentration and showed in vitro cytotoxic activity against a panel of human tumor cell lines similar to that of paclitaxel. Among the cell lines, the cisplatin-resistant IGROV-1/Pt1 cells expressed high levels of integrin αVβ3, making them attractive to be tested in in vivo models. cyclo[DKP-f3-RGD]-PTX 11 displayed sufficient stability in physiological solution and in both human and murine plasma to be a good candidate for in vivo testing. In tumor-targeting experiments against the IGROV-1/Pt1 human ovarian carcinoma xenotransplanted in nude mice, compound 11 exhibited a superior activity compared with paclitaxel, despite the lower (about half) molar dosage used.
- Colombo, Raffaele,Mingozzi, Michele,Belvisi, Laura,Arosio, Daniela,Piarulli, Umberto,Carenini, Nives,Perego, Paola,Zaffaroni, Nadia,De Cesare, Michelandrea,Castiglioni, Vittoria,Scanziani, Eugenio,Gennari, Cesare
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supporting information
p. 10460 - 10474
(2013/02/22)
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- Conjugation of two complementary anti-cancer drugs confers molecular hydrogels as a co-delivery system
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We reported in this communication on the first example of a molecular hydrogel system based on two complementary anti-cancer drugs for chemotherapy.
- Mao, Lina,Wang, Huaimin,Tan, Ming,Ou, Lailiang,Kong, Deling,Yang, Zhimou
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supporting information; experimental part
p. 395 - 397
(2012/02/01)
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- Transferrin-modified c[RGDfK]-paclitaxel loaded hybrid micelle for sequential blood-brain barrier penetration and glioma targeting therapy
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The effective chemotherapy for glioblastoma multiform (GBM) requires a nanomedicine that can both penetrate the blood-brain barrier (BBB) and target the glioma cells subsequently. In this study, Transferrin (Tf) modified cyclo-[Arg-Gly-Asp-d-Phe-Lys] (c[RGDfK])-paclitaxel conjugate (RP) loaded micelle (TRPM) was prepared and evaluated for its targeting efficiency, antiglioma activity, and toxicity in vitro and in vivo. Tf modification significantly enhanced the cellular uptake of TRPM by primary brain microvascular endothelial cells (BMEC) to 2.4-fold of RP loaded micelle (RPM) through Tf receptor mediated endocytosis, resulting in a high drug accumulation in the brain after intravenous injection.The c[RGDfK] modified paclitaxel (PTX) was released from micelle subsequently and targeted to integrin overexpressed glioma cells in vitro, and showed significantly prolonged retention in glioma tumor and peritumoral tissue. Most importantly, TRPM exhibited the strongest antiglioma activity, as the mean survival time of mice bearing intracranial U-87 MG glioma treated with TRPM (42.8 days) was significantly longer than those treated with Tf modified PTX loaded micelle (TPM) (39.5 days), PTX loaded micelle (PM) (34.8 days), Taxol (33.6 days), and saline (34.5 days). Noteworthy, TRPM did not lead to body weight loss compared with saline and was less toxic than TPM. These results indicated that TRPM could be a promising nanomedicine for glioma chemotherapy.
- Zhang, Pengcheng,Hu, Luojuan,Yin, Qi,Feng, Linyin,Li, Yaping
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experimental part
p. 1590 - 1598
(2012/09/08)
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- ANTINEOPLASTIC HYDROGELS, AND ENZYME-INSTRUCTED PREPARATIONS THEREOF
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Disclosed is a general methodology to create nano fibers of therapeutic molecules that have a dual role, as both the delivery vehicle and the drug itself. It is shown that with proper molecular design, the integration of enzymatic reaction and self-assemb
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Page/Page column 40-41
(2011/01/12)
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- THIOLATED PACLITAXELS FOR REACTION WITH GOLD NANOPARTICLES AS DRUG DELIVERY AGENTS
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Thioloated taxane derivatives are linked to colloidal metal particles such as gold nanoparticles for use as antitumor agents. The antitumor agents may be targeted to tumors.
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Page/Page column 76-77
(2009/06/27)
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- Enzyme-instructed molecular self-assembly confers nanofibers and a supramolecular hydrogel of taxol derivative
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(Figure Presented) By covalently connecting taxol with a motif that is prone to self-assemble, we successfully generate the precursor (5a), the hydrogelator (5b), and hydrogel of a taxol derivative without compromising the cytotoxic activity of the taxol.
- Gao, Yuan,Kuang, Yi,Guo, Zu-Feng,Guo, Zhihong,Krauss, Isaac J.,Xu, Bing
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supporting information; experimental part
p. 13576 - 13577
(2010/01/06)
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- DRUG DELIVERY SYSTEM BASED ON REGIOSELECTIVELY AMIDATED HYALURONIC ACID
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New drug delivery systems (DDS) are described containing hyaluronic acid and a therapeutic agent, wherein the therapeutic agent is linked, directly or via a linker, to 6-aminohyaluronic acid and where the linkage of the drug or linker with 6-aminohyaluron
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Page/Page column 33
(2008/06/13)
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