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Preparation of poly(β-L-malic acid)-based charge-conversional nanoconjugates for tumor-specific uptake and cellular delivery.

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In this study, a multifunctional poly(β-L-malic acid)-based nanoconjugate with a pH-dependent charge conversional characteristic was developed for tumor-specific drug delivery. The short branched polyethylenimine-modified poly(β-L-malic acid) (PEPM) was first synthesized. Then, the fragment HAb18

Brain tumor tandem targeting using a combination of monoclonal antibodies attached to biopoly(beta-L-malic acid).

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Tumor-specific targeting using achievements of nanotechnology is a mainstay of increasing efficacy of anti-tumor drugs. To improve drug targeting we covalently conjugated for the first time two different monoclonal antibodies, an anti-mouse transferrin receptor antibody and a mouse autoimmune

New functional degradable and bio-compatible nanoparticles based on poly(malic acid) derivatives for site-specific anti-cancer drug delivery.

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Design of an efficient site-specific drug delivery system based on degradable functional polymers still remains challenging. In this work, we synthesized and characterized three degradable functional polyesters belonging to the poly(malic acid) family: the poly(benzyl malate) (PMLABe), the

Temozolomide delivery to tumor cells by a multifunctional nano vehicle based on poly(β-L-malic acid).

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OBJECTIVE Temozolomide (TMZ) is a pro-drug releasing a DNA alkylating agent that is the most effective drug to treat glial tumors when combined with radiation. TMZ is toxic, and therapeutic dosages are limited by severe side effects. Targeted delivery is thus needed to improve efficiency and reduce

Methanol Extract of Coleus amboinicus (Lour) Exhibited Antiproliferative Activity and Induced Programmed Cell Death in Colon Cancer Cell WiDr.

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Coleus amboinicus(Lour) (CA) has been reported to possess many pharmacological activities. In this study, evaluation of cytotoxicity using brine shrimp lethality bioassay and MTT assay using WiDr cell lines was carried out. The expression of several genes responsible for programmed cell death

Effects of poly(ethylene glycol) grafting density on the tumor targeting efficacy of nanoparticles with ligand modification.

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To evaluate the effects of poly(ethylene glycol) (PEG) grafting density on the tumor targeting efficacy of nanoparticles (NPs) with ligand modification, various amounts of PEG were conjugated to linoleic acid and poly(β-malic acid) double grafted chitosan (LMC) NPs bearing similar substitution

Flavonolignans and other constituents from Lepidium meyenii with activities in anti-inflammation and human cancer cell lines.

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From the roots of Lepidium meyenii Walpers (Brassicaceae) have been isolated and identified 2 flavonolignans, tricin 4'-O-[threo-β-guaiacyl-(7″-O-methyl)-glyceryl] ether (1) and tricin 4'-O-(erythro-β-guaiacyl-glyceryl) ether (2), along with 11 other known compounds, tricin (3), pinoresinol (4),

Advances in Imaging: Brain Tumors to Alzheimer's Disease.

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Professor Black and colleagues have been working to improve the quality and sensitivity of imaging in the early detection of conditions from brain tumors to Alzheimer's disease to enhance treatment protocols and patient management. Professor Black et al introduced nanoparticles to improve MRI

MMP-2 sensitive poly(malic acid) micelles stabilized by π-π stacking enable high drug loading capacity

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Poly(β-l-malic acid) (PMLA) together with its derivatives is an aliphatic polyester with superior bio-properties for anti-tumor drugs. In order to surmount the obstacles of low drug loading and rapid premature release during the circulation of polyester-based micelles, micelles based on

Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid.

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The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2' modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is generated upon exposure to human plasma,

Preparation and biological evaluation of a novel pH-sensitive poly (β-malic acid) conjugate for antitumor drug delivery.

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Poly (β‑malic acid), referred to as PMLA, has been synthesized and introduced as a polymeric drug carrier due to its desirable biological properties. In the present study, a novel pH‑sensitive polymer‑drug conjugate based on PMLA, PMLA‑Hz‑doxorubicin (DOX), was prepared, and another conjugate,

Polymalic acid-based nanobiopolymer provides efficient systemic breast cancer treatment by inhibiting both HER2/neu receptor synthesis and activity.

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Biodegradable nanopolymers are believed to offer great potential in cancer therapy. Here, we report the characterization of a novel, targeted, nanobiopolymeric conjugate based on biodegradable, nontoxic, and nonimmunogenic PMLA [poly(β-l-malic acid)]. The PMLA nanoplatform was synthesized for

Dual-pH Sensitive Charge-reversal Nanocomplex for Tumor-targeted Drug Delivery with Enhanced Anticancer Activity.

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Poly(β-L-malic acid) (PMLA), a natural aliphatic polyester, has been proven to be a promising carrier for anti-cancer drugs. In spite of excellent bio-compatibility, the application of PMLA as the drug carrier for cancer therapy is limited by its low cellular uptake efficiency. The strong negative

Optimal Design of Novel Functionalized Nanoconjugates Based on Polymalic Acid for Efficient Tumor Endocytosis with Enhanced Anticancer Activity.

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To overcome the strong negative charge and improve the endocytosis of poly-β-malic acid (PMLA) as a drug carrier, a pH-sensitive nanoconjugate of PMLA/hyd-PEG5000/PEG2000-TAT/DOX (PHPTD) was developed. The trans activator of transcription (TAT) modified with polyethylene glycol2000(PEG2000) was

In situ gelation of supramolecular hydrogel for anti-tumor drug delivery.

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A supramolecular injectable hydrogel was fabricated. The hydrogel was in situ gelated by the host-guest interaction between alpha-cyclodextrins (alpha-CDs) and methylated poly(ethylene glycol) grafted poly(alpha,beta-malic acid) (mPEG-g-PMA). The hydrogel was characterized by (1)NMR, XRD, DSC, TGA

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