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Related Concept Videos

Prodrugs01:30

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

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Related Experiment Video

Updated: May 19, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
09:56

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

PolyMPC-doxorubicin prodrugs.

Xiangji Chen1, Sangram S Parelkar, Elizabeth Henchey

  • 1Polymer Science & Engineering Department, 120 Governors Drive, University of Massachusetts, Amherst, Massachusetts 01003, USA.

Bioconjugate Chemistry
|August 14, 2012
PubMed
Summary

We developed a polymer-drug conjugate for cancer therapy, linking doxorubicin (DOX) to poly(methacryloyloxyethyl phosphorylcholine) (polyMPC). The conjugate showed pH-dependent drug release and promising anti-cancer activity in cell cultures and mice.

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Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice
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Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
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Last Updated: May 19, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
09:56

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice
08:57

Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice

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Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
10:53

Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions

Published on: October 10, 2016

Area of Science:

  • Polymer Chemistry
  • Drug Delivery Systems
  • Biomedical Engineering

Background:

  • Developing effective drug delivery systems is crucial for cancer therapy.
  • Polymeric conjugates offer advantages in drug solubility, stability, and targeted delivery.
  • Doxorubicin (DOX) is a widely used chemotherapeutic agent with limitations in its free form.

Purpose of the Study:

  • To synthesize and characterize doxorubicin (DOX) conjugated to poly(methacryloyloxyethyl phosphorylcholine) (polyMPC).
  • To evaluate the pH-dependent drug release kinetics of the polyMPC-DOX conjugates.
  • To assess the in vitro and in vivo efficacy and safety of the developed polymer-drug conjugates.

Main Methods:

  • Conjugation of DOX to polyMPC via hydrazone linkages using a one-pot ATRP/click sequence and post-polymerization strategies.
  • Characterization of polymer-drug conjugates, including molecular weight and drug loading.
  • In vitro drug release studies at different pH values (5.0 and 7.4).
  • Cell culture experiments to determine intracellular drug accumulation and IC(50) values.
  • In vivo maximum tolerated dose studies in healthy mice.

Main Results:

  • Two methods for polyMPC-DOX conjugation were established: a one-pot sequence and post-polymerization conjugation.
  • Post-polymerization conjugation yielded higher molecular weight polymers with significantly higher DOX loading.
  • DOX release was pH-dependent, with faster release observed at pH 5.0 compared to pH 7.4, attributed to the hydrazone linkage.
  • Highly loaded polyMPC-DOX conjugates demonstrated enhanced intracellular drug accumulation and lower IC(50) values in cell culture.
  • A polymer with 30 wt % drug loading exhibited a maximum tolerated dose of 30-50 mg/kg DOX equivalent weight in mice.

Conclusions:

  • PolyMPC-DOX conjugates can be synthesized efficiently using either one-pot or post-polymerization methods.
  • The hydrazone linkage ensures pH-sensitive DOX release, beneficial for tumor microenvironments.
  • The developed conjugates show potent anti-cancer activity and acceptable safety profiles, indicating their potential as advanced cancer therapeutics.