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Related Concept Videos

Prodrugs01:30

Prodrugs

2.8K
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...
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Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

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Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

389
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
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Related Experiment Video

Updated: Sep 5, 2025

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

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Degradable polyprodrugs: design and therapeutic efficiency.

Farzad Seidi1,2, Yajie Zhong1, Huining Xiao3

  • 1Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources and International Innovation Center for Forest Chemicals and Materials, Nanjing Forestry University, Nanjing 210037, China. f_seidi@njfu.edu.cn.

Chemical Society Reviews
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PubMed
Summary

Polyprodrugs, polymers of drug monomers, offer enhanced therapeutic properties and controlled drug release. Their complete degradation ensures safe disposal, with tailored linkages enabling targeted delivery and stimuli-responsive breakdown.

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Area of Science:

  • Polymer Chemistry
  • Drug Delivery Systems
  • Nanomedicine

Background:

  • Prodrugs enhance drug efficacy and reduce side effects.
  • Polyprodrugs are polymers of drug monomers designed for gradual therapeutic agent release.
  • Complete degradation of polyprodrugs is crucial for safe in-vivo clearance.

Purpose of the Study:

  • To review the development and applications of polyprodrugs.
  • To highlight the role of covalent bond types in controlling degradation and drug release rates.
  • To explore the potential of stimuli-responsive polyprodrugs for targeted cancer therapy.

Main Methods:

  • Synthesis and characterization of various polyprodrugs based on different polymer backbones (polyesters, polyanhydrides, etc.).
  • Incorporation of stimuli-responsive linkages (redox, pH, light, enzyme) for controlled degradation.
  • Investigation of degradation mechanisms and drug release kinetics.

Main Results:

  • Diverse polyprodrug architectures demonstrate tunable degradation and drug release profiles.
  • Stimuli-responsive linkages enable selective polymer backbone cleavage in targeted environments like tumors.
  • Various polymer classes (polyesters, polyamides, etc.) have been successfully utilized for polyprodrug development.

Conclusions:

  • Polyprodrugs represent a versatile platform for advanced drug delivery.
  • Tailoring polymer structure and linkages allows for precise control over drug release and degradation.
  • Future strategies may combine polyprodrugs with gene delivery and targeting moieties for synergistic therapies.