Related Experiment Video

Updated: Mar 9, 2026

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
09:34

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells

Published on: February 9, 2019

9.5K

Light induced drug release from a folic acid-drug conjugate

M Michael Dcona1, Jonathon E Sheldon2, Deboleena Mitra2

  • 1The Massey Cancer Center, 401 College St., Richmond, VA 23298-0037, USA; Department of Internal Medicine, Virginia Commonwealth University, 1101 E. Marshall St., Richmond, VA 23298, USA.

Bioorganic & Medicinal Chemistry Letters
|January 2, 2017
PubMed

Insights

Researchers developed a novel small-molecule conjugate for targeted cancer therapy. Folic acid delivers doxorubicin to tumor cells, releasing the drug with light for improved efficiency and simplicity.

Area of Science:

  • Oncology
  • Drug Delivery Systems
  • Photochemistry

Background:

  • Targeted cancer therapies aim to increase drug specificity by using delivery vehicles that bind to receptors overexpressed on tumor cells.
  • Folic acid is frequently conjugated to drug carriers to target folate receptors on cancer cells, facilitating cellular uptake.
  • Effective drug release after cellular internalization is crucial to prevent drug sequestration within endosomes.

Purpose of the Study:

  • To synthesize and characterize a small-molecule conjugate for targeted drug delivery.
  • To investigate the light-triggered release of doxorubicin from a folic acid-based construct.
  • To evaluate the advantages of this small-molecule approach over traditional macromolecular drug delivery systems.

Main Methods:

  • Synthesis of a small-molecule conjugate linking folic acid to doxorubicin via a photocleavable linker.
  • High-Performance Liquid Chromatography (HPLC) to assess drug release kinetics.
  • Photochemical activation to trigger doxorubicin release.

Main Results:

  • Successful synthesis of the folic acid-doxorubicin photocleavable conjugate.
  • Demonstration of rapid and highly efficient doxorubicin release upon light exposure, confirmed by HPLC.
  • The small-molecule approach offers enhanced simplicity and efficiency compared to macromolecular systems.

Conclusions:

  • A novel photocleavable small-molecule conjugate enables targeted delivery and light-triggered release of doxorubicin.
  • This strategy offers a promising alternative to macromolecular drug delivery systems for cancer therapy.
  • The simplicity and efficiency of light-triggered release present significant advantages for clinical applications.
Keywords:
Drug releaseEndosomal entrapmentFolic acidHPLCPhotocage

More Related Videos

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies08:54

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

1.6K
Development and Characterization of Fusidic Acid-Loaded Alginate-Aloe vera Based Hydrogel FilmWound Healing04:09

Development and Characterization of Fusidic Acid-Loaded Alginate-Aloe vera Based Hydrogel FilmWound Healing

Published on: December 13, 2024

1.4K

Related Concept Videos

Modified-Release Drug Delivery Systems: Stimuli-Activated01:30

Modified-Release Drug Delivery Systems: Stimuli-Activated

Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also...
58
Modified-Release Drug Delivery Systems: Drug Release Characteristics01:22

Modified-Release Drug Delivery Systems: Drug Release Characteristics

Drug release from modified-release dosage forms is designed to achieve specific therapeutic effects by controlling the rate and extent of drug release. The classification of these drug release systems is based on key pharmacokinetic assumptions: drug disposition follows first-order kinetics, drug release is the rate-limiting step in absorption, and the released drug is rapidly and completely absorbed.There are four major models of drug release patterns. The first model is the slow zero-order...
91
Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
5.4K
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
70
Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
60
Modified-Release Drug Delivery Systems: Influencing Factors01:20

Modified-Release Drug Delivery Systems: Influencing Factors

Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...
94