Related Experiment Video
Updated: May 13, 2026
11:25
Targeting Cysteine Thiols for in Vitro Site-specific Glycosylation of Recombinant Proteins
Published on: October 4, 2017
pH-triggered intracellular release from actively targeting polymer micelles.
Xing Guo1, Chunli Shi, Jie Wang
1Key Laboratory of Advanced Technologies of Materials, Ministry of Education, School of Materials Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China.
Biomaterials
|March 21, 2013
Summary
This study presents a novel pH-sensitive nanocarrier for cancer therapy. The developed drug-conjugated micelle shows enhanced tumor targeting, improved cellular uptake, and superior antitumor efficacy with minimal systemic toxicity.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Chemotherapy faces limitations due to systemic toxicity and low efficacy.
- Nanocarrier systems offer targeted drug delivery to cancer cells, overcoming these limitations.
- Developing advanced drug delivery systems is crucial for improving cancer treatment outcomes.
Purpose of the Study:
- To develop a novel pH-sensitive, folic acid-functionalized micellar nanocarrier for targeted doxorubicin (DOX) delivery.
- To evaluate the enhanced cellular uptake, cytotoxicity, and in vivo performance of the developed nanocarrier compared to controls.
- To assess the potential of this nanocarrier as an effective and safe platform for cancer therapy.
Main Methods:
- Fabrication of doxorubicin (DOX)-conjugated poly(ethylene glycol)-poly(ε-caprolactone) micelles functionalized with folic acid (FA) and a pH-sensitive hydrazone linker (FA-hyd).
- In vitro evaluation using Alamar blue assays, flow cytometry, and confocal laser scanning microscopy (CLSM) to assess cellular uptake and cytotoxicity.
- In vivo pharmacokinetic, biodistribution, and antitumor efficacy studies in relevant models.
Main Results:
- The FA-hyd micelle demonstrated excellent biocompatibility and superior cellular uptake and cytotoxicity in tumor cells compared to control micelles.
- In vivo studies showed prolonged blood circulation time and significant drug enrichment in tumors.
- FA-hyd micelles exhibited the highest safety profile and the best therapeutic efficacy against tumors.
Conclusions:
- The pH-sensitive, FA-functionalized DOX-conjugated micelle (FA-hyd) represents a promising nanocarrier for targeted cancer therapy.
- This system effectively overcomes the limitations of traditional chemotherapy by enhancing drug delivery and reducing systemic toxicity.
- The developed nanocarrier shows significant potential for clinical application in cancer treatment.
More Related Videos
10:53Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
08:39Magnetic and Thermal-sensitive Poly(N-isopropylacrylamide)-based Microgels for Magnetically Triggered Controlled Release
Published on: July 4, 2017
Related Concept Videos
01:30Modified-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 called...
01:11IP3/DAG Signaling Pathway
Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and produces two-second...
01:24Site-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...
01:26Fusion of Secretory Vesicles with the Plasma Membrane
Proteins and neurotransmitters in secretory vesicles can be released from a cell upon vesicle docking, priming, and fusion with the plasma membrane. Vesicles are docked and primed in preparation for the quick exocytosis of their contents in response to a stimulus. The fusion process is mainly carried out by a SNAP Receptor or SNARE complex, consisting of synaptobrevin, syntaxin-1, and SNAP-25.
In 1993, Jim Rothman proposed that the antiparallel pairing of vesicular and transmembrane SNAREs, or...
In 1993, Jim Rothman proposed that the antiparallel pairing of vesicular and transmembrane SNAREs, or...
01:12What are Second Messengers?
Because many receptor binding ligands are hydrophilic, they do not cross the cell membrane and thus their message must be relayed to a second messenger on the inside. There are several second messenger pathways, each with their own way of relaying information. G-protein coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol path is active when the receptor induces phospholipase C to hydrolyze the phospholipid,...
01:19Translocation of Proteins into the Mitochondria
Mitochondrial precursors are translocated to the internal subcompartments via independent mechanisms involving distinct protein machineries called translocases.
Sorting of outer membrane proteins:
Mitochondrial outer membrane proteins are of two types: the transmembrane, beta-barrel porins, and the membrane-anchored, alpha-helical proteins. Beta-barrel porin precursors are translocated by the TOM complex and inserted into the outer mitochondrial membrane by the SAM complex. In contrast,...
Sorting of outer membrane proteins:
Mitochondrial outer membrane proteins are of two types: the transmembrane, beta-barrel porins, and the membrane-anchored, alpha-helical proteins. Beta-barrel porin precursors are translocated by the TOM complex and inserted into the outer mitochondrial membrane by the SAM complex. In contrast,...