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Polymers02:34

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The word polymer is derived from the Greek words “poly” which means “many” and “mer” which means “parts”. Polymers are long chains of molecules composed of repeating units of smaller molecules, known as monomers. They either occur naturally, such as DNA and proteins, or can be constructed synthetically, like plastics. They have varied structural characteristics, such as linear chains, branched chains, or complex networks, that contribute to the...
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Density is an important characteristic of substances, crucial in determining whether an object sinks or floats in a fluid. Its SI unit is kg/m3, and its cgs unit is g/cm3. The density of an object helps in identifying its composition, and also reveals information about the phase of the matter and its substructure. The densities of liquids and solids are roughly comparable, consistent with the fact that their atoms are in close contact. However, gases have much lower densities than liquids and...
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Vesicle budding is orchestrated by distinct cytosolic proteins such as adaptor proteins, coat proteins, and GTPases. To initiate vesicle budding, membrane-bending proteins containing crescent-shaped BAR domains bind to the lipid heads in the bilayer and distort the membrane to form a protein-coated vesicle bud. Adaptors proteins such as AP2 for clathrin-coated vesicles can nucleate on the deformed membrane. Finally, coat proteins such as clathrin or COPI and COPII assemble into a coat forming...
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Membrane-enclosed structures called vesicles transport proteins and lipids across the cell. The vesicles derive their cargo from the plasma membrane, Golgi, ER, or endosome. Coated vesicles are spherical, protein-coated carriers with a 50–100 nm diameter that mediate bidirectional transport between the ER and the Golgi. The distribution of proteins between the ER and Golgi complex is dynamic and is maintained by different coated vesicles. Their formation is driven by the assembly of...
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Related Experiment Video

Updated: Feb 10, 2026

High-Density Lipoprotein-Specific Phospholipid Efflux Assay
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Polymer-coated pH-responsive high-density lipoproteins.

Hyungjin Kim1, Haruki Okamoto1, Arnaud E Felber2

  • 1Institute for Integrated Cell-Material Science (WPI-iCeMS), Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|March 10, 2016
PubMed
Summary
This summary is machine-generated.

This study introduces cationized high-density lipoprotein (catHDL) nanoparticles that improve drug delivery by enhancing endosomal escape. The catHDL/PA complex shows pH-dependent control, boosting anti-cancer drug efficacy in tumor cells.

Keywords:
Anticancer drug deliveryEndosomal escapeInternalizationMembranolytic polymerMildly acidic pH

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Area of Science:

  • Biotechnology
  • Nanomedicine
  • Drug Delivery

Background:

  • Intracellular drug delivery faces challenges like endosomal entrapment and lysosomal degradation.
  • High-density lipoprotein (HDL) is a natural nanocarrier with potential for drug delivery.
  • Controlling nanoparticle uptake and endosomal escape is crucial for effective intracellular delivery.

Purpose of the Study:

  • To develop a pH-dependent nanocarrier system for enhanced intracellular drug delivery.
  • To control the internalization and endosomal escape of cargoes using cationized HDL (catHDL) complexed with a block polymer.
  • To evaluate the efficacy of the developed nanocarrier for delivering anti-cancer drugs.

Main Methods:

  • Preparation of genetically and chemically cationized HDL (catHDL).
  • Complexation of catHDL with an anionic block polymer (poly(ethylene glycol)-block-poly(propyl methacrylate-co-methacrylic acid), PA) to form catHDL/PA.
  • Evaluation of pH-dependent internalization and endosomal escape in human cancer cells.
  • Assessment of anti-cancer drug (doxorubicin, curcumin) delivery and cytotoxicity.

Main Results:

  • catHDL/PA exhibits pH-dependent internalization, inhibited at neutral pH and recovered at acidic pH.
  • A stable, discoidal catHDL/PA complex (approx. 50 nm) was formed, stable in serum.
  • Enhanced endosomal escape of catHDL components and encapsulated drugs (doxorubicin, curcumin) was observed.
  • Enhanced cellular cytotoxicity of delivered anti-cancer drugs was confirmed.

Conclusions:

  • The catHDL/PA complex offers a novel, pH-responsive system for intracellular drug delivery.
  • This nanocarrier system effectively promotes endosomal escape of therapeutic cargoes.
  • catHDL/PA holds potential for improving cancer therapy, particularly in the acidic tumor microenvironment.