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Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

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Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
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The ER synthesizes lipids for building cell membranes and performing cellular functions such as energy storage and signaling. The lipid synthesis machinery embedded in the ER membrane primarily collects all reactants from the cytosol. Following synthesis, the secretory pathway and the ER contact sites distribute these lipids to other cellular organelles. Additionally, the energy-rich triacylglycerides are transported from the ER via lipid droplets.
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Clathrin-coated vesicles use endocytosis to transport receptors and lysosomal hydrolases from the Golgi to the lysosome in the late secretory pathway. Clathrin-mediated endocytosis was the first described endocytic process, and Clathrin-coated vesicles remain one of the most well-studied transport vesicles. The molecular machinery that generates clathrin-coated vesicles comprises over 50 proteins that precisely coordinate vesicle formation. Cell surface receptors concentrated in indented sites...
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The ER, Golgi apparatus, endosomes, and lysosomes work in tandem to modify, sort, and package proteins and lipids. An integrated membrane trafficking network facilitates the back and forth shuttling of molecules within different organelles in the same cell or across the cell membrane.
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Updated: Dec 10, 2025

Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
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Cell-Membrane-Targeted Drug Delivery System Based on Choline-Phosphate-Functionalized β-Cyclodextrin.

Ying Feng1, Qiangwei Xin1, Wanlin Zhang1

  • 1College of Medicine, Southwest Jiaotong University, Chengdu, 610031, P. R. China.

Macromolecular Bioscience
|September 1, 2020
PubMed
Summary

A novel choline phosphate (CP)-functionalized β-cyclodextrin (CP-β-CD) enhances drug delivery by improving solubility and cell uptake. This non-toxic system shows potential for targeted anti-angiogenesis therapies.

Keywords:
apatinibcellular uptakecholine phosphatecyclodextrinzwitterionic

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Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Cyclodextrins are widely used in drug delivery but often suffer from poor water solubility.
  • Targeting cell membranes is crucial for efficient drug delivery and therapeutic efficacy.

Purpose of the Study:

  • To synthesize and characterize a novel zwitterionic choline phosphate (CP)-functionalized β-cyclodextrin (CP-β-CD).
  • To evaluate the potential of CP-β-CD as a drug delivery system for hydrophobic drugs, focusing on solubility, cell uptake, and anti-angiogenesis activity.

Main Methods:

  • Synthesis of CP-β-CD via click chemistry.
  • Solubility studies of CP-β-CD and drug-loaded CP-β-CD.
  • In vitro cytotoxicity assays.
  • Evaluation of anti-angiogenesis activity using apatinib as a model drug.

Main Results:

  • CP-β-CD was successfully synthesized with significantly improved water solubility (816 mg mL⁻¹).
  • CP-β-CD demonstrated excellent cell-membrane targeting and enhanced cellular uptake.
  • Drug-loaded CP-β-CD exhibited potent anti-angiogenesis activity with no observed cytotoxicity.

Conclusions:

  • CP-β-CD is a non-toxic, highly water-soluble cyclodextrin derivative with superior cell internalization efficiency.
  • This novel material holds significant promise for developing advanced drug delivery systems, particularly for hydrophobic drugs targeting angiogenesis.