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Related Concept Videos

Drug Delivery: Parenteral Route01:29

Drug Delivery: Parenteral Route

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The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
309
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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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...
240
Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

329
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
329
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

146
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...
146
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

101
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Polypept(o)ide-Based Core-Shell Bottlebrush Polymers: A Versatile Platform for Drug Encapsulation.

Bonan Zhao1, Jingyuan Wei1, Rüdiger Berger2

  • 1Leiden Academic Center for Drug Research (LACDR), Leiden University, Einsteinweg 55, Leiden, 2333CC, The Netherlands.

Macromolecular Bioscience
|April 22, 2025
PubMed
Summary
This summary is machine-generated.

This study introduces novel core-shell brushes (CSBs) synthesized from polypept(o)ides, demonstrating their potential as nanomedicine platforms. These versatile nanoparticles effectively encapsulate and release the drug dasatinib, showing therapeutic efficacy in glioblastoma cells.

Keywords:
core–shell bottlebrush polymersdrug deliverypolypept(o)ide“grafting‐from” synthesis

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Area of Science:

  • Polymer Chemistry
  • Nanotechnology
  • Materials Science

Background:

  • Cylindrical bottlebrush polymers (CBPs) offer tunable nanoparticle properties via synthesis.
  • Block copolymer side chains facilitate the creation of core-shell nanostructures.

Purpose of the Study:

  • To synthesize polypept(o)ide-based core-shell CBPs (CSBs) using a "grafting-from" approach.
  • To evaluate the potential of these CSBs as a platform for drug encapsulation and delivery.

Main Methods:

  • Synthesized core-shell brushes (CSBs) with a poly-lysine (pLys) backbone and poly(γ-benzyl-l-glutamic acid)-block-polysarcosine (pGlu(OBn)-b-pSar) side chains.
  • Characterized CSB size, molecular weight, and dispersity using size-exclusion chromatography.
  • Investigated drug loading, release kinetics, cellular uptake, and therapeutic efficacy using dasatinib as a model drug.

Main Results:

  • Successfully synthesized CSBs with tunable hydrodynamic radii (17-70 nm) and high molecular weights (1320-4000 kg mol⁻¹).
  • Achieved 10% loading efficiency for dasatinib, with sustained release over 72 hours.
  • Demonstrated cellular uptake into U-87 MG glioblastoma cells and drug-related therapeutic effects.

Conclusions:

  • Polypept(o)ide-based CSBs represent a promising platform for nanomedicine applications.
  • The developed CSBs show potential for targeted drug delivery and cancer therapy.
  • Further optimization, such as covalent drug attachment, could enhance drug release profiles.