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Related Concept Videos

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...
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Colloidal precipitates01:09

Colloidal precipitates

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The high insolubility of some precipitates can result in an unfavorable relative supersaturation. This can lead to colloidal particles with a large surface-to-mass ratio, where adsorption is promoted. For instance, in the precipitation of silver chloride, silver ions are adsorbed on the surface of the colloidal particles, forming a primary layer. This layer attracts ions of opposite charge (such as nitrate ions), forming a diffuse secondary layer of adsorbed ions. This electric double layer...
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Polydopamine Copolymers for Stable Drug Nanoprecipitation.

Danna Niezni1, Yuval Harris1, Hagit Sason1

  • 1Faculty of Biomedical Engineering, Technion-Israel Institute of Technology, Haifa 3200003, Israel.

International Journal of Molecular Sciences
|October 27, 2022
PubMed
Summary

Polydopamine copolymers with a novel In820 comonomer enhance hydrophobic drug nanoprecipitation, improving nanoparticle stability, loading efficiency, and antitumor efficacy for cancer nanomedicine applications.

Keywords:
aggregation-induced emissioncolon cancerdrug deliveryindoliumnanomedicinenanoparticlesnanoprecipitationpolydopamine

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Area of Science:

  • Biomaterials Science
  • Nanomedicine
  • Polymer Chemistry

Background:

  • Polydopamine (PDA) is a mussel-inspired biomaterial with potential in cancer nanomedicine.
  • PDA's utility is limited by insufficient study in stabilizing hydrophobic drugs via nanoprecipitation.
  • Optimizing PDA copolymers is crucial for effective hydrophobic drug delivery systems.

Purpose of the Study:

  • To develop and optimize polydopamine (PDA) copolymers for enhanced hydrophobic drug stabilization during nanoprecipitation.
  • To identify novel comonomers that improve drug loading efficiency, particle size, and nanoparticle stability.
  • To evaluate the therapeutic potential of optimized PDA-based nanoformulations in cancer treatment.

Main Methods:

  • Combinatorial screening of comonomers with PDA using drug aggregation-induced emission (AIE) as a selection criterion.
  • Optimization of copolymer synthesis and nanoprecipitation conditions for hydrophobic drugs.
  • Characterization of nanoparticle properties including stability, encapsulation efficiency, toxicity, and in vitro antitumor efficacy.

Main Results:

  • Identified 1,1,2-Trimethyl-3-(4-sulfobutyl)benz[e]indolium (In820) as a superior comonomer for PDA, outperforming polyethylene glycol modifications.
  • Developed a leading copolymer, poly(dopamine)-poly(L-dopa)-co-In820 (PDA-PDO-In820 1:1:1), demonstrating excellent stabilization of hydrophobic drugs.
  • Achieved nanoparticle stability up to 15 days, high encapsulation efficiency (≥80%), low toxicity, and significant in vitro antitumor efficacy.

Conclusions:

  • PDA copolymers incorporating In820 are highly effective and easily prepared stabilizers for hydrophobic drug nanoprecipitation.
  • This approach significantly enhances nanoformulation properties for improved cancer nanomedicine applications.
  • The developed PDA-PDO-In820 copolymers represent a promising platform for hydrophobic drug delivery.