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Related Concept Videos

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

263
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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Biodegradable dexamethasone polymer capsule for long-term release.

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Biodegradable polymer capsules provide sustained local delivery of dexamethasone (Dex) for inflammatory diseases. Polymer hydrophobicity controls Dex release rate, with more hydrophobic polymers showing slower drug release and effective IL-6 suppression in vitro.

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Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Polymer Chemistry

Background:

  • Inflammatory diseases require effective local drug delivery.
  • Sustained-release implants offer therapeutic advantages over conventional methods.
  • Dexamethasone (Dex) is a potent anti-inflammatory corticosteroid.

Purpose of the Study:

  • To develop and characterize sustained-release dexamethasone (Dex) capsule implants using various biodegradable polymers.
  • To investigate the influence of polymer properties on Dex release kinetics.
  • To evaluate the in vitro therapeutic efficacy and toxicity of the Dex implants.

Main Methods:

  • Fabrication of Dex implants using polycaprolactone (PCL), poly(lactic acid) (PLA), and two ratios of poly(lactic-co-glycolic acid) (PLGA).
  • Drug release studies fitting data to a cylindrical reservoir first-order kinetics model.
  • In vitro efficacy testing using TNF-α stimulated human umbilical vein endothelial cells (HUVECs) to measure IL-6 levels.

Main Results:

  • Drug release rates varied significantly among the polymers, with 50:50 PLGA exhibiting the fastest release and PCL the slowest.
  • Drug release kinetics were strongly correlated with polymer hydrophobicity; more hydrophobic polymers resulted in slower release of the hydrophilic drug.
  • Dex implants effectively suppressed IL-6 levels in HUVECs with minimal toxicity compared to free Dex.

Conclusions:

  • The release rate of dexamethasone from biodegradable implants is predictable and controllable based on polymer hydrophobicity.
  • Sustained-release Dex implants demonstrate significant potential for localized treatment of inflammatory conditions.
  • This study provides a foundation for designing optimized polymer-drug delivery systems for inflammatory disease management.