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Related Concept Videos

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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).
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Vapor Phase Deposition of Electroactive Poly(3,4-ethylenedioxythiophene) onto Electrospun Commodity Polymer Nanofibers
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Electrospun formulations containing crystalline active pharmaceutical ingredients.

Blair Kathryn Brettmann1, Kamyu Cheng, Allan S Myerson

  • 1Department of Chemical Engineering, Massachusetts Institute of Technology, 50 Ames St, E19-502b, Cambridge, Massachusetts 02139, USA.

Pharmaceutical Research
|August 28, 2012
PubMed
Summary

Electrospinning successfully created solid dispersions with crystalline active pharmaceutical ingredients (API), such as albendazole and famotidine, maintaining their crystal form. Resulting tablets showed improved dissolution rates compared to traditional methods.

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Area of Science:

  • Pharmaceutical Technology
  • Materials Science
  • Nanotechnology

Background:

  • Electrospinning is typically used for amorphous solid dispersions.
  • Crystalline active pharmaceutical ingredients (APIs) often exhibit poor solubility and dissolution rates.
  • Developing novel methods to enhance the dissolution of crystalline APIs is crucial for drug formulation.

Purpose of the Study:

  • To explore electrospinning for creating solid dispersions with crystalline APIs.
  • To characterize the properties of electrospun materials containing crystalline drugs.
  • To evaluate the impact of electrospinning on API dissolution.

Main Methods:

  • Free surface electrospinning of poly(vinyl pyrrolidone) (PVP) with crystalline albendazole (ABZ) or famotidine (FAM).
  • Scanning Electron Microscopy (SEM) and Differential Scanning Calorimetry (DSC) for material characterization.
  • X-ray Diffraction (XRD) to confirm crystalline polymorphs and dissolution studies to assess drug release.

Main Results:

  • Electrospun fibers contained significant amounts of crystalline ABZ (31 wt%) and FAM (26 wt%).
  • APIs retained their crystalline polymorphs throughout the electrospinning process.
  • Well-dispersed drug crystals within the polymer fibers led to enhanced dissolution rates in electrospun tablets compared to powder tablets.

Conclusions:

  • Electrospinning is a viable technique for producing solid dispersions with crystalline APIs, not just amorphous ones.
  • The dispersion of crystalline APIs in electrospun fibers improves their dissolution properties.
  • Tablets manufactured from these electrospun mats offer potential advantages over conventional powder compression methods for enhanced drug delivery.