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Solid dispersions enhance solubility, dissolution, and permeability of thalidomide.

Silvana A Barea1, Cristiane B Mattos1, Ariadne C C Cruz2

  • 1a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul , Porto Alegre , Brazil.

Drug Development and Industrial Pharmacy
|December 6, 2016
PubMed
Summary

Solid dispersions (SDs) enhance thalidomide (THD) oral absorption by improving its solubility and dissolution rate. This novel approach offers a promising strategy for optimizing THD biopharmaceutical properties.

Keywords:
Thalidomidepermeabilityself-emulsifyingsolid dispersionsolubility

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Biopharmaceutics

Background:

  • Thalidomide (THD) is a BCS class II drug with significant therapeutic potential but suffers from poor oral absorption due to low solubility and instability.
  • Challenges include chemical instability, high crystallinity, and polymorphism, leading to variable drug absorption.

Purpose of the Study:

  • To develop and characterize solid dispersions (SDs) of thalidomide (THD) using self-emulsifying carriers to enhance its biopharmaceutical properties.
  • To investigate the impact of SD formulation on THD solubility, dissolution, and permeability.

Main Methods:

  • Thalidomide was dispersed in Gelucire® 44/14 and Kolliphor® TPGS, with or without polyvinylpyrrolidone K30 (PVP K30), using the solvent method.
  • Physicochemical characterization included X-ray diffraction and infrared spectroscopy.
  • In vitro techniques such as solubility, dissolution (paddle method), and parallel artificial membrane permeability assay (PAMPA) were employed.

Main Results:

  • Semicrystalline solid dispersions were successfully prepared, with no observed polymorphic transition of the drug.
  • The developed SDs increased apparent thalidomide solubility by 2-3 times for at least 4 hours.
  • Dissolution studies showed approximately 80% drug release within 120 minutes, compared to 40% for pure crystalline THD.
  • Enhanced solubility translated to increased drug flux in the PAMPA assay.

Conclusions:

  • Solid dispersions represent a novel and effective strategy for improving the biopharmaceutical properties of thalidomide.
  • The developed SD formulations show potential for enhancing thalidomide oral absorption and therapeutic efficacy.
  • This study highlights an unexplored avenue for optimizing thalidomide drug delivery.