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Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Magnetic and Thermal-sensitive PolyN-isopropylacrylamide-based Microgels for Magnetically Triggered Controlled Release
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Microparticles Containing Curcumin Solid Dispersion: Stability, Bioavailability and Anti-Inflammatory Activity.

C C C Teixeira1, L M Mendonça1, M M Bergamaschi1

  • 1Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.

AAPS Pharmscitech
|June 5, 2015
PubMed
Summary
This summary is machine-generated.

Spray drying created a curcumin solid dispersion with Gelucire®50/13-Aerosil®, significantly boosting oral bioavailability and anti-inflammatory effects in rats. This scalable method enhances curcumin

Keywords:
bioavailabilityblood leveldissolutionrat paw oedemasolubilityspray dryingthermal analysisturmeric

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Natural Product Chemistry

Background:

  • Curcumin, a natural compound, exhibits poor aqueous solubility and low oral bioavailability.
  • Enhancing curcumin's bioavailability is crucial for its therapeutic applications.
  • Solid dispersion technology offers a promising approach to overcome curcumin's solubility limitations.

Purpose of the Study:

  • To prepare and characterize spray-dried ternary solid dispersions of curcumin with Gelucire®50/13 and Aerosil®.
  • To evaluate the impact of the solid dispersion on curcumin's solubility, dissolution rate, and in vivo oral bioavailability.
  • To assess the anti-inflammatory activity of the curcumin solid dispersion.

Main Methods:

  • Spray drying was employed to formulate ternary solid dispersions of curcumin.
  • Characterization involved calorimetry, infrared spectroscopy, and X-ray powder diffraction.
  • In vivo pharmacokinetic studies in rats and anti-inflammatory assays (rat paw oedema) were conducted.

Main Results:

  • The solid dispersion significantly improved curcumin solubility (up to 3600-fold) and dissolution rate (7.3-fold).
  • Pharmacokinetic studies revealed a 5.5-fold increase in curcumin bioavailability in rat plasma.
  • The solid dispersion demonstrated enhanced anti-inflammatory activity compared to unprocessed curcumin.

Conclusions:

  • Spray-dried ternary solid dispersions of curcumin with Gelucire®50/13-Aerosil® effectively enhance solubility and oral bioavailability.
  • The scalable spray-drying technique makes this formulation industrially viable for pharmaceutical applications.
  • This enhanced curcumin formulation holds potential for chemoprevention of cancer and Alzheimer's disease.