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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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A Tripeptide-Stabilized Nanoemulsion of Oleic Acid
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Optimized Chitosan-Based Nanoemulsion Improves Luteolin Release.

Camila Diedrich1, Isabella C Zittlau1, Najeh M Khalil1

  • 1Pharmaceutical Nanotechnology Laboratory, Universidade Estadual do Centro-Oeste, Guarapuava 85040-167, Brazil.

Pharmaceutics
|June 28, 2023
PubMed
Summary
This summary is machine-generated.

Chitosan-based nanoemulsions effectively encapsulate luteolin (LUT), enhancing its solubility and enabling controlled release for potential therapeutic applications.

Keywords:
chitosandrug releaseoptimizationresponse surface methodologystability

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Area of Science:

  • Nanotechnology
  • Materials Science
  • Pharmacology

Background:

  • Luteolin (LUT), a flavonoid with antioxidant, anti-inflammatory, neuroprotective, and antitumor properties, suffers from poor oral absorption due to limited water solubility.
  • Nanoencapsulation offers a promising strategy to improve the solubility and bioavailability of poorly soluble compounds like LUT.

Purpose of the Study:

  • To develop and optimize chitosan-based nanoemulsions (NECh-LUT) for the encapsulation of luteolin (LUT).
  • To characterize the physicochemical properties and stability of the developed nanoemulsions.
  • To evaluate the in vitro release profile of LUT from the nanoemulsion system.

Main Methods:

  • Formulation of chitosan-based nanoemulsions (NECh-LUT) using a 2^3 factorial design to optimize oil, water, and surfactant concentrations.
  • Characterization of nanoemulsions using dynamic light scattering (DLS) for size and polydispersity index (PDI), zeta potential measurements, and transmission electron microscopy (TEM).
  • Evaluation of encapsulation efficiency, rheological behavior, small-angle X-ray scattering (SAXS), stability studies at room temperature, and in vitro drug release assays.

Main Results:

  • Optimized NECh-LUT exhibited a mean particle diameter of 67.5 nm, PDI of 0.174, and zeta potential of +12.8 mV, with an encapsulation efficiency of 85.49%.
  • TEM confirmed spherical morphology, rheological analysis indicated Newtonian behavior, and SAXS revealed bimodal characteristics.
  • NECh-LUT demonstrated good stability at room temperature for 30 days and sustained LUT release for up to 72 hours.

Conclusions:

  • Chitosan-based nanoemulsions provide an effective system for encapsulating luteolin, significantly improving its solubility and enabling controlled release.
  • The optimized NECh-LUT formulation exhibits favorable physicochemical properties, stability, and drug release kinetics.
  • NECh-LUT holds significant potential as a novel therapeutic option for various disorders requiring luteolin delivery.