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Related Concept Videos

Factors Influencing Drug Absorption: Physicochemical Parameters01:22

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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Design, optimization and characterization of atorvastatin loaded chitosan-based polyelectrolyte complex nanoparticles

Pravin Patil1, Ankit Vankani1, Krutika Sawant1

  • 1Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Vadodara 390001, Gujarat, India.

International Journal of Biological Macromolecules
|June 19, 2024
PubMed
Summary

This study developed atorvastatin (ATO) loaded chitosan-based polyelectrolyte complex nanoparticles (PECN) transdermal patches. The novel patch significantly enhanced ATO skin permeability and bioavailability compared to oral tablets.

Keywords:
AtorvastatinBioavailabilityOptimizationPolyelectrolyte complexTransdermal

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Area of Science:

  • Pharmaceutical Sciences
  • Nanotechnology
  • Drug Delivery Systems

Background:

  • Atorvastatin (ATO) exhibits poor bioavailability, necessitating advanced delivery systems.
  • Chitosan-based polyelectrolyte complex nanoparticles (PECN) offer potential for improved drug delivery.
  • Transdermal patches provide a non-invasive route for drug administration.

Purpose of the Study:

  • To develop and evaluate atorvastatin (ATO) loaded chitosan-based polyelectrolyte complex nanoparticles (PECN) incorporated into a transdermal patch.
  • To enhance the skin permeability and bioavailability of ATO through a novel transdermal delivery system.

Main Methods:

  • ATO-loaded PECN were prepared using the ionic gelation method and optimized with Box-Behnken design.
  • Physicochemical characteristics, in vitro, ex vivo, cell line, and stability studies were conducted.
  • Optimized ATO-PECN were incorporated into transdermal patches, followed by comprehensive evaluation.

Main Results:

  • Optimized ATO-PECN exhibited a particle size of 219.2 ± 5.98 nm, 82.68 ± 2.63% entrapment, and +25.41 ± 3.29 mV zeta potential.
  • ATO-PECN demonstrated sustained drug release, enhanced skin permeation, and increased cell permeability compared to ATO suspension.
  • The transdermal patch showed superior ex vivo skin permeation and significantly improved in vivo pharmacokinetic parameters, confirming enhanced bioavailability.

Conclusions:

  • The developed atorvastatin-loaded PECN transdermal patch is a promising drug delivery system.
  • This novel system effectively enhances the bioavailability of poorly bioavailable drugs like atorvastatin.
  • The study highlights the potential of chitosan-based PECN for advanced transdermal drug delivery applications.