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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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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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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Improved art bioactivity by encapsulation within cyclodextrin carboxylate.

Yao Hu1, David Julian McClements2, Xiaojing Li3

  • 1State Key Laboratory of Food Science and Technology, School of Food Science and Technology, Synergetic Innovation Center of Food Safety and Nutrition, Jiangnan University, Wuxi, Jiangsu 214122, China.

Food Chemistry
|February 26, 2022
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Summary

Artemisinin solubility was improved by forming inclusion complexes with succinic acid modified cyclodextrin. This enhances its potential for oral delivery systems and retains bioactivity.

Keywords:
Cyclodextrin carboxylateE. coliNanocarriersPhytochemicalsS. aureus

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Area of Science:

  • Natural Product Chemistry
  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Artemisinin (Art) is a natural sesquiterpene lactone with diverse bioactivities.
  • Poor water and oil solubility limits Artemisinin's oral formulation applications.

Purpose of the Study:

  • To investigate the formation of host-guest complexes between Artemisinin and succinic acid modified cyclodextrin (SACD).
  • To enhance the solubility and oral delivery potential of Artemisinin.

Main Methods:

  • Formation of Artemisinin-SACD inclusion complexes at a 2:1 M ratio in an aqueous medium.
  • Evaluation of complex formation attributed to SACD cavity size and intermolecular interactions.
  • Assessment of the thermal stability and antibacterial activity of the encapsulated Artemisinin.

Main Results:

  • Successful formation of Artemisinin-SACD inclusion complexes in water.
  • Preservation of Artemisinin's thermal stability within the complexes.
  • Demonstrated antibacterial activity of encapsulated Artemisinin against Gram-positive and Gram-negative bacteria.

Conclusions:

  • Succinic acid modified cyclodextrin effectively improves Artemisinin solubility through complexation.
  • The developed encapsulation technology enables the incorporation of bioactive Artemisinin into oral delivery systems.
  • This approach offers a promising strategy for enhancing the bioavailability and therapeutic applications of Artemisinin.