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When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...
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Improving gallic acid and quercetin bioavailability by polymeric nanoparticle formulation.

Poounima Patil1,2, Suresh Killedar3

  • 1Bharati Vidyapeeth College of Pharmacy, Kolhapur, India.

Drug Development and Industrial Pharmacy
|February 18, 2022
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Summary

Polyherbal nanoparticles encapsulating gallic acid and quercetin show enhanced bioavailability and anti-colon cancer efficacy compared to the extract. This suggests polymeric nanoparticles are a promising strategy for cancer prevention.

Keywords:
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Area of Science:

  • Pharmacology
  • Nanotechnology
  • Oncology

Background:

  • Colorectal cancer (CRC) poses a significant health burden globally.
  • Natural compounds like gallic acid (GA) and quercetin show potential anticancer properties but suffer from poor oral bioavailability.
  • Developing effective delivery systems is crucial for enhancing the therapeutic efficacy of natural anticancer agents.

Purpose of the Study:

  • To evaluate the anticancer activity and pharmacokinetic properties of polyherbal nanoparticles (GA and quercetin nanocomposite) and polyherbal extract (amla and pomegranate fruit peels).
  • To compare the bioavailability and anti-colon cancer efficacy of encapsulated nanoparticles versus the traditional extract in a rat model.
  • To explore the potential of polymeric nanoparticles for colorectal cancer prevention.

Main Methods:

  • Preparation and characterization of polyherbal nanoparticles containing gallic acid and quercetin.
  • Pharmacokinetic studies in normal and DMH-induced colorectal cancer rat models.
  • Assessment of serum-concentration profiles and establishment of pharmacokinetic parameters using a single compartmental model.
  • Evaluation of anticancer activity in vivo.

Main Results:

  • Polyherbal nanoparticles exhibited a sustained release profile.
  • Nanoparticle encapsulation led to a fourfold increase in oral bioavailability compared to the polyherbal extract.
  • Encapsulated GA and quercetin demonstrated improved anti-colon cancer efficacy.
  • Pharmacokinetic parameters indicated enhanced absorption and sustained presence of nanoparticles.

Conclusions:

  • Encapsulating gallic acid and quercetin in polymeric nanoparticles significantly enhances their oral bioavailability and anti-colon cancer efficacy.
  • Polymeric nanoparticles represent a promising novel therapeutic strategy for colorectal cancer prevention.
  • This approach could overcome the limitations of poor bioavailability associated with natural anticancer compounds.