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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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Body: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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Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
345
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
269
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

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Body:Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug...
270
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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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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Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

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Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
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Updated: Feb 28, 2026

Semi-Targeted Ultra-High-Performance Chromatography Coupled to Mass Spectrometry Analysis of Phenolic Metabolites in Plasma of Elderly Adults
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Semi-Targeted Ultra-High-Performance Chromatography Coupled to Mass Spectrometry Analysis of Phenolic Metabolites in Plasma of Elderly Adults

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2-Hydroxypropyl-β-Cyclodextrin-Based Complexes Improve Polyphenol Solubility and Bioaccessibility: Evaluation by

Eleonora Perak Junaković1, Anja Vujnović1, Nada Oršolić2

  • 1Laboratory for Analysis of Veterinary-Medicinal Products, Croatian Veterinary Institute, Savska cesta 143, 10000 Zagreb, Croatia.

Molecules (Basel, Switzerland)
|February 27, 2026
PubMed
Summary

This study developed a validated HPLC-DAD method to quantify propolis polyphenols complexed with HP-β-CD. Complexation improved solubility and stability, but limited intestinal permeation of these beneficial compounds.

Keywords:
HPLC–DADbioaccessibilitycyclodextrinslyophilizationmethod validationpolyphenolspropolis extractsstatic in vitro digestion

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Area of Science:

  • Natural Products Chemistry
  • Analytical Chemistry
  • Pharmacokinetics

Background:

  • Propolis polyphenols offer therapeutic benefits but suffer from poor oral bioavailability.
  • Developing stable, water-soluble propolis formulations is crucial for oral delivery.

Purpose of the Study:

  • To develop and validate an HPLC-DAD method for quantifying propolis polyphenols in HP-β-CD complexes.
  • To evaluate the gastrointestinal behavior and bioaccessibility of these complexed polyphenols.

Main Methods:

  • A green complexation method using 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and lyophilization.
  • Development and validation of an isocratic HPLC-DAD method for polyphenol quantification.
  • Simulated gastrointestinal digestion and intestinal bioaccessibility models.

Main Results:

  • The HPLC-DAD method was linear, sensitive, and precise for analyzing polyphenols in HP-β-CD matrices.
  • HP-β-CD complexation enhanced polyphenol solubility and gastrointestinal stability.
  • Intestinal bioaccessibility varied, but complexation did not enhance intestinal permeation.

Conclusions:

  • Validated analytical methods are essential for studying complexed natural products.
  • HP-β-CD complexation improves propolis polyphenol solubility and stability but has limitations for intestinal absorption.
  • Further strategies are needed to enhance the oral delivery of propolis polyphenols.