Related Experiment Video

Updated: Jun 19, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
07:32

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

Cellular uptake and toxicity of microparticles in a perspective of polymyxin B oral administration

G Coppi1, M Montanari, T Rossi

  • 1Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, via Campi, 183-41100 Modena, Italy. gilberto.coppi@unimore.it

International Journal of Pharmaceutics
|October 20, 2009
PubMed

Insights

Alginate/chitosan microparticles efficiently transport antibiotics into intestinal cells via an energy-dependent process. These microparticles maintain antibiotic efficacy while reducing toxicity, suggesting dual delivery pathways for enhanced therapeutic outcomes.

Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Cell Biology

Background:

  • Alginate/chitosan microparticles were previously developed for targeting polymyxin B to M-cells and the lymphatic system.
  • Investigating alternative transport pathways for microparticle-based drug delivery is crucial for optimizing therapeutic efficacy.

Purpose of the Study:

  • To evaluate the transport capability of alginate/chitosan microparticles by enterocytes.
  • To assess the impact of microparticle encapsulation on polymyxin B's biological activity and cytotoxicity.

Main Methods:

  • Utilized a Caco-2 cell monolayer model to study microparticle-cell interactions.
  • Employed confocal microscopy to visualize and analyze microparticle uptake.
  • Assessed antibiotic activity and cytotoxicity against Vero cell cultures.

Main Results:

  • Microparticles were endocytosed by enterocytes through a saturable, energy-dependent process.
  • The biological activity of polymyxin B was preserved within the microparticles.
  • Microparticle encapsulation reduced the cytotoxicity of polymyxin B.

Conclusions:

  • Alginate/chitosan microparticles demonstrate significant transport ability via enterocytes.
  • These microparticles offer a promising strategy for drug delivery, potentially utilizing simultaneous pathways through M-cells and enterocytes.
  • The findings support the development of these microparticles for enhanced antibiotic delivery and reduced side effects.

More Related Videos

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles09:56

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

Related Concept Videos

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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...
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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 secretion,...
Factors Influencing Drug Absorption: Presystemic Elimination01:24

Factors Influencing Drug Absorption: Presystemic Elimination

The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
Biopharmaceutics and Pharmacokinetics: Overview01:28

Biopharmaceutics and Pharmacokinetics: Overview

Understanding drugs, drug products, and their performance in pharmaceutical science is pivotal. Drugs, whether simple molecules or complex compounds, are designed to interact with the body's biological systems to diagnose, treat, or prevent diseases. Drug products include various delivery systems such as tablets, capsules, injections, and inhalers. The performance of these drug products is gauged by their ability to deliver the active ingredient to the desired site of action at the appropriate...