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Related Concept Videos

Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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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,...
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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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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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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...
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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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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 absorption...
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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 Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

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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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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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Improving oral drug bioavailability with polycations?

Jessica D Schulz1, Marc A Gauthier2, Jean-Christophe Leroux1

  • 1Swiss Federal Institute of Technology Zurich (ETH Zurich), Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, Zurich 8093, Switzerland.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|November 29, 2015
PubMed
Summary
This summary is machine-generated.

Polycations enhance oral drug delivery by protecting therapeutics from degradation and improving absorption across intestinal barriers. These cationic polymers offer a promising strategy for overcoming challenges in oral administration.

Keywords:
ChitosanMacromolecular drug conjugatesMicroparticlesMucoadhesionNanoparticlesOral routePermeation enhancersPoly(amidoamine)Poly(lysine)Polycations

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Area of Science:

  • Pharmaceutical Sciences
  • Biomaterials Science

Background:

  • Oral drug administration faces challenges due to the digestive system's harsh conditions (pH variations, enzymes) and absorption barriers (mucus, epithelium).
  • Large molecules like proteins and nucleic acids often fail to reach systemic circulation due to degradation or size limitations.

Purpose of the Study:

  • To review common polycations used as oral absorption enhancers.
  • To discuss strategies for employing polycations in oral drug delivery systems.

Main Methods:

  • Literature review of polycations investigated for oral drug absorption enhancement.
  • Analysis of mechanisms by which polycations facilitate drug transport across intestinal barriers.

Main Results:

  • Polycations protect drugs from degradation and interact with gastrointestinal mucosa.
  • Cationic polymers promote drug transfer via mechanisms like tight junction opening and altered uptake pathways.

Conclusions:

  • Polycations are effective in improving oral drug absorption for various therapeutics.
  • Methods like co-administration, nanoparticles, and conjugation are key to utilizing polycations for enhanced oral drug delivery.