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Site-Targeted Drug Delivery Systems: Polymeric Carriers

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Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...

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Ex Vivo Red Blood Cell Hemolysis Assay for the Evaluation of pH-responsive Endosomolytic Agents for Cytosolic Delivery of Biomacromolecular Drugs

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pH- and ion-sensitive polymers for drug delivery.

Takayuki Yoshida¹, Tsz Chung Lai, Glen S Kwon

¹Drug Delivery, Pharmaceutical Research and Technology Labs, Astellas Pharma, Inc. , 180 Ozumi, Yaizu, Shizuoka 425-0072 , Japan +81 54 627 6861 ; +81 54 627 9918 ; takayuki.yoshida@astellas.com.

Expert Opinion on Drug Delivery

|August 13, 2013

Summary

pH- and ion-responsive polymers are key for targeted drug delivery systems (DDSs). These materials exploit bodily pH and ion gradients for controlled drug release, improving safety and efficacy.

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Area of Science:

Polymer Science
Materials Science
Biomedical Engineering

Background:

Drug delivery systems (DDSs) are crucial for effective, safe, and convenient drug administration.
pH- and ion-responsive polymers are widely used in DDSs to achieve site-specific drug release by leveraging physiological pH and ion gradients.

Purpose of the Study:

To review the applications of pH- and ion-responsive polymers in drug delivery.
To highlight the mechanisms by which these polymers achieve targeted drug release in various physiological environments.

Main Methods:

Exploration of pH-sensitive cationic and anionic polymers for gastric, intestinal, and tumor-targeted drug delivery.
Investigation of polymers with pH-sensitive linkages and cell-penetrating peptides for intracellular delivery.
Review of ion-sensitive polymers, including ion-exchange resins, for taste-masking and controlled release in oral formulations.

Main Results:

Cationic polymers respond to low gastric pH for drug release, while anionic polymers target high intestinal pH for enhanced bioavailability and colon delivery.
Tumor-targeted DDSs utilize polymers responsive to the acidic tumor microenvironment.
pH-sensitive linkages and ion-exchange resins offer versatile strategies for controlled and site-specific drug release.

Conclusions:

Stimuli-responsive DDSs are vital for site-specific and controlled drug release.
Consideration of physiological pH variations (intraindividual, interindividual, intercellular) is essential for DDS design.
Combining polymers with other components and advancing physiological understanding will drive the development of effective pH- and ion-sensitive DDS products.