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pH- and ion-sensitive polymers for drug delivery
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INTRODUCTION: Drug delivery systems (DDSs) are important for effective, safe, and convenient administration of drugs. pH- and ion-responsive polymers have been widely employed in DDS for site-specific drug release due to their abilities to exploit specific pH- or ion-gradients in the human body. AREAS COVERED: Having pH-sensitivity, cationic polymers can mask the taste of drugs and release drugs in the stomach by responding to gastric low pH. Anionic polymers responsive to intestinal high pH are used for preventing gastric degradation of drug, colon drug delivery and achieving high bioavailability of weak basic drugs. Tumor-targeted DDSs have been developed based on polymers with imidazole groups or poly(β-amino ester) responsive to tumoral low pH. Polymers with pH-sensitive chemical linkages, such as hydrazone, acetal, ortho ester and vinyl ester, pH-sensitive cell-penetrating peptides and cationic polymers undergoing pH-dependent protonation have been studied to utilize the pH gradient along the endocytic pathway for intracellular drug delivery. As ion-sensitive polymers, ion-exchange resins are frequently used for taste-masking, counterion-responsive drug release and sustained drug release. Polymers responding to ions in the saliva and gastrointestinal fluids are also used for controlled drug release in oral drug formulations. EXPERT OPINION: Stimuli-responsive DDSs are important for achieving site-specific and controlled drug release; however, intraindividual, interindividual and intercellular variations of pH should be considered when designing DDSs or drug products. Combination of polymers and other components, and deeper understanding of human physiology are important for development of pH- and ion-sensitive polymeric DDS products for patients.
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“where the basic pH-responsive polymers such as albumin and polyacrylic acid (PAA) swell in basic pH and shrink in acidic pH [41,42].”
From Review of Stimuli-Responsive Polymers in Drug Delivery and Textile Application (2019) · cites this paper as [42]
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“The cationic pH responsive polymers including chitosan, poly(N,N-dimethylaminoethyl methacrylate) (PDMAEMA), and poly(N,N-diethylaminoethyl methacrylate) (PDEAEMA) swell in acidic pH and shrink in basic pH”
From Review of Stimuli-Responsive Polymers in Drug Delivery and Textile Application (2019) · cites this paper as [42]
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Metadata
- Authors
- Yoshida, T., Lai, T. C., Kwon, G. S., & Sako, K.
- Affiliations
- Astellas Pharma (Japan) (JP)
- University of Wisconsin–Madison (US)
- Corresponding author
- Yoshida, Takayuki
- Venue
- Expert Opinion on Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2013-08-09
- Volume
- 10
- Issue
- 11
- Pages
- 1497-1513
- ISSN
- 1742-5247 (ISSN-L)
- 1744-7593
- PMC
- PMC3912992
- OpenAlex
- W2003276331
- Cited by
- 367
- References
- 112
- Citations by year
- 2026: 22 · 2025: 40 · 2024: 40 · 2023: 45 · 2022: 26 · 2021: 32 · 2020: 31 · 2019: 35 · 2018: 38 · 2017: 17 · 2016: 20 · 2015: 14 · 2014: 6
- FWCI
- 1.68
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Expert Opinion on Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Allergy and Infectious Diseases (R01AI101157)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Hydrogels: synthesis, properties, applications
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- pH-responsive polymers, site-specific drug release, cationic polymers, taste masking, colon-targeted drug delivery, anticancer drug delivery, poly(β-amino ester), hydrazone linkage, cell-penetrating peptides, ion exchange resins, sustained drug release, oral drug formulation, gastric pH, intracellular drug delivery
- MeSH terms
- Biological Availability, Chemistry, Pharmaceutical, Delayed-Action Preparations, Pharmaceutical Preparations, Humans, Hydrogen-Ion Concentration, Ions, Polymers, Drug Delivery Systems, Cell-Penetrating Peptides
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