Site-Specific Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (31 March 2026) | Viewed by 1202

Special Issue Editor


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Guest Editor
Laboratory of Biomedicinal Chemistry, College of Pharmacy, Pusan National University, Busan 609‐735, Republic of Korea
Interests: colon-targeted drug delivery; prodrug; codrug; pathologically-targeted drug; molecular pharmacology of anti-colitic agents
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Special Issue Information

Dear Colleagues,

Site-specific drug delivery implies targeting a drug to a certain biological location. Targeted drug delivery leads to selective and effective distribution of a drug into the target site at therapeutic concentrations with limited access to non-target sites, thereby enhancing its therapeutic effectiveness and safety. Due to these therapeutic and toxicological advantages, the delivery technique, which is achieved by various targeting strategies utilizing small molecules, nucleic acid fragments (aptamers), synthetic peptides, recombinant monoclonal antibodies, and natural and genetically engineered cells, has been adopted in drug development and come into clinical reality. Pharmaceutical formulations including nanotechnology can not only be a different targeting strategy but also enhance the therapeutic performance of the aforementioned strategies. This Special Issue welcomes research articles relevant to site-specific drug delivery including biological barriers for it.

Prof. Dr. Yunjin Jung
Guest Editor

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Keywords

  • site-specific drug delivery
  • targeted drug delivery
  • therapeutic effectiveness
  • nanotechnology
  • biological barrier

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Published Papers (1 paper)

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Research

13 pages, 3063 KB  
Article
Colon-Specific Delivery of Probenecid Enhances Therapeutic Activity of the Uricosuric Agent Against Rat Colitis
by Yeonhee Jeong, Jaejeong Kim, Changyu Kang and Yunjin Jung
Pharmaceutics 2025, 17(11), 1454; https://doi.org/10.3390/pharmaceutics17111454 - 11 Nov 2025
Viewed by 944
Abstract
Background/Objectives: Probenecid (PBN) is a uricosuric agent that facilitates the excretion of uric acid and is used to treat gout. Here, a colon-targeted prodrug of PBN was designed to facilitate repositioning as a treatment for inflammatory bowel disease (IBD). Methods: The [...] Read more.
Background/Objectives: Probenecid (PBN) is a uricosuric agent that facilitates the excretion of uric acid and is used to treat gout. Here, a colon-targeted prodrug of PBN was designed to facilitate repositioning as a treatment for inflammatory bowel disease (IBD). Methods: The carboxylic group in PBN was amide-conjugated with the amine groups of acidic amino acids to yield aspartic acid-conjugated PBN (PBN-AA) and glutamic acid-conjugated PBN (PBN-GA). Conjugation with amino acids increased the hydrophilicity of PBN and decreased cell permeability across the Caco-2 cell monolayer. While remaining intact in buffers (pH 1.2, 6.8) and in the small intestinal contents of rats, the conjugates were cleaved to release PBN from the cecal contents of rats, with a significant difference in the maximal conversion percentage between PBN-AA (12%) and PBN-GA (74%). Results: Upon oral gavage, PBN-GA accumulated a much greater amount of PBN in the cecum than PBN alone, thus verifying the in vitro colon specificity of PBN-GA. Oral PBN-GA enhanced the anticolitis effectiveness in dinitrobenzene sulfonic acid-induced rat colitis and limited the systemic absorption of PBN, thus reducing the risk of systemic adverse effects ascribed to PBN. Moreover, PBN-GA therapeutically surpassed sulfasalazine, a currently used anti-IBD drug, in rat colitis. Conclusions: These results suggest that amide conjugation with GA can be used to design a colon-targeting prodrug for PBN. Colon-targeted PBN may not only enhance therapeutic effectiveness but also improve the safety of PBN repositioned for the treatment of IBD and may be a pharmacological alternative for current small-molecule anti-IBD drugs with low efficacy or serious adverse effects with long-term use. Full article
(This article belongs to the Special Issue Site-Specific Drug Delivery)
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