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Special Issue "Chemistry-Based Strategies for Drug Delivery and Targeting"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (28 February 2018)

Special Issue Editor

Guest Editor
Prof. Dr. Rosario Pignatello

NANO-i - Research Centre on Ocular Nanotechnology, Department of Drug Sciences, University of Catania, Catania 95124, Italy
Website | E-Mail
Interests: nanomedicine; lipid- and polymer-based nanoparticles; liposomes; prodrugs; controlled drug release; biomaterials; ocular drug delivery; brain drug delivery

Special Issue Information

Dear Colleagues,

The optimization of a drug molecule from a chemical point of view, e.g., under a structure-activity profile, is often not satisfactory to ensure that the active compound will reach the target tissue/organ at effective levels, or that it attains the necessary concentration in the body. A scarce pharmacokinetic profile is often the cause for putting aside compounds that have shown valid pharmacological outlines and a promising therapeutic future.

Increasing the dosage of drugs cannot be always the right solution, since it can cause severe side effects and can damage healthy cells and organs.

Therefore, in the last few decades, different approaches aiming at modulating the release of drugs and/or targeting them to selective tissues have become an essential partner of the industrial drug development stage. Chemistry-based delivery strategies are potentially able to improve the therapeutic index and safety of active compounds, as well as to give a second chance to ‘old’ drugs that have lost their clinical interest because of unsatisfactory physico-chemical, pharmacokinetic, or toxicological properties.

All these approaches would require a detailed and update knowledge of the biochemical pathways in health and pathological situations and of the enzymatic scenery in different tissues and organs, that can affect the activation of these chemical systems and localized release of the bioactive cargo.

Accepted contributions can be mainly (but not exclusively) focused on recent innovations in the following topics:

  • Prodrug and soft-drug synthesis, characterization, formulation and biological evaluation
  • Chemical delivery systems (CDS), i.e., chemical entities that recognize specific enzymes exclusively at the site of action/metabolism
  • Retrometabolic drug design studies
  • Synthetic strategies to achieve targeting features on a drug molecule
  • Bioconjugate chemistry
  • Polymer-drug conjugates (polymeric prodrugs)
  • Drug conjugation to nanoparticulate carriers
  • Biochemical studies unveiling novel potential biological targets for the chemical delivery systems
  • Hydrophobic ion-pairing.

This Special Issue will be of interest to undergraduate and graduate students, as well as to academy and pharma industry researchers, which are involved in both medicinal chemistry and pharmaceutical technology fields.

Prof. Rosario Pignatello
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • Prodrugs
  • Ion pairs
  • Conjugates
  • Controlled drug delivery
  • Drug targeting

Published Papers

There is no accepted submissions to this special issue at this moment.
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