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Pharmaceutics
Special Issues
Peptide-Based Drug Delivery Systems: From Design to Application
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Peptide-Based Drug Delivery Systems: From Design to Application

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

Deadline for manuscript submissions: 31 August 2026 | Viewed by 2910

Special Issue Editors

Dr. Zoltán Bánóczi

E-Mail Website
Guest Editor
Department of Organic Chemistry, ELTE Eötvös Loránd University, Budapest, Hungary
Interests: cell-penetrating peptide; peptide conjugate; cellular uptake; structure–activity relationship; drug-delivery systems
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Gábor Mező

E-Mail Website
Guest Editor
1. Department of Organic Chemistry, ELTE Eötvös Loránd University, Budapest, Hungary
2. HUN-REN-ELTE Research Group of Peptide Chemistry, Budapest, Hungary
Interests: targeted tumor therapy; peptide–drug conjugates; homing peptides; linker systems
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Drug delivery systems play a crucial role in many cases to get a very efficient drug conjugate. There are several types of these systems, such as peptides, polypeptides, lipids, and nanoparticles. Unfortunately there is not a “magic” solution for the delivery of any kind of drug molecules. For developing the best compound, the optimization of the delivery unit and the construction of the compound should be necessary. Among the delivery system peptides, the base ones are very promising. These molecules can be synthesized and modified in a fast process. The fine-tuning of their properties can be extended by using non-natural amino acid substitutions. Besides drug delivery, they are able to target tissues or specific cells.

This Special Issue aims to emphasize and to highlight the design and applicability of peptide-based drug delivery systems. Original research papers and reviews are welcomed about newly developed peptide-based drug delivery systems, conjugates of these delivery units, structure–activity relationships, and the effect of different chemical modifications. We encourage the publication of comprehensive studies about the influence of the composition of conjugates (e.g., spacer, linker, and the position and order of the parts of the conjugates) and the effect of chemical modifications (e.g., the chemistry of conjugation and amino acid substitutions).  

Dr. Zoltán Bánóczi
Prof. Dr. Gábor Mező
Guest Editors

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 submissions that pass pre-check are 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 250 words) can be sent to the Editorial Office for assessment.

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. Pharmaceutics 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 2900 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.

Keywords

  • drug delivery
  • peptide
  • targeted drug delivery
  • peptide conjugate
  • chemical modification
  • linker systems

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Published Papers (2 papers)

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Research

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21 pages, 6621 KB  
Article
Penetratin an Old Player in the Field of Cell-Penetrating Peptides Is in New Custom—Effect of Aromatic Non-Natural Amino Acid Substitutions
by Dóra Soltész, Ildikó Szabó, Viktor Farkas, Nikolett Borók, Tamás Visnovitz, Dorina Lenzinger, Fülöp Károly Grébecz, Szilvia Bősze and Zoltán Bánóczi
Pharmaceutics 2026, 18(5), 555; https://doi.org/10.3390/pharmaceutics18050555 - 30 Apr 2026
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Abstract
Background/Objectives: Investigating the modified derivatives of known cell-penetrating peptides can highlight the important residues in the peptide sequence and help understand the cellular uptake mechanism better. Moreover, comparing peptides with different fluorescent-dye positions can highlight the importance of the conjugation site. Earlier, [...] Read more.
Background/Objectives: Investigating the modified derivatives of known cell-penetrating peptides can highlight the important residues in the peptide sequence and help understand the cellular uptake mechanism better. Moreover, comparing peptides with different fluorescent-dye positions can highlight the importance of the conjugation site. Earlier, it was demonstrated that the fluorescence quencher 4-((4-(dimethylamino)phenyl)azo)benzoyl (Dabcyl) group can enhance the internalization efficiency of highly cationic oligoarginine peptides. However, its effect in the case of arginine-rich penetratin, a secondary amphipathic cationic CPP, remains undiscovered. Methods: Here, several penetratin derivatives were studied in which the aromatic residues were substituted and the effect of Dabcyl modification was also studied on the cellular uptake of peptides by flow cytometry. Results: The triple Nal-substituted penetratin and dodeca-penetratin with N-terminally positioned carboxyfluoresein (Cf) dye demonstrated remarkable internalization efficiency compared to penetratin. Moreover, almost all the Dabcyl-modified peptides were superior to penetratin except two peptides with C-terminal Cf-labelling. This result highlights the importance of the structure of the conjugate. The position of the cargo molecule may have a high impact on internalization ability. The relatively low cellular uptake of the Trp48 residue-substituted Dabcyl-Pen12 points to the importance of this residue in the cellular uptake of dodeca-penetratin. The confocal microscopic studies revealed that, besides the greater penetration efficiency of Dabcyl penetratin derivatives, these peptides enter the cytoplasm of cells in an increased manner. Conclusions: We identified several intriguing derivatives and expanded the applicability of Dabcyl, while also highlighting its limitations. Additionally, the critical role of Trp48 in the penetratin sequence was reaffirmed, along with the importance of the fluorescent molecule’s position. Full article
(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems: From Design to Application)
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Review

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42 pages, 1224 KB  
Review
BPC-157 as an Investigational Peptide Therapeutic: Biopharmaceutical Challenges, Formulation Strategies, and Translational Development Barriers
by Diana-Maria Mateescu, Dragos-Mihai Gavrilescu, Florin Eugen Constantinescu, Cristian Oancea, Adrian-Cosmin Ilie, Roxana Folescu, Mihaela-Diana Popa, Stela Iurciuc, Camelia-Oana Muresan and Alexandra Enache
Pharmaceutics 2026, 18(5), 625; https://doi.org/10.3390/pharmaceutics18050625 - 20 May 2026
Cited by 1 | Viewed by 1557
Abstract
Background/Objectives: BPC-157 (body protection compound 157) is a synthetic pentadecapeptide derived from a gastric protein fragment with reported cytoprotective and regenerative properties across multiple organ systems. Despite over three decades of preclinical research demonstrating consistent biological activity, its pharmaceutical development remains rudimentary, [...] Read more.
Background/Objectives: BPC-157 (body protection compound 157) is a synthetic pentadecapeptide derived from a gastric protein fragment with reported cytoprotective and regenerative properties across multiple organ systems. Despite over three decades of preclinical research demonstrating consistent biological activity, its pharmaceutical development remains rudimentary, with no approved formulation, no validated dosing regimen, and no completed Phase II clinical trial. This review critically evaluates BPC-157 from a biopharmaceutical and drug development perspective, examining its physicochemical and pharmacokinetic properties, formulation challenges across routes of administration, the pharmacokinetic–pharmacodynamic disconnect that characterizes its preclinical profile, and the regulatory and translational barriers that currently preclude clinical advancement. Methods: A narrative review of the literature was conducted using PubMed/MEDLINE, Embase, and Cochrane Library from database inception to April 2026. Search terms included “BPC-157”, “BPC157”, “body protection compound 157”, “pentadecapeptide”, and “GEPPPGKPADDAGLV”, each combined with “pharmacokinetics”, “formulation”, “biopharmaceutics”, “drug delivery”, “clinical trial”, “toxicology”, and “regulatory”. Patent databases (Espacenet, Google Patents) and regulatory agency websites (FDA, EMA, WADA) were searched independently. Searches were supplemented by forward and backward citation tracking of key references. Articles were selected based on relevance to biopharmaceutical characterization, pharmacokinetics, formulation science, clinical evidence, and regulatory status; pharmacodynamic studies were included insofar as they inform translational development. Evidence was synthesized with emphasis on pharmaceutical characterization, formulation science, and translational feasibility; no formal quality assessment instrument was applied, consistent with the narrative review design. Results: BPC-157 exhibits unusual stability in gastric juice and demonstrates activity via oral, parenteral, and topical routes, yet its human pharmacokinetic profile remains critically undercharacterized despite a recently published formal preclinical ADME study in two species confirming a sub-30-min plasma half-life, linear dose-proportional kinetics, and intramuscular bioavailability of 14–51% depending on species. A plasma half-life of under 30 min—confirmed preclinically and in a preliminary two-subject human pilot—contrasts with prolonged biological effects lasting hours to days—a disconnect with significant implications for dosing strategy and formulation design. No pharmaceutical-grade formulation has been developed or validated. The peptide lacks bcs classification data, permeability characterization, and formal excipient compatibility studies. Available clinical data derive from fewer than 30 subjects across three uncontrolled pilot studies, none of which employed standardized pharmaceutical preparations. Conclusions: BPC-157 presents a compelling but pharmaceutically underdeveloped profile. The primary barrier to clinical translation is not the absence of biological activity, but the absence of fundamental pharmaceutical science: characterized formulations, validated pharmacokinetics, and a coherent drug development strategy. Addressing these biopharmaceutical gaps is a prerequisite for any meaningful clinical program. Full article
(This article belongs to the Special Issue Peptide-Based Drug Delivery Systems: From Design to Application)
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