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Special Issue "Molecular Modification in Designing Next Generation Drug Delivery Systems"

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A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: 31 December 2023 | Viewed by 6038

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Special Issue Editors

Dr. Victor Tuan Giam Chuang

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Guest Editor

Curtin Medical School, Faculty of Health Sciences, Curtin University, Kent Street, Bentley, Perth, WA 6102, Australia
Interests: functionalization of plasma proteins for pharmaceutical applications
Special Issues, Collections and Topics in MDPI journals

Dr. Yu Ishima

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Guest Editor

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Kyoto, Japan
Interests: albumin; drug delivery system; cancer therapy

Special Issue Information

Dear Colleagues,

Absorption improvement, site-specific targeting, and controlled release are the three main goals of drug delivery. Drug delivery systems are engineered to accomplish the treatment outcomes of comfort, compliance, and accuracy in therapy. The molecular modification of drugs is a common drug development approach, but this frequently changes the specificity and affinities of ligand–receptor binding. Furthermore, controlled release for therapy precision could only be achieved through a rigorous drug delivery system architectural design. The development of next-generation drug delivery systems incorporating various technologies, such as analytical and synthetic sciences, DNA recombination and genetic mutation, artificial intelligence, and artificial organ substitutes such as artificial blood, should lead the current one-size-fits-all treatment modality to a much higher precision level of bioresponsivity, whereby a patient may potentially live a life similar to an average healthy person. Articles exhibiting molecular modifications to biomaterials and other drug-carrying and targeting shuttles such as liposomes are sought for this Special Issue. Submissions of articles that elaborate on the use of artificial intelligence, smart technologies, and other cutting-edge technologies that lead to the next generation of drug delivery systems to realise the ultimate objective of precision medicines are particularly encouraged.

Dr. Victor Tuan Giam Chuang
Dr. Yu Ishima
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 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. Pharmaceuticals 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

absorption enhancement
artificial substitutes
biomaterials
bioresponsive
controlled release
drug delivery systems
functionalisation
genetic and chemical modifications
medical devices
nanotechnology
precision medicines
proteins, peptides, and oligonucleotides
routes of administration
smart technology
targeting

Published Papers (6 papers)

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Research

12 pages, 1169 KiB

Open AccessArticle

Brain Delivery of Cisplatin Using Microbubbles in Combination with Ultrasound as an Effective Therapy for Glioblastoma

and

Pharmaceuticals 2023, 16(11), 1599; https://doi.org/10.3390/ph16111599 - 13 Nov 2023

Viewed by 455

Abstract

Glioblastoma is a highly invasive and fatal disease. Temozolomide, a blood–brain barrier (BBB)-penetrant therapeutic agent currently used for glioblastoma, does not exhibit sufficient therapeutic effect. Cisplatin (CDDP), a versatile anticancer drug, is not considered a therapeutic option for glioblastoma due to its low BBB permeability. We previously investigated the utility of microbubbles (MBs) in combination with ultrasound (US) in promoting BBB permeability and reported the efficacy of drug delivery to the brain using a minimally invasive approach. This study aimed to evaluate the feasibility of CDDP delivery to the brain using the combination of MBs and US for the treatment of glioblastoma. We used mice that were implanted with glioma-261 GFP-Luc cells expressing luciferase as the glioblastoma model. In this model, after tumor inoculation, the BBB opening was induced using MBs and US, and CDDP was simultaneously administered. We found that the CDDP concentrations were higher at the glioblastoma site where the US was applied, although CDDP normally cannot pass through the BBB. Furthermore, the survival was longer in mice treated with CDDP delivered via MBs and US than in those treated with CDDP alone or those that were left untreated. These results suggest that the combination of MBs and US is an effective antitumor drug delivery system based on BBB opening in glioblastoma therapy. Full article

(This article belongs to the Special Issue Molecular Modification in Designing Next Generation Drug Delivery Systems)

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23 pages, 7293 KiB

Open AccessArticle

Verubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on Ca²⁺ or Mg²⁺ Cross-Linked Alginate

Pharmaceuticals 2023, 16(10), 1499; https://doi.org/10.3390/ph16101499 - 21 Oct 2023

Viewed by 750

Abstract

Tubulin-targeting agents attract undiminished attention as promising compounds for the design of anti-cancer drugs. Verubulin is a potent tubulin polymerization inhibitor, binding to colchicine-binding sites. In the present work, a series of verubulin analogues containing a cyclohexane or cycloheptane ring 1,2-annulated with pyrimidine moiety and various substituents in positions 2 and 4 of pyrimidine were obtained and their cytotoxicity towards cancer and non-cancerous cell lines was estimated. The investigated compounds revealed activity against various cancer cell lines with IC₅₀ down to 1–4 nM. According to fluorescent microscopy data, compounds that showed cytotoxicity in the MTT test disrupt the normal cytoskeleton of the cell in a pattern similar to that for combretastatin A-4. The hit compound (N-(4-methoxyphenyl)-N,2-dimethyl-5,6,7,8-tetrahydroquinazolin-4-amine) was encapsulated in biocompatible nanocontainers based on Ca²⁺ or Mg²⁺ cross-linked alginate and it was demonstrated that its cytotoxic activity was preserved after encapsulation. Full article

(This article belongs to the Special Issue Molecular Modification in Designing Next Generation Drug Delivery Systems)

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15 pages, 1248 KiB

Open AccessArticle

Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships

Muthipeedika Nibin Joy

Mallikarjuna R. Guda

and

Grigory V. Zyryanov

Pharmaceuticals 2023, 16(9), 1326; https://doi.org/10.3390/ph16091326 - 19 Sep 2023

Viewed by 695

Abstract

Four sets of previously synthesized 4-methyl-7-substituted coumarin derivatives were screened for their in vitro anti-inflammatory and anti-tubercular activities. The anti-inflammatory potential of 3a–t, 5a–o, 6a–n, and 7a–f synthesized compounds was evaluated by an anti-denaturation assay using diclofenac sodium as the reference standard. Evaluation of the anti-tuberculous activity of the mentioned compounds was performed by the Resazurin test method against four different TB strains using rifampicin and isoniazid as reference drugs. Based on the anti-inflammatory results, compounds 3o, 5f, 6c, and 7d proved to be the most active compounds in their respective series. Additionally, compounds 3k–n, 5b–d, 6d–f, 6k, 7a, and 7f were found to be the most potent anti-tuberculous agents. In fact, most of the screened compounds exhibited promising activity profiles compared to the respective standard drugs. The structure–activity connections revealed a few intriguing aspects, indicating that the presence of electron-donating and nitrogen-rich fragments boost the anti-inflammatory effects of the examined compounds. However, the presence of electron-withdrawing substituents was required to boost the anti-tubercular activity of the evaluated compounds. Full article

(This article belongs to the Special Issue Molecular Modification in Designing Next Generation Drug Delivery Systems)

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29 pages, 5462 KiB

Open AccessArticle

Cytotoxic and Infection-Controlled Investigations of Novel Dihydropyridine Hybrids: An Efficient Synthesis and Molecular-Docking Studies

Mallikarjuna R. Guda

Grigory. V. Zyryanov

Amit Dubey

Venkata Subbaiah Munagapati

and

Jet-Chau Wen

Pharmaceuticals 2023, 16(8), 1159; https://doi.org/10.3390/ph16081159 - 15 Aug 2023

Cited by 1 | Viewed by 647

Abstract

A sequence of novel 1,4-dihydropyridines (DHP) and their hybrids was developed using a multicomponent strategy under environmentally benign conditions. In addition, computational studies were performed, and the ligand–protein interactions calculated in different bacteria and two fungal strains. Para-hydroxy-linked DHP (5f) showed the best binding energies of 3.591, 3.916, 8.499 and 6.895 kcal/mol against various pathogens used and other substances received a good docking score. The pathogen resistance potential of the synthesized targets against four bacteria and two fungi showed that whole DHP substances exhibit different levels of resistance to each microorganism. Gram-positive bacteria, which are highly sensitive to all molecules, and the MTCC-1884-encoded fungus strongly rejected the studied compounds compared to comparator drugs. In particular, the 5f candidate showed remarkable antimicrobial activity, followed by the substances 5a, 5b, 5j, 5k and 5l. Furthermore, MIC and MBC/MFC properties showed that 5f had a minimum bacterial concentration of 12.5 μg/mL against E. coli and against two fungal pathogens, with its killing activity being effective even at low concentrations. On the other hand, whole motifs were tested for their cytotoxic activity, revealing that the methoxy and hydroxy-linked compounds (5h) showed greater cytotoxic potency, followed by the two hydroxy linked compounds (5d and 5f). Overall, this synthetic approach used represents a prototype for future nature-favored synthesis methods and these biological results serve as a guide for future therapeutic drug research. However, the computer results play an important role in the further development of biological experiments. Full article

(This article belongs to the Special Issue Molecular Modification in Designing Next Generation Drug Delivery Systems)

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17 pages, 3270 KiB

Open AccessArticle

In Vitro and In Vivo Functional Viability, and Biocompatibility Evaluation of Bovine Serum Albumin-Ingrained Microemulsion: A Model Based on Sesame Oil as the Payload for Developing an Efficient Drug Delivery Platform

Abdulaziz Arif A. Alshammari

Hamdoon A. Mohammed

Majid Jabir

and

Riaz A. Khan

Pharmaceuticals 2023, 16(4), 582; https://doi.org/10.3390/ph16040582 - 12 Apr 2023

Cited by 3 | Viewed by 1485

Abstract

Combination of bovine serum albumin with microemulsions as constituting ingredient biopolymer has long been regarded an innovative method to address the surface functionalization and stability issues in the targeted payload deliveries, thereupon producing effectively modified microemulsions, which are superior in loading capacity, transitional and shelf-stability, as well as site-directed/site-preferred delivery, has become a favored option. The current study aimed to develop an efficient, suitable and functional microemulsion system encapsulating sesame oil (SO) as a model payload towards developing an efficient delivery platform. UV-VIS, FT-IR, and FE-SEM were used to characterize, and analyze the developed carrier. Physicochemical properties assessments of the microemulsion by dynamic light scattering size distributions, zeta-potential, and electron micrographic analyses were performed. The mechanical properties for rheological behavior were also studied. The HFF-2 cell line and hemolysis assays were conducted to ascertain the cell viability, and in vitro biocompatibility. The in vivo toxicity was determined based on a predicted median lethal dose (LD₅₀) model, wherein the liver enzymes’ functions were also tested to assess and confirm the predicted toxicity. Full article

(This article belongs to the Special Issue Molecular Modification in Designing Next Generation Drug Delivery Systems)

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12 pages, 3268 KiB

Open AccessArticle

Increasing Skeletal Muscle Mass in Mice by Non-Invasive Intramuscular Delivery of Myostatin Inhibitory Peptide by Iontophoresis

and

Pharmaceuticals 2023, 16(3), 397; https://doi.org/10.3390/ph16030397 - 06 Mar 2023

Viewed by 1384

Abstract

Sarcopenia is a major public health issue that affects older adults. Myostatin inhibitory-D-peptide-35 (MID-35) can increase skeletal muscle and is a candidate therapeutic agent, but a non-invasive and accessible technology for the intramuscular delivery of MID-35 is required. Recently, we succeeded in the intradermal delivery of various macromolecules, such as siRNA and antibodies, by iontophoresis (ItP), a non-invasive transdermal drug delivery technology that uses weak electricity. Thus, we expected that ItP could deliver MID-35 non-invasively from the skin surface to skeletal muscle. In the present study, ItP was performed with a fluorescently labeled peptide on mouse hind leg skin. Fluorescent signal was observed in both skin and skeletal muscle. This result suggested that the peptide was effectively delivered to skeletal muscle from skin surface by ItP. Then, the effect of MID-35/ItP on skeletal muscle mass was evaluated. The skeletal muscle mass increased 1.25 times with ItP of MID-35. In addition, the percentage of new and mature muscle fibers tended to increase, and ItP delivery of MID-35 showed a tendency to induce alterations in the levels of mRNA of genes downstream of myostatin. In conclusion, ItP of myostatin inhibitory peptide is a potentially useful strategy for treating sarcopenia. Full article

(This article belongs to the Special Issue Molecular Modification in Designing Next Generation Drug Delivery Systems)

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Special Issue "Molecular Modification in Designing Next Generation Drug Delivery Systems"

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