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Pharmaceutics
Special Issues
Novel Devices for the Oral Delivery of Macromolecules
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Novel Devices for the Oral Delivery of Macromolecules

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (20 February 2022) | Viewed by 13781

Special Issue Editors

Dr. Ester Caffarel-Salvador

E-Mail Website
Guest Editor
1. Department of Regenerative Medicine, LEO Pharma, Cambridge, MA, USA
2. Institute for Medical Engineering and Science, Massachusetts Institute of Technology, Cambridge, MA 02139, USA
Interests: microneedles; drug delivery; therapeutic drug monitoring; oral delivery of biologics; insulin; nanoparticles; plasmid DNA; gene therapy
Prof. Dr. Jinyao Liu

E-Mail Website
Guest Editor
Institute of Molecular Medicine, Shanghai Jiao Tong University, Shanghai, China
Interests: oral delivery; drug carrier; controlled release; bacteria; the gut microbiome; intestinal barrier; inflammation; tumor

Special Issue Information

Dear Colleagues,

It is challenging to deliver macromolecules (e.g., proteins, peptides, antibodies, and oligonucleotides) orally due to the delivery barriers and microenvironmental challenges encountered along the gastrointestinal tract. In the last few years, novel medical devices have been developed which are capable of overcoming these barriers and delivering a wide range of molecules in different organs, all the way from the mouth to the colon. Microneedle-based pills, nanostraws, microjets, hydrogels and intestinal patches are some of the device-based solutions that researchers have designed to enable the oral dosing of macromolecules. These alternative delivery methods have the potential to revolutionize many treatments by increasing patient adherence and efficacy while reducing pain and other side effects.

This Special Issue aims to capture the most recent advances to overcome the oral drug delivery barriers of the gastrointestinal tract. We invite reviews and research articles from clinical, academic, and industry settings on “Novel Devices for the Oral Delivery of Macromolecules.”

Dr. Ester Caffarel-Salvador
Prof. Dr. Jinyao Liu
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. 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

  • oral
  • drug delivery
  • microneedles
  • nanostraws
  • microjets
  • buccal
  • gastrointestinal
  • macromolecules
  • biologic
  • peptide
  • devices
  • hydrogels
  • microdevices

Published Papers (4 papers)

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Research

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24 pages, 3104 KiB  
Article
Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery
by Mohammad Raish, Mohd Abul Kalam, Ajaz Ahmad, Mudassar Shahid, Mushtaq Ahmad Ansari, Abdul Ahad, Raisuddin Ali, Yousef A. Bin Jardan, Aws Alshamsan, Musaed Alkholief, Khalid M. Alkharfy, Ibrahim Abdelsalam Abdelrahman and Fahad I. Al-Jenoobi
Pharmaceutics 2021, 13(11), 1921; https://doi.org/10.3390/pharmaceutics13111921 - 12 Nov 2021
Cited by 9 | Viewed by 2365
Abstract
In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux [...] Read more.
In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux method and 5-FU into SEMC was encapsulated by the vacuum-assisted loading method. 5-FU loaded SEMC was coated with Eudragit® RS-100 (ERS) by the organic solvent-evaporation technique under vacuum to avoid the discharge of 5-FU in the stomach and small intestine. Morphological and physicochemical characterization of drug-loaded SEMC (coated/uncoated) was performed by scanning electron microscopy (SEM), FTIR, XRD, and DSC. The encapsulation and drug loading were determined by the direct method, and an in vitro release study was performed in simulated gastric and intestinal fluids (SGF/SIF). The colon-specific delivery of 5-FU from the SEMC was assessed in terms of pharmacokinetics and gastrointestinal tract distribution after oral administration in rats. The successful encapsulation and loading of 5-FU into SEMC by a vacuum-assisted loading technique and its coating with ERS by a solvent-evaporation technique were achieved. SEM images of uncoated SEMC have shown porous structures, and coating with ERS reserved their morphology with a smooth surface and discrete microstructures and the 5% w/v ERS acetone solution. ERS-coated SEMC sustained the release of 5-FU until 24 h in SIF, while it was up to 12 h only from uncoated SEMC. The maximum plasma concentration (Cmax) of 5-FU from uncoated SEMC was 102.82 μg/mL after 1 h, indicating a rapid release of 5-FU in the upper gastrointestinal tract. This concentration decreased quickly with a half-life of 4 h, AUC0-t was 264.1 μg/mL.h, and MRT0-inf was 5.2 h. The Cmax of 5-FU from ERS-coated SEMC was 19.47 μg/mL at 16 h. The Cmax of 5-FU in small intestines was 406.2 μg/g at 1 h from uncoated SEMC and 1271.5 μg/g at 12 h from coated SEMC. Conclusively, a 249.9-fold higher relative bioavailability of 5-FU was achieved with the ERS-coated SEMC in colon tissues than that from uncoated SEMC. Full article
(This article belongs to the Special Issue Novel Devices for the Oral Delivery of Macromolecules)
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14 pages, 3081 KiB  
Article
Oral Gene Therapy of HFD-Obesity via Nonpathogenic Yeast Microcapsules Mediated shRNA Delivery
by Li Zhang, Wan Zhang, Hang Peng, Yankun Li, Tongtong Leng, Chenxi Xie and Long Zhang
Pharmaceutics 2021, 13(10), 1536; https://doi.org/10.3390/pharmaceutics13101536 - 22 Sep 2021
Cited by 7 | Viewed by 1774
Abstract
Obesity is a chronic systemic inflammatory disease, which occurs when energy intake exceeds the energy consumption. Therefore, controlling energy intake or increasing physical consumption can effectively control obesity. However, in reality, it is very difficult for the majority of obese patients to lose [...] Read more.
Obesity is a chronic systemic inflammatory disease, which occurs when energy intake exceeds the energy consumption. Therefore, controlling energy intake or increasing physical consumption can effectively control obesity. However, in reality, it is very difficult for the majority of obese patients to lose weight by autonomously controlling diet. In this study, oral shRNA/yeast microcapsules were constructed with non-virus-mediated IL-1β shRNA interference vectors and non-pathogenic Saccharomyces cerevisiae. Moreover, high-fat diet induced obese mice were established to assess the weight loss effect of IL-1β shRNA/yeast microcapsules via the oral route. After IL-1β shRNA/yeast treatment, body weight and fat weight was reduced. Compared with the control group, higher average food intake but lower energy conversion rate was observed in IL-1β shRNA/yeast group. In addition, lipid metabolism related cytokines and blood glucose concentration in the circulating blood was improved after IL-1β shRNA/yeast treatment. Yeast microcapsules mediated IL-1β shRNA delivery can effectively improve obesity. Noteworthy, this kind of non-diet-controlled weight loss strategy does not need diet control, and shows good biocompatibility. It is good news to obese patients who need to lose weight but cannot control their diet. Full article
(This article belongs to the Special Issue Novel Devices for the Oral Delivery of Macromolecules)
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Review

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24 pages, 2033 KiB  
Review
Future Perspectives of Oral Delivery of Next Generation Therapies for Treatment of Skin Diseases
by Pia Pernille Søgaard, Marianne Lind, Chatpakorn Rassemeena Christiansen, Karsten Petersson, Adam Clauss and Ester Caffarel-Salvador
Pharmaceutics 2021, 13(10), 1722; https://doi.org/10.3390/pharmaceutics13101722 - 18 Oct 2021
Cited by 6 | Viewed by 6065
Abstract
Gene therapies have conspicuously bloomed in recent years as evidenced by the increasing number of cell-, gene-, and oligo-based approved therapies. These therapies hold great promise for dermatological disorders with high unmet need, for example, epidermolysis bullosa or pachyonychia congenita. Furthermore, the recent [...] Read more.
Gene therapies have conspicuously bloomed in recent years as evidenced by the increasing number of cell-, gene-, and oligo-based approved therapies. These therapies hold great promise for dermatological disorders with high unmet need, for example, epidermolysis bullosa or pachyonychia congenita. Furthermore, the recent clinical success of clustered regularly interspaced short palindromic repeats (CRISPR) for genome editing in humans will undoubtedly contribute to defining a new wave of therapies. Like biologics, naked nucleic acids are denatured inside the gastrointestinal tract and need to be administered via injections. For a treatment to be effective, a sufficient amount of a given regimen needs to reach systemic circulation. Multiple companies are racing to develop novel oral drug delivery approaches to circumvent the proteolytic and acidic milieu of the gastrointestinal tract. In this review, we provide an overview of the evolution of the gene therapy landscape, with a deep focus on gene and oligonucleotide therapies in clinical trials aimed at treating skin diseases. We then examine the progress made in drug delivery, with particular attention on the peptide field and drug-device combinations that deliver macromolecules into the gastrointestinal tract. Such novel devices could potentially be applied to administer other therapeutics including genes and CRISPR-based systems. Full article
(This article belongs to the Special Issue Novel Devices for the Oral Delivery of Macromolecules)
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18 pages, 4384 KiB  
Review
Bacteria-Based Microdevices for the Oral Delivery of Macromolecules
by Zhenping Cao, Sisi Lin and Jinyao Liu
Pharmaceutics 2021, 13(10), 1610; https://doi.org/10.3390/pharmaceutics13101610 - 03 Oct 2021
Cited by 10 | Viewed by 2819
Abstract
The oral delivery of macromolecules is quite challenging due to environmental insults and biological barriers encountered along the gastrointestinal (GI) tract. Benefiting from their living characteristics, diverse bacterial species have been engineered as intelligent platforms to deliver various therapeutics. To tackle difficulties in [...] Read more.
The oral delivery of macromolecules is quite challenging due to environmental insults and biological barriers encountered along the gastrointestinal (GI) tract. Benefiting from their living characteristics, diverse bacterial species have been engineered as intelligent platforms to deliver various therapeutics. To tackle difficulties in oral delivery, innovative bacteria-based microdevices have been developed by virtue of advancements in synthetic biology and nanotechnology, with aims to overcome the instability and short half-life of macromolecules in the GI tract. In this review, we summarize the main classes of macromolecules that are produced and delivered through the oral ingestion of bacteria and bacterial derivatives. Furtherly, we discuss the engineering strategies and biomedical applications of these living microdevices in disease diagnosis, bioimaging, and treatment. Finally, we highlight the advantages as well as the limitations of these engineered bacteria used as platforms for the oral delivery of macromolecules and also propose their potential for clinical translation. The results summarized in this review article would contribute to the invention of next-generation bacteria-based systems for the oral delivery of macromolecules. Full article
(This article belongs to the Special Issue Novel Devices for the Oral Delivery of Macromolecules)
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