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Pharmaceutics
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Selected Papers from the 1st International Electronic Conference on Pharmaceutics...
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Selected Papers from the 1st International Electronic Conference on Pharmaceutics (IECP 2020)

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 December 2021) | Viewed by 11344

Special Issue Editors

Dr. Andrea Erxleben

E-Mail Website
Guest Editor
School of Chemistry, National University of Ireland, H91TK33 Galway, Ireland
Interests: pharmaceutical cocrystals; amorphous formulations; control of crystal size and habit
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Elisabetta Gavini

E-Mail Website
Guest Editor
Department of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, Italy
Interests: drug delivery; nanomedicine; nasal route
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues,

This Special Issue comprises selected papers from the Proceedings of the 1st International Electronic Conference on Pharmaceutics (IECP 2020). The conference is set to be held from 20 November to 10 December 2020 on sciforum.net (https://sciforum.net/conference/IECP2020), an online platform for hosting scholarly e-conferences and discussion groups.

This conference will provide a robust common platform for leading scientists working in the broad field of pharmaceutics to share and discuss the latest research and to promote the advancement of this exciting and rapidly changing field.

During the event, a large number of excellent contributions covering key areas of opportunity and challenge were presented. More specifically, the following areas were covered:

  • Formulation of poorly soluble drugs;
  • Cyclodextrins in pharmaceutics;
  • Electrospun/sprayed drug delivery systems;
  • Advances in pharmacokinetics and drug metabolism;
  • Transdermal and topical drug delivery;
  • Brain drug delivery;
  • Nanomedicine for cancer.

Submitted contributions will be subjected to peer review and—upon acceptance—will be published with the aim of rapidly and widely disseminating research results, developments, and applications.

It should be noted that submitted manuscripts should have at least 30% additional, new, and unpublished material compared to the IECP 2020 published paper.

We look forward to receiving your contributions.

Dr. Andrea Erxleben
Prof. Dr. Elisabetta Gavini
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.

Published Papers (4 papers)

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Research

17 pages, 3668 KiB  
Article
Preparation of Magnetic–Luminescent Bifunctional Rapeseed Pod-Like Drug Delivery System for Sequential Release of Dual Drugs
by Junwei Xu, Yunxue Jia, Meili Liu, Xuenan Gu, Ping Li and Yubo Fan
Pharmaceutics 2021, 13(8), 1116; https://doi.org/10.3390/pharmaceutics13081116 - 22 Jul 2021
Cited by 8 | Viewed by 2050
Abstract
Drug delivery systems (DDSs) limited to a single function or single-drug loading are struggling to meet the requirements of clinical medical applications. It is of great significance to fabricate DDSs with multiple functions such as magnetic targeting or fluorescent labeling, as well as [...] Read more.
Drug delivery systems (DDSs) limited to a single function or single-drug loading are struggling to meet the requirements of clinical medical applications. It is of great significance to fabricate DDSs with multiple functions such as magnetic targeting or fluorescent labeling, as well as with multiple-drug loading for enhancing drug efficacy and accelerating actions. In this study, inspired by the dual-chamber structure of rapeseed pods, biomimetic magnetic–luminescent bifunctional drug delivery carriers (DDCs) of 1.9 ± 0.3 μm diameter and 19.6 ± 4.4 μm length for dual drug release were fabricated via double-needle electrospraying. Morphological images showed that the rapeseed pod-like DDCs had a rod-like morphology and Janus dual-chamber structure. Magnetic nanoparticles and luminescent materials were elaborately designed to be dispersed in two different chambers to endow the DDCs with excellent magnetic and luminescent properties. Synchronously, the Janus structure of DDCs promoted the luminescent intensity by at least threefold compared to single-chamber DDCs. The results of the hemolysis experiment and cytotoxicity assay suggested the great blood and cell compatibilities of DDCs. Further inspired by the core–shell structure of rapeseeds containing oil wrapped in rapeseed pods, DDCs were fabricated to carry benzimidazole molecules and doxorubicin@chitosan nanoparticles in different chambers, realizing the sequential release of benzimidazole within 12 h and of doxorubicin from day 3 to day 18. These rapeseed pod-like DDSs with excellent magnetic and luminescent properties and sequential release of dual drugs have potential for biomedical applications such as targeted drug delivery, bioimaging, and sustained treatment of diseases. Full article
(This article belongs to the Special Issue Selected Papers from the 1st International Electronic Conference on Pharmaceutics (IECP 2020))
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15 pages, 3247 KiB  
Article
Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration
by Marta Márquez Valls, Alejandra Martínez Labrador, Lyda Halbaut Bellowa, Doménica Bravo Torres, Paulo C. Granda, Montserrat Miñarro Carmona, David Limón and Ana C. Calpena Campmany
Pharmaceutics 2021, 13(7), 1080; https://doi.org/10.3390/pharmaceutics13071080 - 15 Jul 2021
Cited by 5 | Viewed by 2912
Abstract
The mouth can be affected by important inflammatory processes resulting from localized or systemic diseases such as diabetes, AIDS and leukemia, among others, and are manifested in various types of buccal sores typically presenting pain. This work focuses on the design, formulation, and [...] Read more.
The mouth can be affected by important inflammatory processes resulting from localized or systemic diseases such as diabetes, AIDS and leukemia, among others, and are manifested in various types of buccal sores typically presenting pain. This work focuses on the design, formulation, and characterization of four semisolid formulations for oral mucosa in order to symptomatically treat these painful processes. The formulations have two active pharmaceutical ingredients, triamcinolone acetonide (TA) and lidocaine hydrochloride (LIDO). The formula also contains, as an excipient, Orabase®, which is a protective, hydrophobic, and anhydrous adhesive vehicle, used to retain or facilitate the application of active pharmaceutical ingredients to the oral mucosa. After designing the formulations, an analytical method for TA was validated using HPLC so as to achieve reliable analytical results. Franz-type diffusion cells were used to perform drug release studies using synthetic membrane, and permeation studies using buccal mucosa, estimating the amount and rate of TA permeated across the tissue. Additionally, sublingual permeation studies were carried out to evaluate a scenario of a continuous contact of the tongue with the applied formulation. Permeation fluxes and the amount of TA retained within sublingual mucosa were similar to those in buccal mucosa, also implying anti-inflammatory activity in the part of the tongue that is in direct contact with the formulation. In addition, the dynamic conditions of the mouth were recreated in terms of the presence of phosphate buffered saline, constant movement of the tongue, pH, and temperature, using dissolution equipment. The amount of TA released into the phosphate buffered saline in dynamic conditions (subject to being ingested) is well below the normal oral doses of TA, for which the formulation can be considered safe. The formulations applied to buccal or sublingual mucosas under dynamic conditions permit the successful retention of TA within either tissue, where it exerts anti-inflammatory activity. The four formulations studied show a pseudoplastic and thixotropic behavior, ideal for topical application. These results evidence the potential of these topical formulations in the treatment of inflammatory processes in the buccal mucosa. Full article
(This article belongs to the Special Issue Selected Papers from the 1st International Electronic Conference on Pharmaceutics (IECP 2020))
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13 pages, 3374 KiB  
Article
Anti-Fn14 Antibody-Conjugated Nanoparticles Display Membrane TWEAK-Like Agonism
by Ahmed Aido, Olena Zaitseva, Harald Wajant, Matej Buzgo and Aiva Simaite
Pharmaceutics 2021, 13(7), 1072; https://doi.org/10.3390/pharmaceutics13071072 - 13 Jul 2021
Cited by 3 | Viewed by 2953
Abstract
Conventional bivalent IgG antibodies targeting a subgroup of receptors of the TNF superfamily (TNFSF) including fibroblast growth factor-inducible 14 (anti-Fn14) typically display no or only very limited agonistic activity on their own and can only trigger receptor signaling by crosslinking or when bound [...] Read more.
Conventional bivalent IgG antibodies targeting a subgroup of receptors of the TNF superfamily (TNFSF) including fibroblast growth factor-inducible 14 (anti-Fn14) typically display no or only very limited agonistic activity on their own and can only trigger receptor signaling by crosslinking or when bound to Fcγ receptors (FcγR). Both result in proximity of multiple antibody-bound TNFRSF receptor (TNFR) molecules, which enables engagement of TNFR-associated signaling pathways. Here, we have linked anti-Fn14 antibodies to gold nanoparticles to mimic the “activating” effect of plasma membrane-presented FcγR-anchored anti-Fn14 antibodies. We functionalized gold nanoparticles with poly-ethylene glycol (PEG) linkers and then coupled antibodies to the PEG surface of the nanoparticles. We found that Fn14 binding of the anti-Fn14 antibodies PDL192 and 5B6 is preserved upon attachment to the nanoparticles. More importantly, the gold nanoparticle-presented anti-Fn14 antibody molecules displayed strong agonistic activity. Our results suggest that conjugation of monoclonal anti-TNFR antibodies to gold nanoparticles can be exploited to uncover their latent agonism, e.g., for immunotherapeutic applications. Full article
(This article belongs to the Special Issue Selected Papers from the 1st International Electronic Conference on Pharmaceutics (IECP 2020))
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15 pages, 2552 KiB  
Article
Development and Validation of an HPLC–MS/MS Method for Pioglitazone from Nanocarriers Quantitation in Ex Vivo and In Vivo Ocular Tissues
by Esther Miralles-Cardiel, Marcelle Silva-Abreu, Ana Cristina Calpena and Isidre Casals
Pharmaceutics 2021, 13(5), 650; https://doi.org/10.3390/pharmaceutics13050650 - 03 May 2021
Cited by 7 | Viewed by 2137
Abstract
Pioglitazone (PGZ) is an oral anti-hyperglycemic agent, belongs to the class of thiazolidinediones, and is used for the treatment of diabetes mellitus type 2. In recent years, its anti-inflammatory activity has also been demonstrated in the literature for different diseases, including ocular inflammatory [...] Read more.
Pioglitazone (PGZ) is an oral anti-hyperglycemic agent, belongs to the class of thiazolidinediones, and is used for the treatment of diabetes mellitus type 2. In recent years, its anti-inflammatory activity has also been demonstrated in the literature for different diseases, including ocular inflammatory processes. Additionally, this drug belongs to Class II of the Biopharmaceutical Classification System, i.e., slightly soluble and highly permeable. The main objective of this study was to validate a new analytical HPLC-MS/MS method to quantify free-PGZ and PGZ from polymeric NPs to conduct nanoparticle application studies loaded with this active ingredient to transport it within ocular tissues. An accurate, sensitive, selective, reproducible and high throughput HPLC-MS/MS method was validated to quantify PGZ in cornea, sclera, lens, aqueous humor, and vitreous humor. The chromatographic separation was achieved in 10 min on a Kinetex C18 column. Linear response of PGZ was observed over the range of 5–100 ng/mL. The recovery of free-PGZ or PGZ from NPs was in the range of 85–110% in all tissues and levels tested. The intra-day and inter-day precision were <5% and <10%, respectively. The extracts were shown to be stable in various experimental conditions in all matrices studied. The range of concentrations covered by this validation is 80–1600 µg/kg of PGZ in ocular tissues. It is concluded that this method can be applied to quantify PGZ for in vivo and ex vivo biodistribution studies related to the ocular administration of free-PGZ and PGZ from nanoparticles. Full article
(This article belongs to the Special Issue Selected Papers from the 1st International Electronic Conference on Pharmaceutics (IECP 2020))
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