Featured Papers in Biopharmaceutics

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Biopharmaceutics".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 3841

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Guest Editor
Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers University, Piscataway, NJ 08854, USA
Interests: drug delivery; nanotechnology; biopharmaceutics; pharmacokinetics; absorption; permeability; AIDS; cancer

Special Issue Information

Dear Colleagues,

We are pleased to announce a Special Issue entitled “Feature Papers in Biopharmaceutics”. This is a collection of important high-quality papers discussing new knowledge or new cutting-edge developments in the biopharmaceutics field, in the hope of making a great contribution to the community. Topic areas include the roles of membrane transporters and receptors in drug delivery and disposition, targeted drug delivery, and the physical and chemical properties drugs and delivery systems as they relate to bioavailability, pharmacokinetics, pharmacokinetics, and toxicology effects.

We invite researchers to submit original research articles and reviews in this field. All articles published in this Special Issue are subject to rigorous peer review and editorial selection. We intend for this issue to be the best forum for disseminating excellent research findings as well as sharing innovative ideas in the field.

Prof. Dr. Patrick Sinko
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 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 (2 papers)

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16 pages, 3529 KiB  
Article
Lipophilicity and ADMET Analysis of Quinoline-1,4-quinone Hybrids
by Monika Kadela-Tomanek, Maria Jastrzębska, Elwira Chrobak and Ewa Bębenek
Pharmaceutics 2023, 15(1), 34; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15010034 - 22 Dec 2022
Cited by 5 | Viewed by 1493
Abstract
Lipophilicity is one of the basic properties of a potential drug determining its solubility in non-polar solvents and, consequently, its ability to passively penetrate the cell membrane, as well as the occurrence of various pharmacokinetic processes, including adsorption, distribution, metabolism, excretion, and toxicity [...] Read more.
Lipophilicity is one of the basic properties of a potential drug determining its solubility in non-polar solvents and, consequently, its ability to passively penetrate the cell membrane, as well as the occurrence of various pharmacokinetic processes, including adsorption, distribution, metabolism, excretion, and toxicity (ADMET). Heterocyclic compounds containing a nitrogen atom play a significant role in the search for new drugs. In this study, lipophilicity as well as other physicochemical, pharmacokinetic and toxicity properties affecting the bioavailability of the quinolone-1,4-quinone hybrids are presented. Lipophilicity was determined experimentally as well as theoretically using various computer programs. The tested compounds showed low values of experimental lipophilicity and its relationship with the type of 1,4-quinone moiety. Introduction of the nitrogen atom reduced the lipophilicity depending on the position at the 5,8-quinolinedione moiety. The bioavailability of the tested compounds was determined in silico using the ADMET parameters. The obtained parameters showed that most of the hybrids can be used orally and do not exhibit neurotoxic effects. Similarity analysis was used to examine the relationship between the ADMET parameters and experimental lipophilicity. The ability of hybrids to interact with biological targets was characterized by global reactivity descriptors. The molecular docking study showed that the hybrids can inhibit the BCL-2 protein. Full article
(This article belongs to the Special Issue Featured Papers in Biopharmaceutics)
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14 pages, 2513 KiB  
Article
Protective Effects of Choline against Inflammatory Cytokines and Characterization of Transport in Motor Neuron-like Cell Lines (NSC-34)
by Sana Latif and Young-Sook Kang
Pharmaceutics 2022, 14(11), 2374; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14112374 - 04 Nov 2022
Cited by 3 | Viewed by 1502
Abstract
Choline, a component of the neurotransmitter acetylcholine, is essential for nervous system functions, brain development, and gene expression. In our study, we investigated the protective effect and transport characteristics of choline in amyotrophic lateral sclerosis (ALS) model cell lines. We used the wild-type [...] Read more.
Choline, a component of the neurotransmitter acetylcholine, is essential for nervous system functions, brain development, and gene expression. In our study, we investigated the protective effect and transport characteristics of choline in amyotrophic lateral sclerosis (ALS) model cell lines. We used the wild-type (WT) motor neuron-like hybrid cell line (NSC-34/hSOD1WT) as a control and the mutant-type (MT; NSC-34/hSOD1G93A) as a disease model. The uptake of [3H]choline was time-, pH-, and concentration-dependent. [3H]Choline transport was sodium-dependent, and, upon pretreatment with valinomycin, induced membrane depolarization. Gene knockdown of Slc44a1 revealed that choline-like transporter 1 (CTL1) mediates the transport of choline. In NSC-34 cell lines, the specific choline transporter inhibitor, hemicholinium-3 demonstrated significant inhibition. Donepezil and nifedipine caused dose-dependent inhibition of [3H]choline uptake by the MT cell line with minimal half inhibitory concentration (IC50) values of 0.14 mM and 3.06 mM, respectively. Four-day pretreatment with nerve growth factor (NGF) resulted in an inhibitory effect on [3H]choline uptake. Choline exerted protective and compensatory effects against cytokines mediators. Hence, the choline transport system CLT1 may act as a potential target for the delivery of novel pharmacological drugs, and the combination of drugs with choline can help treat symptoms related to ALS. Full article
(This article belongs to the Special Issue Featured Papers in Biopharmaceutics)
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