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Pharmaceutical Development

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 May 2021) | Viewed by 14694

Special Issue Editor


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Guest Editor
Department of Science and Engineereing of Oxide Materials and Nanomaterials, Faculty of Applied Chemistry and Materials Science, Politehnica University of Bucharest, RO-011061 Bucharest, Romania
Interests: synthesis and characterization of nanobiomaterials; polymers; pharmaceutical nanotechnology; drug delivery; anti-biofilm surfaces; nanomodified surfaces; natural products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue will cover the latest research and development activities in the pharmacological industry by addressing the recent advances in the interdisciplinary research fields of drug development, drug delivery systems, and pharmaceutical biotechnology.

The pharmaceutical industry is faced with continuously emerging challenges such as difficulties in assessing toxicological profiles, years-long trials, and high costs. Recent trends focus on developing and promoting novel strategies for the processes of drug discovery and drug delivery.

Emergent approaches are concerned with novel drug delivery systems and smart drug delivery technologies, which are able to specifically target the sites of disease and release the drug in a controllable manner. The drug will further act by activating or inhibiting the function of a specific molecule, which will result in a beneficial therapeutic effect on the patient. Significant advantages of the smart drug delivery systems involve the reduced frequency of the dosage and the associated side effects and the more uniform effect of the drug.

A different direction in pharmaceutical sciences is pharmaceutical biotechnology, which studies the application of recombinant DNA technology, microbiology, genomics, proteomics, and industrial biotechnology. Furthermore, the application of biomarkers in the field of pharmaceutical development could enhance the efficiency of drugs by selecting the most appropriate patients using a specific mechanism, optimize the dosage, and provide earlier results for clinical development.

The subject of this Special Issue could represent a possible bridge between academia and industry that could lead to improvements in pharmacological development.

Topics:

  • Pharmaceutical formulation and manufacture;
  • Pharmacokinetics and pharmacodynamics;
  • Computer-assisted drug design;
  • Biopharmaceuticals;
  • Biomaterials in drug delivery;
  • Vaccine delivery systems;
  • Gene delivery systems;
  • Medical devices for drug delivery;
  • Advanced drug delivery systems and breakthrough therapies.

 

Assoc. Prof. Dr. Alexandru Mihai Grumezescu

Guest Editor

Manuscript Submission Information

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Keywords

  • Drug delivery
  • Drug targeting
  • Medical devices
  • Vaccine
  • Drug design
  • Pharmacokinetics
  • Pharmacodynamics

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Published Papers (3 papers)

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Research

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16 pages, 14322 KiB  
Article
The Influence of pH Values on the Rheological, Textural and Release Properties of Carbomer Polacril® 40P-Based Dental Gel Formulation with Plant-Derived and Synthetic Active Components
by Yuliia Maslii, Olena Ruban, Giedre Kasparaviciene, Zenona Kalveniene, Anna Materiienko, Liudas Ivanauskas, Agne Mazurkeviciute, Dalia M. Kopustinskiene and Jurga Bernatoniene
Molecules 2020, 25(21), 5018; https://doi.org/10.3390/molecules25215018 - 29 Oct 2020
Cited by 33 | Viewed by 4704
Abstract
The physicochemical properties, especially pH value of dental medicines, have significant influence on the health of oral cavity tissues. The pH of formulations should correspond to the value of saliva pH (5.5–8.0). For carbomer-based gels, the required pH value is obtained by neutralizing [...] Read more.
The physicochemical properties, especially pH value of dental medicines, have significant influence on the health of oral cavity tissues. The pH of formulations should correspond to the value of saliva pH (5.5–8.0). For carbomer-based gels, the required pH value is obtained by neutralizing them with alkaline components, which leads to their structuring (thickening). This affects the physical properties of the gel, its residence time at the application site and the rate of release of active pharmaceutical ingredient. Therefore, the main purpose of this study is to evaluate the rheological, textural, and biopharmaceutical properties of Carbomer Polacril® 40P-based dental gel depending on the pH value. Evaluation of the rheological properties of gel preparations were performed by measuring the structural viscosity of the samples as a function of pH and temperature. The textural properties of the gel were evaluated by performing tests regarding back extrusion and spreadability. Carbomer Polacril® 40P-based gels haven’t shown noticeable thixotropic behavior, and were characterized by plastic flow in the whole studied pH range. The structural viscosity at the selected average pH value hasn’t differed at storage (25 °C) and application (37 °C) temperature. Texture studies of dental gels have shown a strong correlation with rheoparameters. Their rheological behavior and textural properties haven’t changed significantly between the pH range of 5.5–6.6. The relatively narrow range of working pH values does not affect the change in the viscosity of the preparation significantly and, consequently, does not affect the release of APIs from the developed Carbomer Polacril® 40P-based dental gel. Full article
(This article belongs to the Special Issue Pharmaceutical Development)
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18 pages, 4421 KiB  
Article
Melanogenic Inhibition and Toxicity Assessment of Flavokawain A and B on B16/F10 Melanoma Cells and Zebrafish (Danio rerio)
by Nurshafika Mohd Sakeh, Nurliyana Najwa Md Razip, Farah Idayu Mohd Ma’in, Mohammad Nazri Abdul Bahari, Naimah Latif, Muhammad Nadeem Akhtar, Zetty Norhana Balia Yusof and Syahida Ahmad
Molecules 2020, 25(15), 3403; https://doi.org/10.3390/molecules25153403 - 28 Jul 2020
Cited by 9 | Viewed by 4112
Abstract
Excessive production of melanin implicates hyperpigmentation disorders. Flavokawain A (FLA) and flavokawain B (FLB) have been reported with anti-melanogenic activity, but their melanogenic inhibition and toxicity effects on the vertebrate model of zebrafish are still unknown. In the present study, cytotoxic as well [...] Read more.
Excessive production of melanin implicates hyperpigmentation disorders. Flavokawain A (FLA) and flavokawain B (FLB) have been reported with anti-melanogenic activity, but their melanogenic inhibition and toxicity effects on the vertebrate model of zebrafish are still unknown. In the present study, cytotoxic as well as melanogenic effects of FLA and FLB on cellular melanin content and tyrosinase activity were evaluated in α-MSH-induced B16/F10 cells. Master regulator of microphthalmia-associated transcription factor (Mitf) and the other downstream melanogenic-related genes were verified via quantitative real time PCR (qPCR). Toxicity assessment and melanogenesis inhibition on zebrafish model was further observed. FLA and FLB significantly reduced the specific cellular melanin content by 4.3-fold and 9.6-fold decrement, respectively in α-MSH-induced B16/F10 cells. Concomitantly, FLA significantly reduced the specific cellular tyrosinase activity by 7-fold whilst FLB by 9-fold. The decrement of melanin production and tyrosinase activity were correlated with the mRNA suppression of Mitf which in turn down-regulate Tyr, Trp-1 and Trp-2. FLA and FLB exhibited non-toxic effects on the zebrafish model at 25 and 6.25 µM, respectively. Further experiments on the zebrafish model demonstrated successful phenotype-based depigmenting activity of FLA and FLB under induced melanogenesis. To sum up, our findings provide an important first key step for both of the chalcone derivatives to be further studied and developed as potent depigmenting agents. Full article
(This article belongs to the Special Issue Pharmaceutical Development)
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Review

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22 pages, 1738 KiB  
Review
Shortcut Approaches to Substance Delivery into the Brain Based on Intranasal Administration Using Nanodelivery Strategies for Insulin
by Toshihiko Tashima
Molecules 2020, 25(21), 5188; https://doi.org/10.3390/molecules25215188 - 7 Nov 2020
Cited by 42 | Viewed by 4826
Abstract
The direct delivery of central nervous system (CNS) drugs into the brain after administration is an ideal concept due to its effectiveness and non-toxicity. However, the blood–brain barrier (BBB) prevents drugs from penetrating the capillary endothelial cells, blocking their entry into the brain. [...] Read more.
The direct delivery of central nervous system (CNS) drugs into the brain after administration is an ideal concept due to its effectiveness and non-toxicity. However, the blood–brain barrier (BBB) prevents drugs from penetrating the capillary endothelial cells, blocking their entry into the brain. Thus, alternative approaches must be developed. The nasal cavity directly leads from the olfactory epithelium to the brain through the cribriform plate of the skull bone. Nose-to-brain drug delivery could solve the BBB-related repulsion problem. Recently, it has been revealed that insulin improved Alzheimer’s disease (AD)-related dementia. Several ongoing AD clinical trials investigate the use of intranasal insulin delivery. Related to the real trajectory, intranasal labeled-insulins demonstrated distribution into the brain not only along the olfactory nerve but also the trigeminal nerve. Nonetheless, intranasally administered insulin was delivered into the brain. Therefore, insulin conjugates with covalent or non-covalent cargos, such as AD or other CNS drugs, could potentially contribute to a promising strategy to cure CNS-related diseases. In this review, I will introduce the CNS drug delivery approach into the brain using nanodelivery strategies for insulin through transcellular routes based on receptor-mediated transcytosis or through paracellular routes based on escaping the tight junction at the olfactory epithelium. Full article
(This article belongs to the Special Issue Pharmaceutical Development)
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