Advances in Improving Drug Dissolution, Solubility, and Bioavailability

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: closed (31 January 2022) | Viewed by 5216

Special Issue Editor

Department of Physical Chemistry, Faculty of Pharmacy, Collegium Medicum of Bydgoszcz, Nicolaus Copernicus University in Toruń, Kurpińskiego 5, 85-950 Bydgoszcz, Poland
Interests: pharmacy; physical pharmacy; physical chemistry; biomaterials; environmental chemistry
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Special Issue Information

Dear Colleagues,

In recent years, many studies have focused on how to improve drug delivery and bioavailability. The increased interest in this field is associated with the development of various disciplines such as nanotechnology, crystal engineering, materials engineering, polymer science, and even 3D printing technology. Poor bioavailability of pharmaceuticals is often related to their low solubility or low dissolution rate. Overcoming this problem requires the introduction of significant structural changes in pharmaceutically active ingredients, such as amorphization or the addition of excipients acting as solubilizers (multicomponent crystals, pharmaceutical eutectics, etc.). Another important problem affecting poor drug bioavailability is their low cell membrane permeability. In this case, various types of drug carriers can be helpful, including those prepared using nanotechnological techniques. In addition, in many cases it is necessary to achieve controlled drug release, which involves reaching its optimal bioavailability. It is worth noting that theoretical methods such as QSPR, molecular dynamics, and quantum-chemical computations have been successfully used to improve drug delivery. Many research projects in this field consist in virtual screenings such as in silico modeling of co-crystallization and of interactions in multicomponent systems.

The purpose of the Special Issue “Advances in Improving Drug Dissolution, Solubility, and Bioavailability” is to present the latest research on the improvement of drug bioavailability, including all dosage forms and the results of modifying important drug physicochemical properties such as solubility, dissolution rate, and cell membrane permeability.

Dr. Maciej Przybyłek
Guest Editor

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Keywords

  • Bioavailability
  • Drug Delivery
  • Solubility
  • Dissolution Rate
  • Permeability
  • ADME
  • Pharmacokinetics
  • Biopharmaceutics Classification System
  • Cocrystals
  • Pharmaceutical Eutectics
  • Amorphous Drugs
  • Co-Amorphous Drug Formulations
  • Nutraceuticals
  • Nanomaterials
  • Cyclodextrins
  • Macromolecular Carriers
  • Micronization
  • Liquid Dosage Forms

Published Papers (2 papers)

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Research

15 pages, 4136 KiB  
Article
Study of Different Crystal Habits of Aprepitant: Dissolution and Material Attributes
by Satyajit R. Datir, Dinesh Kumar, Pradeep Kumar, Sanyog Jain, Arvind Kumar Bansal, Bhargavi Nallamothu, Samarth D. Thakore and Mrudula H. Bele
Appl. Sci. 2021, 11(12), 5604; https://0-doi-org.brum.beds.ac.uk/10.3390/app11125604 - 17 Jun 2021
Cited by 6 | Viewed by 3144
Abstract
In the present study, aprepitant (APT) was selected to find its suitable crystal habit, which can improve its existing poor dissolution and manufacturing processability. Solvents were screened out for solubility analysis of APT and further crystal habit modification. Solid-state characterization studies like powder [...] Read more.
In the present study, aprepitant (APT) was selected to find its suitable crystal habit, which can improve its existing poor dissolution and manufacturing processability. Solvents were screened out for solubility analysis of APT and further crystal habit modification. Solid-state characterization studies like powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and Fourier infrared spectroscopy (FTIR) distinguished that tabular crystal habit was generated from acetone (APT-AC) and long tabular crystal habit was generated from ethyl acetate (APT-EA). Kawakita analysis and powder flow property studies showed that APT-EA is cohesive, has poor flow property and low bulk density compared to APT-AC (p < 0.05). Heckel plots reflected that APT-EA shows higher fragmentation and particle rearrangement during the initial stages as indicated by the higher intercept values. Higher slopes in APT-EA and APT-AC confirmed better plasticity but lower yield pressure in APT-AC proved good plastic deformation compared to APT-EA (p < 0.05). The dissolution profile of the APT-EA was found to be better than that of APT-AC. Overall, it can be concluded that APT-AC crystal habit has a better flow rate, tensile strength, and plasticity whereas APT-EA has better dissolution. Full article
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15 pages, 1533 KiB  
Article
Design, Synthesis, and Cell Lines Studies of Oleanolic Acid—Hydrogen Sulfide Donor Hybrids
by Fenqin Zhao, Jinyu Li, Kexin Yue, Beibei Song, Erying Sun, Xinru Cheng, Jing Ma and Lin Yan
Appl. Sci. 2021, 11(8), 3364; https://0-doi-org.brum.beds.ac.uk/10.3390/app11083364 - 08 Apr 2021
Cited by 1 | Viewed by 1377
Abstract
In order to develop new oleanolic acid (OA) derivatives endowed with improved antitumor activities, for the first time, a number of new hybrid compounds were reported by combining OA or 3-oxooleanolic acid with appropriate H2S-donor moiety, coupled via a suitable linker. [...] Read more.
In order to develop new oleanolic acid (OA) derivatives endowed with improved antitumor activities, for the first time, a number of new hybrid compounds were reported by combining OA or 3-oxooleanolic acid with appropriate H2S-donor moiety, coupled via a suitable linker. The anti-tumor evaluation indicated that they exhibited excellent anti-cancer activities against the tested cancer cell lines. Moreover, 18d with 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione moiety as H2S donor and β-alanine as the linker, showed more potent cytotoxicity against the tested cancer cell lines than OA and 3-oxooleanolic acid, especially for A549 cells. Furthermore, the preferred compound, 18d, preferentially accumulates in cancer cells (13.6 μM) over the matched normal cells LO2 (>100 μM) in vitro. The improved antitumor activity of this hybrid was probably due to its H2S-releasing capability. Full article
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