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Pharmaceutics
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Strategies for Enhancing the Bioavailability of Poorly Soluble Drugs, 2nd...
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Strategies for Enhancing the Bioavailability of Poorly Soluble Drugs, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (20 September 2023) | Viewed by 3784

Special Issue Editor

Dr. Rodolfo Pinal

E-Mail Website
Guest Editor
Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, West Lafayette, IN 47906, USA
Interests: solubility; solubilization; amorphous; cocrystals; extrusion; polymers; excipients; films
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioavailability is crucial for the successful development of pharmaceutical products, be it a novel drug or a new formulation of an existing drug. The interplay between drug solubility/solubilization and bioavailability is particularly interesting and relevant from both scientific and commercial standpoints, respectively. Bioavailability is the result of interweaving underlying physical and physiological phenomena. Accordingly, progress toward enhancing the bioavailability of poorly soluble drugs entails a multi-disciplinary approach, involving, among other things, physical characterization of solids, solution chemistry, pharmaceutical excipients, pharmaceutical processing, drug transporters and absorption enhancers. With the advent of patient-centric formulations, it is more important than ever to gather published sources detailing the latest advances toward a fundamental understanding of the bioavailability–solubility relationship from the various perspectives of sub-disciplines involved in this important pharmaceutical subject. This Special Issue of Pharmaceutics is brought to you with that aim.

Dr. Rodolfo Pinal
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.

Keywords

  • absorption enhancers
  • additive manufacturing
  • amorphous
  • co-crystals
  • co-processed excipients
  • extrusion
  • lipid formulations
  • lipid nanoparticles
  • pharmaceutical material science
  • particle engineering
  • patient-centric
  • polymers
  • polymorphs
  • self-emulsifying delivery systems
  • solid dispersions
  • solubility
  • solubilization
  • spray-drying
  • supersaturation
  • transporters

Published Papers (3 papers)

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Research

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25 pages, 3429 KiB  
Article
Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity
by Ewa Garbiec, Natalia Rosiak, Przemysław Zalewski, Lidia Tajber and Judyta Cielecka-Piontek
Pharmaceutics 2023, 15(12), 2653; https://doi.org/10.3390/pharmaceutics15122653 - 21 Nov 2023
Cited by 4 | Viewed by 987
Abstract
Genistein, an isoflavone known for its antioxidant and antidiabetic effects, suffers from the drawback of low solubility. To overcome this limitation, co-amorphous systems were synthesized by incorporating amino acids that were chosen through computational methods. The confirmation of the amorphous state of lysine [...] Read more.
Genistein, an isoflavone known for its antioxidant and antidiabetic effects, suffers from the drawback of low solubility. To overcome this limitation, co-amorphous systems were synthesized by incorporating amino acids that were chosen through computational methods. The confirmation of the amorphous state of lysine and arginine-containing systems was ascertained by X-ray powder diffraction. Subsequently, the characterization of these systems was extended by employing thermo-gravimetry, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanning electron microscopy. The investigation also included an assessment of the physical stability of the samples during storage. The apparent solubility of the systems was studied in an aqueous medium. To evaluate the in vitro permeability through the gastrointestinal tract, the parallel artificial membrane permeability assay was employed. The biological properties of the systems were assessed with regard to their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl and cupric ion-reducing antioxidant capacity assays, as well as their ability to inhibit α-glucosidase. The systems’ glass transition temperatures were determined, and their homogeneity confirmed via differential scanning calorimetry analysis, while Fourier-transform infrared spectroscopy analysis provided data on molecular interactions. Stability was maintained for the entire 6-month storage duration. The co-amorphous system containing lysine displayed the most pronounced apparent solubility improvement, as well as a significant enhancement in antioxidant activity. Notably, both systems demonstrated superior α-glucosidase inhibition relative to acarbose, a standard drug for managing type 2 diabetes. The results indicate that co-amorphous systems with lysine and arginine have the potential to significantly enhance the solubility and biological activity of genistein. Full article
(This article belongs to the Special Issue Strategies for Enhancing the Bioavailability of Poorly Soluble Drugs, 2nd Edition)
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16 pages, 1702 KiB  
Article
Tunable Drug Release Rate Using Modular Oral Dosage Forms
by Mario A. Cano-Vega, Laura M. Arango-Salazar and Rodolfo Pinal
Pharmaceutics 2023, 15(7), 1905; https://doi.org/10.3390/pharmaceutics15071905 - 08 Jul 2023
Viewed by 1065
Abstract
Oral dosage forms with adjustable drug release profiles were prepared using progesterone (PGR) as a poorly-soluble model drug. The dosage forms were made as stack assemblies of functional modules. The modules were made as PGR-carrying HPMC films cut into wafer-like circular pieces. Two [...] Read more.
Oral dosage forms with adjustable drug release profiles were prepared using progesterone (PGR) as a poorly-soluble model drug. The dosage forms were made as stack assemblies of functional modules. The modules were made as PGR-carrying HPMC films cut into wafer-like circular pieces. Two types of modules were used in the study; one exhibited comparatively fast drug release and the other slow release. The fast vs. slow release of each type of film utilized resulted from the grade of HPMC used in each case. Drug loading in the assembly was controlled through the total number of modules. By adjusting the proportions of the two types of modules, it is possible to fine-tune the drug release rate of the multi-layer assemblies to a wide range of profiles, bracketed between a high and low end, corresponding to the inherently fastest or slowest release obtainable with the specific materials and procedures employed. This procedure is suitable for adjusting the spring-and-parachute parameters for enhancing/optimizing the bioavailability of poorly-soluble drugs, and for developing patient-centric formulations. Full article
(This article belongs to the Special Issue Strategies for Enhancing the Bioavailability of Poorly Soluble Drugs, 2nd Edition)
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Review

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28 pages, 2088 KiB  
Review
Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
by Madan Sai Poka, Marnus Milne, Anita Wessels and Marique Aucamp
Pharmaceutics 2023, 15(11), 2557; https://doi.org/10.3390/pharmaceutics15112557 - 30 Oct 2023
Viewed by 1327
Abstract
Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs [...] Read more.
Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs have been created in recent years, but these polymer-based SDs exhibit the major drawback of recrystallisation upon storage. Also, the use of high-molecular-weight polymers with increased chain lengths brings forth problems such as increased viscosity and unnecessary bulkiness in the resulting dosage form. An ideal SD carrier should be hydrophilic, non-hygroscopic, have high hydrogen-bonding propensity, have a high glass transition temperature (Tg), and be safe to use. This review discusses sugars and polyols as suitable carriers for SDs, as they possess several ideal characteristics. Recently, the use of low-molecular-weight excipients has gained much interest in developing SDs. However, there are limited options available for safe, low molecular excipients, which opens the door again for sugars and polyols. The major points of this review focus on the successes and failures of employing sugars and polyols in the preparation of SDs in the past, recent advances, and potential future applications for the solubility enhancement of poorly water-soluble drugs. Full article
(This article belongs to the Special Issue Strategies for Enhancing the Bioavailability of Poorly Soluble Drugs, 2nd Edition)
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