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Pharmaceuticals
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Pharmaceutical Formulation Characterization Design
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Pharmaceutical Formulation Characterization Design

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 7045

Special Issue Editors

Dr. Tamás Sovány

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Guest Editor
Institute of Pharmaceutical Technology and Regulatoy Affairs, University of Szeged, Eötvös u.6., 6720 Szeged, Hungary
Interests: solid dosage forms; tablets; quality by design; factorial design; artificial neural network
Special Issues, Collections and Topics in MDPI journals
Dr. Katalin Kristó

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Guest Editor
Institute of Pharmaceutical Technology and Regulatoy Affairs, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary
Interests: buccal polymer films; mucoadhesion; proteins; quality by design; permeation enhancing
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues,

This Special Issue in "Pharmaceuticals" is dedicated to reporting the latest scientific results in the field of "Formulation Characterization Design". At present, it is very important that, before the industrial production of pharmaceuticals, a given pharmaceutical form is extensively tested, which includes various structural tests, physical tests, and pharmacokinetic tests. It is necessary to find out whether there is any change in the active ingredient during pharmaceutical technological processes and whether this could influence the development of the effect. It is necessary to understand the relationships between different structural properties, the dissolution profile, and effect development in order to be able to design medicines more efficiently based on new knowledge. Appropriate planning is also very important, and this can be achieved primarily through risk analysis, the Quality by Design (QbD) approach, and the use of factorial experimental design (DoE). It is possible to determine the design space, which provides accurate information provides information about the Critical Process Parameter (CPP) values, within which the product with the quality target product profile (QTPP) will be suitable. Based on these, we can gain new knowledge and connections that are essential for efficient production later on. This Special Issue primarily publishes results related to the above-mentioned topic or some part of it, mainly in the field of solid dosage form formulation or intermediate products that can be used in them.

Dr. Tamás Sovány
Dr. Katalin Kristó
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. Pharmaceuticals 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

  • quality by design
  • factorial design
  • design space
  • solid dosage forms
  • risk assessment
  • critical process parameters
  • quality target product profile

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Published Papers (7 papers)

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Research

18 pages, 933 KiB  
Article
Formulation, Quality Control and Stability Study of Pediatric Oral Dextrose Gel
by Edouard Lamy, Caroline Orneto, Oumil Her Abdou Ali, Lyna Kireche, Fanny Mathias, Cyrielle Bouguergour, Florence Peyron, Nicolas Primas, Christophe Sauzet, Philippe Piccerelle, Anne-Marie Maillotte, Veronique Brevaut-Malaty, Pascal Rathelot, Patrice Vanelle and Christophe Curti
Pharmaceuticals 2025, 18(2), 204; https://doi.org/10.3390/ph18020204 - 3 Feb 2025
Viewed by 266
Abstract
Background/Objective: Little information is available on the stability and quality controls of compounded 40% dextrose gel required to ensure its safe use in the treatment and prevention of neonatal hypoglycemia. Whether its efficacy relies on buccal absorption also remains uncertain. This study investigates [...] Read more.
Background/Objective: Little information is available on the stability and quality controls of compounded 40% dextrose gel required to ensure its safe use in the treatment and prevention of neonatal hypoglycemia. Whether its efficacy relies on buccal absorption also remains uncertain. This study investigates the stability, microbiological safety, rheological properties and dextrose diffusion of a compounded 40% oral dextrose gel, ensuring it can be widely compounded and stored for clinical use. Methods: A 40% dextrose gel compounded with anhydrous dextrose, carboxymethylcellulose, citric acid, sorbic acid and sterile water was subjected to quality control measures including a dextrose content assay, degradation product analysis, microbiological testing and preservative efficacy. Stability studies were conducted at refrigerated (4–8 °C) and ambient temperatures for 7 days and 3 months, respectively. Rheological properties were assessed, and dextrose permeation was measured through an artificial membrane model that mimics a biological membrane. Results: The compounded gel demonstrated stability for up to 7 days at ambient temperature and 90 days when refrigerated. The dextrose content remained within the acceptable range (90–110%) and microbiological tests confirmed compliance with safety standards. The gel exhibited the consistent rheological properties and shear-thinning behavior appropriate for oral mucosal administration. In vitro permeation studies showed no evidence of dextrose diffusion with a long lag time followed by a low steady-state permeation flux. Conclusions: This study validates the compounding process of a stable 40% oral dextrose gel formulation for neonatal hypoglycemia management, which meets quality control criteria and can be safely administered in clinical practice, offering a cost-effective and safe alternative for neonatal care. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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24 pages, 7156 KiB  
Article
Nose-to-Brain Delivery of Chitosan-Grafted Leciplexes for Promoting the Bioavailability and Antidepressant Efficacy of Mirtazapine: In Vitro Assessment and Animal Studies
by Amani M. El Sisi, Essam M. Eissa, Ahmed H. E. Hassan, Marina A. Bekhet, Fatma I. Abo El-Ela, Eun Joo Roh, Rasha M. Kharshoum and Adel A. Ali
Pharmaceuticals 2025, 18(1), 46; https://doi.org/10.3390/ph18010046 - 3 Jan 2025
Viewed by 620
Abstract
Background/Objectives: Mirtazapine (MRZ) is a psychotropic drug prescribed to manage serious sorts of depression. By virtue of its extensive initial-pass metabolic process with poor water solubility, the ultimate bioavailability when taken orally is a mere 50%, necessitating repeated administration. The current inquiry [...] Read more.
Background/Objectives: Mirtazapine (MRZ) is a psychotropic drug prescribed to manage serious sorts of depression. By virtue of its extensive initial-pass metabolic process with poor water solubility, the ultimate bioavailability when taken orally is a mere 50%, necessitating repeated administration. The current inquiry intended to fabricate nose-to-brain chitosan-grafted cationic leciplexes of MRZ (CS-MRZ-LPX) to improve its pharmacokinetic weaknesses and boost the pharmacodynamics aspects. Methods: Primarily, MRZ-loaded leciplexes (MRZ-LPXs) were fabricated and tailored employing a central composite design (CCD). Vesicle diameter size (VS), entrapment efficiency (EE %), cumulative MRZ release percentage (CMRZR %), and total quantity penetrating after twenty-four hours (Q24) were the four parameters assessed. Then, the determined optimum formulation was coated with chitosan (CS-MRZ-LPX) and utilized in pharmacodynamics investigations and in vivo biologic distribution studies in Wistar male rats. Results: The customized MRZ-LPX formulation had a diameter size of 186.2 ± 3.5 nm and drug EE of 45.86 ± 0.76%. Also, the tailored MRZ-LPX formulation had a cumulative amount of MRZ released of 76.66 ± 3.06% and the total Q24 permeated was 383.23 ± 13.08 µg/cm2. Intranasal delivery of the tailored CS-MRZ-LPX revealed notably superior pharmacokinetic attributes inside the brain and circulation compared to the orally administered MRZ suspension and the intranasal free drug suspension (p < 0.05); the relative bioavailability was 370.9% and 385.6% for plasma and brain, respectively. Pharmacodynamics’ and immunohistopathological evaluations proved that optimum intranasal CS-MRZ-LPX boosted antidepressant activity compared to the oral and free nasal drug administration. Conclusions: CS-MRZ-LPX tailored formulation can potentially be regarded as a prospective nano platform to boost bioavailability and enhance pharmacodynamics efficacy. Ultimately, intranasal CS-MRZ-LPX can be considered a promising avenue for MRZ targeted brain delivery as an antidepressant. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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18 pages, 5994 KiB  
Article
Study of the Effect of Temperature on the Production of Carrageenan-Based Buccal Films and Optimization of the Process Parameters
by Katalin Kristó, Anahita Sangestani, Alharith A. A. Hassan, Hala Rayya, Krisztián Pamlényi, András Kelemen and Ildikó Csóka
Pharmaceuticals 2024, 17(12), 1737; https://doi.org/10.3390/ph17121737 - 22 Dec 2024
Viewed by 800
Abstract
Background/Objectives: Films in the mouth offer a promising alternative drug delivery system for oral administration, with several advantages over traditional oral formulations. Furthermore, their non-invasive nature and easy administration make them conducive to increasing patient compliance. The use of active agents in these [...] Read more.
Background/Objectives: Films in the mouth offer a promising alternative drug delivery system for oral administration, with several advantages over traditional oral formulations. Furthermore, their non-invasive nature and easy administration make them conducive to increasing patient compliance. The use of active agents in these films can further improve their drug delivery properties, making them an even more useful drug delivery system. Methods: In this research, carrageenan was used as a polymer, while glycerine was added as a plasticizer, furthermore, lidocaine hydrochloride and diclofenac sodium were used as the active agents. The prepared films were characterized by analytical techniques. Results: The results showed that glycerine reduced the mucoadhesivity and breaking hardness of the films and increasing the temperature made the films brittle. These results are also confirmed by the statistical analysis. Based on the FTIR results, glycerine can be used in films without structural changes. Conclusions: Based on the findings, films prepared from a solution with a concentration of 1.5% carrageenan and 1.5% glycerine at 70 °C are suitable as a drug delivery system for use on the buccal mucosa when combined with active agents. Carrageenan was successfully used as a carrier for two different types of active agents. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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20 pages, 2396 KiB  
Article
Modelling of Cetylpyridinium Chloride Availability in Complex Mixtures for the Prediction of Anti-Microbial Activity Using Diffusion Ordered Spectroscopy, Saturation Transfer Difference and 1D NMR
by Cameron Robertson, Sayoni Batabyal, Darren Whitworth, Tomris Coban, Angharad Smith, Alessandra Montesanto, Robert Lucas and Adam Le Gresley
Pharmaceuticals 2024, 17(12), 1570; https://doi.org/10.3390/ph17121570 - 22 Nov 2024
Viewed by 1077
Abstract
Background/Objectives: A range of NMR techniques, including diffusion ordered spectroscopy (DOSY) were used to characterise complex micelles formed by the anti-microbial cationic surfactant cetylpyridium chloride and to quantify the degree of interaction between cetylpyridium chloride and hydroxyethyl cellulose in a variety of commercially [...] Read more.
Background/Objectives: A range of NMR techniques, including diffusion ordered spectroscopy (DOSY) were used to characterise complex micelles formed by the anti-microbial cationic surfactant cetylpyridium chloride and to quantify the degree of interaction between cetylpyridium chloride and hydroxyethyl cellulose in a variety of commercially relevant formulations as a model for the disk retention assay. Methods: This NMR-derived binding information was then compared with the results of formulation analysis by traditional disk retention assay (DRA) and anti-microbial activity assays to assess the suitability of these NMR techniques for the rapid identification of formulation components that could augment or retard antimicrobial activity DRA. Results: NMR showed a strong ability to predict anti-microbial activity for a diverse range of formulations containing cetylpyridinium chloride (CPC). Conclusions: This demonstrates the value of this NMR-based approach as a rapid, relatively non-destructive method for screening commercial experimental anti-microbial formulations for efficacy and further helps to understand the interplay of excipients and active ingredients. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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10 pages, 1465 KiB  
Article
Optical Microscopy as a Tool for Assessing Parenteral Nutrition Solution Stability: A Proof of Concept
by Luis Otero-Millán, Brais Bea-Mascato, Jose Luis Legido Soto, María Carmen Martín de la Cruz, Noemi Martínez-López-De-Castro and Natividad Lago-Rivero
Pharmaceuticals 2024, 17(10), 1330; https://doi.org/10.3390/ph17101330 - 5 Oct 2024
Viewed by 833
Abstract
Background/Objectives: Parenteral nutrition (PN) is used when enteral feeding is not possible. It is a complex mixture of nutrients that must meet a patient’s needs but can face stability issues, such as lipid emulsion destabilisation and precipitate formation. Stability studies are complex, [...] Read more.
Background/Objectives: Parenteral nutrition (PN) is used when enteral feeding is not possible. It is a complex mixture of nutrients that must meet a patient’s needs but can face stability issues, such as lipid emulsion destabilisation and precipitate formation. Stability studies are complex, and the methodologies used are very varied in the literature. In addition, many studies are outdated and use outdated components. This study conducts a stability analysis of PN solutions using optical microscopy. Methods: Samples were prepared according to clinical practice standards and previous studies. We used a counting chamber for optical microscopic observations and different storage conditions (RT, 4 °C 1–14 days). Results: Precipitates larger than 5 µm were found in 8 out of 14 samples after 14 days of storage at room temperature, and none were observed in refrigerated samples. More lipid globules larger than 5 µm were detected in samples stored at room temperature than in those stored in a refrigerator after 14 days. Additionally, the number of large globules generally increased from day 1 to day 14 in most samples. Conclusions: The observed precipitates were probably calcium oxalate crystals, the formation of which is possible in PN but is not expected under the usual storage conditions in a hospital environment. Prolonged storage time and storage at room temperature increases the formation of these precipitates. These findings highlight the importance of using filters during both the preparation and administration of PN to prevent large particles from reaching patients. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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18 pages, 1778 KiB  
Article
In Vitro Study of Cyano-Phycocyanin Release from Hydrogels and Ex Vivo Study of Skin Penetration
by Daiva Galinytė, Jurga Bernatoniene, Modestas Žilius, Kristina Rysevaitė-Kyguolienė, Arūnas Savickas, Jūratė Karosienė, Vitalis Briedis, Dainius Haroldas Pauža and Nijolė Savickienė
Pharmaceuticals 2024, 17(9), 1224; https://doi.org/10.3390/ph17091224 - 17 Sep 2024
Viewed by 1388
Abstract
Background: This study explored the most suitable materials for incorporating cyano-phycocyanin (C-PC) into hydrogels, focusing on maintaining the C-PC’s long-term structural integrity and stabilityNext, the release of C-PC from the hydrogels and its skin penetration were investigated. Methods: A series of 1% ( [...] Read more.
Background: This study explored the most suitable materials for incorporating cyano-phycocyanin (C-PC) into hydrogels, focusing on maintaining the C-PC’s long-term structural integrity and stabilityNext, the release of C-PC from the hydrogels and its skin penetration were investigated. Methods: A series of 1% (w/w) C-PC hydrogels was prepared using various gelling agents and preservatives. Spectrophotometric measurements compared the amount of C-PC in the hydrogels to the initially added amount. After selecting the most suitable gelling agent and preservative, two C-PC hydrogels, with and without propylene glycol (PG) (Sigma-Aldrich, St. Louis, MO, USA), were produced for further testing. In vitro release studies utilized modified Franz-type diffusion cells, while ex vivo skin-permeation studies employed Bronaugh-type cells and human skin. Confocal laser scanning microscopy analyzed C-PC accumulation in the skin. Results: The findings demonstrated that sodium alginate (Sigma-Aldrich, St. Louis, MO, USA), hydroxyethyl cellulose (HEC) (Sigma-Aldrich, St. Louis, MO, USA), and SoligelTM (Givaudan, Vernier, Switzerland) are effective biopolymers for formulating hydrogels while maintaining C-PC stability. After 6 h, C-PC release from the hydrogel containing PG was approximately 10% or 728.07 (±19.35) μg/cm2, significantly higher than the nearly 7% or 531.44 (±26.81) μg/cm2 release from the hydrogel without PG (p < 0.05). The ex vivo qualitative skin-permeation study indicated that PG enhances C-PC penetration into the outermost skin layer. Conclusion: PG’s ability to enhance the release of C-PC from the hydrogel, coupled with its capacity to modify the skin barrier ex vivo, facilitates the penetration of C-PC into the stratum corneum. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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32 pages, 7235 KiB  
Article
pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy
by Essam M. Eissa, Amani M. El Sisi, Marina A. Bekhet, Fatma I. Abo El-Ela, Rasha M. Kharshoum, Adel A. Ali, Majed Alrobaian and Ahmed M. Abdelhaleem Ali
Pharmaceuticals 2024, 17(8), 978; https://doi.org/10.3390/ph17080978 - 24 Jul 2024
Cited by 2 | Viewed by 1703
Abstract
The present research emphasizes fabrication alongside the assessment of an innovative nano-vesicular membranous system known as invasomes (NVMs) laden with Mirtazapine for rectal administration. This system could circumvent the confines of orally administered counterparts regarding dose schedules and bioavailability. Mirtazapine invasomes were tailored [...] Read more.
The present research emphasizes fabrication alongside the assessment of an innovative nano-vesicular membranous system known as invasomes (NVMs) laden with Mirtazapine for rectal administration. This system could circumvent the confines of orally administered counterparts regarding dose schedules and bioavailability. Mirtazapine invasomes were tailored by amalgamating phospholipid, cineole, and ethanol through a thin-film hydration approach rooted in the Box–Behnken layout. Optimization of composition parameters used to fabricate desired NVMs’ physicochemical attributes was undertaken using the Design-Expert® program. The optimal MRZ-NVMs were subsequently transformed to a pH-triggered in situ rectal gel followed by animal pharmacodynamic and pharmacokinetic investigations relative to rectal plain gel and oral suspension. The optimized NVMs revealed a diameter size of 201.3 nm, a z potential of −28.8 mV, an entrapment efficiency of 81.45%, a cumulative release within 12 h of 67.29%, and a cumulative daily permeated quantity of 468.68 µg/cm2. Compared to the oral suspension, pharmacokinetic studies revealed a 2.85- and 4.45-fold increase in calculated rectal bioavailability in circulation and brain, respectively. Pharmacodynamic and immunohistopathology evaluations exposed superior MRZ-NVMs attributed to the orally administered drug. Consequently, rectal MRZ-NVMs can potentially be regarded as a prospective nanoplatform with valuable pharmacokinetics and tolerability assets. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation Characterization Design)
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