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Pharmaceutics
Special Issues
Recent Advances in Oral Solid Dosages
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Recent Advances in Oral Solid Dosages

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

Deadline for manuscript submissions: closed (31 July 2023) | Viewed by 12197

Special Issue Editors

Prof. Dr. ‪Dumitru Lupuliasa

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Guest Editor
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Interests: pharmaceutical forms manufacturing; drug preformulation and formulation; drug release; biopharmaceutical charcterization
Special Issues, Collections and Topics in MDPI journals
Dr. Anca Lucia Pop

E-Mail Website1 Website2
Guest Editor
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Interests: nutritional evaluation; nutritional biomarkers; practical nutrition; metabolic disease; diabetes
Special Issues, Collections and Topics in MDPI journals
Dr. Emma Adriana Ozon

E-Mail Website1 Website2
Guest Editor
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Interests: drug design; development, optimization, and manufacturing of pharmaceutical products; pre- and post-compression parameters for solid dosage forms; preformulating studies on pharmaceuticals; physico-chemical characterization of materials; cyclodextrin inclusion complexes; drug delivery systems; pharmaceutical processes; drug release profiles; quality of pharmaceutical forms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Worldwide, oral solid dosages, ranging from conventional to innovative systems, are the most utilized pharmaceutical forms. Due to their increased adherence among patients, oral solid dosages are at the center of multiple types of research, being the most studied pharmaceutical products. As pharmaceutical technology is continuously progressing through the development of new excipients and new manufacturing techniques, further studies should be performed to improve the actual state of the drug market. In all stages of the solid dosage development process, many factors should be considered, and several challenges must be addressed. Through the appropriate optimization of the preformulation, formulation and manufacturing processes of solid dosages, many limitations, such as poor drug stability, release, or bioavailability, can be overcome. Oral solid dosages include a great variety of formulations, and it is essential to establish a suitable system for each active ingredient as a function of its behavior and physicochemical properties, in order to achieve the high performance of the final product.

Prof. Dr. ‪Dumitru Lupuliasa
Dr. Anca Lucia Pop
Dr. Emma Adriana Ozon
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. 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

  • preformulation studies
  • oral solid dosages development
  • pharmaceutical formulation
  • food supplements formulation
  • direct compression
  • tablets
  • oral powders
  • hot-melt extrusion
  • 3D drug manufacturing
  • oral nano pharmaceuticals
  • solid dosages stability
  • release kinetics
  • kinetics and pharmacodynamics in oral forms
  • oral and gastrointestinal absorption barrier in oral forms
  • the influence of the oral and gastrointestinal microbiota on oral pharmaceutical forms

Published Papers (7 papers)

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Research

18 pages, 3145 KiB  
Article
The Study of the Cytotoxicity, Proliferative and Microbiological Activity of the Medicated Chewing Gum with Ascorbic Acid and Lysozyme Hydrochloride Using Different Culture of Cells
by Yuliia Maslii, Liudmyla Garmanchuk, Olena Ruban, Taisa Dovbynchuk, Nataliia Herbina, Giedre Kasparaviciene and Jurga Bernatoniene
Pharmaceutics 2023, 15(7), 1894; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15071894 - 5 Jul 2023
Viewed by 1395
Abstract
Medicated chewing gum with lysozyme hydrochloride and ascorbic acid as active pharmaceutical ingredients was developed for application in dentistry. The aim of this research was to study the cytotoxicity, proliferative, and microbiological activities of the active ingredients in different types of cell cultures. [...] Read more.
Medicated chewing gum with lysozyme hydrochloride and ascorbic acid as active pharmaceutical ingredients was developed for application in dentistry. The aim of this research was to study the cytotoxicity, proliferative, and microbiological activities of the active ingredients in different types of cell cultures. The preclinical study of active pharmaceutical ingredients and their combinations was carried out using culture lines such as HepG2 (human hepatocarcinoma cells), Hek293 (human embryonic kidney cells), and MAEC (mouse aortic endothelial cells). MTT assays were used to analyse cytotoxicity and proliferative activity, while the state of antioxidant protection was assessed by the content of sulfhydryl groups and catalase activity. The determination of lipid peroxidation products was based on the level of TBA-active products. As a microbiological model for studying the effect of the developed dental medicine on the ability of the oral cavity microorganisms to form biofilms, the following strains were used: Streptococcus mutans, Staphylococcus aureus, Staphylococcus epidermidis, Lactobacillus plantarum, and Candida albicans. The optical density of the formed biofilm was evaluated by the intensity of the experimental sample’s colour on a StatFax 303 Plus photometer at a wavelength of 630 nm. The combination of ascorbic acid and lysozyme hydrochloride in the established concentrations (20 mg and 10 mg per 1 gum, respectively) resulted in a slight stimulation of cell proliferation without any toxic effects and increased antioxidant protection, preventing the development of oxidative stress. It was found that, in contrast to the separately used active substances, the combination of lysozyme hydrochloride and ascorbic acid inhibits the biofilm formation of all studied microorganisms and shows the ability to destroy diurnal biofilms of L. plantarum and fungi of the genus Candida, indicating potentiation and summation of the active pharmaceutical ingredients’ composition effects in the developed dental medicine. Due to the observed positive pharmacological and microbiological action, the combination of lysozyme hydrochloride and ascorbic acid in the medicated chewing gum serves as a promising tool for the prevention and treatment of infectious and inflammatory diseases of the periodontium and mucous membranes and the prevention of caries. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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25 pages, 5444 KiB  
Article
In Vivo Acute Toxicity and Immunomodulation Assessment of a Novel Nutraceutical in Mice
by Tatiana Onisei, Bianca-Maria Tihăuan, Georgiana Dolete, Mădălina Axinie (Bucos), Manuela Răscol and Gheorghița Isvoranu
Pharmaceutics 2023, 15(4), 1292; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15041292 - 20 Apr 2023
Viewed by 1120
Abstract
Achieving and maintaining a well-balanced immune system has righteously become an insightful task for the general population and an even more fundamental goal for those affected by immune-related diseases. Since our immune functions are indispensable in defending the body against pathogens, diseases and [...] Read more.
Achieving and maintaining a well-balanced immune system has righteously become an insightful task for the general population and an even more fundamental goal for those affected by immune-related diseases. Since our immune functions are indispensable in defending the body against pathogens, diseases and other external attacks, while playing a vital role in maintaining health and modulating the immune response, we require an on-point grasp of their shortcoming as a foundation for the development of functional foods and novel nutraceuticals. Seeing that immunoceuticals are considered effective in improving immune functions and reducing the incidence of immunological disorders, the main focus of this study was to assess the immunomodulatory properties and possible acute toxicity of a novel nutraceutical with active substances of natural origin on C57BL/6 mice for 21 days. We evaluated the potential hazards (microbial contamination and heavy metals) of the novel nutraceutical and addressed the acute toxicity according to OECD guidelines of a 2000 mg/kg dose on mice for 21 days. The immunomodulatory effect was assessed at three concentrations (50 mg/kg, 100 mg/kg and 200 mg/kg) by determining body and organ indexes through a leukocyte analysis; flow cytometry immunophenotyping of lymphocytes populations and their subpopulations (T lymphocytes (LyCD3+), cytotoxic suppressor T lymphocytes (CD3+CD8+), helper T lymphocytes (CD3+CD4+), B lymphocytes (CD3−CD19+) and NK cells (CD3−NK1.1.+); and the expression of the CD69 activation marker. The results obtained for the novel nutraceutical referred to as ImunoBoost indicated no acute toxicity, an increased number of lymphocytes and the stimulation of lymphocyte activation and proliferation, demonstrating its immunomodulatory effect. The safe human consumption dose was established at 30 mg/day. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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14 pages, 4289 KiB  
Article
Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release
by Jun-Pil Jee, Young Hoon Kim, Jun Hak Lee, Kyoung Ah Min, Dong-Jin Jang, Sung Giu Jin and Kwan Hyung Cho
Pharmaceutics 2023, 15(3), 932; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15030932 - 13 Mar 2023
Cited by 1 | Viewed by 1598
Abstract
This study aimed to develop electrolyte complexes of paliperidone (PPD) with various particle sizes using cation-exchange resins (CERs) to enable controlled release (both immediate and sustained release). CERs of specific particle size ranges were obtained by sieving commercial products. PPD–CER complexes (PCCs) were [...] Read more.
This study aimed to develop electrolyte complexes of paliperidone (PPD) with various particle sizes using cation-exchange resins (CERs) to enable controlled release (both immediate and sustained release). CERs of specific particle size ranges were obtained by sieving commercial products. PPD–CER complexes (PCCs) were prepared in an acidic solution of pH 1.2 and demonstrated a high binding efficiency (>99.0%). PCCs were prepared with CERs of various particle sizes (on average, 100, 150, and 400 μm) at the weight ratio of PPD to CER (1:2 and 1:4). Physicochemical characterization studies such as Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy between PCCs (1:4) and physical mixtures confirmed PCC formation. In the drug release test, PPD alone experienced a complete drug release from PCC of >85% within 60 min and 120 min in pH 1.2 and pH 6.8 buffer solutions, respectively. Alternatively, PCC (1:4) prepared with CER (150 μm) formed spherical particles and showed an almost negligible release of PPD in pH 1.2 buffer (<10%, 2 h) while controlling the release in pH 6.8 buffer (>75%, 24 h). The release rate of PPD from PCCs was reduced with the increase in CER particle size and CER ratio. The PCCs explored in this study could be a promising technology for controlling the release of PPD in a variety of methods. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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21 pages, 3694 KiB  
Article
Amorphous Solid Dispersions Layered onto Pellets—An Alternative to Spray Drying?
by Marius Neuwirth, Sebastian K. Kappes, Michael U. Hartig and Karl G. Wagner
Pharmaceutics 2023, 15(3), 764; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15030764 - 24 Feb 2023
Viewed by 2319
Abstract
Spray drying is one of the most frequently used solvent-based processes for manufacturing amorphous solid dispersions (ASDs). However, the resulting fine powders usually require further downstream processing when intended for solid oral dosage forms. In this study, we compare properties and performance of [...] Read more.
Spray drying is one of the most frequently used solvent-based processes for manufacturing amorphous solid dispersions (ASDs). However, the resulting fine powders usually require further downstream processing when intended for solid oral dosage forms. In this study, we compare properties and performance of spray-dried ASDs with ASDs coated onto neutral starter pellets in mini-scale. We successfully prepared binary ASDs with a drug load of 20% Ketoconazole (KCZ) or Loratadine (LRD) as weakly basic model drugs and hydroxypropyl-methyl-cellulose acetate succinate or methacrylic acid ethacrylate copolymer as pH-dependent soluble polymers. All KCZ/ and LRD/polymer mixtures formed single-phased ASDs, as indicated by differential scanning calorimetry, X-ray powder diffraction and infrared spectroscopy. All ASDs showed physical stability for 6 months at 25 °C/65% rH and 40 °C/0% rH. Normalized to their initial surface area available to the dissolution medium, all ASDs showed a linear relationship of surface area and solubility enhancement, both in terms of supersaturation of solubility and initial dissolution rate, regardless of the manufacturing process. With similar performance and stability, processing of ASD pellets showed the advantages of a superior yield (>98%), ready to use for subsequent processing into multiple unit pellet systems. Therefore, ASD-layered pellets are an attractive alternative in ASD-formulation, especially in early formulation development at limited availability of drug substance. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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15 pages, 5962 KiB  
Article
Screening of Fenofibrate-Simvastatin Solid Dispersions in the Development of Fixed-Dose Formulations for the Treatment of Lipid Disorders
by Agata Górniak, Hanna Czapor-Irzabek, Adrianna Złocińska, Agnieszka Gawin-Mikołajewicz and Bożena Karolewicz
Pharmaceutics 2023, 15(2), 603; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15020603 - 10 Feb 2023
Cited by 1 | Viewed by 1414
Abstract
The combination of statins and fibrates in the treatment of lipid abnormalities effectively regulates individual lipid fraction levels. In this study, the screening and assessment of the physicochemical properties of simvastatin-fenofibrate solid dispersions were performed. Fenofibrate and simvastatin were processed using the kneading [...] Read more.
The combination of statins and fibrates in the treatment of lipid abnormalities effectively regulates individual lipid fraction levels. In this study, the screening and assessment of the physicochemical properties of simvastatin-fenofibrate solid dispersions were performed. Fenofibrate and simvastatin were processed using the kneading method in different weight ratios, and the resulting solid dispersions were assessed using differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), contact angle, as well as dissolution tests. The obtained results confirmed the formation of a simple eutectic phase diagram, with a eutectic point containing 79 wt% fenofibrate and 21 wt% simvastatin, lack of chemical interactions between the ingredients, and simvastatin impact on improving fenofibrate dissolution profile, due to the formation of crystalline solid dispersions by the kneading method. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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15 pages, 1075 KiB  
Article
Synergistic Combination of Irinotecan and Rapamycin Orally Delivered by Nanoemulsion for Enhancing Therapeutic Efficacy of Pancreatic Cancer
by Yu-Hsuan Liu, Ling-Chun Chen, Wen-Ting Cheng, Pu-Sheng Wei, Chien-Ming Hsieh, Ming-Thau Sheu, Shyr-Yi Lin, Hsiu-O Ho and Hong-Liang Lin
Pharmaceutics 2023, 15(2), 473; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15020473 - 31 Jan 2023
Cited by 1 | Viewed by 1739
Abstract
In recent years, combining different types of therapy has emerged as an advanced strategy for cancer treatment. In these combination therapies, oral delivery of anticancer drugs is more convenient and compliant. This study developed an irinotecan/rapamycin-loaded oral lecithin-based self-nanoemulsifying nanoemulsion preconcentrate (LB [...] Read more.
In recent years, combining different types of therapy has emerged as an advanced strategy for cancer treatment. In these combination therapies, oral delivery of anticancer drugs is more convenient and compliant. This study developed an irinotecan/rapamycin-loaded oral lecithin-based self-nanoemulsifying nanoemulsion preconcentrate (LBSNENPir/ra) and evaluated its synergistic combination effects on pancreatic cancer. LBSNENP loaded with irinotecan and rapamycin at a ratio of 1:1 (LBSNENPir10/ra10) had a better drug release profile and smaller particle size (<200 nm) than the drug powder. Moreover, LBSNENPir10/ra10 exhibited a strong synergistic effect (combination index [CI] < 1.0) in cell viability and combination effect studies. In the tumor inhibition study, the antitumor activity of LBSNENPir10/ra10/sily20 against MIA PaCa-2 (a human pancreatic cancer cell line) was significantly increased compared with the other groups. When administered with rapamycin and silymarin, the area under the curve and the maximum concentration of irinotecan significantly improved compared with the control. We successfully developed an irinotecan/rapamycin-loaded oral self-nanoemulsifying nanoemulsion system to achieve treatment efficacy for pancreatic cancer. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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17 pages, 7119 KiB  
Article
Controlled Release of Felodipine from 3D-Printed Tablets with Constant Surface Area: Influence of Surface Geometry
by Kasitpong Thanawuth, Sontaya Limmatvapirat, Catleya Rojviriya and Pornsak Sriamornsak
Pharmaceutics 2023, 15(2), 467; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15020467 - 31 Jan 2023
Cited by 5 | Viewed by 1523
Abstract
In this study, 3D-printed tablets with a constant surface area were designed and fabricated using polylactic acid (PLA) in the outer compartment and polyvinyl alcohol and felodipine (FDP) in the inner compartment. The influences of different surface geometries of the inner compartment, namely, [...] Read more.
In this study, 3D-printed tablets with a constant surface area were designed and fabricated using polylactic acid (PLA) in the outer compartment and polyvinyl alcohol and felodipine (FDP) in the inner compartment. The influences of different surface geometries of the inner compartment, namely, round, hexagon, square, and triangle, on drug release from 3D-printed tablets were also studied. The morphology and porosity of the inner compartment were determined using scanning electron microscopy and synchrotron radiation X-ray tomographic microscopy, respectively. Additionally, drug content and drug release were also evaluated. The results revealed that the round-shaped geometry seemed to have the greatest total surface area of the inner compartment, followed by square-shaped, hexagon-shaped, and triangle-shaped geometries. FDP-loaded 3D-printed tablets with triangle and hexagon surface geometries had the slowest drug release (about 80% within 24 h). In the round-shaped and square-shaped 3D-printed tablets, complete drug release was observed within 12 h. Furthermore, the drug release from triangle-shaped 3D-printed tablets with double the volume of the inner compartment was faster than that of a smaller volume. This was due to the fact that a larger tablet volume increased the surface area contacting the medium, resulting in a faster drug release. The findings indicated that the surface geometry of 3D-printed tablets with a constant surface area affected drug release. This study suggests that 3D printing technology may be used to develop oral solid dosage forms suitable for customized therapeutic treatments. Full article
(This article belongs to the Special Issue Recent Advances in Oral Solid Dosages)
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