Spray Drying in the Pharmaceutical and Nutraceutical Field

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (30 September 2024) | Viewed by 12960

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Guest Editor
Department of Pharmaceutical Sciences, Università del Piemonte Orientale (UPO), Largo Donegani 2, 28100 Novara, Italy
Interests: pre-formulation studies; solid state of biomolecules; stabilizer excipients; thermal analysis; drug delivery systems; spray drying; spray congealing; freeze drying

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Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale “A. Avogadro”, Largo Donegani 2, 28100 Novara, Italy
Interests: food chemistry; gas chromatography; liquid chromatography; mass spectrometry; polyphenols; volatile compounds; wine chemistry; extraction; fermentation; prebiotic compounds
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Guest Editor
Food Science and Technology Program, Department of Life Sciences, Beijing Normal University-Hong Kong Baptist University United International College, Zhuhai 519087, China
Interests: food science; phytochemicals; nutraceuticals; pharmaceuticals; functional foods; molecular nutrition; cell biology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Spray drying is one of the most established means used in the pharmaceutical and food industries to convert liquids into powders. This continuous mechanical process allows for obtaining dry formulations characterized by enhanced shelf-life. Due to the short contact time of the feed liquid with the hot drying medium, spray drying is widely used for the microencapsulation of heat-sensitive and valuable bioactive molecules, in addition to volatile compounds. Another advantage of spray drying is the possibility of modulating the physicochemical and technological characteristics of the powders, and hence the final product quality, by opportunely setting the formulation and process parameters. Technological adjuvants can be used, which may be mixed with the material to be dried, to enhance the process yield and simultaneously to further reduce the thermal stress on bioactive compounds during the drying process. The proper choice of process parameters is important to the scalability of spray drying.

We are pleased to invite you to contribute to this Special Issue entitled “Spray Drying in the Pharmaceutical and Nutraceutical Field”. Your outstanding research will support scientists in tackling the challenges encountered in the obtainment of powders suitable for their formulation into pharmaceuticals and nutraceuticals.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following: pharmaceutical, nutraceutical and food sciences, biotechnology and the chemical industry.

We look forward to receiving your contributions.

Dr. Lorella Giovannelli
Dr. Matteo Bordiga
Prof. Dr. Baojun Xu
Guest Editors

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Keywords

  • encapsulation
  • microencapsulation
  • controlled release
  • nutraceuticals
  • pharmaceuticals
  • powder structure
  • process optimization
  • drying adjuvants
  • scale-up process

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Published Papers (5 papers)

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Research

13 pages, 4033 KiB  
Article
Use of Poly(vinyl alcohol) in Spray-Dried Dispersions: Enhancing Solubility and Stability of Proteolysis Targeting Chimeras
by Lena Mareczek, Lena K. Mueller, Laura Halstenberg, Thomas M. Geiger, Michael Walz, Min Zheng and Felix Hausch
Pharmaceutics 2024, 16(7), 924; https://doi.org/10.3390/pharmaceutics16070924 - 11 Jul 2024
Cited by 1 | Viewed by 1254
Abstract
PROTACs, proteolysis targeting chimeras, are bifunctional molecules inducing protein degradation through a unique proximity-based mode of action. While offering several advantages unachievable by classical drugs, PROTACs have unfavorable physicochemical properties that pose challenges in application and formulation. In this study, we show the [...] Read more.
PROTACs, proteolysis targeting chimeras, are bifunctional molecules inducing protein degradation through a unique proximity-based mode of action. While offering several advantages unachievable by classical drugs, PROTACs have unfavorable physicochemical properties that pose challenges in application and formulation. In this study, we show the solubility enhancement of two PROTACs, ARV-110 and SelDeg51, using Poly(vinyl alcohol). Hereby, we apply a three-fluid nozzle spray drying set-up to generate an amorphous solid dispersion with a 30% w/w drug loading with the respective PROTACs and the hydrophilic polymer. Dissolution enhancement was achieved and demonstrated for t = 0 and t = 4 weeks at 5 °C using a phosphate buffer with a pH of 6.8. A pH shift study on ARV-110-PVA is shown, covering transfer from simulated gastric fluid (SGF) at pH 2.0 to fasted-state simulated intestinal fluid (FaSSIF) at pH 6.5. Additionally, activity studies and binding assays of the pure SelDeg51 versus the spray-dried SelDeg51-PVA indicate no difference between both samples. Our results show how modern enabling formulation technologies can partially alleviate challenging physicochemical properties, such as the poor solubility of increasingly large ‘small’ molecules. Full article
(This article belongs to the Special Issue Spray Drying in the Pharmaceutical and Nutraceutical Field)
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22 pages, 5511 KiB  
Article
Development of Cyclodextrin-Based Mono and Dual Encapsulated Powders by Spray Drying for Successful Preservation of Everlasting Flower Extract
by Nada Ćujić Nikolić, Miloš Jovanović, Milica Radan, Zorica Lazarević, Dubravka Bigović, Smilja Marković, Nataša Jovanović Lješković and Katarina Šavikin
Pharmaceutics 2024, 16(7), 861; https://doi.org/10.3390/pharmaceutics16070861 - 27 Jun 2024
Viewed by 3699
Abstract
The study aimed to develop encapsulation systems to maintain the preservation of everlasting (Helichrysum plicatum) flower extract polyphenols. Spray-dried encapsulates were formulated using β-cyclodextrin (BCD) and 2-hydroxypropyl-β-cyclodextrin (HPBCD) as supramolecular hosts, and their macromolecule mixtures with the conventional carriers, maltodextrin (MD) [...] Read more.
The study aimed to develop encapsulation systems to maintain the preservation of everlasting (Helichrysum plicatum) flower extract polyphenols. Spray-dried encapsulates were formulated using β-cyclodextrin (BCD) and 2-hydroxypropyl-β-cyclodextrin (HPBCD) as supramolecular hosts, and their macromolecule mixtures with the conventional carriers, maltodextrin (MD) and whey protein (WP). The obtained microparticles were comparatively assessed regarding technological, physicochemical, and phytochemical properties. The highest yields were achieved by combining cyclodextrins with whey protein (73.96% for WP+BCD and 75.50% for WP+HPBCD compared to 62.48% of pure extract). The extract–carrier interactions and thermal stability were evaluated by FTIR and DSC analysis, suggesting successful entrapment within the carriers. Carriers reduced the particle diameter (3.99 to 4.86 μm compared to 6.49 μm of pure extract), classifying all encapsulates as microsystems. Carrier blends made the particle size distribution uniform, while SEM analysis revealed the production of more spherical and less aggregated particles. The HPBCD provided the highest encapsulation efficiency, with the highest content of detected aglycones and slightly lower values of their glycosylated forms. An analysis of the dual macromolecule encapsulation systems revealed the highest bioactive preservation potential for SHE+MD+BCD and SHE+WP+HPBCD. Overall, macromolecule combinations of cyclodextrins and conventional biopolymers in the spray-drying process can enhance the functional properties of H. plicatum extract. Full article
(This article belongs to the Special Issue Spray Drying in the Pharmaceutical and Nutraceutical Field)
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27 pages, 2066 KiB  
Article
Spray-Drying Microencapsulation of Bauhinia ungulata L. var. obtusifolia Aqueous Extract Containing Phenolic Compounds: A Comparative Study Using Different Wall Materials
by Myrth Soares do Nascimento Remígio, Teresa Greco, José Otávio Carréra Silva Júnior, Attilio Converti, Roseane Maria Ribeiro-Costa, Alessandra Rossi and Wagner Luiz Ramos Barbosa
Pharmaceutics 2024, 16(4), 488; https://doi.org/10.3390/pharmaceutics16040488 - 2 Apr 2024
Cited by 2 | Viewed by 1370
Abstract
Species belonging to the Bauhinia genus, usually known as “pata-de-vaca”, are popularly used to treat diabetes. Bauhinia ungulata var. obtusifolia (Ducke) Vaz is among them, of which the leaves are used as a tea for medicinal purposes in the Amazon region. A microencapsulation [...] Read more.
Species belonging to the Bauhinia genus, usually known as “pata-de-vaca”, are popularly used to treat diabetes. Bauhinia ungulata var. obtusifolia (Ducke) Vaz is among them, of which the leaves are used as a tea for medicinal purposes in the Amazon region. A microencapsulation study of lyophilized aqueous extract from Bauhinia ungulata leaves, which contain phenolic compounds, using five different wall materials (maltodextrin DE 4-7, maltodextrin DE 11-14; β-cyclodextrin; pectin and sodium carboxymethylcellulose) is described in this paper. The microstructure, particle size distribution, thermal behavior, yield, and encapsulation efficiency were investigated and compared using different techniques. Using high-performance liquid chromatography, phenolics, and flavonoids were detected and quantified in the microparticles. The microparticles obtained with a yield and phenolics encapsulation efficiency ranging within 60–83% and 35–57%, respectively, showed a particle size distribution between 1.15 and 5.54 µm, spherical morphology, and a wrinkled surface. Among them, those prepared with sodium carboxymethylcellulose or pectin proved to be the most thermally stable. They had the highest flavonoid content (23.07 and 21.73 mg RUTE/g Extract) and total antioxidant activity by both the DPPH (376.55 and 367.86 µM TEq/g Extract) and ABTS (1085.72 and 1062.32 µM TEq/g Extract) assays. The chromatographic analyses allowed for quantification of the following substances retained by the microparticles, chlorogenic acid (1.74–1.98 mg/g Extract), p-coumaric acid (0.06–0.08 mg/g Extract), rutin (11.2–12.9 mg/g Extract), and isoquercitrin (0.49–0.53 mg/g Extract), compounds which considered to responsible for the antidiabetic property attributed to the species. Full article
(This article belongs to the Special Issue Spray Drying in the Pharmaceutical and Nutraceutical Field)
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19 pages, 3393 KiB  
Article
Spray-Dried Powder Containing Cannabigerol: A New Extemporaneous Emulgel for Topical Administration
by Alice Picco, Lorena Segale, Ivana Miletto, Federica Pollastro, Silvio Aprile, Monica Locatelli, Elia Bari, Maria Luisa Torre and Lorella Giovannelli
Pharmaceutics 2023, 15(12), 2747; https://doi.org/10.3390/pharmaceutics15122747 - 8 Dec 2023
Viewed by 1889
Abstract
Cannabigerol (CBG), a cannabinoid from Cannabis sativa L., recently attracted noteworthy attention for its dermatological applications, mainly due to its anti-inflammatory, antioxidant, and antimicrobial effectiveness similar to those of cannabidiol (CBD). In this work, based on results from studies of in vitro permeation [...] Read more.
Cannabigerol (CBG), a cannabinoid from Cannabis sativa L., recently attracted noteworthy attention for its dermatological applications, mainly due to its anti-inflammatory, antioxidant, and antimicrobial effectiveness similar to those of cannabidiol (CBD). In this work, based on results from studies of in vitro permeation through biomimetic membranes performed with CBG and CBD in the presence and in the absence of a randomly substituted methyl-β-cyclodextrin (MβCD), a new CBG extemporaneous emulgel (oil-in-gel emulsion) formulation was developed by spray-drying. The powder (SDE) can be easily reconstituted with purified water, leading to a product with chemical-physical and technological characteristics that are comparable to those of the starting emulgels (E). Thermogravimetric analysis (TGA), attenuated total reflection-Fourier transformed infrared spectroscopy (ATR-FTIR), x-ray powder diffraction (XRPD), and high-performance liquid chromatography (HPLC) analyses demonstrated that the spray-drying treatment did not alter the chemical properties of CBG. This product can represent a metered-dosage form for the localized treatment of cutaneous afflictions such as acne and psoriasis. Full article
(This article belongs to the Special Issue Spray Drying in the Pharmaceutical and Nutraceutical Field)
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17 pages, 2610 KiB  
Article
Driving Spray Drying towards Better Yield: Tackling a Problem That Sticks Around
by Pavithra Sundararajan, Justin Moser, Lisa Williams, Tiffany Chiang, Colin Riordan, Matthew Metzger, Fan Zhang-Plasket, Fang Wang, John Collins and Joseph Williams
Pharmaceutics 2023, 15(8), 2137; https://doi.org/10.3390/pharmaceutics15082137 - 14 Aug 2023
Cited by 6 | Viewed by 3450
Abstract
Powder deposition and accumulation on walls of spray drying chamber has been known to impact spray drying processes, resulting in lower yield, frequent shutdowns, and downtimes. Critical factors that impact the extent and rate of wall deposition have been studied extensively in the [...] Read more.
Powder deposition and accumulation on walls of spray drying chamber has been known to impact spray drying processes, resulting in lower yield, frequent shutdowns, and downtimes. Critical factors that impact the extent and rate of wall deposition have been studied extensively in the chemical and food industry. In this paper, we present an atypical process yield issue wherein acceptable yield is obtained during the first batch of spray drying but undergoes significant yield loss in consecutive batches. Through understanding the interplay of the process, material properties, and equipment, we identify key mechanisms that are playing a role in causing the process yield issue. These mechanisms include surface roughness of the inner wall of the spray dryer, variation in gas flow due to the introduction of process analytical technology, start-up and shutdown operating parameters that expose the wall deposited powder from the prior batch to temperatures close to the onset of glass transition temperature and cause depression of its glass transition temperature. These factors result in more wall accumulation and impact the yield in subsequent batches. By correcting for most of these factors, the yield reduction issue was mitigated, and processing efficiency was improved. Full article
(This article belongs to the Special Issue Spray Drying in the Pharmaceutical and Nutraceutical Field)
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