Advanced Spray Drying Technology in Pharmaceutical Formulations: Novel Applications Using Polymeric and Lipidic Excipients

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

Deadline for manuscript submissions: 20 July 2024 | Viewed by 5834

Special Issue Editors

Department of Pharmaceutical Technology, Faculty of Health Sciences, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: drug formulation; characterization of dosage forms; formulation of natural products with therapeutic perspectives
Special Issues, Collections and Topics in MDPI journals
Department of Pharmaceutical Technology, Faculty of Health Sciences, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: drug formulation; tableting; extrusion/spheronization; hot melt extrusion; spray drying; amorphous solid dispersions; electrospinning; natural products; experimental designs

Special Issue Information

Dear Colleagues,

Spray drying is a continuous manufacturing process that was widely applied in the distant past in the chemical industries. Over the years, research led to its transformation from purely chemical/food applications to a cGMP-compliant pharmaceutical and biotechnological process. Formulation and process optimization have leveraged our understanding of the underlying mechanisms and enabled improved product development, even at early stages. Spray drying has been widely utilized for particle engineering, preparation of (amorphous) solid dispersions, and encapsulation of drugs and sensitive substances such as biologicals, microorganisms, and essential oils. A major aspect of the success of these applications lies in the use of synthetic and natural polymers as well as lipidic molecules as carriers, protective wall-forming excipients, or binders for subsequent tableting of spray drying products. This Special Issue welcomes contributions of original research work and reviews reporting established and emerging technologies in the area of advanced spray drying using synthetic and natural polymeric and lipidic excipients for the formulation of pharmaceuticals and biological therapeutic agents aiming for protection and targeted delivery.

Prof. Dr. Ioannis Nikolakakis
Dr. Ioannis Partheniadis
Guest Editor

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Keywords

  • spray drying
  • particle engineering
  • amorphous solid dispersions
  • dry powder
  • inhalation
  • biologics
  • lipidic carriers
  • protection
  • controlled delivery
  • targeted delivery
  • scale-up

Published Papers (4 papers)

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Research

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15 pages, 1344 KiB  
Article
Pullulan-Based Spray-Dried Mucoadhesive Microparticles for Sustained Oromucosal Drug Delivery
by Ting Liu, Xiang Gong, Yang Cai, Hao-Ying Li and Ben Forbes
Pharmaceutics 2024, 16(4), 460; https://doi.org/10.3390/pharmaceutics16040460 - 26 Mar 2024
Viewed by 177
Abstract
Mucoadhesive microparticles for oromucosal drug delivery offer several advantages, including intimate contact with the mucosa, delivery to less accessible regions, extended residence time, sustained drug release, reduced irritation, and improved patient compliance. In this study, pullulan was used to prepare mucoadhesive spray-dried microparticles [...] Read more.
Mucoadhesive microparticles for oromucosal drug delivery offer several advantages, including intimate contact with the mucosa, delivery to less accessible regions, extended residence time, sustained drug release, reduced irritation, and improved patient compliance. In this study, pullulan was used to prepare mucoadhesive spray-dried microparticles for delivering benzydamine hydrochloride (BZH) to oral mucosa. The BZH-pullulan spray-dried microparticles had a mean size of <25 μm with an angle of repose values between 25.8–36.6°. Pullulan markedly extended drug-release time to >180 min, ~9 times greater than the duration (i.e., 20 min) reportedly achieved by chitosan. Kinetic analysis showed the drug-release rate was concentration dependent and jointly controlled by drug diffusion and polymer chain relaxation. Further, pullulan was mucoadhesive and was able to retain up to 78.8% w/w of microencapsulated gold nanoparticle probes at the mucosal membrane. These data strongly suggest that BZH-pullulan microparticles have great potential for oromucosal drug delivery, by providing elongated residence time in situ and sustained drug release for the treatment of local diseases. Full article
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21 pages, 3126 KiB  
Article
Development of Inhalable Spray Dried Nitrofurantoin Formulations for the Treatment of Emphysema
by Mathew N. Leslie, Nirmal Marasini, Zara Sheikh, Paul M. Young, Daniela Traini and Hui Xin Ong
Pharmaceutics 2023, 15(1), 146; https://doi.org/10.3390/pharmaceutics15010146 - 31 Dec 2022
Cited by 1 | Viewed by 1359
Abstract
A central characteristic of emphysematous progression is the continuous destruction of the lung extracellular matrix (ECM). Current treatments for emphysema have only addressed symptoms rather than preventing or reversing the loss of lung ECM. Nitrofurantoin (NF) is an antibiotic that has the potential [...] Read more.
A central characteristic of emphysematous progression is the continuous destruction of the lung extracellular matrix (ECM). Current treatments for emphysema have only addressed symptoms rather than preventing or reversing the loss of lung ECM. Nitrofurantoin (NF) is an antibiotic that has the potential to induce lung fibrosis as a side effect upon oral administration. Our study aims to repurpose NF as an inhalable therapeutic strategy to upregulate ECM expression, thereby reversing the disease progression within the emphysematous lung. Spray-dried (SD) formulations of NF were prepared in conjunction with a two-fluid nozzle (2FN) and three-fluid nozzle (3FN) using hydroxypropyl methylcellulose (HPMC) and NF at 1:1 w/w. The formulations were characterized for their physicochemical properties (particle size, morphology, solid-state characteristics, aerodynamic behaviour, and dissolution properties) and characterized in vitro with efficacy studies on human lung fibroblasts. The 2FN formulation displayed a mass mean aerodynamic diameter (MMAD) of 1.8 ± 0.05 µm and fine particle fraction (FPF) of 87.4 ± 2.8% with significantly greater deposition predicted in the lower lung region compared to the 3FN formulation (MMAD: 4.4 ± 0.4 µm; FPF: 40 ± 5.8%). Furthermore, drug dissolution studies showed that NF released from the 2FN formulation after 3 h was significantly higher (55.7%) as compared to the 3FN formulation (42.4%). Importantly, efficacy studies in human lung fibroblasts showed that the 2FN formulation induced significantly enhanced ECM protein expression levels of periostin and Type IV Collagen (203.2% and 84.2% increase, respectively) compared to untreated cells, while 3FN formulations induced only a 172.5% increase in periostin and a 38.1% increase in type IV collagen. In conclusion, our study highlights the influence of nozzle choice in inhalable spray-dried formulations and supports the feasibility of using SD NF prepared using 2FN as a potential inhalable therapeutic agent to upregulate ECM protein production. Full article
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18 pages, 4059 KiB  
Article
Modification of Whey Proteins by Sonication and Hydrolysis for the Emulsification and Spray Drying Encapsulation of Grape Seed Oil
by Khashayar Sarabandi, Fardin Tamjidi, Zahra Akbarbaglu, Katarzyna Samborska, Pouria Gharehbeglou, Mohammad Saeed Kharazmi and Seid Mahdi Jafari
Pharmaceutics 2022, 14(11), 2434; https://doi.org/10.3390/pharmaceutics14112434 - 10 Nov 2022
Cited by 5 | Viewed by 1537
Abstract
In this study, whey protein concentrate (WPC) was sonicated or partially hydrolyzed by Alcalase, then examined as an emulsifier and carrier for the emulsification and spray drying of grape seed oil (GSO)-in-water emulsions. The modification treatments increased the free amino acid content and [...] Read more.
In this study, whey protein concentrate (WPC) was sonicated or partially hydrolyzed by Alcalase, then examined as an emulsifier and carrier for the emulsification and spray drying of grape seed oil (GSO)-in-water emulsions. The modification treatments increased the free amino acid content and antioxidant activity (against DPPH and ABTS free radicals), as well as, the solubility, emulsifying, and foaming activities of WPC. The modified WPC-stabilized emulsions had smaller, more homogeneous droplets and a higher zeta potential as compared to intact WPC. The corresponding spray-dried powders also showed improved encapsulation efficiency, oxidative stability, reconstitution ability, flowability, solubility, and hygroscopicity. The morphology of particles obtained from the primary WPC (matrix type, irregular with surface pores) and modified WPC (reservoir type, wrinkled with surface indentations), as well as the oxidative stability of the GSO were influenced by the functional characteristics and antioxidant activity of the carriers. Changes in the secondary structures and amide regions of WPC, as well as the embedding of GSO in its matrix, were deduced from FTIR spectra after modifications. Partial enzymolysis had better results than ultrasonication; hence, the WPC hydrolysates are recommended as emulsifiers, carriers, and antioxidants for the delivery and protection of bioactive compounds. Full article
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Review

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42 pages, 3407 KiB  
Review
Recent Advances in the Microencapsulation of Essential Oils, Lipids, and Compound Lipids through Spray Drying: A Review
by Diego Mauricio Sánchez-Osorno, María Camila López-Jaramillo, Angie Vanesa Caicedo Paz, Aída Luz Villa, María S. Peresin and Julián Paul Martínez-Galán
Pharmaceutics 2023, 15(5), 1490; https://doi.org/10.3390/pharmaceutics15051490 - 13 May 2023
Cited by 3 | Viewed by 1883
Abstract
In recent decades, the microcapsules of lipids, compound lipids, and essential oils, have found numerous potential practical applications in food, textiles, agricultural products, as well as pharmaceuticals. This article discusses the encapsulation of fat-soluble vitamins, essential oils, polyunsaturated fatty acids, and structured lipids. [...] Read more.
In recent decades, the microcapsules of lipids, compound lipids, and essential oils, have found numerous potential practical applications in food, textiles, agricultural products, as well as pharmaceuticals. This article discusses the encapsulation of fat-soluble vitamins, essential oils, polyunsaturated fatty acids, and structured lipids. Consequently, the compiled information establishes the criteria to better select encapsulating agents as well as combinations of encapsulating agents best suited to the types of active ingredient to be encapsulated. This review shows a trend towards applications in food and pharmacology as well as the increase in research related to microencapsulation by the spray drying of vitamins A and E, as well as fish oil, thanks to its contribution of omega 3 and omega 6. There is also an increase in articles in which spray drying is combined with other encapsulation techniques, or modifications to the conventional spray drying system. Full article
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