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Journal of Controlled Release :... Nov 2022While all the siRNA drugs on the market target the liver, the lungs offer a variety of currently undruggable targets which could potentially be treated with RNA...
While all the siRNA drugs on the market target the liver, the lungs offer a variety of currently undruggable targets which could potentially be treated with RNA therapeutics. Hence, local, pulmonary delivery of RNA nanoparticles could finally enable delivery beyond the liver. The administration of RNA drugs via dry powder inhalers offers many advantages related to physical, chemical and microbial stability of RNA and nanosuspensions. The present study was therefore designed to test the feasibility of engineering spray dried lipid nanoparticle (LNP) powders. Spray drying was performed using 5% lactose solution (m/V), and the targets were set to obtain nanoparticle sizes after redispersion of spray-dried powders around 150 nm, a residual moisture level below 5%, and RNA loss below 15% at maintained RNA bioactivity. The LNPs consisted of an ionizable cationic lipid which is a sulfur-containing analog of DLin-MC3-DMA, a helper lipid, cholesterol, and PEG-DMG encapsulating siRNA. Prior to the spray drying, the latter process was simulated with a novel dual emission fluorescence spectroscopy method to preselect the highest possible drying temperature and excipient solution maintaining LNP integrity and stability. Through characterization of physicochemical and aerodynamic properties of the spray dried powders, administration criteria for delivery to the lower respiratory tract were fulfilled. Spray dried LNPs penetrated the lung mucus layer and maintained bioactivity for >90% protein downregulation with a confirmed safety profile in a lung adenocarcinoma cell line. Additionally, the spray dried LNPs successfully achieved up to 50% gene silencing of the house keeping gene GAPDH in ex vivo human precision-cut lung slices at without increasing cytokine levels. This study verifies the successful spray drying procedure of LNP-siRNA systems maintaining their integrity and mediating strong gene silencing efficiency on mRNA and protein levels both in vitro and ex vivo. The successful spray drying procedure of LNP-siRNA formulations in 5% lactose solution creates a novel siRNA-based therapy option to target respiratory diseases such as lung cancer, asthma, COPD, cystic fibrosis and viral infections.
Topics: Humans; Powders; RNA, Small Interfering; Lactose; Administration, Inhalation; Spray Drying; Particle Size; Respiratory Aerosols and Droplets; Nanoparticles; Dry Powder Inhalers; Lung; Lipids; Aerosols
PubMed: 36126785
DOI: 10.1016/j.jconrel.2022.09.021 -
Polimery W Medycynie 2022In this review, benefits and drawbacks of the process of spray drying and nano spray drying with regard to the manufacturing of polymeric particles for pharmaceutical... (Review)
Review
In this review, benefits and drawbacks of the process of spray drying and nano spray drying with regard to the manufacturing of polymeric particles for pharmaceutical applications are discussed. Spray drying has been used for many years in the food, chemical and pharmaceutical industries for converting liquids into solids, in order to form products of uniform appearance. The construction of spray dryer enables to atomize the liquid into small droplets, which ensures a large surface area for heat and mass transfer, and significantly shortens the processing. Each droplet dries to an individual solid microparticle of characteristic features that can be tailored by optimizing formulation variables and critical process parameters. Since spray drying technology is easy to scale up and can be used for drying almost any drug in a solution or suspension, there are numerous examples of products in clinical use, in which this process has been successfully applied to improve drug stability, enhance bioavailability or control its release rate. In recent years, nano spray drying technology has been proposed as a method for lab-scale manufacturing of nanoparticles. Such an approach is of particular interest at early stages of drug development, when a small amount of new chemical entities is available. Here, the nebulization technique is used for feed atomization, while laminar gas flow in the drying chamber ensures gentle drying conditions. Moreover, electrostatic collectors have gradually replaced cyclone separators, ensuring high effectiveness in producing solid nanoparticles, even if a small volume of the sample is processed.
Topics: Technology, Pharmaceutical; Drug Industry; Spray Drying; Nanoparticles; Drug Stability; Polymers; Particle Size
PubMed: 35959704
DOI: 10.17219/pim/152230 -
Molecules (Basel, Switzerland) Aug 2020The application of the spray drying technique in the food industry for the production of a broad range of ingredients has become highly desirable compared to other... (Review)
Review
The application of the spray drying technique in the food industry for the production of a broad range of ingredients has become highly desirable compared to other drying techniques. Recently, the spray drying technique has been applied extensively for the production of functional foods, pharmaceuticals and nutraceuticals. Encapsulation using spray drying is highly preferred due to economic advantages compared to other encapsulation methods. Encapsulation of oils using the spray drying technique is carried out in order to enhance the handling properties of the products and to improve oxidation stability by protecting the bioactive compounds. Encapsulation of oils involves several parameters-including inlet and outlet temperatures, total solids, and the type of wall materials-that significantly affect the quality of final product. Therefore, this review highlights the application and optimization of the spray drying process for the encapsulation of oils used as food ingredients.
Topics: Desiccation; Food Industry; Functional Food; Plant Oils
PubMed: 32858785
DOI: 10.3390/molecules25173873 -
Polymers Oct 2023Enzyme-treated cellulose nanofibrils (CNFs) were produced via a lab-scale mass colloider using bleached kraft pulp (BKP) to evaluate their processability and power...
Enzyme-treated cellulose nanofibrils (CNFs) were produced via a lab-scale mass colloider using bleached kraft pulp (BKP) to evaluate their processability and power requirements during refining and spray-drying operations. To evaluate the energy efficiency in the CNF refining process, the net energy consumption, degree of polymerization (DP), and viscosity were determined. Less energy was consumed to attain a given fines level by using the endoglucanase enzymes. The DP and viscosity were also decreased using the enzymes. The morphological properties of the enzyme-pretreated spray-dried CNF powders (SDCNFs) were measured. Subsequently, the enzyme-pretreated SDCNFs were added to a PP matrix with MAPP as a coupling agent. The mixture was then compounded through a co-rotating twin-screw extruder to determine whether the enzyme treatment of the CNFs affects the mechanical properties of the composites. Compared to earlier studies on enhancing PMCs with SDCNF powders, this research investigates the use of enzyme-pretreated SDCNF powders. It was confirmed that the strength properties of PP increased by adding SDCNFs, and the strength properties were maintained after adding enzyme-pretreated SDCNFs.
PubMed: 37896330
DOI: 10.3390/polym15204086 -
Therapeutic Delivery May 2019
Topics: Administration, Inhalation; Freeze Drying; Humans; Powders; RNA, Small Interfering
PubMed: 31094296
DOI: 10.4155/tde-2019-0018 -
Human Vaccines & Immunotherapeutics Oct 2017Spray drying is a promising method for the stabilization of vaccines, which are usually formulated as liquids. Usually, vaccine stability is improved by spray drying in... (Review)
Review
Spray drying is a promising method for the stabilization of vaccines, which are usually formulated as liquids. Usually, vaccine stability is improved by spray drying in the presence of a range of excipients. Unlike freeze drying, there is no freezing step involved, thus the damage related to this step is avoided. The edge of spray drying resides in its ability for particles to be engineered to desired requirements, which can be used in various vaccine delivery methods and routes. Although several spray dried vaccines have shown encouraging preclinical results, the number of vaccines that have been tested in clinical trials is limited, indicating a relatively new area of vaccine stabilization and delivery. This article reviews the current status of spray dried vaccine formulations and delivery methods. In particular it discusses the impact of process stresses on vaccine integrity, the application of excipients in spray drying of vaccines, process and formulation optimization strategies based on Design of Experiment approaches as well as opportunities for future application of spray dried vaccine powders for vaccine delivery.
Topics: Administration, Oral; Animals; Chemistry, Pharmaceutical; Desiccation; Drug Compounding; Humans; Influenza Vaccines; Mice; Nasal Sprays; Particle Size; Powders; Vaccine Potency; Vaccines
PubMed: 28925794
DOI: 10.1080/21645515.2017.1356952 -
Foods (Basel, Switzerland) May 2023Bioactive peptides derived from enzymatic hydrolysis are gaining attention for the production of supplements, pharmaceutical compounds, and functional foods. However,... (Review)
Review
Bioactive peptides derived from enzymatic hydrolysis are gaining attention for the production of supplements, pharmaceutical compounds, and functional foods. However, their inclusion in oral delivery systems is constrained by their high susceptibility to degradation during human gastrointestinal digestion. Encapsulating techniques can be used to stabilize functional ingredients, helping to maintain their activity after processing, storage, and digestion, thus improving their bioaccessibility. Monoaxial spray-drying and electrospraying are common and economical techniques used for the encapsulation of nutrients and bioactive compounds in both the pharmaceutical and food industries. Although less studied, the coaxial configuration of both techniques could potentially improve the stabilization of protein-based bioactives via the formation of shell-core structures. This article reviews the application of these techniques, both monoaxial and coaxial configurations, for the encapsulation of bioactive peptides and protein hydrolysates, focusing on the factors affecting the properties of the encapsulates, such as the formulation of the feed solution, selection of carrier and solvent, as well as the processing conditions used. Furthermore, this review covers the release, retention of bioactivity, and stability of peptide-loaded encapsulates after processing and digestion.
PubMed: 37238822
DOI: 10.3390/foods12102005 -
Expert Opinion on Drug Delivery Jan 2018The rising demand for pharmaceutical particles with tailored physicochemical properties has opened new markets for spray drying especially for solubility enhancement,... (Review)
Review
INTRODUCTION
The rising demand for pharmaceutical particles with tailored physicochemical properties has opened new markets for spray drying especially for solubility enhancement, improving inhalation medicines and stabilization of biopharmaceuticals. Despite this, the spray drying literature is scattered and often does not address the principles underpinning robust development of pharmaceuticals. It is therefore necessary to present clearer picture of the field and highlight the factors influencing particle design and scale-up.
AREAS COVERED
The review presents a systematic analysis of the trends in development of particle delivery systems using spray drying. This is followed by exploring the mechanisms governing particle formation in the process stages. Particle design factors including those of equipment configurations and feed/process attributes were highlighted. Finally, the review summarises the current industrial approaches for upscaling pharmaceutical spray drying.
EXPERT OPINION
Spray drying provides the ability to design particles of the desired functionality. This greatly benefits the pharmaceutical sector especially as product specifications are becoming more encompassing and exacting. One of the biggest barriers to product translation remains one of scale-up/scale-down. A shift from trial and error approaches to model-based particle design helps to enhance control over product properties. To this end, process innovations and advanced manufacturing technologies are particularly welcomed.
Topics: Administration, Inhalation; Chemistry, Pharmaceutical; Desiccation; Drug Delivery Systems; Dry Powder Inhalers; Equipment Design; Humans; Particle Size; Solubility; Technology, Pharmaceutical
PubMed: 28423954
DOI: 10.1080/17425247.2017.1321634 -
Materials (Basel, Switzerland) Jul 2022Spray drying is a widely used method of converting liquid material (aqueous or organic solutions, emulsions and suspensions) into a dry powder. Good flowability, narrow... (Review)
Review
Spray drying is a widely used method of converting liquid material (aqueous or organic solutions, emulsions and suspensions) into a dry powder. Good flowability, narrow size distribution, and controllable morphology are inherent in powders produced by spray drying. This review considers the granulation factors that influence the final properties of the silicon nitride dried powders. The first group includes the types of atomizers, manifolds, and drying chamber configurations. The process parameters fall into the second group and include the following: inlet temperature, atomizing air flow, feed flow rate, drying gas flow rate, outlet temperature, and drying time. Finally, the last group, feedstock parameters, includes many factors such as feed surface tension, feed viscosity, solvent type, solid particle concentration, and additives. Given the large number of factors affecting morphology, particle size and moisture, optimizing the spray drying process is usually achieved by the "trial and error" approach. Nevertheless, some factors such as the effect of a solvent, dispersant, binder, and sintering additives considered in the literature that affect the SiN granulation process were reviewed in the work. By summarizing the data available on silicon nitride powder production, the authors attempt to tackle the problem of its emerging demand in science and industry.
PubMed: 35888466
DOI: 10.3390/ma15144999 -
Food Science & Nutrition Apr 2020In this study, the chitosan-based release microspheres were prepared by spray drying method. Chitosan was used as the carrier material, and extract, extract, and...
In this study, the chitosan-based release microspheres were prepared by spray drying method. Chitosan was used as the carrier material, and extract, extract, and extract (the mass ratio was 2:7:5) were active substance. The spray drying preparation process of microsphere was optimized by single factor experiment and L (3) orthogonal design. Drug loading (DL), particle size, and sustained release performance of microspheres were investigated. The mass fraction of chitosan was 1.5%, the mass ratio of drug to chitosan was 1:3, the inlet air temperature was 130°C, and the injection rate was 400 ml/hr. The chitosan-based microspheres prepared under the above conditions had a smooth surface, and the DL was 23.87 ± 0.93%; the average particle diameter was 10.27 ± 1.05 μm, and the encapsulation efficiency (EE) of the microspheres was 91.28 ± 1.04%. The preparation process of chitosan-based drug microsphere prepared by spray drying method was simple and stable. The prepared microspheres in this paper showed a sustained release effect in vitro.
PubMed: 32328259
DOI: 10.1002/fsn3.1479