Understanding the Impact of Protein–Excipient Interactions on Physical Stability of Spray-Dried Protein Solids

Appropriate pretreatment of proteins and addition of xanthan gum (XG) has the potential to improve the stability of oil-in-water (O/W) emulsions. However, the factors that regulate the enhancement and the mechanism are still not clear, which restricts the realization of improving the emulsion stability by directional design of its structure. Therefore, the effects of whey protein micro-gel particles (WPMPs) and WPMPs-XG complexes on the stability of O/W emulsion were investigated in this article to provide theoretical support. WPMPs with different structures were prepared by pretreatment (controlled high-speed shear treatment of heat-set WPC gels) at pH 3.5–8.5. The impact of initial WPC structure and XG addition on Turbiscan Indexes, mean droplet size and the peroxide values of O/W emulsions was investigated. The results indicate that WPMPs and XG can respectively inhibit droplet coalescence and gravitational separation to improve the physical stability of WPC-stabilized O/W emulsions. The pretreatment significantly enhanced the oxidative stability of WPC-stabilized O/W emulsions. The addition of XG did not necessarily enhance the oxidative stability of O/W emulsions. Whether the oxidative stability of the O/W emulsion with XG is increased or decreased depends on the interface structure of the protein-XG complex. This study has significant implications for the development of novel structures containing lipid phases that are susceptible to oxidation.

Download Full-text

Designing enhanced spray dried particles for inhalation: A review of the impact of excipients and processing parameters on particle properties

Powder Technology ◽

10.1016/j.powtec.2021.02.031 ◽

2021 ◽

Vol 384 ◽

pp. 313-331

Author(s):

Nasser Alhajj ◽

Niall J. O'Reilly ◽

Helen Cathcart

Keyword(s):

Processing Parameters ◽

Particle Properties ◽

The Impact ◽

Spray Dried

Download Full-text

Freeze versus Spray Drying for Dry Wild Thyme (Thymus serpyllum L.) Extract Formulations: The Impact of Gelatin as a Coating Material

10.20944/preprints202105.0358.v1 ◽

2021 ◽

Author(s):

Aleksandra A. Jovanović ◽

Steva M. Lević ◽

Vladimir B. Pavlovic ◽

Smilja B. Markovic ◽

Rada V. Pjanovic ◽

...

Keyword(s):

Spray Drying ◽

Dry Weight ◽

Drying Process ◽

Scanning Calorimetry ◽

Coating Agent ◽

Microwave Assisted ◽

Freeze Dried ◽

Wild Thyme ◽

The Impact ◽

Spray Dried

Freeze drying was compared with spray drying regarding feasibility to process wild thyme drug in order to obtain dry formulations at laboratory scale starting from liquid extracts produced by different extraction methods: maceration, heat-, ultrasound-, and microwave-assisted extractions. Higher powder yield (based on the dry weight prior to extraction) was achieved by freeze than spray drying and lower loss of total polyphenol content (TPC) and total flavonoid content (TFC) due to the drying process. Gelatin as a coating agent (5% w/w) provided better TPC recovery by 70% in case of lyophilization and higher powder yield in case of spray drying by diminishing material deposition on the wall of the drying chamber. The resulting gelatin-free and gelatin-containing powders carried polyphenols in amount ~190 and 53-75 mg gallic acid equivalents GAE/g of powder, respectively. Microwave-assisted extract formulation distinguished from others by higher content of polyphenols, proteins and sugars, higher bulk density and lower solubility. The type of the drying process affected mainly position of the gelatin-derived -OH and amide bands in FTIR spectra. Spray dried formulations compared to freeze dried expressed higher thermal stability as confirmed by differential scanning calorimetry analysis and higher diffusion coefficient; the last feature can be associated with the lower specific surface area of irregularly shaped freeze-dried particles (151-223 µm) compared to small microspheres (~8 µm) in spray-dried powder.

Download Full-text

Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component

Pharmaceutics ◽

10.3390/pharmaceutics12030197 ◽

2020 ◽

Vol 12 (3) ◽

pp. 197 ◽

Cited By ~ 6

Author(s):

Mahbubur Rahman ◽

Stephanie Ahmad ◽

James Tarabokija ◽

Nathaniel Parker ◽

Ecevit Bilgili

Keyword(s):

Solid Dispersions ◽

Sodium Dodecyl ◽

Minor Component ◽

Amorphous Solid ◽

Amorphous Solid Dispersions ◽

Acetone Water ◽

Poorly Soluble ◽

A Minor ◽

The Impact ◽

Spray Dried

This study aimed to elucidate the impact of a common anionic surfactant, sodium dodecyl sulfate (SDS), along with hydroxypropyl cellulose (HPC) and Soluplus (Sol) on the release of griseofulvin (GF), a poorly soluble drug, from amorphous solid dispersions (ASDs). Solutions of 2.5% GF and 2.5%–12.5% HPC/Sol with 0.125% SDS/without SDS were prepared in acetone–water and spray-dried. The solid-state characterization of the ASDs suggests that GF–Sol had better miscibility and stronger interactions than GF–HPC and formed XRPD-amorphous GF, whereas HPC-based ASDs, especially the ones with a lower HPC loading, had crystalline GF. The dissolution tests show that without SDS, ASDs provided limited GF supersaturation (max. 250%) due to poor wettability of Sol-based ASDs and extensive GF recrystallization in HPC-based ASDs (max. 50%). Sol-based ASDs with SDS exhibited a dramatic increase in supersaturation (max. 570%), especially at a higher Sol loading, whereas HPC-based ASDs with SDS did not. SDS did not interfere with Sol’s ability to inhibit GF recrystallization, as confirmed by the precipitation from the supersaturated state and PLM imaging. The favorable use of SDS in a ternary ASD was attributed to both the wettability enhancement and its inability to promote GF recrystallization when used as a minor component along with Sol.

Download Full-text

Long-Term Physical (In)Stability of Spray-Dried Amorphous Drugs: Relationship with Glass-Forming Ability and Physicochemical Properties

Pharmaceutics ◽

10.3390/pharmaceutics11090425 ◽

2019 ◽

Vol 11 (9) ◽

pp. 425 ◽

Cited By ~ 4

Author(s):

Edueng ◽

Bergström ◽

Gråsjö ◽

Mahlin

Keyword(s):

Glass Transition ◽

Transition Temperature ◽

Glass Transition Temperature ◽

Physicochemical Properties ◽

Physical Stability ◽

Glass Forming Ability ◽

Melt Quenching ◽

Glass Forming ◽

Spray Dried

This study shows the importance of the chosen method for assessing the glass-forming ability (GFA) and glass stability (GS) of a drug compound. Traditionally, GFA and GS are established using in situ melt-quenching in a differential scanning calorimeter. In this study, we included 26 structurally diverse glass-forming drugs (i) to compare the GFA class when the model drugs were produced by spray-drying with that when melt-quenching was used, (ii) to investigate the long-term physical stability of the resulting amorphous solids, and (iii) to investigate the relationship between physicochemical properties and the GFA of spray-dried solids and their long-term physical stability. The spray-dried solids were exposed to dry (<5% RH) and humid (75% RH) conditions for six months at 25 °C. The crystallization of the spray-dried solids under these conditions was monitored using a combination of solid-state characterization techniques including differential scanning calorimetry, Raman spectroscopy, and powder X-ray diffraction. The GFA/GS class assignment for 85% of the model compounds was method-dependent, with significant differences between spray-drying and melt-quenching methods. The long-term physical stability under dry condition of the compounds was predictable from GFA/GS classification and glass transition and crystallization temperatures. However, the stability upon storage at 75% RH could not be predicted from the same data. There was no strong correlation between the physicochemical properties explored and the GFA class or long-term physical stability. However, there was a slight tendency for compounds with a relatively larger molecular weight, higher glass transition temperature, higher crystallization temperature, higher melting point and higher reduced glass transition temperature to have better GFA and better physical stability. In contrast, a high heat of fusion and entropy of fusion seemed to have a negative impact on the GFA and physical stability of our dataset.

Download Full-text