Nano spray drying for encapsulation of pharmaceuticals

Arpagaus, Cordin; Collenberg, Andreas; Rütti, David; Assadpour, Elham; Jafari, Seid Mahdi

doi:10.1016/j.ijpharm.2018.05.037

Cited by 315 publications

(140 citation statements)

References 123 publications

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“…14 Lyophilization and spray drying are commonly used techniques to dry nanosuspensions of drugs. 15 Nevertheless, powders generated, particularly using lyophilization, appear to have inadequate flowability, and therefore require further processing, such as granulation, or the addition of excipients in substantial amounts. 16 In addition, the expense, time, and energy required by lyophilization are not favored in commercial-scale production.…”

Section: Introductionmentioning

confidence: 99%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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Introduction: Presenting poorly water-soluble drugs as nanoparticles has shown to be an effective technique in enhancing drug dissolution rate, intrinsic solubility, and thus oral bioavailability. Nevertheless, working with nanoparticles introduces many challenges, one of which is their physical instability. Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing. Methods: The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures. Using a novel, but scalable, spraying technique, GBD nanocrystals were loaded onto commonly used tablet fillers, water-soluble lactose monohydrate (LAC), and water insoluble microcrystalline cellulose (MCC). Conventional tableting processes were then used to convert the powders generated into a tablet dosage form. Results: Studies of redispersibility showed considerable preservation of size characteristics of GBD nanocrystals during downstream processing with redispersibility indices of 105 and 118 for GBD-LAC and GBD-MCC, respectively. Characterization by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy showed that the powders generated powders contained nanosized crystals of GBD which adhered to carrier surfaces. Powder flowability was characterized using Hausner ratio (HR) and Carr's index (CI). GBD-LAC-loaded particles exhibited poor flowability with CI and HR of 37.5% and 1.60, respectively, whilst GBD-MCC particles showed a slightly improved flowability with CI and HR of 26.47% and 1.36, respectively. The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability. Conclusion: Higher dissolution rates were observed from the nanocrystal-based tablets compared to the microsized and commercial drug formulations. Moreover, the novel nanocrystal tablet dosage forms showed enhanced in vivo performance with area under the plasma concentrationtime curve in the first 24 hours values 1.97 and 2.24 times greater than that of marketed tablets.

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Section: Introductionmentioning

confidence: 99%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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“…This technique allows that the rapid evaporation of solvents (water) during the drying process keeps the droplet temperature low and is possible to produce encapsulated systems with heat sensitive. (Arpagaus et al, 2018;Arpagaus, 2019a).…”

Section: Introductionmentioning

confidence: 99%

Dehydration of protein lactoferrin-glycomacropeptide nanohydrogels

et al. 2020

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A B S T R A C TProtein based nanohydrogels have recently gained interest due their high ability to carry and deliver active compounds. However, one of the limitations of using protein-based systems is their high sensitivity to physicochemical stresses during processing and storage. Protein-based formulations are commonly prepared as solid dosage forms once their stability can be achieved in the solid rather than in the liquid state. One of the methods to improve the stability of protein-based systems is drying, being freeze and spray drying the most popular methods. Nanohydrogels composed of lactoferrin and glycomacropeptide were developed by thermal gelation and dried using a freeze-dryer (CHRIST -Alpha 1-4 LD plus, Germany) and a nano spray dryer B-90 (BÜCHI Labortechnik AG, Switzerland). For nano spray-drying different experimental conditions were tested such as: the inlet temperature (80, 100 and 120 � C) and the hole size of the vibrating membrane in the spray cap (4 μm and 7 μm), while for freeze drying the nanohydrogels where maintained at À 40 � C for a drying period of about 24 h. The physicochemical properties of the resulting dried nanohydrogels were compared through different techniques: differential scanning calorimetry (DSC), thermogravimetry (TGA), X-ray diffraction (XRD) and scanning electron microscopy (SEM). DSC shows an endothermic peak ranging from 82 to 90 � C, indicating that during the drying methodologies the second denaturation peak of lactoferrin (around 90 � C) is maintained. No significant differences (p < 0.05) for denaturation peak temperatures were observed when different inlet temperatures or spray cap size were applied during the nano spray-drying conditions. When compared with freeze-drying it is possible to observe that a denaturation peak around the same range of temperatures was detected, also indicating that this drying process did not affect the denaturation of the protein. XRD results of nanohydrogels dried by freeze-drying revealed that crystallinity is significantly higher when compared with spray-dried nanohydrogels, explaining the lower thermal degradation observed in TGA for freeze-dried nanohydrogels. Nanohydrogels morphology after the drying process was evaluated by SEM. Nanohydrogels obtained by nano spray dryer B-90 allowed identifying the presence of particles with spherical shape, while nanohydrogels obtained by freeze drying had a sponge-like appearance. This work shows the influence of the drying process of protein-based nanohydrogels in their physical-chemical properties, thus pointing at which will be the preferred technology to be used in a future industrial application.

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“…Spray-drying is a method with the most potential, which allows producing the particles with the desired size distribution in a controllable manner [7][8][9]. Changing of the conditions during spray-drying provides control both on the particle size and shape, and at the same time provides low residual solvent content in the particle [10].…”

Section: Introductionmentioning

confidence: 99%

Formation of microspherical particles of albumin with model drug using spray drying process

2019

Biointerface Res Appl Chem

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Spray drying method enables to produce microspherical particles with narrow size distribution. Production of such microparticles is relevant for the development of the advanced systems for inhalation delivery of drugs. The aerosol particles diameter must be between 1 and 3 μm. Composite microparticles based on bovine serum albumin and model drug phenacetin were produced in the present work using the spray-drying method. The absence of a crystalline phase of the drug in composite microparticles was verified using several physicochemical methods. The average radius of the produced microparticles was found to be 1 μm based on the results from scanning electron microscopy. The rate of the dissolution of the drug included in microparticles is faster than that of crystalline phenacetin. The obtained results can be used for the development of the method for preparation of composite microparticles based on protein molecules using the spray-drying technique.

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Nano spray drying for encapsulation of pharmaceuticals

Cited by 315 publications

References 123 publications

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Dehydration of protein lactoferrin-glycomacropeptide nanohydrogels

Formation of microspherical particles of albumin with model drug using spray drying process

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