Formulation and evaluation of inhalable microparticles of Rizatriptan Benzoate processed by spray freeze-drying

shokouh, Mahsa Keyhan; Faghihi, Hooshang; Darabi, Maryam; Mirmoeini, Maryam Sadat; Vatanara, Alireza

doi:10.1016/j.jddst.2021.102356

Cited by 7 publications

(6 citation statements)

References 32 publications

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“…Aside from patients with respiratory disorders benefiting from local drug delivery through inhalation, those patients suffering from diseases including osteoporosis, diabetes, hormone deficiency and migraine (Keyhan shokouh et al 2021 ) could enjoy the simplicity and non-invasiveness of such administration way (Dhahir et al 2021 ). From a pharmacokinetic view, pulmonary delivery systems’ superiorities are large surface area (70–140 m 2 ), fast absorption and less enzymatic activity than oral route; it also bypasses first pass metabolism of the liver (Miyamoto et al 2021 ).…”

Section: Local and Systemic Delivery Of Dried-powder Biopharmaceuticalsmentioning

confidence: 99%

“…Alongside this, we also review that dried powder inhalers have mainly focused on local drug delivery for treating respiratory diseases. Aside from patients suffering from pulmonary diseases benefiting from local drug delivery through inhalation, those patients with diabetes, osteoporosis, and hormone deficiency (Keyhan shokouh et al 2021 ) could enjoy the simplicity and non-invasiveness of such administration way (Emami et al 2018a , b ; Emami et al 2019 ; Dhahir et al 2021 ).…”

Section: Introductionmentioning

confidence: 99%

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Recent progress in drying technologies for improving the stability and delivery efficiency of biopharmaceuticals

Emami

Shokooh

Yazdi

2022

J. Pharm. Investig.

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Background Most biopharmaceuticals are developed in liquid dosage forms that are less stable than solid forms. To ensure the stability of biopharmaceuticals, it is critical to use an effective drying technique in the presence of an appropriate stabilizing excipient. Various drying techniques are available for this purpose, such as freeze drying or lyophilization, spray drying, spray freeze-drying, supercritical fluid drying, particle replication in nonwetting templates, and fluidized bed drying. Area covered In this review, we discuss drying technologies and their applications in the production of stable solid-state biopharmaceuticals, providing examples of commercially available products or clinical trial formulations. Alongside this, we also review how different analytical methods may be utilized in the evaluation of aerosol performance and powder characteristics of dried protein powders. Finally, we assess the protein integrity in terms of conformational and physicochemical stability and biological activity. Expert opinion With the aim of treating either infectious respiratory diseases or systemic disorders, inhaled biopharmaceuticals reduce both therapeutic dose and cost of therapy. Drying methods in the presence of optimized protein/stabilizer combinations, produce solid dosage forms of proteins with greater stability. A suitable drying method was chosen, and the process parameters were optimized based on the route of protein administration. With the ongoing trend of addressing deficiencies in biopharmaceutical production, developing new methods to replace conventional drying methods, and investigating novel excipients for more efficient stabilizing effects, these products have the potential to dominate the pharmaceutical industry in the future.

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Section: Local and Systemic Delivery Of Dried-powder Biopharmaceuticalsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Recent progress in drying technologies for improving the stability and delivery efficiency of biopharmaceuticals

Emami

Shokooh

Yazdi

2022

J. Pharm. Investig.

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“…SFD can also be preferred to SD for thermolabile substances (i.e., biopharmaceuticals) since low temperatures are involved and thermal degradation is less likely to occur [28]. Moreover, the biomolecular structure is protected from phase separation since the crystallisation of excipients, solutes partitioning, and pH changes are reduced due to the high freezing rate [18,26,29,30]. Consequently, the drug is efficiently embedded into the excipient, increasing both the API bioavailability and the aerodynamic properties of particles [30].…”

Section: Introductionmentioning

confidence: 99%

“…SFD has been used in the formulation of different drugs for pulmonary delivery, including rizatriptan benzoate [29], voriconazole [33], cyclosporine A [32], clarithromycin [15], budesonide [34], proteins [22,35], and small interfering RNA [36]. This technique is especially suitable for generating carrier-free inhalable particles, an attractive formulation which does not require a coarse carrier (lactose) to have adequate flowability.…”

Section: Introductionmentioning

confidence: 99%

Tailoring Dry Microparticles for Pulmonary Drug Delivery: Ultrasonic Spray Freeze-Drying with Mannitol and Salbutamol Sulphate

Pasero,

Susa,

Chiavarino

et al. 2023

Processes

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Spray freeze-drying has emerged as a valid alternative to traditional spray drying to produce therapeutic dry microparticles. In particular, the spherical shape and high porosity of spray freeze-dried microparticles make them suitable for pulmonary drug delivery through dry powder inhalers. However, an appropriate particle size and fine particle fraction are required to guarantee lung deposition. This study used ultrasonic spray freeze-drying to generate dry microparticles composed of mannitol either alone or added with the bronchodilator salbutamol sulphate. The influence of the solid concentration and the feed flow rate on the particle size, morphology, surface area, porosity, and crystallinity was investigated. Growing particle size was observed, increasing the concentration and feed flow rate. Similarly, the addition of the drug led to a larger particle size and surface area. The in vitro simulation of drug deposition highlighted the dependence of the aerodynamic properties on the solid concentration and feed flow rate. Due to the lower density and particle geometric size, the highest fine particle fraction (26%) and smallest mass median aerodynamic diameter (4.4 μm) were reached at the lowest solid concentration and feed flow rate.

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“…Therefore, it is an attractive method among different particle engineering methods. [14][15][16] The general principle of this method is atomization of feed solution into liquid nitrogen and then lyophilization of frozen droplets to allow the solvent to be sublimated at low temperature and vacuum conditions (Figure 1). 7,8 Spraying and rapid freezing of the droplets and sublimation of ice particles in this method create porous spherical particles.…”

Section: Introductionmentioning

confidence: 99%

Screening of Cyclodextrins in the Processing of Buserelin Dry Powders for Inhalation Prepared by Spray Freeze-Drying

Rostamnezhad¹,

Mireskandari²,

Rouini³

et al. 2023

Adv Pharm Bull

Self Cite

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In this study, we prepared inhalable buserelin microparticles using the spray freeze-drying (SFD) method for pulmonary drug delivery. Raffinose as a cryoprotectant carrier was combined with two levels of five different cyclodextrins (CDs) and then processed by SFD. Dry powder diameters were evaluated by laser light scattering and morphology was determined by scanning electron microscopy (SEM). Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis were utilized for the determination of crystalline structures. The aerodynamic properties of the spray freeze-dried powders were evaluated by twin stage impinger (TSI) and the stability of prepared samples was assessed under normal and accelerated conditions. The prepared powders were mostly porous spheres and the size of microparticles ranged from 9.08 to 13.53 μm, which are suitable as spray-freeze dried particles. All formulations showed amorphous structure confirmed by DSC and XRD. The aerosolization performance of the formulation containing buserlin, raffinose and 5% beta-cyclodextrin (β-CD), was the highest and its fine particle fraction (FPF) was 69.38%. The more circular and separated structures were observed in higher concentrations of CDs, which were compatible with FPFs. The highest stability was obtained in the formulation containing hydroxypropyl beta-cyclodextrin (HP-β-16. CD) 5%. On the contrary, sulfobutylether beta-cyclodextrin (SBE-β-CD) 5% bearing particles showed the least stability. By adjusting the type and ratio of CDs in the presence of raffinose, the prepared formulations could effectively enhance the aerosolization and stability of buserelin. Therefore, they can be proposed as a suitable career for lung drug delivery.

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Formulation and evaluation of inhalable microparticles of Rizatriptan Benzoate processed by spray freeze-drying

Cited by 7 publications

References 32 publications

Recent progress in drying technologies for improving the stability and delivery efficiency of biopharmaceuticals

Recent progress in drying technologies for improving the stability and delivery efficiency of biopharmaceuticals

Tailoring Dry Microparticles for Pulmonary Drug Delivery: Ultrasonic Spray Freeze-Drying with Mannitol and Salbutamol Sulphate

Screening of Cyclodextrins in the Processing of Buserelin Dry Powders for Inhalation Prepared by Spray Freeze-Drying

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