Solid-state Protein Formulations

Angkawinitwong, Ukrit; Sharma, Garima; Khaw, PT; Brocchini, Steve; Williams, Gareth R.

doi:10.4155/tde.14.98

Cited by 32 publications

(16 citation statements)

References 138 publications

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“…Thus, ES technology can be applied for the solid formulation of various biopharmaceuticals such as enzymes, peptides, proteins, monoclonal antibodies, oligonucleotides and live cells [8][9][10][11]. As both freeze and spray drying can induce degradation of biopharmaceuticals, they are typically formulated with various excipients to preserve the activity, amongst which the most commonly used excipients are sugars (like mannitol, saccharose, and trehalose being the typical choices) [5,12,13]. The exact protection mechanism is not known, but there are two hypotheses (namely the vitrification and water replacement hypotheses), that explain the protective effect of sugars on the active pharmaceutical ingredient (API) stability [14,15].…”

mentioning

confidence: 99%

Electrospinning scale-up and formulation development of PVA nanofibers aiming oral delivery of biopharmaceuticals

Hirsch¹,

Vass²,

Démuth³

et al. 2019

Express Polym. Lett.

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The application of biopharmaceuticals for oral administration is a topic of great interest in the pharmaceutical industry due to the inherent advantages of oral delivery [1]. Biopharmaceutical formulations are more stable in the solid state than in liquid form; in addition, it has many advantages like storage at ambient temperature, longer shelf-life, easier product shipping and the possibility of controlled drug delivery [2]. Currently, the pharmaceutical industry is typically applying freeze drying and spray drying processes in order to obtain solid biopharmaceuticals, however, both technologies have disadvantages [3,4]. Freeze drying is a time-consuming batch technology, has high energy consumption, and the freezing can cause degradation of the biomolecules. On the contrary, spray drying can be operated continuously, is more economical, but can induce inactivation of heat-sensitive molecules, due to the high drying temperature. Electrospinning (ES), which is originally a fiber drawing technology, can be a promising alternative for continuous drying technologies, providing Abstract. Electrospinning is a promising drying technology providing a rapid and gentle drying at ambient temperature, thus electrospinning of polyvinyl alcohol aqueous solutions was investigated for the solid formulation of biopharmaceuticals. The commonly used single-needle electrospinning does not have adequate productivity to satisfy the industrial requirements, therefore our aim was to study the scale-up of the technology by using high-speed electrospinning. High molecular weight polyethylene oxide as a secondary polymer was applied to enhance the fiber formation of polyvinyl alcohol. While polyvinyl alcohol-polyethylene oxide formulations resulted in adequate fiber formation it was not possible to process them further as the friability of the fibers was too low. In order to increase the friability, the effect of adding various sugars (mannitol, glucose, lactose, saccharose, and trehalose) was investigated. The results showed that mannitol was the best friability enhancing excipient because of its crystallinity and low moisture content in the fibrous sample. In contrast, glucose, lactose, saccharose, and trehalose were amorphous with higher moisture content and fibers containing these were grindable only after post-drying.

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confidence: 99%

Electrospinning scale-up and formulation development of PVA nanofibers aiming oral delivery of biopharmaceuticals

Hirsch¹,

Vass²,

Démuth³

et al. 2019

Express Polym. Lett.

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“…It was reported that GS were stored in a formulated dried conditions, and were capable of retaining their functionality up to 2 years . We suggest that the stents had undergone a freeze‐drying bioprocessing procedure to allow solid state storage . Another consideration unique to vascular stents is the need to be crimped onto a delivery system.…”

Section: Engineering Considerations For In Situ Endothelializationmentioning

confidence: 98%

“…[ 143 ] We suggest that the stents had undergone a freeze-drying bioprocessing procedure to allow solid state storage. [ 144 ] Another consideration unique to vascular stents is the need to be crimped onto a delivery system. The effect of crimping on immobilized biomolecules could be unknown.…”

Section: Practicality In Translational Pathwaysmentioning

confidence: 99%

In situ Endothelialization: Bioengineering Considerations to Translation

Pang

Farhatnia

Godarzi

et al. 2015

Small

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Improving patency rates of current cardiovascular implants remains a major challenge. It is widely accepted that regeneration of a healthy endothelium layer on biomaterials could yield the perfect blood-contacting surface. Earlier efforts in pre-seeding endothelial cells in vitro demonstrated success in enhancing patency, but translation to the clinic is largely hampered due to its impracticality. In situ endothelialization, which aims to create biomaterial surfaces capable of self-endothelializing upon implantation, appears to be an extremely promising solution, particularly with the utilization of endothelial progenitor cells (EPCs). Nevertheless, controlling cell behavior in situ using immobilized biomolecules or physical patterning can be complex, thus warranting careful consideration. This review aims to provide valuable insight into the rationale and recent developments in biomaterial strategies to enhance in situ endothelialization. In particular, a discussion on the important bio-/nanoengineering considerations and lessons learnt from clinical trials are presented to aid the future translation of this exciting paradigm.

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“…In general, crystalline substances are vital for the delivery of many drugs. Protein crystals have shown significant benefits in the delivery of biopharmaceuticals to achieve optimal concentration, higher bioavailability and appropriately adjustable and sustained release of the therapeutic agent [, ].…”

Section: Protein Crystal Growth; Practical Aspects Of Protein Crystalmentioning

confidence: 99%

Recent experimental and theoretical studies on protein crystallization

Nanev

2016

Crystal Research and Technology

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Crystals are required to determine three-dimensional structures of proteins and other bio-molecules via X-ray diffraction. This is the prime cause for the keen interest in protein crystallization. Recently published experimental and theoretical studies on protein crystal nucleation and growth are reviewed, and the prospects of protein-based crystalline pharmaceuticals mass-production are considered. A new insight into protein crystal nucleation is presented from a physical perspective. It refers to modeling nuclei number density as a definite (curved) surface where each point has two coordinates, supersaturation and time. In doing so, theoretical S-shaped dependences of nuclei number densities on both supersaturation and time are found. These dependences are confirmed experimentally by plotting insulin crystal nucleation data. Growth of protein crystals of narrow size distribution is monitored to establish crystal polydispersity cause. Ostwald ripening is considered as a postgrowth stage of the crystallization process.

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Solid-state Protein Formulations

Cited by 32 publications

References 138 publications

Electrospinning scale-up and formulation development of PVA nanofibers aiming oral delivery of biopharmaceuticals

Electrospinning scale-up and formulation development of PVA nanofibers aiming oral delivery of biopharmaceuticals

In situ Endothelialization: Bioengineering Considerations to Translation

Recent experimental and theoretical studies on protein crystallization

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