Screening of novel excipients for freeze-dried protein formulations

Holm, Tobias Palle; Meng-Lund, Helena; Rantanen, Jukka; Jørgensen, Lene

doi:10.1016/j.ejpb.2021.01.008

Cited by 9 publications

(3 citation statements)

References 71 publications

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“…Therefore, mannitol was developed into many types of granules and mixture granules. It is marketed as a pharmaceutical excipient for the direct tableting of oral disintegration tablets and as a bulking agent and protectant for freeze-drying [ 163 , 164 ]. It also can be used as a modifier in combination with other excipients to produce a multi-function composite excipient by co-processing methods [ 165 , 166 ].…”

Section: Mannitolmentioning

confidence: 99%

Surface Modifiers on Composite Particles for Direct Compaction

Chen

Liu²,

Zhu³

et al. 2022

Pharmaceutics

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Direct compaction (DC) is considered to be the most effective method of tablet production. However, only a small number of the active pharmaceutical ingredients (APIs) can be successfully manufactured into tablets using DC since most APIs lack adequate functional properties to meet DC requirements. The use of suitable modifiers and appropriate co-processing technologies can provide a promising approach for the preparation of composite particles with high functional properties. The purpose of this review is to provide an overview and classification of different modifiers and their multiple combinations that may improve API tableting properties or prepare composite excipients with appropriate co-processed technology, as well as discuss the corresponding modification mechanism. Moreover, it provides solutions for selecting appropriate modifiers and co-processing technologies to prepare composite particles with improved properties.

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Section: Mannitolmentioning

confidence: 99%

Surface Modifiers on Composite Particles for Direct Compaction

Chen

Liu²,

Zhu³

et al. 2022

Pharmaceutics

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“…In the development of live attenuated vaccines, some chemical and physical reactions can easily destroy the structure of the virus surface proteins and internal nucleic acids [35]. Before vacuum drying, freezing damage is an important reason for the decline in food and drug quality.…”

Section: Discussionmentioning

confidence: 99%

Optimization of Heat-Resistance Technology for a Duck Hepatitis Lyophilized Live Vaccine

et al. 2022

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In this study, to improve the quality of a live attenuated vaccine for duck viral hepatitis (DHV), the lyophilization of a heat-resistant duck hepatitis virus vaccine was optimized. The optimized heat protectors were made of 10% sucrose, 1.2% pullulan, 0.5% PVP, and 1% arginine, etc., with a titer freeze-drying loss of ≤0.50 Lg. The vaccine product’s valence measurements demonstrated the following: the vaccine could be stored at 2–8 °C for 18 months with a virus titer loss ≤0.91 Lg; at 37 °C for 10 days with a virus valence loss ≤0.89 Lg; and at 45 °C for 3 days with a virus titer loss ≤0.90 Lg. Regarding safety, no deaths occurred in two-day-old ducklings immunized with a 10 times dose vaccine; their energy, diet, and weight gain were all normal, demonstrating that the DHV heat-resistant vaccines were safe for ducklings and did not cause any immune side effects. Duck viral hepatitis freeze-dried vaccine began to produce antibodies at 7 d after immunization, reached above 5.0 on 14 d, and reached above 7.0 on 21 d, showing a continuous upward trend. This indicates that duck viral hepatitis vaccine has a good immunogen level. The optimization of the freeze-drying process saves costs and also improves the quality of the freeze-drying products, which provides important theoretical and technical support for the further study of vaccine products.

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“…According to the references [ 25 ] and the results of the preliminary experiments, the following six lyophilization protectants, which are L-lysine [ 26 ], maltose [ 27 ], oligomannose [ 28 ], chitosan [ 29 ], mannitol [ 30 ], and sorbitol [ 15 ] were selected. The final concentrations of oligomannose, chitosan, and mannitol lyophilized protectants were 0.005%, 0.025%, 0.05%, 0.25%, and 0.5% ( w / v ).…”

Section: Methodsmentioning

confidence: 99%

Lyoprotectant Formulation and Optimization of the J-Aggregates Astaxanthin/BSA/Chitosan Nanosuspension

et al. 2023

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Astaxanthin is a carotenoid with excellent antioxidant activity. However, this small lipid-soluble molecule is insoluble in water and has low stability. Although this situation can be improved when astaxanthin is prepared as a nanosuspension, the aqueous form is still not as convenient and safe as the dry powder form for storage, transport, and use. The lyophilization process provides better protection for thermosensitive materials, but this leads to collapse and agglomeration between nanoparticles. To improve this situation, appropriate lyophilization protectants are needed to offer support between the nanoparticles, such as sugars, amino acids, and hydroxy alcohols. The purpose of this work is to screen lyophilization protectants by single-factor experiments and response surface optimization experiments and then explore the optimal ratio of compound lyophilization protectants, and finally, make excellent astaxanthin/BSA/chitosan nanosuspension (ABC-NPs) lyophilized powder. The work shows that the optimal ratio of the compounding lyophilization protectant is 0.46% oligomeric mannose, 0.44% maltose, and 0.05% sorbitol (w/v). The ABC-NPs lyophilized powder prepared under the above conditions had a re-soluble particle size of 472 nm, with a ratio of 1.32 to the particle size of the sample before lyophilization. The lyophilized powder was all in the form of a pink layer. The sample was fluffy and dissolved entirely within 10 s by shaking with water. Consequently, it is expected to solve the problem of inconvenient storage and transportation of aqueous drugs and to expand the application of nanomedicine powders and tablets.

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Screening of novel excipients for freeze-dried protein formulations

Cited by 9 publications

References 71 publications

Surface Modifiers on Composite Particles for Direct Compaction

Surface Modifiers on Composite Particles for Direct Compaction

Optimization of Heat-Resistance Technology for a Duck Hepatitis Lyophilized Live Vaccine

Lyoprotectant Formulation and Optimization of the J-Aggregates Astaxanthin/BSA/Chitosan Nanosuspension

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