The stabilization of biopharmaceuticals: current understanding and future perspectives

Song, Jae Geun; Lee, Sang Hoon; Han, Hyo-Kyung

doi:10.1007/s40005-017-0341-9

Cited by 24 publications

(5 citation statements)

References 237 publications

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“…Various physical instabilities, such as unfolding, adsorption, denaturation, aggregation, and precipitation, may occur during the drying process. Deamination, oxidation, β-elimination, hydrolysis, racemization, isomerization, and disulfide exchange are irreversible reactions that are considered chemical degradations for biopharmaceuticals [ 71 , 72 ]. Physicochemical parameters such as moisture content, temperature, crystallinity of the formulation, and additives have a significant impact on these unfavorable reactions [ 20 ].…”

Section: Stabilizers For Dried-powder Protein Formulationsmentioning

confidence: 99%

Drying Technologies for the Stability and Bioavailability of Biopharmaceuticals

et al. 2018

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Solid dosage forms of biopharmaceuticals such as therapeutic proteins could provide enhanced bioavailability, improved storage stability, as well as expanded alternatives to parenteral administration. Although numerous drying methods have been used for preparing dried protein powders, choosing a suitable drying technique remains a challenge. In this review, the most frequent drying methods, such as freeze drying, spray drying, spray freeze drying, and supercritical fluid drying, for improving the stability and bioavailability of therapeutic proteins, are discussed. These technologies can prepare protein formulations for different applications as they produce particles with different sizes and morphologies. Proper drying methods are chosen, and the critical process parameters are optimized based on the proposed route of drug administration and the required pharmacokinetics. In an optimized drying procedure, the screening of formulations according to their protein properties is performed to prepare a stable protein formulation for various delivery systems, including pulmonary, nasal, and sustained-release applications.

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Section: Stabilizers For Dried-powder Protein Formulationsmentioning

confidence: 99%

Drying Technologies for the Stability and Bioavailability of Biopharmaceuticals

et al. 2018

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“…The therapeutic use of biomolecules has been substantially increased by the development of biotechnology techniques, and various peptides and proteins have been shown to have therapeutic potential against various diseases. However, these biomolecules have therapeutic limitations owing to chemical and physical instability, high susceptibility to proteolytic degradation, and short circulation half-life requiring multiple injections (Mundargi et al 2008;Song et al 2017). Several strategies for sustained parenteral form and alternative administration route of drugs have been suggested as solutions to the therapeutic limitations of biomolecules (Shire et al 2004;Tyler et al 2016).…”

Section: Protein and Peptide Deliverymentioning

confidence: 99%

Poly(lactic acid)/poly(lactic-co-glycolic acid) particulate carriers for pulmonary drug delivery

Emami

Yazdi

2019

J. Pharm. Investig.

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Background Pulmonary route is an attractive target for both systemic and local drug delivery, with the advantages of a large surface area, rich blood supply, and absence of first-pass metabolism. Numerous polymeric micro/nanoparticles have been designed and studied for controlled and targeted drug delivery to the lung. Area covered Among the natural and synthetic polymers for polymeric particles, poly(lactic acid) (PLA) and poly(lacticco-glycolic acid) (PLGA) have been widely used for the delivery of anti-cancer agents, anti-inflammatory drugs, vaccines, peptides, and proteins because of their highly biocompatible and biodegradable properties. This review focuses on the characteristics of PLA/PLGA particles as carriers of drugs for efficient delivery to the lung. Furthermore, the manufacturing techniques of the polymeric particles, and their applications for inhalation therapy were discussed. Expert opinion Compared to other carriers including liposomes, PLA/PLGA particles present a high structural integrity providing enhanced stability, higher drug loading, and prolonged drug release. Adequately designed and engineered polymeric particles can contribute to a desirable pulmonary drug delivery characterized by a sustained drug release, prolonged drug action, reduction in the therapeutic dose, and improved patient compliance.

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“…Due to the important effect on both the physical and chemical stability of proteins, pH is one of the critical factors in formulation of proteins as well as stability in gastric pH of protein drugs is very important. Generally, buffer systems could mediate protein stabilization depending on proper pH ranges for each protein [52]. However, it is suggested that proliposomes are stable in various pH conditions of gastrointestinal tract.…”

Section: Resultsmentioning

confidence: 99%

Optimization of Polyarginine-Conjugated PEG Lipid Grafted Proliposome Formulation for Enhanced Cellular Association of a Protein Drug

et al. 2019

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The purpose of this study was to develop an oral proliposomal powder of protein using poly-l-arginine-conjugated 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) (DSPE-PEG) (PLD) for enhancing cellular association upon reconstitution and to compare its effects with a non-grafted and PEGylated formulation. Cationic proliposome (CATL), PLD-grafted CATL (PLD-CATL), PEGylated CATL (PEG CATL), and PLD grafted-PEG CATL (PLD-PEG CATL) were prepared and compared. Successful conjugation between poly-l-arginine and DSPE-PEG was confirmed by 1H NMR and FT-IR. PLD was successfully grafted onto the proliposomal powder during the slurry process. Although reconstituted liposomal sizes of CATL and PLD-CATL were increased by agglomeration, PEGylation reduced the agglomeration and increased the encapsulation. The viabilities of cells treated with both CATL and PLD-CATL formulations were low but increased following PEGylation. With regard to cellular association, PLD-CATL enhanced cellular association/uptake more rapidly than did CATL. Upon PEGylation, PEG CATL showed a lower level of cellular association/uptake compared with CATL while PLD-PEG CATL did not exhibit the rapid cellular association/uptake as seen with PLD-CATL. However, PLD-PEG CATL still enhanced the higher cellular association/uptake than PEG CATL did without PLD. In conclusion, proliposomes with PLD could accelerate cellular association/uptake but also caused high cellular toxicity. PEGylation reduced cellular toxicity and also changed the cellular association pattern of the PLD formulation.

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The stabilization of biopharmaceuticals: current understanding and future perspectives

Cited by 24 publications

References 237 publications

Drying Technologies for the Stability and Bioavailability of Biopharmaceuticals

Drying Technologies for the Stability and Bioavailability of Biopharmaceuticals

Poly(lactic acid)/poly(lactic-co-glycolic acid) particulate carriers for pulmonary drug delivery

Optimization of Polyarginine-Conjugated PEG Lipid Grafted Proliposome Formulation for Enhanced Cellular Association of a Protein Drug

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