Drying technology strategies for colon-targeted oral delivery of biopharmaceuticals

Vass, Panna; Démuth, Balázs; Hirsch, Edit; Nagy, Brigitta; Andersen, Sune Klint; Vígh, Tamás; Verreck, Geert; Csontos, István; Nagy, Zsombor Kristóf; Marosi, György

doi:10.1016/j.jconrel.2019.01.023

Cited by 85 publications

(51 citation statements)

References 191 publications

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“…[ 6 ] So far, over 65 nanomedicines in the form of liposomes, [ 7 ] nanocrystals, [ 8 ] inorganic nanoparticles, [ 7 ] polymeric nanoparticles, [ 9 ] nanocapsules, [ 10 ] and protein nanoparticles [ 7 ] are approved for clinical use ( Table 2 and Figure ). Various approaches have been used to engineer biopharmaceuticals into micro‐ or nanoscale structures to enhance their therapeutic potency, including physical fabrication, [ 11 ] covalent molecular modification, [ 12 ] encapsulation by biodegradable hydrogels based on natural and synthetic polymers, [ 13 ] and nanostructuring processes. [ 1b,14 ] Integration of these nanoscale systems with biopharmaceuticals offers excellent promise for future drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Nanocarrier‐Mediated Cytosolic Delivery of Biopharmaceuticals

Xing

Wang

et al. 2020

Adv Funct Materials

125

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Biopharmaceuticals have emerged to play a vital role in disease treatment and have shown promise in the rapidly expanding pharmaceutical market due to their high specificity and potency. However, the delivery of these biologics is hindered by various physiological barriers, owing primarily to the poor cell membrane permeability, low stability, and increased size of biologic agents. Since many biological drugs are intended to function by interacting with intracellular targets, their delivery to intracellular targets is of high relevance. In this review, the authors summarize and discuss the use of nanocarriers for intracellular delivery of biopharmaceuticals via endosomal escape and, especially, the routes of direct cytosolic delivery by means including the caveolae‐mediated pathway, contact release, intermembrane transfer, membrane fusion, direct translocation, and membrane disruption. Strategies with high potential for translation are highlighted. Finally, the authors conclude with the clinical translation of promising carriers and future perspectives.

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Section: Introductionmentioning

confidence: 99%

Nanocarrier‐Mediated Cytosolic Delivery of Biopharmaceuticals

Xing

Wang

et al. 2020

Adv Funct Materials

125

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“…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.…”

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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“…The similar encapsulation efficiency values of EE% (i.e., 98.1 ± 6.4% and 97.5 ± 7.1% for N1 and N2, respectively) suggest that the electrospinning is essentially a physical drying process without any drug loss to the environment, although reactive electrospinning has been reported in literature [ 52 , 53 , 54 ]. Drying at an extremely rapid rate should be a unique advantage of electrospinning over many other bottom-up methods used for creating nanomedicines [ 55 , 56 ].…”

Section: Resultsmentioning

confidence: 99%

Energy-Saving Electrospinning with a Concentric Teflon-Core Rod Spinneret to Create Medicated Nanofibers

et al. 2020

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Although electrospun nanofibers are expanding their potential commercial applications in various fields, the issue of energy savings, which are important for cost reduction and technological feasibility, has received little attention to date. In this study, a concentric spinneret with a solid Teflon-core rod was developed to implement an energy-saving electrospinning process. Ketoprofen and polyvinylpyrrolidone (PVP) were used as a model of a poorly water-soluble drug and a filament-forming matrix, respectively, to obtain nanofibrous films via traditional tube-based electrospinning and the proposed solid rod-based electrospinning method. The functional performances of the films were compared through in vitro drug dissolution experiments and ex vivo sublingual drug permeation tests. Results demonstrated that both types of nanofibrous films do not significantly differ in terms of medical applications. However, the new process required only 53.9% of the energy consumed by the traditional method. This achievement was realized by the introduction of several engineering improvements based on applied surface modifications, such as a less energy dispersive air-epoxy resin surface of the spinneret, a free liquid guiding without backward capillary force of the Teflon-core rod, and a smaller fluid–Teflon adhesive force. Other non-conductive materials could be explored to develop new spinnerets offering good engineering control and energy savings to obtain low-cost electrospun polymeric nanofibers.

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Drying technology strategies for colon-targeted oral delivery of biopharmaceuticals

Cited by 85 publications

References 191 publications

Nanocarrier‐Mediated Cytosolic Delivery of Biopharmaceuticals

Nanocarrier‐Mediated Cytosolic Delivery of Biopharmaceuticals

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

Energy-Saving Electrospinning with a Concentric Teflon-Core Rod Spinneret to Create Medicated Nanofibers

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