DESIGN, DEVELOPMENT AND CHARACTERIZATION OF CARFILZOMIB NPDDS Article Swipe
K. Sushma
,
Nuggehalli M. Ravindra
·
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.31032/ijbpas/2021/10.9.1022
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.31032/ijbpas/2021/10.9.1022
Carfilzomib, a recently FDA-approved proteasome inhibitor, has remarkable anti-myeloma (MM) activity.However, its effectiveness is limited by associated severe side-effects, short circulation half-life, and limited solubility.Here, we report the engineering of liposomal carfilzomib nanoparticles to overcome these problems and enhance the therapeutic efficacy of carfilzomib by increasing tumoral drug accumulation while decreasing systemic toxicity.As an effort to formulate more efficient carfilzomib NPs for systemic administration, this research work is an endeavour to optmize the amount of polymer/ stabilizer, concentration of stabilizer and amount of carfilzomib required to get the ideal NPs using three different biodegradable and biocompatible polymers.The ideal particle size, PCL, PLGA and PLA NPs were prepared and selected for the in-vitro and in-vivo study.PLGA carfilzomib nanoparticles were efficiently taken up by MM cells, demonstrated proteasome inhibition, induced apoptosis, and exhibited enhanced cytotoxicity against MM cells.Based on the results it was observed that quality NPs with 100 % EE, high DC and % recovery were obtained using,20 mg of PCL (PCL/F68/05), 100 mg of PLGA (PLGA/F68/09) and 50 mg of PLA (PLA/F68/07) with 0.5 % PF 68 as stabilizer.The reason for high EE in case of the prepared PNPs may be due to low aqueous solubility of carfilzomib, fast rate of precipitation of polymer during preparation and selection of polymer solvent with high vapour pressure and the low viscosity of the internal phase.The prepared PNPs were characterized for their shape and structure using SEM, TEM and AFM.Taken together, this study establishes the successful synthesis of liposomal carfilzomib nanoparticles that demonstrate improved therapeutic index and the potential to improve patient outcome in MM.
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- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.31032/ijbpas/2021/10.9.1022
- https://doi.org/10.31032/ijbpas/2021/10.9.1022
- OA Status
- diamond
- References
- 4
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4200550036
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4200550036Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.31032/ijbpas/2021/10.9.1022Digital Object Identifier
- Title
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DESIGN, DEVELOPMENT AND CHARACTERIZATION OF CARFILZOMIB NPDDSWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2021Year of publication
- Publication date
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2021-09-25Full publication date if available
- Authors
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K. Sushma, Nuggehalli M. RavindraList of authors in order
- Landing page
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https://doi.org/10.31032/ijbpas/2021/10.9.1022Publisher landing page
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https://doi.org/10.31032/ijbpas/2021/10.9.1022Direct link to full text PDF
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YesWhether a free full text is available
- OA status
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diamondOpen access status per OpenAlex
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https://doi.org/10.31032/ijbpas/2021/10.9.1022Direct OA link when available
- Concepts
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Carfilzomib, Characterization (materials science), Medicine, Nanotechnology, Materials science, Multiple myeloma, Internal medicine, Proteasome inhibitorTop concepts (fields/topics) attached by OpenAlex
- Cited by
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0Total citation count in OpenAlex
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4Number of works referenced by this work
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10Other works algorithmically related by OpenAlex
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