Comparison of physioochcmical characteristics and stability ot'tnrec novel tormulanons or pacutaxcl: Abraxane, manoxei, ana usnexoi rm -...
`
`rage I. on .4
`
`AACR Meeting
`Abstracts Online
`
`HOME HELP FEEDBACK HOW TO CITE ABSTRACTS ARCHIVE CME INFORMATION SEARCH
`
`Cancer Research
`
`Cancer Epidemiology Biomarkers 3. Prevention
`Molecular Cancer Research
`
`Cancer Prevention Journals Portal
`Annuai Meeting Education Book
`
`Clinical Cancer Research
`
`Molecular Cancer Therapeutics
`Cancer Prevention Research
`
`Cancer Reviews Online
`Meeting Abstracts Oniine
`
`Institution: IHCYTE CORPORAHON | Sign In via User NamegPasswwd
`
`QUICK SEARCH:
`
`[advance
`
`{RI-film”
`El '9"
`
`Keywordts):
`
`99th AACR Annual Meeting-- Apr 12-16, 2008; San Diego, CA
`
`This Article
`
`,........W Services I
`
`Drug Delivery and Targeting: Poster Presentations
`Proffered Abstracts
`'
`
`Abstract #5622
`
`Comparison of physicochemical
`characteristics and stability of three novel
`formulations of paclitaxel: Abraxane,
`Nanoxel, and Genexol PM
`
`I Simil rartici s n if
`ur al
`as Download to citag'gn manager
`600319 Scholar
`
`? _L_s_v_miceb R.9_.._nN-
`I Artiglgg by; Desai, N.
`
`Pqu
`I
`1g,_r'j;igle§ 91 Ron, N.
`0,3,, "-
`, Mich,
`
`Niles Ron, Jon Cordia, Andrew Yang, Sherry Ci, Phjthi Nguyen, Melissa Hughs and Neil Desai
`
`Abraxis Bioscience, Inc., Los Angeles, CA
`
`Background: Abraxane (Abraxis BioScicncc, Inc, Los Angclcs, CA, approved in USA and Canada),
`
`Nanoer (Dabur Pharma, H.P., India, approved in India), and Gencxol PM (Samyang Pharmaceuticals,
`Seoul, Korea, approved in Korea) are 3 commercially approved, novel formulations of paclitaxel.
`
`Abraxanc consists of albumin-bound injectablc nan0particlcs of paclitaxcl, while Gcncxol and Nanoxel
`(utilizing cosolvents) are polymeric-micellc formulations. Abraxane and Genexol are lyophilized
`
`products approved for 25°C :I: 2°C storage, while Nanoer is a liquid formulation approved for 2-8°C
`
`storage. This study investigated the physicochemical characteristics and short-term stability of the 3
`
`products under recommended clinical use conditions and under accelerated conditions.
`
`Methods: The drugs were reconstituted and prepared per the instructions provided in the respective
`
`package inserts. Abraxane and Genexol were reconstituted using the recommended saline diluent, while
`
`Nanoer was mixed and diluted in 10% dextrose. Each drug was reconstituted to 0.7 mg/mL and 5
`
`mg/mL. Physical stability was monitored both visually and microscopically; particle size was measured
`and monitored over time at room temperature (RT, measured to be 23°C) and 40°C using photon
`
`correlation spectroscopy (PCS) (Zetasizer 3000, Malvcrn, UK). Chemical purity was measured by
`reduced reversed-phase HPLC (Shimadzu Scientific Instnnnents, MD).
`Results: Following reconstitution, Abraxane was determined to be stable both physically and chemically
`
`Abraxis EX2022
`
`Actavis LLC v. Abraxis Bioscience, LLC
`|PR2017-01100
`
`

`

`Comparison ofphysioochemical characteristics and‘stability of three novel formulations ofpsclitaxel: Abraxane, Nanoer, and Genexol PM -...
`
`Page 2 of 2
`
`at RT and 40°C over 24 hrs, with no evidence ofnanoparticle size growth at either 0.7_ mg/mL or 5
`mg/mL. While reconstituted Genexol was stable at RT over 24 hrs, micelle instability resulting in
`
`precipitation of paclitaxel in the form of large needle-like crystals for both 0.7 mg/mL and 5 mg/mL
`
`formulations was seen betWeen 2 to 4 hrs at 40°C. These observations were confirmed using orthogonal
`
`techniques, visual assessment from photomicrographs, and PCS particle size measurement. For Nanoer
`
`at 0.7 mg/mL, a minor, but consistent, increase in particle size was observed at RT over 24 hrs.
`
`However, significant aggregation, particle-size growth, and crystallization were seen within 4 hrs at 40°
`
`C. HPLC data comparing pre- and post-filtration confirmed that the crystal formation for both Nanoer
`
`and Gencxol resulted from paclitaxel precipitation and aggregation, In addition, analytical results
`
`showed that Nanoer had slightly lower paclitaxel purity as compared to either Abraxane or Genexol.
`
`Conclusions: Nanoparticle albumin-bound paclitaxel, Abraxane, showed excellent physicochemical
`
`stability as compared to the micellar formulations, Nanoer and Genexol. Particle size growth and
`
`crystal formation were readily apparent in Nanoer and Genexol, especially in the short term under
`accelerated conditions.
`
`This Article
`
`Services
`
`I Similar articles In this journal
`I Downloag to citation manager
`
`Google Scholar
`
`H A '
`
`fish
`
`n N.
`
`I Articles by, Qgsai. N.
`
`PubMed
`
`H Articles by RonI N.
`'11 Articlesb Desai N.
`
`