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Research Article

Polymeric micelles of suberoylanilide hydroxamic acid to enhance the anticancer potential in vitro and in vivo

    Sri Vishnu Kiran Rompicharla

    Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India

    These authors contributed equally and should be considered first authors

    Search for more papers by this author

    ,
    Prakruti Trivedi

    Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India

    These authors contributed equally and should be considered first authors

    Search for more papers by this author

    ,
    Preeti Kumari

    Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India

    ,
    Pratyusha Ghanta

    Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India

    ,
    Balaram Ghosh

    Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India

    &
    Swati Biswas

    *Author for correspondence:

    E-mail Address: swati.biswas@hyderabad.bits-pilani.ac.in

    Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India

    Published Online:https://doi.org/10.2217/nnm-2016-0321

    Aim: To improve the bioavailability and anticancer potential of suberoylanilide hydroxamic acid (SAHA) by developing a drug-loaded polymeric nanomicellar system. Methods: SAHA-loaded Poly(ethylene glycol)-block-poly(caprolactone) (PEG-PCL) micelles were developed, and physico-chemically characterized. In vitro cellular uptake, viability and apoptosis-inducing ability of the SAHA-PEG-PCL micelles were investigated. In vivo anticancer activity was evaluated in C57BL/6 mice-bearing tumor. Results: The SAHA-PEG-PCL micelles had optimum size (∼130 nm) with an entrapment efficiency of approximately 67%. The SAHA-PEG-PCL induced stronger cell cycle arrest in G2/M phase leading to higher rate of apoptosis compared to free SAHA. SAHA-PEG-PCL demonstrated significant tumor suppression compared to free SAHA in vivo. Conclusion: The physicochemical properties and the antitumor efficacy of SAHA were improved by encapsulating in polymeric micelles.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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