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In Vitro and Ex Vivo Evaluations of Lipid Anti-Cancer Nanoformulations: Insights and Assessment of Bioavailability Enhancement

AAPS PharmSciTech volume 17, pages 553–571 (2016)Cite this article

Abstract

Lipid-based nanoformulations have been extensively investigated for improving oral efficacy of plethora of drugs. Chemotherapeutic agents remain a preferred option for effective management of cancer; however, most chemotherapeutic agents suffer from limitation of poor oral bioavailability that is associated with their physicochemical properties. Drug delivery via lipid-based nanosystems possesses strong rational and potential for improving oral bioavailability of such anti-cancer molecules through various mechanisms, viz. improving their gut solubilisation owing to micellization, improving mucosal permeation, improving lymphatic uptake, inhibiting intestinal metabolism and/or inhibiting P-glycoprotein efflux of molecules in the gastrointestinal tract. Various in vitro characterization techniques have been reported in literature that aid in getting insights into mechanisms of lipid-based nanodevices in improving oral efficacy of anti-cancer drugs. The review focuses on different characterization techniques that can be employed for evaluation of lipid-based nanosystems and their role in effective anti-cancer drug delivery.

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Acknowledgments

Authors would like to acknowledge the University Grants Commission for providing fellowship to Dr. Ankitkumar Jain and the Lady Tata Memorial Trust for providing fellowship to Mr. Vivek Dhawan.

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Affiliations

  1. Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai, 400098, India

    Ankitkumar S. Jain, Vivek V. Dhawan & Mangal S. Nagarsenker

  2. INEB–Instituto de Engenharia Biomédica, Universidade do Porto Rua do Campo Alegre, 823 - 4150-180, Porto, Portugal

    Bruno Sarmento

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  1. Ankitkumar S. Jain
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  2. Vivek V. Dhawan
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  4. Mangal S. Nagarsenker
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Correspondence to Mangal S. Nagarsenker.

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Jain, A.S., Dhawan, V.V., Sarmento, B. et al. In Vitro and Ex Vivo Evaluations of Lipid Anti-Cancer Nanoformulations: Insights and Assessment of Bioavailability Enhancement. AAPS PharmSciTech 17, 553–571 (2016). https://doi.org/10.1208/s12249-016-0522-2

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Keywords

  • bioavailability
  • ex vivo
  • in vitro
  • lipid
  • nanosystems