Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems

Rajneet Kaur Khurana, Balan Louis Gaspar, Gail Welsby, O P Katare, Kamalinder K Singh, Bhupinder Singh

Research output: Contribution to journalArticle

7 Citations (Scopus)
73 Downloads (Pure)

Abstract

The current research work encompasses the development, characterization, and evaluation of self-assembled phospholipidic nano-mixed miceller system (SPNMS) of a poorly soluble BCS Class IV xanthone bioactive, mangiferin (Mgf) functionalized with co-delivery of vitamin E TPGS. Systematic optimization using I-optimal design yielded self-assembled phospholipidic nano-micelles with a particle size of < 60 nm and > 80% of drug release in 15 min. The cytotoxicity and cellular uptake studies performed using MCF-7 and MDA-MB-231 cell lines demonstrated greater kill and faster cellular uptake. The ex vivo intestinal permeability revealed higher lymphatic uptake, while in situ perfusion and in vivo pharmacokinetic studies indicated nearly 6.6- and 3.0-folds augmentation in permeability and bioavailability of Mgf. In a nutshell, vitamin E functionalized SPNMS of Mgf improved the biopharmaceutical performance of Mgf in rats for enhanced anticancer potency.

Original languageEnglish
Pages (from-to)617-632
Number of pages16
JournalDrug Delivery and Translational Research
Volume8
Issue number3
Early online date10 Apr 2018
DOIs
Publication statusPublished - 30 Jun 2018

Keywords

  • Bioavailability
  • Breast cancer
  • Cellular uptake
  • Mangiferin
  • P-gp efflux
  • Pharmacokinetics
  • Quality bydesign (QbD)
  • Self-assembled phospholipidic nano-mixed miceller system (SPNMS)
  • Vitamin E TPGS nanomicelles

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