Journal
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
Volume 8, Issue 3, Pages 617-632Publisher
SPRINGER HEIDELBERG
DOI: 10.1007/s13346-018-0498-4
Keywords
Breast cancer; Quality by design (QbD); Mangiferin; Vitamin E TPGS nanomicelles; Self-assembled phospholipidic nano-mixed miceller system (SPNMS); Pharmacokinetics; Bioavailability; P-gp efflux; Cellular uptake
Funding
- University Grant Commission (UGC), New Delhi, India under the RFMS scheme [5-94/2007(BSR)]
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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 N 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 Mg. In a nutshell, vitamin E functionalized SPNMS of Mgf improved the biopharmaceutical performance of Mgf in rats for enhanced anticancer potency.
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