Phospholipid-Based Topical Nano-Hydrogel of Mangiferin: Enhanced Topical Delivery and Improved Dermatokinetics

Mangiferin is a herbal drug that has proven anticancer potential. Owing to its lower aqueous solubility and poor oral bioavailability, the full pharmacological potential of this bioactive drug has not fully been explored. In the present study, phospholipid-based microemulsion systems were developed to bypass oral delivery. The globule size of the developed nanocarriers was less than 150 nm and the drug entrapment was >75% with a drug loading ~25%. The developed system offered a controlled release pattern following the Fickian drug release. This enhanced mangiferin’s in vitro anticancer activity by four-fold, the cellular uptake was observed to be improved by three-fold on the MCF-7 cells. Ex vivo dermatokinetic studies showed substantial topical bioavailability with a prolonged residence time. The findings provide a simple technique to administer mangiferin via a topical route promising a safer, topically bioavailable and effective treatment option for breast cancer. Such scalable carriers with immense topical delivery potential may provide a better option for present-day topical products of a conventional nature.

4.1. Materials

Mangiferin and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) were purchased from Sigma-Aldrich, St. Louis, MO, USA. The hydrochloric acid, chloroform, isopropyl palmitate (IPP) and methanol was obtained from SDFCL Chem. Limited, India, whereas the buffer reagents, i.e., disodium hydrogen phosphate, sodium chloride and potassium dihydrogen phosphate were supplied by CDH Pvt. Ltd., New Delhi, India. Gelucire 44/14, Labrasol ALF and Labrafil M 1944 CS were procured from Gattefossè, Lyon, France. The acetonitrile was obtained from Spectrochem, Mumbai, India. Phospholipid (Phospholipon 90 G) was procured from Lipoid, Ludwigshafen, Germany.

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Alkholifi, F.K.; Alam, A.; Foudah, A.I.; Yusufoglu, H.S. Phospholipid-Based Topical Nano-Hydrogel of Mangiferin: Enhanced Topical Delivery and Improved Dermatokinetics. Gels 2023, 9, 178.
https://doi.org/10.3390/gels9030178

excipients formulation