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Chitosan Coated Luteolin Nanostructured Lipid Carriers: Optimization, In Vitro-Ex Vivo Assessments and Cytotoxicity Study in Breast Cancer Cells

Sadaf Jamal Gilani, May Bin‐Jumah, Md. Rizwanullah, Syed Sarim Imam, Khalid Imtiyaz, Sultan Alshehri, Mohd. Moshahid Alam Rizvi

2021Coatings63 citationsDOIOpen Access PDF

Abstract

In the present study, luteolin (LTN)-encapsulated chitosan (CS) coated nanostructured lipid carriers (NLCs) were formulated using the melt emulsification ultrasonication technique. NLCs were optimized by using the 33-QbD approach for improved in vitro efficacy against breast cancer cell lines. The optimized LTN-CS-NLCs were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The prepared LTN-CS-NLCs showed particle size (PS), polydispersity index (PDI), and entrapment efficiency (%EE) in the range between 101.25 nm and 158.04 nm, 0.11 and 0.20, and 65.55% and 95.37%, respectively. Coating of NLCs with CS significantly increased the particle size, encapsulation efficiency, and zeta potential changes positively. Moreover, slow-release rate of LTN was achieved during 24 h of study for LTN-CS-NLCs. In addition, optimized LTN-CS-NLCs showed significantly higher mucoadhesion, gastrointestinal stability, and intestinal permeation compared to non-coated LTN-NLCs and LTN suspension. Furthermore, LTN-CS-NLCs showed statistically enhanced antioxidant potential as well as dose and time-dependent cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated LTN-NLCs and pure LTN. On the basis of the above findings, it may be stated that chitosan-coated LTN-NLCs represents a great potential for breast cancer management.

Topics & Concepts

Zeta potentialCytotoxicityChitosanIn vivoSonicationChemistryDispersityParticle sizeIn vitroEx vivoPermeationBiophysicsNanotechnologyNuclear chemistryMaterials scienceNanoparticleBiochemistryChromatographyOrganic chemistryBiologyBiotechnologyMembranePhysical chemistryAdvancements in Transdermal Drug DeliveryNanoparticle-Based Drug DeliveryAdvanced Drug Delivery Systems