Gadag, S.Narayan, R.Nayak, A.S.Catalina Ardila, D.Sant, S.Yogendra, Y.Garg, S.Nayak, U.Y.2026-02-052021International Journal of Pharmaceutics, 2021, 606, , pp. -3785173https://doi.org/10.1016/j.ijpharm.2021.120877https://idr.nitk.ac.in/handle/123456789/23082Resveratrol (RVT) is one of the potent anticancer phytochemicals which has shown promising potential for breast cancer therapy. However, its short half-life and low bioavailability is a major hurdle in its effective use. In this study, we have developed nanostructured lipid carriers (NLCs) of RVT to enable localized delivery of the drug to the breast tissues using microneedle arrays to improve effectiveness. The NLCs were optimized using the Design of Experiments approach and characterized for their particle size, polydispersity index, zeta potential and entrapment efficiency. The RVT-NLCs delivered using microneedle array 1200 showed a higher permeation of RVT across the skin with lower skin retention compared to pure RVT. Further, RVT-NLCs showed higher anticancer activity on MDA-MB-231 breast cancer cell lines and enhanced internalization compared to pure RVT. Moreover, the RVT-NLCs were found to inhibit the migration of MDA-MB-231 breast cancer cell lines. Preclinical studies in rats showed that RVT-NLCs delivered via microneedles demonstrated a remarkable increase in the C<inf>max</inf>, T<inf>max</inf> and AUC<inf>0-inf</inf>, and a higher localization in breast tissue compared to pure RVT administered orally. These results suggests that the RVT-NLCs administered by microneedle array system is an effective strategy for the local delivery of RVT for breast cancer therapy. © 2021 Elsevier B.V.lipid nanoparticleresveratroldrug carrierlipidnanomaterialanimal cellanimal experimentanimal modelanimal tissueantineoplastic activityarea under the curveArticlebreast cancerbreast tissuecancer therapycontrolled studydispersitydrug blood leveldrug delivery systemdrug dosage form comparisondrug half lifedrug retentionelimination rate constantfemaleIC50in vitro studyinternalization (cell)maximum concentrationMDA-MB-231 cell linemean residence timemigration inhibitionnonhumanparticle sizeplasma concentration-time curvepreclinical studyrattime to maximum plasma concentrationtissue distributionzeta potentialanimalneoplasmAnimalsDrug CarriersDrug Delivery SystemsLipidsNanostructuresNeoplasmsParticle SizeRatsResveratrol