TY - JOUR
T1 - Development and preclinical evaluation of microneedle-assisted resveratrol loaded nanostructured lipid carriers for localized delivery to breast cancer therapy
AU - Gadag, Shivaprasad
AU - Narayan, Reema
AU - Nayak, Archana S.
AU - Catalina Ardila, Diana
AU - Sant, Shilpa
AU - Nayak, Yogendra
AU - Garg, Sanjay
AU - Nayak, Usha Y.
N1 - Funding Information:
This project was supported by the Science and Engineering Research Board, Dept. of Science and Technology, New Delhi, India (EMR/2016/007006). This work is also supported by the National Institute of Health (NIH R37CA232209) award to Dr Shilpa Sant.
Funding Information:
The authors are thankful to Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India for providing the necessary facilities for the research work, and to DST-SAIF, Cochin, India for TEM analysis. We are grateful to Ms. Tianling Hou for the training on the handling of cell lines. This project was supported by the Science and Engineering Research Board, Dept. of Science and Technology, New Delhi, India (EMR/2016/007006). This work is also supported by the National Institute of Health (NIH R37CA232209) award to Dr Shilpa Sant.
Publisher Copyright:
© 2021 Elsevier B.V.
PY - 2021/9/5
Y1 - 2021/9/5
N2 - Resveratrol (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 Cmax, Tmax and AUC0-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.
AB - Resveratrol (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 Cmax, Tmax and AUC0-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.
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U2 - 10.1016/j.ijpharm.2021.120877
DO - 10.1016/j.ijpharm.2021.120877
M3 - Article
AN - SCOPUS:85111264491
SN - 0378-5173
VL - 606
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
M1 - 120877
ER -
