TY - JOUR
T1 - Design, development and evaluation of Resveratrol transdermal patches for breast cancer therapy
AU - Gadag, Shivaprasad
AU - Narayan, Reema
AU - Nayak, Yogendra
AU - Garg, Sanjay
AU - Nayak, Usha Y.
N1 - 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. Authors are thankful to Dr Pritesh Bhat and Dr Sudharsan Pandiyan, Schrödinger, Bengaluru, India, for their guidance in computational studies.
Funding Information:
This work was supported by the Science and Engineering Research Board, Department of Science and Technology, New Delhi, India (EMR/2016/007006).
Publisher Copyright:
© 2022 Elsevier B.V.
PY - 2023/2/5
Y1 - 2023/2/5
N2 - Resveratrol (RVT) is a polyphenolic phytoestrogen which has shown antiproliferative activity in breast cancer. However, its low bioavailability and short half-life have restricted its use. The current study aimed to develop transdermal patches of RVT and evaluate its site-specific delivery for breast cancer therapy. Different penetration enhancers were screened using a computational tool, quantitative structure propery relationship (QSPR). The best permeation of RVT was observed in a patch comprising hydroxypropyl methylcellulose (HPMC) E15LV: HPMC-K4M: polyvinyl pyrrolidone (PVP) K30 in the ratio of 3:1:2 as release controlling polymers with Glycerol:Capryol 90 (4:1) as penetration enhancer and plasticizer. To assess the localized delivery of RVT, the patch was applied to the breast of female rats. Higher breast tissue disposition with lower systemic concentration was observed compared to oral administration, demonstrated by increased AUC and MRT. Further, the optimized RVT patches were tested in 7,12-Dimethylbenz[a]anthracene (DMBA) induced rat mammary cancer. Compared to oral RVT, the application of RVT tansdermal patches significantly reduced the tumor volume and serum CA 15–3, a cancer biomarker. Thus, the RVT transdermal patch may be a viable approach for ensuring high local concentration of drug for site-specific delivery in breast cancer therapy.
AB - Resveratrol (RVT) is a polyphenolic phytoestrogen which has shown antiproliferative activity in breast cancer. However, its low bioavailability and short half-life have restricted its use. The current study aimed to develop transdermal patches of RVT and evaluate its site-specific delivery for breast cancer therapy. Different penetration enhancers were screened using a computational tool, quantitative structure propery relationship (QSPR). The best permeation of RVT was observed in a patch comprising hydroxypropyl methylcellulose (HPMC) E15LV: HPMC-K4M: polyvinyl pyrrolidone (PVP) K30 in the ratio of 3:1:2 as release controlling polymers with Glycerol:Capryol 90 (4:1) as penetration enhancer and plasticizer. To assess the localized delivery of RVT, the patch was applied to the breast of female rats. Higher breast tissue disposition with lower systemic concentration was observed compared to oral administration, demonstrated by increased AUC and MRT. Further, the optimized RVT patches were tested in 7,12-Dimethylbenz[a]anthracene (DMBA) induced rat mammary cancer. Compared to oral RVT, the application of RVT tansdermal patches significantly reduced the tumor volume and serum CA 15–3, a cancer biomarker. Thus, the RVT transdermal patch may be a viable approach for ensuring high local concentration of drug for site-specific delivery in breast cancer therapy.
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U2 - 10.1016/j.ijpharm.2022.122558
DO - 10.1016/j.ijpharm.2022.122558
M3 - Article
C2 - 36592891
AN - SCOPUS:85146009640
SN - 0378-5173
VL - 632
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
M1 - 122558
ER -
