Development and preclinical evaluation of microneedle-assisted resveratrol loaded nanostructured lipid carriers for localized delivery to breast cancer therapy.
Development and preclinical evaluation of microneedle-assisted resveratrol loaded nanostructured lipid carriers for localized delivery to breast cancer therapy.
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DOI：
10.1016/j.ijpharm.2021.120877
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发表时间：
2021-09-05
影响因子：
5.8
通讯作者：
Nayak UY
中科院分区：
文献类型：
--
作者：
Gadag S;Narayan R;Nayak AS;Catalina Ardila D;Sant S;Nayak Y;Garg S;Nayak UY
白藜芦醇（Resveratrol，RVT）是一种有效的抗肿瘤植物化学物质，在乳腺癌治疗中显示出良好的应用前景。然而，其半衰期短和生物利用度低是其有效使用的主要障碍。在这项研究中，我们开发了RVT的纳米结构脂质载体（NLC），以便使用微针阵列将药物局部递送到乳腺组织，以提高有效性。使用实验设计方法优化NLC，并表征其粒径、多分散性指数、zeta电位和包封率。与纯RVT相比，使用微针阵列1200递送的RVT-NLC显示出RVT穿过皮肤的更高渗透性，具有更低的皮肤保留。此外，与纯RVT相比，RVT-NLC对MDA-MB-231乳腺癌细胞系显示出更高的抗癌活性和增强的内化。此外，发现RVT-NLC抑制MDA-MB-231乳腺癌细胞系的迁移。大鼠临床前研究表明，与口服纯RVT相比，通过微针递送的RVT-NLC显示出Cmax、Tmax和AUC 0-inf显著增加，并且在乳腺组织中的定位更高。这些结果表明，通过微针阵列系统施用RVT-NLC是局部递送RVT用于乳腺癌治疗的有效策略。
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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