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经皮传递白藜芦醇包封脂质体制剂用于黑色素瘤化学预防。

Skin delivery of resveratrol encapsulated lipidic formulation for melanoma chemoprevention.

机构信息

Department of Pharmaceutics, SVKM's Dr Bhanuben Nanavati College of Pharmacy , Mumbai , India.

Abbott Healthcare Pvt. Ltd., MIDC , Mumbai , India.

出版信息

J Microencapsul. 2019 Sep;36(6):535-551. doi: 10.1080/02652048.2019.1649481. Epub 2019 Aug 8.

DOI:10.1080/02652048.2019.1649481
PMID:31353993
Abstract

An unmet need for patient friendly products can be achieved with novel, biocompatible lipidic formulations which encapsulate and prolong release of medicaments. The aim of this study was to develop a commercially scalable resveratrol-loaded solid-lipid microparticulate (SLM) topical gel for melanoma chemoprevention. Preformulation studies were conducted and drug-excipient interactions examined using infra-red spectroscopy and differential scanning calorimetry (DSC). Resveratrol-loaded SLM topical gel was prepared and evaluated by and parameters. Spherical microparticles of 2.98 μm average size were obtained and DSC thermograms provide evidence of trans-resveratrol encapsulation. and drug diffusion studies revealed sustained release profiles. Optimised SLM gel provides optimum antioxidant, tyrosinase inhibition, cytotoxicity in B16F10 melanoma cell line and apoptosis efficacy. studies on C57BL mice exhibit significant tumour reduction. Promising role of trans-resveratrol-loaded SLM topical gel in melanoma chemoprevention is proven.

摘要

具有生物相容性的新型脂质体制剂可以满足患者对药物的需求,这些制剂可以包裹药物并延长其释放时间。本研究旨在开发一种可商业化的、载有白藜芦醇的固体脂质微球(SLM)局部凝胶,用于预防黑色素瘤。通过红外光谱和差示扫描量热法(DSC)对预配方研究和药物-赋形剂相互作用进行了研究。通过 和 参数来制备和评价载有白藜芦醇的 SLM 局部凝胶。获得了平均粒径为 2.98 μm 的球形微球,DSC 热图谱证明了反式白藜芦醇的包封。 和 药物扩散研究显示出持续释放的特性。优化后的 SLM 凝胶具有最佳的抗氧化、酪氨酸酶抑制、对 B16F10 黑色素瘤细胞系的细胞毒性和凋亡功效。C57BL 小鼠的研究表明肿瘤明显减少。证明了载有反式白藜芦醇的 SLM 局部凝胶在预防黑色素瘤中的应用具有广阔的前景。

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