Objective: 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.

Methods: 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 in vitro and in vivo parameters.

Results: Spherical microparticles of 2.98 μm average size were obtained and DSC thermograms provide evidence of trans-resveratrol encapsulation. In vitro and ex vivo drug diffusion studies revealed sustained release profiles. Optimised SLM gel provides optimum antioxidant, tyrosinase inhibition, cytotoxicity in B16F10 melanoma cell line and apoptosis efficacy. In vivo studies on C57BL mice exhibit significant tumour reduction.

Conclusion: Promising role of trans-resveratrol-loaded SLM topical gel in melanoma chemoprevention is proven.

目的：可以通过新颖，生物相容的脂质制剂来实现对患者友好产品的未满足需求，这种脂质制剂可以封装并延长药物的释放时间。这项研究的目的是开发一种商业上可扩展的负载白藜芦醇的固体脂质微颗粒（SLM）局部用凝胶，用于黑色素瘤的化学预防。

方法：进行了制剂前研究，并使用红外光谱和差示扫描量热法（DSC）检查了药物-赋形剂的相互作用。制备负载白藜芦醇的SLM局部凝胶，并通过体外和体内参数进行评估。

结果：获得了平均粒径为2.98μm的球形微粒，DSC热分析图提供了反式白藜芦醇包封的证据。体外和离体药物扩散研究显示了持续释放曲线。优化的SLM凝胶可提供最佳的抗氧化剂，酪氨酸酶抑制作用，B16F10黑色素瘤细胞系的细胞毒性和凋亡功效。对C57BL小鼠的体内研究显示出明显的肿瘤减少。

结论：证实了反式白藜芦醇负载的SLM局部凝胶在黑色素瘤化学预防中的重要作用。