In the present investigation, imiquimod (IMQ) was coupled to oleic acid (OLA; IMQ-OLA) to synthesise prodrug to reduce crystallinity that later amalgamated with oil-in-water (o/w) emulsion cream (IMQ-OLA cream) for the treatment of melanoma tumour. The synthesis of IMQ-OLA prodrug was verified by FT-IR, ¹HNMR and mass spectroscopy. The crystalline lattice of IMQ was transformed to somewhat amorphous structure in IMQ-OLA prodrug. IMQ-OLA cream retained 35.6% of IMQ within skin, significantly (p < 0.05) higher than 22.3% and 10.6% retained by marketed IMQ cream and IMQ solution, respectively. IMQ-OLA cream suppressed the melanoma tumour to 70.3 mm³ in C57BL6J mice as compared to 72.6 mm³ tumour, reduced by marketed IMQ cream with no significant difference (p > 0.05) at day 32 over 17-day period of treatment. IMQ-OLA cream followed the multiple mechanisms of cell death. IMQ-OLA cream warrants further in depth investigations for translating in to a clinically viable topical dermal product.

在本研究中，将咪喹莫特（IMQ）与油酸（OLA; IMQ-OLA）偶联以合成前药，以降低结晶度，随后将其与水包油（o / w）乳化霜（IMQ-OLA霜）合并使用。黑色素瘤的治疗。IMQ-OLA前药的合成已通过FT-IR，¹ HNMR和质谱进行了验证。IMQ-OLA前药中的IMQ晶格转变为某种无定形结构。IMQ-OLA乳霜在皮肤内保留IMQ的35.6％，显着（p  <0.05）分别高于市售IMQ乳霜和IMQ溶液的22.3％和10.6％。IMQ-OLA霜将C57BL6J小鼠的黑色素瘤肿瘤抑制为70.3 mm ³，而72.6 mm ³在上市 后17天的第32天，通过市售的IMQ乳膏降低了肿瘤，无显着差异（p > 0.05）。IMQ-OLA霜遵循多种细胞死亡机制。IMQ-OLA乳膏值得进一步深入研究，以转化为临床上可行的局部皮肤产品。