目的 评价异补骨脂素纳米结构脂质载体（IPRN-NLC）的体外溶出行为，并考察其对小鼠黑色素瘤B₁₆F₁₀细胞增殖、黑色素合成及酪氨酸酶活性的影响。方法 采用透析袋法测定IPRN-NLC在72 h内的累积溶出量并绘制溶出曲线，MTT法测定B₁₆F₁₀细胞增殖情况，多巴氧化法测定酪氨酸酶活性，GENMED细胞黑色素含量比色法测定黑色素合成。结果 在72 h时体外累积溶出量IPRN-NLC为67.31%，IPRN-物理混合物为90.30%，IPRN-DMSO为98.67%，IPRN-混悬液为53.34%。IPRN在一定质量浓度范围内可以促进B₁₆F₁₀细胞增殖，提高酪氨酸酶活性，增加黑色素的合成，且同质量浓度的IPRN-NLC对B₁₆F₁₀的作用显著高于IPRN溶液（P<0.05）。结论 IPRN-NLC不仅具有缓释作用，还可以增加药物的溶解度；在一定质量浓度范围内与细胞具有较好的生物相容性，能显著提高细胞酪氨酸酶活性，促进黑色素合成。

Objective To evaluate the in vitro dissolution characteristic of IPRN-NLC and to study its effects on B₁₆F₁₀ cells proliferation, melanin synthesis, and tyrosinase activity. Methods The dynamic dialysis was employed to compare the in vitro dissolution of IPRN and IPRN-NLC; MTT assay was used to detect the proliferation of B₁₆F₁₀; The tyrosinase activity was determined by L-DOPA-oxidation; The melain content was determined by GENMED Cell Melanin Quantitative Assay Kit. Results The accumulation dissolution of IPRN-NLC was 67.31% within 72 h, which showed sustained release; While the dissolution of IPRN-suspension, IPRN-physical mixture, and IPRN-DMSO were 53.34%, 90.30%, and 98.67%, respectively. The IPRN-NLC could significantly promote the proliferation, tyrosinase activity and melanin content compared with IPRN DMSO groups (P < 0.05) at the same concentration. Conclusion IPRN-NLC could increase the solubility of the drug with sustained release, and showed good cell biology intermiscibility, which could significantly increase the effects on B₁₆F₁₀ cells.

国家自然科学基金资助项目（81573696）；全军重大科研计划（BKJ16J025，BKJ16J011）