Despite the tremendous development of oncology, prostate cancer remains a debilitating malignancy. One of the most promising approaches to addressing this issue is to exploit the advancements of nanomedicine in combination with well-established nuclear medicine and radiotherapy. Following this idea, we have developed a radioisotope nanocarrier platform of electron-beam-synthesized nanogels based on poly(acrylic acid). We have developed a functionalization protocol, showing the very high (>97%) efficiency of the conjugation in targeting a ligand–bombesin derivative. This engineered peptide can bind gastrin-releasing peptide receptors overexpressed in prostate cancer cells; moreover, it bears a radioisotope-chelating moiety. Our nanoplatform exhibits very promising performance in vitro; the radiolabeled nanocarriers maintained high radiochemical purity of >90% in both the labeling buffer and human serum for up to 14 days. The application of the targeted nanocarrier allowed also effective and specific uptake in PC-3 prostate cancer cells, up to almost 30% after 4 h, which is a statistically significant improvement in comparison to carrier-free radiolabeled peptides. Although our system requires further studies for more promising results in vivo, our study represents a vital advancement in radionanomedicine—one of many steps that will lead to effective therapy for castration-resistant prostate cancer.
尽管肿瘤学领域取得了巨大进展，前列腺癌仍是一种使人衰弱的恶性肿瘤。解决这一难题最有前景的途径之一，是将纳米医学的进展与成熟的核医学及放射治疗技术相结合。基于这一理念，我们开发了一种基于聚丙烯酸的电子束合成纳米凝胶放射性同位素纳米载体平台。我们建立了功能化方案，证明靶向配体——蛙皮素衍生物的偶联效率极高（>97%）。该工程化肽段既能与前列腺癌细胞中过表达的生长激素释放肽受体结合，又具备放射性同位素螯合功能基团。我们的纳米平台在体外实验中展现出极具前景的性能：放射性标记纳米载体在标记缓冲液和人血清中均能保持>90%的高放射化学纯度，持续时间长达14天。靶向纳米载体的应用使PC-3前列腺癌细胞实现了高效特异性摄取——4小时后摄取率接近30%，与游离放射性标记肽段相比具有统计学显著提升。尽管本系统仍需进一步研究以获得更理想的体内实验结果，但本研究代表了放射纳米医学领域的重要进展——这将是推动去势抵抗性前列腺癌有效治疗的众多关键步骤之一。
肿瘤(癌症)患者之家