Dissolving microneedles integrated with pH-responsive micelles containing AIEgen with ultra-photostability for enhancing melanoma photothermal therapy.,Biomaterials Science

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Dissolving microneedles integrated with pH-responsive micelles containing AIEgen with ultra-photostability for enhancing melanoma photothermal therapy.
Biomaterials Science ( IF 5.8 ) Pub Date : 2020-09-10 , DOI: 10.1039/d0bm00914h
Sihui Wei ₁ , Guilan Quan , Chao Lu , Xin Pan , Chuanbin Wu

Affiliation

Photothermal therapy (PTT) based on aggregation-induced emission luminogen (AIEgen) is very promising for superficial tumor therapy due to the superior photostability and photothermal conversion efficiency of AIEgens. However, the systemic administration of AIEgen remains challenging, mainly because of solubility dissatisfaction and biodistribution. Here, a dissolving microneedle (MN) system loaded with AIEgen (NIR950) was developed for topical administration to treat malignant skin tumor melanoma. Firstly, NIR950-loaded polymeric micelles (NIR950@PMs) were prepared via a nanoprecipitation method to increase the drug solubility. Then, micelles were concentrated on needle tips of MN (NIR950@PMs@MN) by a two-step molding method. NIR950@PMs showed no distinct decline in emission intensity under continuous laser irradiation for an hour. Moreover, the pH-responsive micelles can be protonated in an acidic tumor microenvironment to facilitate the intracellular uptake. By virtue of dissolving MN, NIR950@PMs could rapidly accumulate at the tumor site and reach a suitable temperature for killing cancer cells under laser irradiation. With only single administration and one-time laser irradiation, the NIR950@PMs@MN could notably eliminate melanoma tumors with a low dose of NIR950. Overall, this dissolving MN system loaded with NIR950 showed remarkable photostability and also achieved a valid photothermal effect, which indicate great potential for clinical superficial tumor therapy.

中文翻译：

溶解的微针与含有AIEgen的pH响应胶束整合在一起，具有超光稳定性，可增强黑色素瘤的光热疗法。

基于聚集诱导发射发光原（AIEgen）的光热疗法（PTT）由于表面活性剂的优异光稳定性和光热转换效率而在浅表肿瘤治疗中非常有前途。然而，AIEgen的全身给药仍然具有挑战性，主要是由于溶解度不满意和生物分布。在这里，开发了一种装有AIEgen（NIR950）的可溶性微针（MN）系统，用于局部给药以治疗恶性皮肤肿瘤黑色素瘤。首先，通过以下方法制备了载有NIR950的聚合物胶束（NIR950 @ PMs）一种增加药物溶解度的纳米沉淀方法。然后，通过两步成型法将胶束集中在MN（NIR950 @ PMs @ MN）的针尖上。NIR950 @ PMs在连续激光照射一个小时后，发射强度没有明显下降。此外，pH响应胶束可以在酸性肿瘤微环境中质子化，以促进细胞内摄取。通过溶解MN，NIR950 @ PMs可以迅速聚集在肿瘤部位，并达到合适的温度以在激光照射下杀死癌细胞。仅需单次给药和一次性激光照射，NIR950 @ PMs @ MN即可以低剂量的NIR950显着消除黑色素瘤。总体而言，装有NIR950的可溶解MN系统显示出显着的光稳定性，并且还达到了有效的光热效果，

更新日期：2020-10-13

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