基于壳聚糖的搭载光源可溶性微针的制备与评价

Preparation and evaluation of chitosan-based light source-loaded soluble microneedles

摘要:

光动力疗法与给药微针(microneedle, MN)相结合为治疗肿瘤提供了一种安全有效的途径。本文设计了一种基于壳聚糖搭载高能光子的可控缓释型载药微针贴片(LED-losartan-HEMA/ CS-MN, LLH-CSMN)，重点研究了其制备工艺，并且以氯沙坦为模型药物对微针阵列的形貌尺寸进行了表征，探究了LLH-CSMN的力学性能、皮肤穿刺性能、缓释性能以及高能光子在长时间工作下的光热性能。结果表明，基于壳聚糖搭载高能光子的微针贴片能够有效地在皮肤表面打开通道进行药物递送，并进行光动力治疗。同时，体外透皮扩散试验表明，以氯沙坦为模型药物制备的微针在1 h内释放了约30%的药物，在1 d内总共释放了约60%的药物，随后进行缓慢释放，在6 d后最终释放了93%的药物，LLH-CSMN具有可控缓释特性以及良好的长效光辅助治疗效果，为肿瘤治疗提供了一个新的安全有效途径。

Abstract:

The combination of photodynamic therapy and drug delivery microneedle (MN) provides a safe and effective way to treat tumors. In this paper, we designed a controlled and sustained-release drug-loaded microneedle patch (LED-losartan-HEMA/CS-MN, LLH-CSMN) based on chitosan loaded with high-energy photons, investigated its preparation process, and characterized the morphology and size of the microneedle array with losartan as the model drug. The mechanical properties of LLH-CSMN, skin puncture properties, slow release properties and the photothermal properties of high energy photons under long-term operation were investigated. The experimental results showed that the chitosan-based microneedle patch loaded with high-energy photons can effectively open channels on the skin surface for drug delivery and photodynamic therapy. At the same time, the in vitro percutaneous diffusion experiment showed that the microneedles prepared with losartan as the model drug released about 30% of the drug within 1 h, about 60% of the drug in total within 1 d, followed by slow release, and finally released 93% of the drug after 6 d. LLH-CSMN has controllable slow-release characteristics and good long-term photoassisted therapy effect. It provides a new safe and effective way for tumor treatment.