Radmard Ariana, Banga Ajay K
Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.
Pharmaceutics. 2024 Feb 22;16(3):308. doi: 10.3390/pharmaceutics16030308.
Lurasidone, an antipsychotic medication for schizophrenia, is administered daily via oral intake. Adherence is a critical challenge, given that many schizophrenia patients deny their condition, thus making alternative delivery methods desirable. This study aimed to deliver lurasidone by the transdermal route and provide therapeutic effects for three days. Passive diffusion was found to be insufficient for lurasidone delivery. The addition of chemical enhancers increased permeation, but it was still insufficient to reach the designed target dose from a patch, so a microneedle patch array was fabricated by using biodegradable polymers. For prolonged and effective delivery, the drug was encapsulated in Poly (lactic-co-glycolic acid) (PLGA) nanoparticles which were made using the solvent evaporation method and incorporated in microneedles. Effervescent technology was also employed in the preparation of the microneedle patch to facilitate the separation of the needle tip from the patch. Once separated, only the needle tip remains embedded in the skin, thus preventing premature removal by the patient. The microneedles demonstrated robust preformation in a characterization test evaluating their insertion capacity, mechanical strength, and the uniformity of microneedle arrays, and were able to deliver a dose equivalent to 20 mg oral administration. Therefore, the potential of a transdermal delivery system for lurasidone using microneedles with nanoparticles was demonstrated.
鲁拉西酮是一种用于治疗精神分裂症的抗精神病药物,通过口服方式每日给药。鉴于许多精神分裂症患者否认自己的病情,坚持服药是一项严峻挑战,因此需要其他给药方式。本研究旨在通过透皮途径递送鲁拉西酮,并提供三天的治疗效果。研究发现被动扩散不足以递送鲁拉西酮。添加化学增强剂可增加渗透,但仍不足以从贴片达到设计的目标剂量,因此使用可生物降解聚合物制备了微针贴片阵列。为了实现长效有效递送,将药物封装在采用溶剂蒸发法制备的聚乳酸-羟基乙酸共聚物(PLGA)纳米颗粒中,并将其掺入微针中。微针贴片的制备还采用了泡腾技术,以促进针尖与贴片分离。一旦分离,只有针尖留在皮肤中,从而防止患者过早移除。在评估微针插入能力、机械强度和微针阵列均匀性的表征测试中,微针表现出良好的预制性,并且能够递送相当于口服20毫克的剂量。因此,证明了使用带有纳米颗粒的微针进行鲁拉西酮透皮给药系统的潜力。