纳米大小的固体散布装载的primaquine和chloroquine溶解微阵列贴片,用于改善由Plasmodium vivax引起的疟疾的治疗
Qonita Kurnia Anjani1, Fabiana Volpe-Zanutto2, Khuriah Abdul Hamid3
1School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK; Fakultas Farmasi, Universitas Megarezky, Jl. Antang Raya No. 43, Makassar 90234, Indonesia.
概括
新型溶解微阵列贴片 (MAPs) 提供了改善的疟疾vivax治疗,通过使得皮肤内持续输送primaquine (PQ) 和chloroquine (CQ),降低了多达99.2%的寄生虫病. 这种方法可以提高药物坚持性和患者的治疗结果.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 寄生虫学的寄生虫学
背景情况:
- 疟疾vivax是一个重要的全球健康问题,导致广泛的疾病和死亡率.
- 目前的治疗方法,如普里马基因 (PQ) 和基因 (CQ) 面临挑战,包括患者不良坚持和胃肠道副作用由于频繁的口服剂量.
- 皮内药物输送提供了一种替代途径,以克服口服疟疾药物治疗的局限性.
研究的目的:
- 开发和评估基于纳米尺寸固体分散的溶解微阵列补丁 (MAPs),用于增强皮肤内输送原 (PQ) 和 (CQ).
- 在疟疾模型中评估开发的MAPs的体外药物释放,体外生物相容性,体内药理动力学和体内疗效.
主要方法:
- 开发溶解微阵列贴片 (MAPs),结合纳米大小的PQ和CQ的固体分散.
- 在体外皮肤透性研究和药物有效载荷传递的评估.
- 在体外细胞毒性测试以评估生物相容性.
- 在老鼠中进行的药理动力学研究,以确定随时间推移的血药物度概况.
- 在小鼠疟疾模型中进行有效性研究,以测量降低寄生虫血症.
主要成果:
- 溶解MAP证明了在体外有效的药物递送,释放高达~60%的CQ和~42%的PQ.
- 在细胞测试中,MAPs表现出可接受的生物相容性.
- 在老鼠体内药理动力学研究显示,PQ和CQ的血水平持续超过7天.
- 用小鼠进行的疗效研究显示,在接受PQ-MAP和CQ-MAP治疗后,疟疾寄生病血症显著减少 (高达99.2%).
结论:
- 纳米尺寸的溶解MAP为抗疟疾药物PQ和CQ的持续皮内输送提供了一个有希望的平台.
- 这种新型药物输送系统有可能克服与当前疟疾vivax治疗相关的坚持性和副作用问题.
- 开发的MAP可以通过改善患者的治疗结果和治疗疗效来彻底改变疟疾治疗,特别是在特有地区.
相关概念视频
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...
01:29Malaria
Malaria pathogenesis in humans reflects a delicate interplay between parasite biology and host response. Clinical illness reflects a host’s immune response to the parasite’s asexual replication cycle, which is often asymptomatic in individuals with partial immunity. From the parasite's perspective, transmission between mosquito and human with minimal host pathology is evolutionarily advantageous. Among the six Plasmodium species infecting humans, P. falciparum and P. vivax dominate in global...
01:15Anthelminthic Agents
Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
01:21Antiprotozoal Agents
Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...