Department of Chemistry, College of Physical Sciences, Federal University of Agriculture, Abeokuta (FUNAAB) PMB, Abeokuta, 2240, Nigeria.
Department of Chemistry, Graduate School of Science and Technology, Kumamoto University, 2-39-1 Kurokami, Chuo-ku, Kumamoto, 860-8555, Japan.
Sci Rep. 2018 Feb 15;8(1):3078. doi: 10.1038/s41598-018-21351-8.
The use of nanocarriers in drug delivery is a breakeven research and has received a clarion call in biomedicine globally. Herein, two newly nano-biomaterials: MCM-41 encapsulated quinine (MCM-41 ⊃ QN) (1) and 3-phenylpropyl silane functionalized MCM-41 loaded QN (pMCM-41 ⊃ QN) (2) were synthesized and well characterized. 1 and 2 along with our two already reported nano-antimalarial drugs (MCM-41 ⊃ ATS) (3) and 3-aminopropyl silane functionalized MCM-41 contained ATS (aMCM-41 ⊃ ATS) (4) were screened in vitro for their activity against P. falciparium W2 strain, cytotoxicity against BGM cells and in vivo for their activity against Plasmodium bergheiNK65. 1 has the highest antimalarial activity in vivo against P. berghei NK65, (ED: < 0.0625 mg/kg body weight) and higher mean survival time compared to the other nano biomaterials or unencapsulated drugs at doses higher than 0.0625 mg/kg body weight. This encapsulation strategy of MCM-41 ⊃ QN (1) stands very useful and effective in delivering the drug to the target cells compared to other delivery systems and therefore, this encapsulated drug may be considered for rational drug design.
纳米载体在药物传递中的应用是一项具有挑战性的研究,在全球生物医学领域引起了广泛关注。在此,我们合成了两种新型纳米生物材料:介孔硅 MCM-41 封装奎宁(MCM-41⊃QN)(1)和 3-苯基丙基硅烷功能化介孔硅 MCM-41 负载奎宁(pMCM-41⊃QN)(2),并对其进行了充分的表征。我们还对 1 和 2 以及之前报道的两种纳米抗疟药物(介孔硅 MCM-41 封装青蒿琥酯(MCM-41⊃ATS)(3)和 3-氨基丙基硅烷功能化介孔硅 MCM-41 负载青蒿琥酯(aMCM-41⊃ATS)(4)进行了体外筛选,以评估它们对 P. falciparium W2 株的活性、对 BGM 细胞的细胞毒性以及对 Plasmodium bergheiNK65 的体内活性。在体内,1 对 P. bergheiNK65 的抗疟活性最高(ED:<0.0625mg/kg 体重),与其他纳米生物材料或未封装药物相比,在高于 0.0625mg/kg 体重的剂量下,其平均存活时间更长。与其他给药系统相比,MCM-41⊃QN(1)的这种封装策略在将药物递送到靶细胞方面非常有用和有效,因此,这种封装药物可能被认为是一种合理的药物设计。