Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.
Medicinal Chemistry and Pharmacognosy Division, College of Pharmacy, The Ohio State University, Columbus, OH, USA.
Expert Opin Drug Deliv. 2020 Jan;17(1):97-110. doi: 10.1080/17425247.2020.1700227. Epub 2019 Dec 6.
: To test the hypothesis that miltefosine (MTF)-polyphenol co-loaded second-generation nano-transfersomes (SGNTs) can be an effective approach for the topical treatment of cutaneous leishmaniasis (CL).: The co-loaded SGNTs with various MTF-polyphenol combinations were developed, evaluated and compared for the entrapment efficiency, vesicle size, deformability index, permeation, cytotoxicity, and anti-leishmanial potential, using both and models.: The co-loaded SGNTs were spherical in shape, with an average size of 119 ± 1.5 nm and a high entrapment efficiency of 73.7 ± 3.7%. The study displayed a 3.2-fold higher permeation of MTF when entrapped in co-loaded SGNTs, whereas cytotoxicity potential of co-loaded SGNTs was 43.2% higher than the MTF solution. A synergistic interaction was observed between MTF and apigenin (APG) among all polyphenols and an 8.0-fold lower IC was found against amastigotes of DsRed , compared with the plain MTF solution. Moreover, the studies displayed a 9.5-fold reduced parasitic burden in the infected BALB/c mice treated with MTF-APG co-loaded SGNTs gel.: The potential of MTF-APG co-loaded SGNTs topical formulation is established for the first time as an effective drug delivery strategy against CL.
: 为了验证米替福新（MTF）-多酚共载第二代纳米转体（SGNTs）可作为治疗皮肤利什曼病（CL）的局部治疗的有效方法这一假说：制备了具有不同 MTF-多酚组合的共载 SGNTs，并用 和 模型对其包封效率、囊泡大小、变形指数、渗透、细胞毒性和抗利什曼原虫活性进行了评估和比较。: 共载 SGNTs 呈球形，平均粒径为 119±1.5nm，包封效率高达 73.7±3.7%。研究显示，当 MTF 被共载 SGNTs 包封时，其渗透能力提高了 3.2 倍，而共载 SGNTs 的细胞毒性比 MTF 溶液高 43.2%。在所有多酚中，MTF 和芹菜素（APG）之间观察到协同作用，与普通 MTF 溶液相比，对 DsRed 感染的巨噬细胞中的无鞭毛体的 IC 降低了 8.0 倍。此外，研究显示，用 MTF-APG 共载 SGNTs 凝胶治疗感染的 BALB/c 小鼠，寄生虫负荷降低了 9.5 倍。: 首次证实了 MTF-APG 共载 SGNTs 局部制剂作为治疗 CL 的有效药物递送策略的潜力。
