Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Al-Jouf, Saudi Arabia.
Department of Pharmacy, College of Health Sciences, Arsi University, Asella, Ethiopia.
Artif Cells Nanomed Biotechnol. 2023 Dec;51(1):604-617. doi: 10.1080/21691401.2023.2274526. Epub 2023 Nov 1.
Niosomes (NS) are the promising and novel carrier of the drug for effective transdermal delivery. Apigenin (AN) is a natural bioactive compound and has various pharmacological activities. AN is poorly water soluble which directly affects therapeutic efficacy. The aim of this research work was to develop the AN-NS gel to improve transdermal delivery. The thin-film hydration method was used for the development of AN-NS. The optimized AN-NS (AN-NS2) has a vesicle size of 272.56 ± 12.49 nm, PDI is 0.249, zeta potential is -38.7 mV, and entrapment efficiency of 86.19 ± 1.51%. The FTIR spectra of the AN-NS2 depicted that AN encapsulated in the NS matrix. AN-NS2 formulation was successfully incorporated into chitosan gel and evaluated. The optimized AN-NS2 gel (AN-NS2G4) has 2110 ± 14cps of viscosity, 10.40 ± 0.21g.cm/sec of spreadability, and 99.65 ± 0.53% of drug content. AN-NS2G4 displayed significantly ( < 0.05) higher AN released (67.64 ± 3.03%) than pure AN-gel (37.31 ± 2.87%). AN-NS2G4 showed the Korsmeyer Peppas release model. AN-NS2G4 displayed significantly ( < 0.05) higher antioxidant activity (90.72%) than pure AN (64.53%) at 300 µg/ml. AN-NS2G4 displayed significantly ( < 0.05) higher % inhibition of swelling than pane AN-gel in carrageenin-induced paw oedema in rats. The finding concluded that niosomes-laden gel is a good carrier of drugs to improve transdermal delivery and therapeutic efficacy.
毫微粒(NS)是一种有前途的新型药物载体,可有效实现经皮给药。芹菜素(AN)是一种天然生物活性化合物,具有多种药理活性。但 AN 的水溶性较差,这直接影响了其治疗效果。本研究工作的目的是开发载有 AN 的毫微粒凝胶以改善经皮给药。采用薄膜水化法制备 AN-NS。优化后的 AN-NS(AN-NS2)的囊泡粒径为 272.56 ± 12.49nm,PDI 为 0.249,Zeta 电位为-38.7mV,包封率为 86.19 ± 1.51%。AN-NS2 的傅里叶变换红外(FTIR)光谱表明,AN 被包裹在 NS 基质中。成功地将 AN-NS2 制剂掺入壳聚糖凝胶中并进行了评价。优化后的 AN-NS2 凝胶(AN-NS2G4)的粘度为 2110 ± 14cps,铺展性为 10.40 ± 0.21g.cm/sec,药物含量为 99.65 ± 0.53%。与纯 AN 凝胶(37.31 ± 2.87%)相比,AN-NS2G4 显示出显著更高的 AN 释放率(67.64 ± 3.03%)。AN-NS2G4 符合 Korsmeyer-Peppas 释放模型。在 300μg/ml 时,与纯 AN(64.53%)相比,AN-NS2G4 表现出显著更高的抗氧化活性(90.72%)。与纯 AN 凝胶相比,AN-NS2G4 能显著抑制(p < 0.05)角叉菜胶诱导的大鼠足肿胀。研究结果表明,载有毫微粒的凝胶是一种改善经皮给药和治疗效果的良好药物载体。