a Department of Pharmaceutical Technology , College of Pharmacy, University of Tanta , Tanta , Egypt.
J Liposome Res. 2018 Sep;28(3):209-217. doi: 10.1080/08982104.2017.1343835. Epub 2017 Jul 2.
Niosomes have been claimed to enhance intestinal absorption and to widen the absorption window of acidic drugs. This was reported after monitoring the intestinal absorption in situ. Accordingly, the aim of this work was to investigate the effect of niosomal encapsulation on intestinal absorption and oral bioavailability of nateglinide. This was conducted with the goal of correlation between in situ intestinal absorption and in vivo availability. The drug was encapsulated into proniosomes. The niosomes resulting after hydration of proniosomes were characterized with respect to vesicle size and drug entrapment efficiency. The in situ rabbit intestinal absorption of nateglinide was monitored from its aqueous solution and niosomes. Streptozotocin was used to induce diabetes in albino rats which were then used to assess the hypoglycemic effect of nateglinide after oral administration of aqueous dispersion and niosomal systems. The prepared vesicles were in the nanoscale with the recorded size being 283 nm. The entrapment efficiency depended on the pH of the formulation. The in situ intestinal absorption reflected non-significant alteration in the membrane transport parameters of the drug after niosomal encapsulation compared with the free drug solution. In contrast, niosomes showed significant improvement in the rate and extent of the hypoglycemic effect compared with the unprocessed drug. This discrepancy can be attributed to different transport pathway for the drug after niosomal inclusion with the vesicles undergoing translymphatic transport which can minimize presystemic metabolism. However, this requires confirmatory investigations. In conclusion niosomes can enhance oral bioavailability of nateglinide with the absorption being through nontraditional pathway.
尼奥斯omes 据称可以增强肠道吸收，并拓宽酸性药物的吸收窗口。这是在原位监测肠道吸收后报道的。因此，本工作的目的是研究尼奥斯ome 包封对那格列奈的肠道吸收和口服生物利用度的影响。目的是将原位肠道吸收与体内可用性相关联。将药物包封到前体尼奥斯omes 中。将前体尼奥斯omes 水合后得到的尼奥斯omes ，其特征在于囊泡大小和药物包封效率。通过监测那格列奈在其水溶液和尼奥斯omes 中的原位兔肠吸收来进行。链脲佐菌素用于诱导白化大鼠的糖尿病，然后在口服水性分散体和尼奥斯ome 系统后评估那格列奈的降血糖作用。制备的囊泡处于纳米级，记录的粒径为 283nm。包封效率取决于制剂的 pH 值。与游离药物溶液相比，尼奥斯ome 包封后药物的膜转运参数没有明显变化，这反映了原位肠道吸收。相比之下，尼奥斯ome 与未加工药物相比，显著改善了降血糖作用的速度和程度。这种差异可以归因于尼奥斯ome 包封后药物的不同传输途径，囊泡通过 translymphatic 转运，这可以最小化药物的预系统代谢。然而，这需要进一步的验证研究。总之，尼奥斯ome 可以增强那格列奈的口服生物利用度，其吸收途径是非传统途径。
