Nanotechnology Laboratory, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh, India.
Nanomedicine. 2012 Oct;8(7):1162-71. doi: 10.1016/j.nano.2011.12.006. Epub 2011 Dec 26.
Diclofenac lipid nanoemulsions (DLNEs) were prepared with different compositions. Based on size, PDI, zeta potential, and in vitro drug release, the optimized DLNEs (DLNE-4 and DLNE-7) were developed and evaluated for drug content, entrapment efficiencies, and stability in comparison to the control formulation (DLNE-1). The albumin was coupled to DLNE-7 globules (DLNE-8) by water soluble carbodiimide (EDC) method, purified, and quantified by modified Bradford method. The pharmacokinetic study was conducted in inflammation (granuloma air pouch model) induced rats. The maximum peak concentration of DLNE-8 was almost fourfold to fivefold in comparison to drug solution in granuloma air pouch fluid (GAPF). The therapeutic availability (TA) of DLNE-8 was 2.89, 2.34, and 1.66 times that of drug solution, DLNE-4 and DLNE-7, respectively. The GAPF/serum ratio of diclofenac from DLNE-8 was above one at all time points indicating the targeting potential of albumin ligated LNEs to inflammatory sites.
This study demonstrates targeted delivery of diclofenac to an inflammatory environment using the granuloma air pouch model and diclofenac nanoemulsions with different compositions.
制备了不同组成的双氯芬酸脂质纳米乳剂（DLNEs）。基于粒径、PDI、zeta 电位和体外药物释放，开发并评价了优化的 DLNEs（DLNE-4 和 DLNE-7），与对照制剂（DLNE-1）相比，对其药物含量、包封效率和稳定性进行了评价。通过水溶性碳化二亚胺（EDC）法将白蛋白偶联到 DLNE-7 胶束（DLNE-8）上，通过改良 Bradford 法进行纯化和定量。在炎症（气囊肿肉芽肿模型）诱导的大鼠中进行了药代动力学研究。与在气囊肿液（GAPF）中的药物溶液相比，DLNE-8 的最大峰浓度几乎提高了四倍到五倍。DLNE-8 的治疗利用率（TA）分别是药物溶液、DLNE-4 和 DLNE-7 的 2.89、2.34 和 1.66 倍。在所有时间点，来自 DLNE-8 的双氯芬酸的 GAPF/血清比值均高于 1，表明白蛋白结合 LNEs 对炎症部位具有靶向潜力。
本研究通过使用不同组成的双氯芬酸纳米乳剂和气囊肿肉芽肿模型，证明了双氯芬酸在炎症环境中的靶向传递。
