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Effect of polymer charge on the formation and stability of anti-inflammatory drug loaded nanostructured lipid carriers: physicochemical approach

机译:聚合物电荷对负载抗炎药的纳米结构脂质载体形成和稳定性的影响:理化方法

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Nanostructured lipid carriers (NLCs), with potential drug delivery capabilities, were formulated using soy lecithin (SLC), tristearin (TS) and palmitic acid (PA) in the absence and presence of two anti-inflammatory drugs, diclofenac sodium (DNa) and indomethacin (IMC). Tween 60 was used as a stabilizer separately and in combination with sodium carboxymethyl cellulose (NaCMC, anionic), polyethylene glycol (PEG, nonionic) and an N,N-dimethyl-N-dodecyl derivative of hydroxyethyl cellulose (LM200, cationic). Both DNa and IMC substantially decreased the size and increased the polydispersity index (PDI) of the NLCs. The hydrodynamic parameters, viz., size, zeta potential, and polydispersity index, as well as the thermal behaviour of the NLCs, depended on the type and charge of the added polymers. Weak interactions between the drug and lipid matrices in the bulk mixtures were confirmed through FT-IR studies. The NLC formulations exhibited lower entrapment efficiency and loading content in the case of DNa compared to IMC due to the higher ionic nature of the former drug. The polymers influenced the entrapment efficiency and loading ability of the NLCs in case of both DNa and IMC. 85% of the entrapped DNa was released from the NLC, compared to 54% release in the case of IMC; the drug release rates were higher for the PEG and NaCMC coated systems. LM200 delayed the drug release process with respect to NaCMC and PEG. Both DNa- and IMC-loaded NLCs inhibited the growth of Gram-positive bacteria, Bacillus amyloliquefaciens. It was concluded that the physicochemical properties of NLCs could effectively be modified using polymers; thus, the biomimetic characteristics of lipids and architectural advantage of polymers can be combined to yield a superior drug delivery system.
机译:在不存在和存在两种抗炎药,双氯芬酸钠(DNa)和抗炎药的情况下,使用大豆卵磷脂(SLC),三硬脂精(TS)和棕榈酸(PA)配制具有潜在药物递送功能的纳米结构脂质载体(NLC)。消炎痛(IMC)。吐温60分别用作稳定剂,并与羧甲基纤维素钠(NaCMC,阴离子),聚乙二醇(PEG,非离子)和羟乙基纤维素的N,N-二甲基-N-十二烷基衍生物(LM200,阳离子)结合使用。 DNa和IMC都大大减小了NLC的尺寸,并增加了NLC的多分散指数(PDI)。流体力学参数,即大小,ζ电势和多分散指数以及NLC的热行为,取决于所添加聚合物的类型和电荷。通过FT-IR研究证实了药物与大体积混合物中脂质基质之间的弱相互作用。与DMC相比,由于DNa的NLC制剂具有更高的离子性质,因此其包埋效率和载药量均较低。在DNa和IMC的情况下,聚合物都会影响NLC的包封效率和负载能力。 NLC释放了85%的捕获DNa,而IMC则为54%; PEG和NaCMC包被系统的药物释放速率更高。 LM200延迟了针对NaCMC和PEG的药物释放过程。含有DNa和IMC的NLC均抑制革兰氏阳性细菌解淀粉芽孢杆菌的生长。结论是,使用聚合物可以有效地改变NLC的理化性质。因此,可以将脂质的仿生特性和聚合物的结构优势相结合,以产生优异的药物递送系统。

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