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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Formulation, characterisation and in vivo evaluation of lipid-based nanocarrier for topical delivery of diflunisal
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Formulation, characterisation and in vivo evaluation of lipid-based nanocarrier for topical delivery of diflunisal

机译:用于双氟尼醛局部递送的脂质基纳米载体的配制,表征和体内评价

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摘要

Diflunisal (DIF) is non-steroidal anti-inflammatory drug used in the treatment of rheumatoid arthritis, osteoarthritis. The current engrossment was aimed at formulation and assessment of DIF-loaded solid lipid nanoparticles (SLNs) for topical/dermal application. SLNs formulated by hot homogenisation method based on microemulsification technique were spherical with a mean size of 124.0 +/- 2.07nm; PDI 0.294 +/- 0.15. The cumulative amount permeated/area was 109.99 +/- 0.008 mu g/cm(2), along with permeation flux (6.30 +/- 0.09 mu g/cm(2)/h) and skin retention (11.74 +/- 0.155 mu g/cm(2)) across mice skin. The SLNs of DIF showed significant decrease in fluid volume, granuloma tissue weight, leukocyte count/mm(3) after application of SLN formulation in mice air pouch model. Similarly, in mice ear oedema and rat paw oedema model, there was 2.30 and 1.29 time increase in percentage inhibition of oedema after SLN formulation application, respectively, as compared with conventional cream. Hence, the SLNs of DIF may prove to be a potential nanocarrier to effectively treat the local inflammatory conditions associated with arthritis.
机译:Diflunisal(DIF)是用于治疗类风湿关节炎,骨关节炎的非甾体类抗炎药。目前的研究目的在于配制和评估用于局部/皮肤应用的DIF固体脂质纳米颗粒(SLN)。通过基于微乳化技术的热均质法制备的SLN为球形,平均粒径为124.0 +/- 2.07nm; PDI 0.294 +/- 0.15。渗透/面积的累积量为109.99 +/- 0.008μg / cm(2),以及渗透通量(6.30 +/- 0.09 mu g / cm(2)/ h)和皮肤滞留(11.74 +/- 0.155 mu g / cm(2))。在小鼠气囊模型中应用SLN制剂后,DIF的SLNs表现出体液量,肉芽肿组织重量,白细胞计数/ mm(3)显着降低。类似地,在小鼠耳部水肿和大鼠爪水肿模型中,与常规乳膏相比,SLN制剂应用后的水肿抑制百分比分别增加了2.30和1.29倍。因此,DIF的SLN可能被证明是有效治疗与关节炎相关的局部炎症性疾病的潜在纳米载体。

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