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以负荷恩诺沙星的二十二烷酸固体脂质纳米粒混悬液作为口服和肌肉内持续释放制剂在猪中的应用。

Exploitation of enrofloxacin-loaded docosanoic acid solid lipid nanoparticle suspension as oral and intramuscular sustained release formulations for pig.

机构信息

a MAO Key Laboratory for Detection of Veterinary Drug Residues , Huazhong Agricultural University , Wuhan , China.

b National Reference Laboratory of Veterinary Drug Residues (HZAU) , Huazhong Agricultural University , Wuhan , China.

出版信息

Drug Deliv. 2019 Dec;26(1):273-280. doi: 10.1080/10717544.2019.1580798.

Abstract

In our previous study, enrofloxacin-loaded docosanoic acid solid lipid nanoparticles (SLNs) could be effectively delivered to cells in vitro. In this study, its properties and exploitation as possible oral and intramuscular sustained release formulations for pigs were studied after being made into suspension. The re-dispersed time and sedimentation rate of the nanosuspension were 55 s and 1, respectively. It showed good stability when stored away from light and sustained release in pH = 7.4 PBS buffer. The suspension exhibited no irritation at the injection site and good palatability. Compared with commercial injection and soluble powder, the nanosuspension increased the bioavailability of enrofloxacin by 1.63 and 2.38 folds, and extended the mean residence time (MRT) of the drug from 11.27 and 12.33 to 37.76 and 35.15 h after intragastric and intramuscular administration, respectively. These results suggest that docosanoic acid SLN suspension (DAS) might be a promising oral and intramuscular sustained release formulation to enhance the pharmacological activity of enrofloxacin.

摘要

在我们之前的研究中,载恩诺沙星的二十二酸固体脂质纳米粒(SLNs)可以有效地递送到体外细胞。在这项研究中,将其制成混悬剂后,研究了其作为猪口服和肌肉内缓释制剂的特性和应用。纳米混悬剂的再分散时间和沉降率分别为 55 秒和 1。在避光条件下储存时具有良好的稳定性,并在 pH = 7.4 的 PBS 缓冲液中持续释放。混悬剂在注射部位无刺激性,口感良好。与市售注射液和可溶性粉相比,纳米混悬剂使恩诺沙星的生物利用度分别提高了 1.63 倍和 2.38 倍,使药物的平均驻留时间(MRT)分别从灌胃和肌肉注射后的 11.27 和 12.33 小时延长至 37.76 和 35.15 小时。这些结果表明,二十二酸 SLN 混悬剂(DAS)可能是一种有前途的口服和肌肉内缓释制剂,可增强恩诺沙星的药理活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0e6/6427631/aa85d2887276/IDRD_A_1580798_F0001_C.jpg

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