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糖尿病动物模型开放性切口创面外用利奈唑胺纳米乳剂的制剂与评价

Formulation and Evaluation of Topical Linezolid Nanoemulsion for Open Incision Wound in Diabetic Animal Model.

作者信息

Haider Faheem, Khan Barkat Ali, Khan Muhammad Khalid

机构信息

Drug Delivery and Cosmetics Lab (DDCL), Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, D.I. Khan, 29050, Pakistan.

出版信息

AAPS PharmSciTech. 2022 Apr 28;23(5):129. doi: 10.1208/s12249-022-02288-8.

Abstract

The present study aimed to investigate the role of topical nanoemulsion of linezolid in attenuating diabetic wound by delivering the drug to the target tissue. The nanoemulsions (NEs) were prepared by high-pressure homogenization and subjected to thermodynamic stability, pH, droplet size, viscosity, surface charge, polydispersity index (PDI), entrapment efficiency, drug content, and in vitro drug release. All formulations were thermodynamically stable. The pH was in the range of 5 to 6. The viscosities of LZD-0, LZD-1, LZD-2, and LZD-3 were recorded as 68.75 ± 2.23 mPas, 69.56 ± 2.11 mPas, 96.45 ± 3.39 mPas, and 45.5 ± 1.12 mPas respectively. LZD-1 exhibited droplet size of 376.5 nm ± 0.98, surface charge - 22.5mV, and PDI 0.387. Drug content and entrapment efficiency of LZD-1 were found to be 93 ± 3.31 % and 72 ± 1.67 %, respectively. LZD-1 released 80 ± 2.87% of drug. Due to significant (P < 0.05) in vitro results, LZD-1 formulation was selected for in vivo evaluation. Diabetes was induced in Sprague-Dawley rats using intraperitoneal streptozotocin injection at dose of 50 mg/kg. Open-incision wounds were inflicted among all diabetic rats at dorsal shaved area. Randomly, all rats were divided into positive control (blank formulation), negative control (no formulation), and test group (LZD-1). Wound healing occurred in order of test group > positive control > negative control. Skin histology and tensile strength also revealed significant results. The study concluded that topical nanoemulsion of linezolid may open new horizon in treating diabetic wounds.

摘要

本研究旨在通过将利奈唑胺递送至靶组织来研究其局部纳米乳剂在减轻糖尿病伤口方面的作用。纳米乳剂(NEs)通过高压均质法制备,并进行了热力学稳定性、pH值、液滴大小、粘度、表面电荷、多分散指数(PDI)、包封率、药物含量和体外药物释放等方面的测定。所有制剂在热力学上均稳定。pH值在5至6范围内。LZD-0、LZD-1、LZD-2和LZD-3的粘度分别记录为68.75±2.23 mPas、69.56±2.11 mPas、96.45±3.39 mPas和45.5±1.12 mPas。LZD-1的液滴大小为376.5 nm±0.98,表面电荷为-22.5 mV,PDI为0.387。LZD-1的药物含量和包封率分别为93±3.31%和72±1.67%。LZD-1释放了80±2.87%的药物。由于体外结果具有显著性(P<0.05),因此选择LZD-1制剂进行体内评价。使用剂量为50 mg/kg的腹腔注射链脲佐菌素在Sprague-Dawley大鼠中诱导糖尿病。在所有糖尿病大鼠背部剃毛区域造成开放性切口伤口。随机将所有大鼠分为阳性对照组(空白制剂)、阴性对照组(无制剂)和试验组(LZD-1)。伤口愈合情况依次为试验组>阳性对照组>阴性对照组。皮肤组织学和拉伸强度也显示出显著结果。该研究得出结论,利奈唑胺局部纳米乳剂可能为治疗糖尿病伤口开辟新的前景。

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