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载有百里醌的脂质体对药物敏感和耐药的安全性及治疗效果

Safety and Therapeutic Efficacy of Thymoquinone-Loaded Liposomes against Drug-Sensitive and Drug-Resistant .

作者信息

Allemailem Khaled S, Alnuqaydan Abdullah M, Almatroudi Ahmad, Alrumaihi Faris, Aljaghwani Aseel, Khalilullah Habibullah, Younus Hina, Khan Arif, Khan Masood A

机构信息

Department of Medical Laboratories, College of Applied Medical Sciences, Qassim University, Buraydah 51452, Saudi Arabia.

Department of Medical Biotechnology, College of Applied Medical Sciences, Qassim University, Buraydah 51452, Saudi Arabia.

出版信息

Pharmaceutics. 2021 May 8;13(5):677. doi: 10.3390/pharmaceutics13050677.

Abstract

In the present study, we investigated the activity of free thymoquinone (TQ) or liposomal thymoquinone (Lip-TQ) in comparison to standard antibiotic amoxicillin (AMX) against the drug-sensitive and drug-resistant . A liposomal formulation of TQ was prepared and characterized and its toxicity was evaluated by analyzing the hematological, liver and kidney function parameters. TQ was effective against both drug-sensitive and drug-resistant as shown by the findings of drug susceptibility testing and time kill kinetics. Moreover, the therapeutic efficacy of TQ or Lip-TQ against was assessed by the survival rate and the bacterial load in the lung tissues of treated mice. The mice infected with drug-sensitive exhibited a 90% survival rate on day 30 post treatment with Lip-TQ at a dose of 10 mg/kg, whereas the mice treated with AMX (10 mg/kg) had a 100% survival rate. On the other hand, the mice infected with drug-resistant had a 70% survival rate in the group treated with Lip-TQ, whereas AMX was ineffective against drug-resistant and all the mice died within day 30 after the treatment. Moreover, Lip-TQ treatment effectively reduced the bacterial load in the lung tissues of the mice infected with the drug-sensitive and drug-resistant . Moreover, the blood of the mice treated with Lip-TQ had reduced levels of inflammation markers, leukocytes and neutrophils. The results of the present study suggest that Lip-TQ may prove to be an effective therapeutic formulation in the treatment of the drug-sensitive or drug-resistant infection as well.

摘要

在本研究中,我们研究了游离百里醌(TQ)或脂质体百里醌(Lip-TQ)与标准抗生素阿莫西林(AMX)相比,对药敏和耐药菌的活性。制备并表征了TQ的脂质体制剂,并通过分析血液学、肝脏和肾脏功能参数来评估其毒性。药敏试验和时间杀菌动力学结果表明,TQ对药敏和耐药菌均有效。此外,通过存活率和治疗小鼠肺组织中的细菌载量来评估TQ或Lip-TQ对细菌的治疗效果。用10 mg/kg剂量的Lip-TQ治疗后30天,感染药敏菌的小鼠存活率为90%,而用AMX(10 mg/kg)治疗的小鼠存活率为100%。另一方面,感染耐药菌的小鼠在Lip-TQ治疗组中的存活率为70%,而AMX对耐药菌无效,所有小鼠在治疗后30天内死亡。此外,Lip-TQ治疗有效降低了感染药敏和耐药菌的小鼠肺组织中的细菌载量。此外,用Lip-TQ治疗的小鼠血液中的炎症标志物、白细胞和中性粒细胞水平降低。本研究结果表明,Lip-TQ可能被证明是治疗药敏或耐药菌感染的有效治疗制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/507c/8151670/8021a7e160a0/pharmaceutics-13-00677-g001.jpg

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