百里香醌
生物利用度
药代动力学
药理学
体内
脂质体
化学
胰腺癌
医学
癌症
内科学
生物化学
抗氧化剂
生物
生物技术
作者
Hari Krishnareddy Rachamalla,Santanu Bhattacharya,Ajaz Ahmad,Kathyayani Sridharan,Vijay Sagar Madamsetty,Sujan Kumar Mondal,Enfeng Wang,Shamit K. Dutta,Basit L. Jan,Sudhakar Jinka,Madan Mohan Chandra Sekhar Jaggarapu,Venu Yakati,Debabrata Mukhopadhyay,Khalid M. Alkharfy,Rajkumar Banerjee
出处
期刊:Nanomedicine
日期:2021-04-01
卷期号:16 (8): 641-656
被引量:4
标识
DOI:10.2217/nnm-2020-0470
摘要
Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.
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