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Bioavailability Enhancement of Cepharanthine via Pulmonary Administration in Rats and Its Therapeutic Potential for Pulmonary Fibrosis Associated with COVID-19 Infection.
Li, Jian; Chen, Guangrui; Meng, Zhiyun; Wu, Zhuona; Gan, Hui; Zhu, Xiaoxia; Han, Peng; Liu, Taoyun; Wang, Fanjun; Gu, Ruolan; Dou, Guifang.
  • Li J; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Chen G; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Meng Z; School of Basic Medical Sciences, Anhui Medical University, Hefei 230032, China.
  • Wu Z; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Gan H; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Zhu X; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Han P; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Liu T; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Wang F; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Gu R; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
  • Dou G; Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
Molecules ; 27(9)2022 Apr 24.
Article in English | MEDLINE | ID: covidwho-1810048
ABSTRACT
Cepharanthine (CEP) has excellent anti-SARS-CoV-2 properties, indicating its favorable potential for COVID-19 treatment. However, its application is challenged by its poor dissolubility and oral bioavailability. The present study aimed to improve the bioavailability of CEP by optimizing its solubility and through a pulmonary delivery method, which improved its bioavailability by five times when compared to that through the oral delivery method (68.07% vs. 13.15%). An ultra-performance liquid chromatography tandem-mass spectrometry (UPLC-MS/MS) method for quantification of CEP in rat plasma was developed and validated to support the bioavailability and pharmacokinetic studies. In addition, pulmonary fibrosis was recognized as a sequela of COVID-19 infection, warranting further evaluation of the therapeutic potential of CEP on a rat lung fibrosis model. The antifibrotic effect was assessed by analysis of lung index and histopathological examination, detection of transforming growth factor (TGF)-ß1, interleukin-6 (IL-6), α-smooth muscle actin (α-SMA), and hydroxyproline level in serum or lung tissues. Our data demonstrated that CEP could significantly alleviate bleomycin (BLM)-induced collagen accumulation and inflammation, thereby exerting protective effects against pulmonary fibrosis. Our results provide evidence supporting the hypothesis that pulmonary delivery CEP may be a promising therapy for pulmonary fibrosis associated with COVID-19 infection.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Pulmonary Fibrosis / COVID-19 / COVID-19 Drug Treatment Type of study: Experimental Studies / Prognostic study Topics: Long Covid Limits: Animals / Humans Language: English Journal subject: Biology Year: 2022 Document Type: Article Affiliation country: Molecules27092745

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Pulmonary Fibrosis / COVID-19 / COVID-19 Drug Treatment Type of study: Experimental Studies / Prognostic study Topics: Long Covid Limits: Animals / Humans Language: English Journal subject: Biology Year: 2022 Document Type: Article Affiliation country: Molecules27092745