A Novel Cryptococcal Meningitis Therapy: The Combination of Amphotericin B and Posaconazole Promotes the Distribution of Amphotericin B in the Brain Tissue.

The deficient brain tissue distribution of amphotericin B (AMPB) seriously restricts its treatment for the clinical efficacy of cryptococcus neoformans meningitis (CNM). We strive to develop a tactic to increase its concentration in brain tissue. We aimed to investigate whether the combination of AM...

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Publicado en:BioMed Research International pp. 1 - 12
Autores principales: Yang, Ming, Cheng, Lin, Dai, Qing, Yang, Bo, Yuan, Qian, Yu, MingJie, Feng, Wei, Sun, Fengjun, Xia, Peiyuan
Formato: pictorial research tables/charts Journal Article
Publicado: Wiley-Blackwell 11/29/2020
Acceso en línea:Ver este registro en EBSCOhost
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      dt: 11/29/2020
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      pub: Wiley-Blackwell
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        10.1155/2020/8878158
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        atl: A Novel Cryptococcal Meningitis Therapy: The Combination of Amphotericin B and Posaconazole Promotes the Distribution of Amphotericin B in the Brain Tissue.
      aug:
        au:
          Yang, Ming
          Cheng, Lin
          Dai, Qing
          Yang, Bo
          Yuan, Qian
          Yu, MingJie
          Feng, Wei
          Sun, Fengjun
          Xia, Peiyuan
        affil: Department of Pharmacy, The First Affiliated Hospital of Third Military Medical University (Army Medical University), Chongqing 400038, China
      sug:
        subj:
          Meningitis, Cryptococcal Drug Therapy
          Amphotericin B Pharmacokinetics
          Antibiotics, Antifungal Pharmacokinetics
          Antibiotics, Combined Pharmacodynamics
          Treatment Outcomes Evaluation
          Animal Studies
          Mice
          In Vitro Studies
          Chromatography, High Pressure Liquid
          Amphotericin B Blood
          Brain Drug Effects
          Molecular Docking Simulation
          Ultrafiltration
          Albumins Blood
          Antibiotics, Antifungal Blood
          Staining and Labeling Methods
          Bacterial Colonization Drug Effects
          Microbial Culture and Sensitivity Tests
          Antibiotics, Antifungal Administration and Dosage
          Dose-Response Relationship, Drug
          Neurons
          Proteins
          Cell Proliferation
      ab: The deficient brain tissue distribution of amphotericin B (AMPB) seriously restricts its treatment for the clinical efficacy of cryptococcus neoformans meningitis (CNM). We strive to develop a tactic to increase its concentration in brain tissue. We aimed to investigate whether the combination of AMPB and posaconazole (POS) could be more effective in the treatment of CNM and to elucidate its potential mechanisms. HPLC analysis was used to analyze the concentration of AMPB in mouse serum, brain tissue, and BCECs cells. Schrodinger molecular docking, in vitro plasma balance dialysis, and ultrafiltration analysis were performed to evaluate the combinative effect of AMPB and POS with serum albumin and POS on AMPB plasma protein binding. H&E staining and colonization culture experiment of CN were employed to assess the effect of POS on the efficacy of AMPB. POS + AMPB significantly reduced the concentration of plasma total AMPB and increased its concentration in the brain tissue. However, the P-gp inhibitor zosuquidar, BCRP inhibitor Ko143, and a common inhibitor of both, elacridar, had no significant effect on its concentration. Molecular docking, balance dialysis, and ultrafiltration analysis showed that AMPB and POS had potential binding properties to serum albumin. Meanwhile, 4 and 8 μg/mL POS could significantly increase the concentration of free AMPB in plasma. POS and three inhibitors all had no significant effect on the uptake of AMPB by BCECs, but serum albumin had. The therapeutic effect of CNM in mice was confirmed that AMPB and AMPB+POS could restrain the infiltration of neutrophils and lymphocytes in cortical neurons and improve the bleeding and markedly inhibit the proliferation of CN. Collectively, we propose that POS competitively binds to the plasma protein sites of AMPB, thereby increasing its level in the brain tissue. Meanwhile, POS could enhance the efficacy of AMPB in the treatment of CNM, which may be independent of P-gp and BCRP proteins.
      pubtype: Academic Journal
      doctype:
        pictorial
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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