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Development of venetoclax with 2-hydroxypropyl-beta-cyclodextrin inclusion complex for improved bioavailability.
Patil, Smalant Kishor; Chary, Padakanti Sandeep; Maddipatla, Sarvan; Madhavi, Y V; Singothu, Siva; Bhandari, Vasundhra; Pardhi, Ekta; Bansal, Kuldeep Kumar; Mehra, Neelesh Kumar.
Afiliación
  • Patil SK; Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Chary PS; Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Maddipatla S; Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Madhavi YV; Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Singothu S; Department of Pharmacoinformatics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Bhandari V; Department of Pharmacoinformatics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Pardhi E; Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
  • Bansal KK; Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Turku, Finland.
  • Mehra NK; Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
J Biomol Struct Dyn ; : 1-18, 2024 Jan 21.
Article en En | MEDLINE | ID: mdl-38247232
ABSTRACT
Cyclodextrin complexes loaded with venetoclax for improved solubility and therapeutic efficacy as repurposed drug. The venetoclax-cyclodextrin inclusion complex was prepared using kneading method. Primarily in-silico molecular docking study was performed to examine the possible interaction between venetoclax and hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and extensively characterized. The in-vitro studies were performed using A-549 lung epithelial cancer cells. The in-vivo pharmaco-kinetic studies was performed on wistar rats. The aqueous solubility of venetoclax was increased upto 3.16 folds, as compared with pure venetoclax with entrapment efficiency (EE%) was determined 95.44 ± 0.3%. In-vitro cytotoxicity studies were carried on A-549 lung epithelial cancer cells, wherein BCL-2 receptors were highly over-expressed and IC 50 values for venetoclax and venetoclax- HP-ß-CD complex was calculated at 24 and 48 hrs in the order of 1.241 µg/ml, 0.68 µg/ml and 0.757719 µg/ml, 0.6125 µg/mL, respectively. The oral bioavailability was increased 4.03 times compared to the pure drug. The venetoclax-HP-ß-CD inclusion complexes showed the increased aqueous solubility with improved anticancer activities.Communicated by Ramaswamy H. Sarma.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Biomol Struct Dyn Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Biomol Struct Dyn Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido