Summary of Enhancing the Oral Bioavailability of Asenapine Maleate with Bio-enhancer: An In-Silico Assisted In Vivo Pharmacokinetic Study

Document Type

Article

Abstract

Background: The study titled “Interaction of Natural Bio-enhancers with Enzymes CYP1A2 and CYP3A4” conducted by Akhil Suresh and Dr. Usha Y Nayak explores the molecular dynamics of specific bio-enhancers when interacting with crucial enzymes in the liver. This research is essential for understanding how bio-enhancers can potentially improve the bioavailability of drugs like asenapine maleate (AM) metabolized by these enzymes.

Research Goals and Hypotheses: The primary goal of the study is to identify and analyze the binding interactions of selected bio-enhancers with the enzymes CYP1A2 and CYP3A4. The hypothesis is that specific bio-enhancers can significantly alter enzyme activity, thereby enhancing drug efficacy and reducing required dosages.

Methodological Approach:

  1. Molecular Dynamics Simulations: Advanced simulations were performed to model the interactions between bio-enhancers and enzymes. Key parameters such as binding scores, energy minimization, and interaction types (hydrophobic, polar, etc.) were analyzed.
  2. In vivo Pharmacokinetic Studies: Experiments were conducted on Wistar rats to observe the pharmacokinetic behavior of bio-enhancers, assessing their absorption, distribution, metabolism, and excretion (ADME) profiles.

Results and Discoveries:

  1. Simulation Outcomes: The simulations revealed that bio-enhancers, particularly AM, demonstrated significant interactions with CYP1A2 and CYP3A4. Key binding sites and interaction types were identified, with binding scores providing a quantifiable measure of interaction strength.
  2. Pharmacokinetic Data: The in vivo studies confirmed that these bio-enhancers could influence the pharmacokinetics of drugs metabolized by the target enzymes, potentially leading to enhanced bioavailability and efficacy.

Citation to the base paper: V.M. Gambhire, N.S. Ranpise, Enhanced oral delivery of asenapine maleate from solid lipid nanoparticles: pharmacokinetic and brain distribution evaluations, Asian J. Pharm 12 (3) (2018 Sept) 152–161.

Publication Date

2022

Recommended Citation

Suresh, A., Narayan, R., Tummala, H. P., Matcha, S., Mallayasamy, S., Nayak, Y., Puralae Channabasavaiah, J., & Nayak, U. Y. (2022). Enhancing the oral bioavailability of asenapine maleate with bio-enhancer: An in-silico assisted in-vivo pharmacokinetic study. Journal of Drug Delivery Science and Technology, 70, 103215. https://doi.org/10.1016/j.jddst.2022.103215

Publication Date

2022

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