Abstract
Zanamivir is currently used for the treatment of H1N1 and H5N1 influenza viruses. Due to its highly hydrophilic property, zanamivir has poor oral bioavailability. Liposomal formulations are known to improve oral absorption of hydrophilic drugs. The present study investigates the effect of liposomes encapsulating zanamivir on the permeation of zanamivir across Caco-2 monolayers. Among the formulations studied, neutral liposomes composed of Phospholipon® 90 G and cholesterol at molar ratio of 7:3 gave the highest entrapment efficiency of zanamivir. The extrusion of liposomes loading zanamivir (LZV) resulted in the reduced-size liposomal zanamivir (RLZV), which had mean diameter at 283±42 nm and gave higher encapsulation efficiency of zanamivir at 34.69±6.37% compared to 28.32±5.25%. Transport studies across Caco-2 cell monolayers showed that the apparent permeation coefficients (Papp) of LZV and RLZV were respectively 2.2- and 3.0-fold greater than that of zanamivir solution. The Papp of RLZV was 1.4-fold higher than that of LZV. On the basis of these results, liposomes are able to improve permeability of zanamivir across the Caco-2 monolayers, thereby possibly enhancing oral bioavailability of zanamivir.
Keywords: Absorption, Caco-2 cells, characterization, drug transport, liposomes, zanamivir, In Vitro Evaluation, Intestinal Absorption, Liposomal formulations, neuraminidase inhibitor
Current Drug Delivery
Title: Characterization and In Vitro Evaluation of Intestinal Absorption of Liposomes Encapsulating Zanamivir
Volume: 8 Issue: 4
Author(s): Boontarika Boonyapiwat, Narong Sarisuta and Sarinnate Kunastitchai
Affiliation:
Keywords: Absorption, Caco-2 cells, characterization, drug transport, liposomes, zanamivir, In Vitro Evaluation, Intestinal Absorption, Liposomal formulations, neuraminidase inhibitor
Abstract: Zanamivir is currently used for the treatment of H1N1 and H5N1 influenza viruses. Due to its highly hydrophilic property, zanamivir has poor oral bioavailability. Liposomal formulations are known to improve oral absorption of hydrophilic drugs. The present study investigates the effect of liposomes encapsulating zanamivir on the permeation of zanamivir across Caco-2 monolayers. Among the formulations studied, neutral liposomes composed of Phospholipon® 90 G and cholesterol at molar ratio of 7:3 gave the highest entrapment efficiency of zanamivir. The extrusion of liposomes loading zanamivir (LZV) resulted in the reduced-size liposomal zanamivir (RLZV), which had mean diameter at 283±42 nm and gave higher encapsulation efficiency of zanamivir at 34.69±6.37% compared to 28.32±5.25%. Transport studies across Caco-2 cell monolayers showed that the apparent permeation coefficients (Papp) of LZV and RLZV were respectively 2.2- and 3.0-fold greater than that of zanamivir solution. The Papp of RLZV was 1.4-fold higher than that of LZV. On the basis of these results, liposomes are able to improve permeability of zanamivir across the Caco-2 monolayers, thereby possibly enhancing oral bioavailability of zanamivir.
Export Options
About this article
Cite this article as:
Boonyapiwat Boontarika, Sarisuta Narong and Kunastitchai Sarinnate, Characterization and In Vitro Evaluation of Intestinal Absorption of Liposomes Encapsulating Zanamivir, Current Drug Delivery 2011; 8 (4) . https://dx.doi.org/10.2174/156720111795767915
DOI https://dx.doi.org/10.2174/156720111795767915 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advancements in Robotic and AI-based Drug Discovery and Delivery for Neurological Disorders
Neurological disorders, including Alzheimer's disease, Parkinson's disease, epilepsy, and brain tumors, pose significant challenges in drug delivery due to the blood-brain barrier's intricate structure and the complexity of neuronal networks. Traditional drug delivery methods often fall short in reaching therapeutic concentrations within the central nervous system, limiting treatment efficacy and ...read more
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Nanoemulsions in cancer therapy
Solid tumors are characterized by leaky vascular structure, defective angiogenesis and high interstitial fluid load, providing opportunities for nanoparticles to preferentially exudate and be retained in tumors. This phenomenon is commonly referred to as the enhanced permeability and retention (EPR) effect, which is considered to be an important reason why ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Triazole as Potent Anti-cancer Agent- A Pharmacophoric Scaffold
Current Cancer Therapy Reviews Kallikrein-Kinin System Mediated Inflammation in Alzheimers Disease In Vivo
Current Alzheimer Research Secretory Leukocyte Protease Inhibitor: More than Just A Protease Inhibitor
Current Immunology Reviews (Discontinued) Genetic Signatures in the Treatment of Stroke
Current Pharmaceutical Design Acute Respiratory Failure in Obstetric Patients
Current Women`s Health Reviews Computational Analysis of Interactions of Argadin with Chitotriosidase, Chitinase and Acidic Mammalian Chitinase: Hints for Specific Inhibitor Design
Letters in Drug Design & Discovery Clinical and Prognostic Implications of Cognitive Dysfunction and Depression in COPD
Current Respiratory Medicine Reviews Cytokines as a Therapeutic Target for Allergic Diseases: A Complex Picture
Current Pharmaceutical Design The Role of HTS in Drug Discovery at the University of Michigan
Combinatorial Chemistry & High Throughput Screening Beta-Blockers as First Line Treatment of Hypertension: A Proponents View
Current Hypertension Reviews Regulatory T Cells and Allergic Disease
Inflammation & Allergy - Drug Targets (Discontinued) Inhibition of Mitogen-Activated Protein Kinases (MAPKs) as a Strategy to Prevent Intimal Hyperplasia Following Cardiovascular Interventions
Vascular Disease Prevention (Discontinued) Lipid-based Nano-phytomedicines for Disease Treatment and Theranostic Applications
Current Nanomedicine Clinical Aspects of Clara Cell 10-kDa Protein / Uteroglobin (Secretoglobin 1A1)
Current Pharmaceutical Design Therapeutic Potentials of A2B Adenosine Receptor Ligands: Current Status and Perspectives
Current Pharmaceutical Design Putative Immune Regulatory Role of Statins
Current Immunology Reviews (Discontinued) Erythropoietin Withdrawal Leads to the Destruction of Young Red Cells at the Endothelial-Macrophage Interface
Current Pharmaceutical Design Role of Physician Gender in the Quality of Care of Cardiometabolic Diseases
Current Pharmaceutical Design Predicting Drug Efficacy Using Integrative Models for Chronic Respiratory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Genetic Susceptibility to Autoimmune Disorders: Clues from Gene Association and Gene Expression Studies
Current Molecular Medicine