Lipid and Polymeric Based Antibiotic Nanosystems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 3651

Special Issue Editors


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Guest Editor
University of KwaZulu-Natal, Durban, South Africa
Interests: drug delivery; synthetic chemistry; polymers; lipids; antimicrobials; nanomedicine

E-Mail Website
Guest Editor
United States International University Africa
Interests: drug delivery; synthetic chemistry; polymers; lipids; antimicrobials; nanomedicine

Special Issue Information

Dear Colleagues,

The current global crisis of antibiotic resistance and the decline in the introduction of new antibiotics are major barriers to the optimal treatment of bacterial infections. Significantly, secondary bacterial infections are also being reported as complications observed with the treatment of COVID-19, cancer, and diabetic patients. Rationally developed lipid- and polymer-based antibiotic drug delivery nanosystems are showing significant potential for improving treatment of bacterial infections associated with various diseases and for overcoming resistance. The synthesis of new materials and innovative designs of new lipid and polymeric nanosystems, together with the recent emergence of stimuli-responsive and biomimetic principles, are driving the surge in advanced medicines for antibiotics.

This Special Issue will highlight advances being made in and the current status of lipid- and polymer-based antibiotic nanosystems for combating and preventing bacterial infections. Pharmaceutics is a Q1 journal in the field of pharmaceutical sciences with an impact factor of 4.421. We invite the submission of both original research papers and review articles focusing on the design, development, and in vitro/in vivo/in silico characterization of innovative lipid- and polymer-based antibiotic drug delivery systems.

Prof. Thirumala Govender
Dr. Calvin A. Omolo
Guest Editors

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Keywords

  • lipids
  • polymers
  • antibiotic resistance
  • nanoantibiotics
  • nanosystems
  • stimuli response
  • biomimetic
  • drug delivery

Published Papers (1 paper)

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Research

30 pages, 6917 KiB  
Article
Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus
by Daniel Hassan, Calvin A. Omolo, Victoria Oluwaseun Fasiku, Ahmed A Elrashedy, Chunderika Mocktar, Bongani Nkambule, Mahmoud E. S. Soliman and Thirumala Govender
Pharmaceutics 2020, 12(11), 1093; https://doi.org/10.3390/pharmaceutics12111093 - 14 Nov 2020
Cited by 22 | Viewed by 3358
Abstract
Globally, human beings continue to be at high risk of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA); and current treatments are being depleted due to antimicrobial resistance. Therefore, the synthesis and formulation of novel materials is essential for combating antimicrobial resistance. The [...] Read more.
Globally, human beings continue to be at high risk of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA); and current treatments are being depleted due to antimicrobial resistance. Therefore, the synthesis and formulation of novel materials is essential for combating antimicrobial resistance. The study aimed to synthesize a quaternary bicephalic surfactant (StBAclm) and thereof to formulate pH-responsive vancomycin (VCM)-loaded quatsomes to enhance the activity of the antibiotic against MRSA. The surfactant structure was confirmed using 1H, 13C nuclear magnetic resonance (NMR), Fourier-transform infrared spectroscopy (FT-IR), and high-resolution mass spectrometry (HRMS). The quatsomes were prepared using a sonication/dispersion method and were characterized using various in vitro, in vivo, and in silico techniques. The in vitro cell biocompatibility studies of the surfactant and pH-responsive vancomycin-loaded quatsomes (VCM-StBAclm-Qt1) revealed that they are biosafe. The prepared quatsomes had a mean hydrodynamic diameter (MHD), polydispersity index (PDI), and drug encapsulation efficiency (DEE) of 122.9 ± 3.78 nm, 0.169 ± 0.02 mV, and 52.22 ± 8.4%, respectively, with surface charge switching from negative to positive at pH 7.4 and pH 6.0, respectively. High-resolution transmission electron microscopy (HR-TEM) characterization of the quatsomes showed spherical vesicles with MHD similar to the one obtained from the zeta-sizer. The in vitro drug release of VCM from the quatsomes was faster at pH 6.0 compared to pH 7.4. The minimum inhibitory concentration (MIC) of the drug loaded quatsomes against MRSA was 32-fold and 8-fold lower at pH 6.0 and pH 7.4, respectively, compared to bare VCM, demonstrating the pH-responsiveness of the quatsomes and the enhanced activity of VCM at acidic pH. The drug-loaded quatsomes demonstrated higher electrical conductivity and a decrease in protein and deoxyribonucleic acid (DNA) concentrations as compared to the bare drug. This confirmed greater MRSA membrane damage, compared to treatment with bare VCM. The flow cytometry study showed that the drug-loaded quatsomes had a similar bactericidal killing effect on MRSA despite a lower (8-fold) VCM concentration when compared to the bare VCM. Fluorescence microscopy revealed the ability of the drug-loaded quatsomes to eradicate MRSA biofilms. The in vivo studies in a skin infection mice model showed that groups treated with VCM-loaded quatsomes had a 13-fold decrease in MRSA CFUs when compared to the bare VCM treated groups. This study confirmed the potential of pH-responsive VCM-StBAclm quatsomes as an effective delivery system for targeted delivery and for enhancing the activity of antibiotics. Full article
(This article belongs to the Special Issue Lipid and Polymeric Based Antibiotic Nanosystems)
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