NLC-Based Rifampicin Delivery System: Development and Characterization for Improved Drug Performance Against <i>Staphylococcus aureus</i>

NLC-Based Rifampicin Delivery System: Development and Characterization for Improved Drug Performance Against <i>Staphylococcus aureus</i>

<b>Background/Objectives</b>: Rifampicin is a typical antibiotic used for the treatment of <i>Staphylococcus aureus</i> (<i>S. aureus</i>) infections; however, its clinical utility is limited by poor aqueous solubility, chemical instability, and increasing bacteri...

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Bibliographic Details
Main Authors: Javiera Carrasco-Rojas, Felipe I. Sandoval, Christina M. A. P. Schuh, Carlos F. Lagos, Javier O. Morales, Francisco Arriagada, Andrea C. Ortiz
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Pharmaceutics
Subjects:
nanostructured lipid carrier
antibiotic
rifampicin
drug release
<i>Staphylococcus aureus</i>
HepG2 cell
Online Access:https://www.mdpi.com/1999-4923/17/6/799
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Summary:<b>Background/Objectives</b>: Rifampicin is a typical antibiotic used for the treatment of <i>Staphylococcus aureus</i> (<i>S. aureus</i>) infections; however, its clinical utility is limited by poor aqueous solubility, chemical instability, and increasing bacterial resistance. Nanostructured lipid carriers (NLCs) offer a promising strategy to improve drug solubility, stability, and antimicrobial performance. <b>Methods</b>: In this study, rifampicin-loaded NLC (NLC-RIF) was developed using a hot homogenization with a low energy method and characterized in terms of particle size, polydispersity index, zeta potential, encapsulation efficiency, colloidal stability, and drug loading. <b>Results:</b> In vitro release studies under sink conditions demonstrated a biphasic release pattern, best described by the Korsmeyer–Peppas model, suggesting a combination of diffusion and matrix erosion mechanisms. Antimicrobial activity against <i>S. aureus</i> revealed a substantial increase in potency for NLC-RIF, with an IC<sub>50</sub> of 0.46 ng/mL, approximately threefold lower than that of free rifampicin. Cytotoxicity assays in HepG2 cells confirmed over 90% cell viability across all tested concentrations. <b>Conclusions</b>: These findings highlight the potential of NLC-RIF as a biocompatible and effective nanocarrier system for enhancing rifampicin delivery and antibacterial activity.
ISSN:1999-4923

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