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In Vitro Nephrotoxicity and Permeation of Vancomycin Hydrochloride Loaded Liposomes
Nicole Papp1, Jeffin Panicker1, John Rubino1
1Department of Pharmaceutical Sciences, Midwestern University, 555 31st Street, Downers Grove, IL 60515, USA.
Pharmaceutics
|June 24, 2022
Summary
Encapsulating vancomycin hydrochloride in PEGylated liposomes reduces its fetal toxicity by limiting its passage across the maternal-fetal barrier. This liposomal drug delivery system shows promise for safer antibiotic use during pregnancy.
Area of Science:
- Pharmacology
- Drug Delivery
- Nanotechnology
Background:
- Drug toxicity to the fetus is a significant concern, often related to the drug's ability to cross the maternal-fetal barrier.
- Increasing a drug's molecular size is a strategy to limit its penetration across biological barriers.
Purpose of the Study:
- To investigate the encapsulation of vancomycin hydrochloride, a nephrotoxic antibiotic, into liposomes to reduce fetal toxicity.
- To evaluate the characteristics and in vitro performance of PEGylated and non-PEGylated liposomes containing vancomycin hydrochloride.
Main Methods:
- Vancomycin hydrochloride was encapsulated in PEGylated and non-PEGylated liposomes using thin-film hydration/freeze-thaw and reverse-phase evaporation methods.
- Liposomes were characterized by size, zeta potential, encapsulation efficiency, in vitro release, cytotoxicity assays (NRK-52 E cells), and permeability studies across placental and kidney cell barriers.
Main Results:
- PEGylated liposomes loaded with vancomycin hydrochloride (VHCL-lipo) were successfully prepared with sizes under 200 nm.
- VHCL-lipo exhibited faster drug release and enhanced viability of NRK-52E kidney cells compared to free vancomycin.
- In vitro studies showed reduced permeability of VHCL-lipo across human placental and dog kidney cell barriers compared to free vancomycin hydrochloride.
Conclusions:
- Encapsulation of vancomycin hydrochloride in PEGylated liposomes effectively reduces its permeability across biological barriers.
- This approach suggests a potential strategy to mitigate the nephrotoxicity and improve the safety profile of vancomycin hydrochloride during pregnancy.
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