# Nano Antibiotic Delivery for Treating MRSA Infections

> **NIH NIH R56** · WAYNE STATE UNIVERSITY · 2020 · $374,752

## Abstract

PROJECT SUMMARY
Superbugs such as Methicillin-resistant Staphylococcus aureus (MRSA) is a global healthcare problem which
exhibits high rates of morbidity and mortality amongst patients. While variant strains of bacterial resistance
continue to emerge, the development of newer and more potent antibiotics has not kept pace, with urgent and
burgeoning unmet need for several resistant infections including MRSA. It is thus imperative to find alternative
solutions, such as to package current antibiotics into novel targeted delivery systems that can selectively deliver
antibiotics at the site of the infection and smartly evade the bacterial barriers and for better therapeutic response
with high safety.
We for the first time, developed a folate decorated VAN nano-antibiotic (LVAN) that showed pronounced
accumulation at the site of infection, leading to enhanced killing of MRSA strains in vitro and in vivo as compared
to the commercially available VAN that forms the basis for further exploration. The goal of this project is to further
develop and optimize a library of folate containing stimuli responsive nano-antibiotics with very high vancomycin
(VAN) loading (~50% wt/wt) that will yield significant bactericidal activity against strains of MRSA while
demonstrating high safety. Specifically, we will develop bacterial colony-responsive nano-antibiotic library
synthesis for optimized killing of MRSA and selective delivery/release to improve infection treatment followed by
determining the most optimal nano-antibiotic formulation by susceptibility testing and use of a validated PK/PD
model against MRSA strains. These select few (1-2) nano-antibiotic formulation containing VAN will then be
tested in vivo using a mouse thigh infection model against validated strains of MRSA followed by evaluation of
biodistribution and kidney toxicity using a well characterized rat model.
It is expected that the targeted nano-antibiotic formulation of VAN developed herein on systemic administration
will show selective accumulation at the site of MRSA infection and exhibit controlled antibiotic release over an
extended period of at least 72 hours improving efficacy. In addition, the liposomal formulation will be safer than
commercially available VAN because of the expected lower dose exposure and the alternative route of
elimination by the liver.
With respect to positive outcomes, the work proposed in this application is expected to yield a safe and robust
stimuli-responsive targeted nano-antibiotic formulation with high VAN loading that will have a major impact on
improving the lives of MRSA infected patients. Since the formulation has a high drug loading with minimum side
effects, the patient can be administered with therapeutic doses of VAN without any major adverse reactions or
events. Furthermore, since the formulation utilizes FDA-approved excipients we do not see any outward difficulty
in scale up and translation of the technology from the bench to the bedside.

## Key facts

- **NIH application ID:** 10212571
- **Project number:** 1R56AI151033-01
- **Recipient organization:** WAYNE STATE UNIVERSITY
- **Principal Investigator:** Arun Iyer
- **Activity code:** R56 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $374,752
- **Award type:** 1
- **Project period:** 2020-08-18 → 2022-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10212571

## Citation

> US National Institutes of Health, RePORTER application 10212571, Nano Antibiotic Delivery for Treating MRSA Infections (1R56AI151033-01). Retrieved via AI Analytics 2026-05-27 from https://api.ai-analytics.org/grant/nih/10212571. Licensed CC0.

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