Pyramid-Shaped PEG-PCL-PEG Polymeric-Based Model Systems for Site-Specific Drug Delivery of Vancomycin with Enhance Antibacterial Efficacy | Zendy

Sima Singh | Zendy; Majed Alrobaian | Zendy; Nagashekhara Molugulu | Zendy; Nikhil Agrawal | Zendy; Arshid Numan | Zendy; Prashant Kesharwani | Zendy

Open Access

Pyramid-Shaped PEG-PCL-PEG Polymeric-Based Model Systems for Site-Specific Drug Delivery of Vancomycin with Enhance Antibacterial Efficacy

Author(s) -

Sima Singh,

Majed Alrobaian,

Nagashekhara Molugulu,

Nikhil Agrawal,

Arshid Numan,

Prashant Kesharwani

Publication year - 2020

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.9b04064

Subject(s) - peg ratio , drug delivery , hemolysis , ethylene glycol , vancomycin , biocompatibility , chemistry , cytotoxicity , staphylococcus aureus , in vitro , biochemistry , organic chemistry , medicine , bacteria , biology , immunology , finance , economics , genetics

Antibacterial resistance remains a major global problem due to frequent prescriptions, leading to significant toxicities. To overcome the limitations of antibiotic therapy, it is highly desirable to provide site-specific delivery of drugs with controlled release. Inspired by the biocompatible, biodegradable, and site-specific mimicking behavior of poly(ethylene glycol) (PEG) and poly(caprolactone) (PCL), we developed vancomycin-PEG-PCL-PEG conjugates to maximize the pharmacological effects and minimize the side effects. Drug-loaded vancomycin-PEG-PCL-PEG conjugates are influenced by size, shape, surface area, encapsulation efficiency, in vitro drug release, hemolysis assay, cytotoxicity, and antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and bacterial kill kinetics. The results demonstrated that vancomycin (VCM) release from PEG-PCL-PEG triblock revealed a biphasic manner. Hemolysis assay showed the nonprescription nature of VCM-PEG-PCL-PEG. Cytotoxicity studies confirmed the biocompatibility of VCM-PEG-PCL-PEG. The in vitro antibacterial results showed enhance activity with minimum inhibitory concentration compared to bare VCM. Molecular dynamics simulation study revealed that binding between VCM and PEG-PCL-PEG by hydrophobic interactions offers molecular encapsulation and steric barrier to drug degradation. This newly developed therapeutic delivery system can offer to enhance activity and delivery VCM against MRSA.

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