Language

English

Publication Date

6-1-2024

Journal

Journal of Controlled Release

DOI

10.1016/j.jconrel.2024.04.029

PMID

38648957

PMCID

PMC11705614

PubMedCentral® Posted Date

1-7-2025

PubMedCentral® Full Text Version

Author MSS

Abstract

Continuous and aberrant activation of myofibroblasts is the hallmark of pathological fibrosis (e.g., abnormal wound healing). The deposition of excessive extracellular matrix (ECM) components alters or increases the stiffness of tissue and primarily accounts for multiple organ dysfunctions. Among various proteins, Cadherin-11 (CDH11) has been reported to be overexpressed on myofibroblasts in fibrotic tissues. Anti-apoptotic proteins such as (B cell lymphoma-2) (BCL-2) are also upregulated on myofibroblasts. Therefore, we hypothesize that CDH11 could be a targeted domain for cell-specific drug delivery and targeted inhibition of BCL-2 to ameliorate the development of fibrosis in the skin. To prove our hypothesis, we have developed liposomes (LPS) conjugated with CDH11 neutralizing antibody (antiCDH11) to target cell surface CDH11 and loaded these LPS with a BCL-2 inhibitor, Navitoclax (NAVI), to induce apoptosis of CDH11 expressing fibroblasts. The developed LPS were evaluated for physicochemical characterization, stability, in vitro therapeutic efficacy using dermal fibroblasts, and in vivo therapeutic efficacy in bleomycin-induced skin fibrosis model in mice. The findings from in vitro and in vivo studies confirmed that selectivity of LPS was improved towards CDH11 expressing myofibroblasts, thereby improving therapeutic efficacy with no indication of adverse effects. Hence, this novel research work represents a versatile LPS strategy that exhibits promising potential for treating skin fibrosis.

Keywords

Animals, Liposomes, Apoptosis, Fibrosis, Cadherins, Skin, Humans, Fibroblasts, Aniline Compounds, Sulfonamides, Bleomycin, Proto-Oncogene Proteins c-bcl-2, Mice, Inbred C57BL, Antibodies, Neutralizing, Mice, Male, Cadherin 11, Dermal fibrosis, Lipid nanoparticle, Myofibroblast, Scleroderma

Published Open-Access

yes

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