Peptide Functionalization of Emulsion-Based Nanocarrier to Improve Uptake across Blood

Peptide Functionalization of Emulsion-Based Nanocarrier to Improve Uptake across Blood–Brain Barrier

Published:2024-07-30 Issue:8 Volume:16 Page:1010
ISSN:1999-4923
Container-title:Pharmaceutics
language:en
Short-container-title:Pharmaceutics

Author:

De Capua Alberta¹²,Vecchione Raffaele¹^ORCID,Sgambato Cinzia¹²,Chino Marco³^ORCID,Lagreca Elena¹^ORCID,Lombardi Angela³^ORCID,Netti Paolo Antonio¹²⁴

Affiliation:

1. Center for Advanced Biomaterials for Health Care (CABHC), Istituto Italiano di Tecnologia, Largo Barsanti e Matteucci 53, 80125 Napoli, Italy

2. Department of Chemical Materials and Industrial Production (DICMaPI), University of Naples Federico II, P.le Tecchio 80, 80125 Naples, Italy

3. Department of Chemical Sciences, University of Naples Federico II, Complesso Universitario Monte S. Angelo, Via Cintia 21, 80126 Naples, Italy

4. Interdisciplinary Research Centre on Biomaterials (CRIB), University of Naples Federico II, P.le Tecchio 80, 80125 Naples, Italy

Abstract

New strategies for enhancing drug delivery to the blood–brain barrier (BBB) represent a major challenge in treating cerebral diseases. Nanoemulsion-based nanocarriers represent an ideal candidate to improve drug delivery thanks to their versatility in functionalization and cargo protection. In this work, a paclitaxel-loaded nano-emulsion has been firstly functionalized and stabilized with two layers constituted of chitosan and hyaluronic acid, and, secondly, the latter has been conjugated to the CRT peptide. CRT is a bioactive peptide that selectively recognizes bEnd.3 cells, a model of the BBB, thanks to its interactions with transferrin (Tf) and its receptor (TfR). Cytotoxic results showed a 41.5% higher uptake of CRT functionalized nano-emulsion than the negative control, demonstrating the ability of this novel tool to be accumulated in brain endothelium tissue. Based upon these results, our approach can be fully generalizable to the design of multifunctional nanocarriers for delivery of therapeutic agents to the central nervous systems.

Funder

EU funding within the MUR PNRR “National Center for Gene Therapy and Drugs based on RNA Technology”

Publisher

MDPI AG

Link

https://www.mdpi.com/1999-4923/16/8/1010/pdf

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