One-step solid-oil-water emulsion for sustained bioactive ranibizumab release

BACKGROUND: The advent of therapeutic proteins highlights the need for delivery systems that protect and extend the duration of its action. Ranibizumab-VEGF is one such drug used for treating wet AMD. This paper describes a facile method to sustain bioactive ranibizumab release from PLGA-based particles.

METHODS: Two emulsion techniques were explored namely: water-in-oil-in-water (WOW) and solid-in-oil-in-water (SOW) emulsion. The bioactivity of ranibizumab was evaluated by comparing its binding capability to VEGF, measured with ELISA to total protein measured by microBCA.

RESULTS: During the emulsion process, contact of ranibizumab with the water-oil interface is the main destabilizing factor and this can be prevented with the use of amphiphilic PVA and solid-state protein in WOW and SOW emulsion respectively. In vitro release of the ranibizumab-loaded particles indicated that a 15-day release could be achieved with SOW particles while the WOW particles generally suffered from a burst release. Released ranibizumab was capable of inhibiting endothelial cell growth indicating its retention of bioactivity. The suppression of burst release from the SOW particles was attributed to the relatively smooth surface morphology of the SOW microparticles.

CONCLUSIONS: The use of SOW encapsulation in modulating ranibizumab release while maintaining their bioactivity has been highlighted.

Medienart:

E-Artikel

Erscheinungsjahr:

2018

Erschienen:

2018

Enthalten in:

Zur Gesamtaufnahme - volume:15

Enthalten in:

Expert opinion on drug delivery - 15(2018), 12 vom: 07. Dez., Seite 1143-1156

Sprache:

Englisch

Beteiligte Personen:

Chua, Hui Yee [VerfasserIn]
Lui, Yuan Siang [VerfasserIn]
Bhuthalingam, Ramya [VerfasserIn]
Agrawal, Rupesh [VerfasserIn]
Wong, Tina [VerfasserIn]
Preiser, Peter Rainer [VerfasserIn]
Venkatraman, Subbu [VerfasserIn]

Links:

Volltext

Themen:

1SIA8062RS
Angiogenesis Inhibitors
Bioactive
Delayed-Action Preparations
Emulsions
Journal Article
PLGA
Polylactic Acid-Polyglycolic Acid Copolymer
Ranibizumab
Research Support, Non-U.S. Gov't
Solvent emulsion-evaporation
Sustained release
ZL1R02VT79

Anmerkungen:

Date Completed 15.04.2019

Date Revised 15.04.2019

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1080/17425247.2018.1538209

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM28988960X