Development of PLGA micro- and nanorods with high capacity of surface ligand conjugation for enhanced targeted delivery

• Published in: Asian journal of pharmceutical sciences Vol. 14; no. 1; pp. 86 - 94
• Main Authors: Cao, Jiafu, Choi, Jin-Seok, Oshi, Murtada A., Lee, Juho, Hasan, Nurhasni, Kim, Jihyun, Yoo, Jin-Wook
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01-01-2019; Shenyang Pharmaceutical University; Elsevier
• Subjects: Film-stretching method; Particle shape; PLGA nanoparticles; Surface modification; Targeted drug delivery; Surface modification; Film-stretching method; Targeted drug delivery; Particle shape; PLGA nanoparticles
• ISSN: 1818-0876; 2221-285X
• DOI: 10.1016/j.ajps.2018.08.008

Particle shape has been recognized as one of the key properties of nanoparticles in biomedical applications including targeted drug delivery. Targeting ability of shape-engineered particles depends largely on targeting ligands conjugated on the particle surface. However, poor capacity for surface ligand conjugation remains a problem in anisotropic nanoparticles made with biodegradable polymers such as PLGA. In this study, we prepared anisotropic PLGA nanoparticles with abundant conjugatable surface functional groups by a film stretching-based fabrication method with poly (ethylene-alt-maleic acid) (PEMA). Scanning electron microscopy images showed that microrods and nanorods were successfully fabricated by the PEMA-based film stretching method. The presence of surface carboxylic acid groups was confirmed by confocal microscopy and zeta potential measurements. Using the improved film-stretching method, the amount of protein conjugated to the surface of nanorods was increased three-fold. Transferrin-conjugated, nanorods fabricated by the improved method exhibited higher binding and internalization than unmodified counterparts. Therefore, the PEMA-based film-stretching system presented in this study would be a promising fabrication method for non-spherical biodegradable polymeric micro- and nanoparticles with high capacity of surface modifications for enhanced targeted delivery.
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