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. 2023 Jan 3;15(1):175.
doi: 10.3390/pharmaceutics15010175.

Effects of Particle Geometry for PLGA-Based Nanoparticles: Preparation and In Vitro/In Vivo Evaluation

Meryem Kaplan  1   2 , Kıvılcım Öztürk  1 , Süleyman Can Öztürk  3 , Ece Tavukçuoğlu  4 , Güneş Esendağlı  4 , Sema Calis  1
Affiliations

Effects of Particle Geometry for PLGA-Based Nanoparticles: Preparation and In Vitro/In Vivo Evaluation

Meryem Kaplan et al. Pharmaceutics. .

Abstract

The physicochemical properties (size, shape, zeta potential, porosity, elasticity, etc.) of nanocarriers influence their biological behavior directly, which may result in alterations of the therapeutic outcome. Understanding the effect of shape on the cellular interaction and biodistribution of intravenously injected particles could have fundamental importance for the rational design of drug delivery systems. In the present study, spherical, rod and elliptical disk-shaped PLGA nanoparticles were developed for examining systematically their behavior in vitro and in vivo. An important finding is that the release of the encapsulated human serum albumin (HSA) was significantly higher in spherical particles compared to rod and elliptical disks, indicating that the shape can make a difference. Safety studies showed that the toxicity of PLGA nanoparticles is not shape dependent in the studied concentration range. This study has pioneering findings on comparing spherical, rod and elliptical disk-shaped PLGA nanoparticles in terms of particle size, particle size distribution, colloidal stability, morphology, drug encapsulation, drug release, safety of nanoparticles, cellular uptake and biodistribution. Nude mice bearing non-small cell lung cancer were treated with 3 differently shaped nanoparticles, and the accumulation of nanoparticles in tumor tissue and other organs was not statistically different (p > 0.05). It was found that PLGA nanoparticles with 1.00, 4.0 ± 0.5, 7.5 ± 0.5 aspect ratios did not differ on total tumor accumulation in non-small cell lung cancer.

Keywords: PLGA; anisotrop; biodistribution; cellular uptake; drug delivery; human serum albumin; nanoparticles; particle shape.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Production of differently shaped nanoparticles by film stretching method using texture analyzer.
Figure 2
Figure 2
Particle size distribution of (A,B) blank and (C,D) HSA loaded nanoparticles.
Figure 3
Figure 3
TEM images of differently shaped blank PLGA nanoparticles ((A) Spherical; (B) Rod; (C) Elliptical disk).
Figure 4
Figure 4
HSA release profiles from differently shaped nanoparticles at pH 7.4 (n = 3). Data were expressed as the mean ± SD, error bars were not visible due to SD values being too small.
Figure 5
Figure 5
Cell viability profiles of blank SNs, RNs, and EDNs for (A) 24 h and (B) 48 h.
Figure 6
Figure 6
(A) Mean fluorescent intensities (MFI) of nanoparticles were measured by flow cytometry and the representative flow cytometry histograms were given (* p < 0.05 spherical compared with elliptical disk, ** p < 0.05 rod compared with elliptical disk). (B) Representative fluorescent microscopy images of A549 cells treated with SNs, RNs, and EDNs, cells were stained using DAPI (blue) for nucleus. Red fluorescence shows PLGA (FKR560).
Figure 7
Figure 7
Biodistribution of differently shaped nanoparticles in NSCLC tumor-bearing CD-1 nude mice. (A) Fluorescence images of tumor and major organs (B) MFI values were obtained from tumor and organs after FKR560-labelled PLGA solutions and FKR560-labelled PLGA-based NP applications.
See this image and copyright information in PMC

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