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. 2021 May 11;13(5):687.
doi: 10.3390/pharmaceutics13050687.

Ferulic Acid-Loaded Polymeric Nanoparticles for Potential Ocular Delivery

Alessia Romeo  1 , Teresa Musumeci  1   2 , Claudia Carbone  1   2 , Angela Bonaccorso  1 , Simona Corvo  1 , Gabriella Lupo  3 , Carmelina Daniela Anfuso  3 , Giovanni Puglisi  1 , Rosario Pignatello  1   2
Affiliations

Ferulic Acid-Loaded Polymeric Nanoparticles for Potential Ocular Delivery

Alessia Romeo et al. Pharmaceutics. .

Abstract

Ferulic acid (FA) is an antioxidant compound that can prevent ROS-related diseases, but due to its poor solubility, therapeutic efficacy is limited. One strategy to improve the bioavailability is nanomedicine. In the following study, FA delivery through polymeric nanoparticles (NPs) consisting of polylactic acid (NPA) and poly(lactic-co-glycolic acid) (NPB) is proposed. To verify the absence of cytotoxicity of blank carriers, a preliminary in vitro assay was performed on retinal pericytes and endothelial cells. FA-loaded NPs were subjected to purification studies and the physico-hemical properties were analyzed by photon correlation spectroscopy. Encapsulation efficiency and in vitro release studies were assessed through high performance liquid chromatography. To maintain the integrity of the systems, nanoformulations were cryoprotected and freeze-dried. Morphology was evaluated by a scanning electron microscope. Physico-chemical stability of resuspended nanosystems was monitored during 28 days of storage at 5 °C. Thermal analysis and Fourier-transform infrared spectroscopy were performed to characterize drug state in the systems. Results showed homogeneous particle populations, a suitable mean size for ocular delivery, drug loading ranging from 64.86 to 75.16%, and a controlled release profile. The obtained systems could be promising carriers for ocular drug delivery, legitimating further studies on FA-loaded NPs to confirm efficacy and safety in vitro.

Keywords: PLA; PLGA; antioxidant; controlled release; endothelial cell; retinal pericytes.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Cytotoxicity of NPA and NPB NPs on primary endothelial cells after (A) 24 h and (B) 48 h of incubation and on primary retinal pericytes cells after (C) 24 h and (D) 48 h of incubation at different concentrations (5; 2.5; 1; 0.5; 0.25 mg/mL). Three independent experiments were performed in sixfold. Error bars depict the S.D. of the mean. t-test was used to calculate statistical significance of the percentages obtained versus control group. [ns = not significant (p > 0.05); * = significant (p < 0.05); ** = very significant (p < 0.01); *** = extremely significant (p < 0.001)].
Figure 2
Figure 2
Mean size, PDI (A) and zeta potential (B) of the samples NPA-FA and NPB-FA. t-test was used to calculate statistical significance of the percentages obtained versus control group. [ns = not significant (p > 0.05); * = significant (p < 0.05); *** = extremely significant (p < 0.001)].
Figure 3
Figure 3
In vitro release profiles of pure drug, NPA-FA and NPB-FA in phosphate buffered solution (pH 7.4) at 37 °C.
Figure 4
Figure 4
SEM micrographies of: (A) NPA (B) NPB-FA (C) NPB and (D) NPB-FA.
Figure 5
Figure 5
Mean size (A) index of polydispersion (B) zeta potential (C) osmolarity (D) and pH (E) of the samples stored at 5 °C.
Figure 6
Figure 6
(A) DSC and (B) FT-IR curves of FA (a) PLA polymer (b) HP-β-CD (c) unloaded NPA (d) and FA-loaded NPA nanoparticles (e).
Figure 7
Figure 7
(A) DSC and (B) FT-IR curves of FA (a) PLGA polymer (b) HP-β-CD (c) unloaded NPB (d) and FA-loaded NPB nanoparticles (e).
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