Ocular Penetration of fluorometholone-loaded PEG-PLGA Nanoparticles Functionalized With cell-penetrating Peptides

González-Pizarro, Roberto; Parrotta, Graziella; Vera, Rodrigo; Galindo, Ruth; Kjeldsen, Frank; Badı́a, Josefa; Baldomà, Laura; Espina, Marta; García, María L.

doi:10.2217/nnm-2019-0201

Cited by 45 publications

(34 citation statements)

References 48 publications

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“…Due to this positive charge, its incorporation in the NPs modifies the characteristic negative charge of the PLGA NPs. Moreover, modifications of the negative ZP of nanocarriers after peptide incorporation have also been observed by other authors [ 42 ]. Taking into account that the mucus layer itself is an anionic polyelectrolyte at a neutral pH value, the neutrality of PLGA (E1P47) NPs might minimize the PLGA electrostatic repulsion with the mucus layer and therefore contribute to the residence of the NPs loaded with E1P47 in the mucosa.…”

Section: Resultssupporting

confidence: 73%

Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide

et al. 2020

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The effective use of fusion inhibitor peptides against cervical and colorectal infections requires the development of sustained release formulations. In this work we comparatively study two different formulations based on polymeric nanoparticles and lipid vesicles to propose a suitable delivery nanosystem for releasing an HIV-1 fusion inhibitor peptide in vaginal mucosa. Polymeric nanoparticles of poly-d,l-lactic-co-glycolic acid (PLGA) and lipid large unilamellar vesicles loaded with the inhibitor peptide were prepared. Both formulations showed average sizes and polydispersity index values corresponding to monodisperse systems appropriate for vaginal permeation. High entrapment efficiency of the inhibitor peptide was achieved in lipid vesicles, which was probably due to the peptide’s hydrophobic nature. In addition, both nanocarriers remained stable after two weeks stored at 4 °C. While PLGA nanoparticles (NPs) did not show any delay in peptide release, lipid vesicles demonstrated favorably prolonged release of the peptide. Lipid vesicles were shown to improve the retention of the peptide on ex vivo vaginal tissue in a concentration sufficient to exert its pharmacological effect. Thus, the small size of lipid vesicles, their lipid-based composition as well as their ability to enhance peptide penetration on vaginal tissue led us to consider this formulation as a better nanosystem than polymeric nanoparticles for the sustained delivery of the HIV-1 fusion inhibitor peptide in vaginal tissues.

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Section: Resultssupporting

confidence: 73%

Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide

et al. 2020

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“…For testing the penetration of the polymeric NPs, the depth and area of penetration inside the dentinal tubules were measured using extracted single‐rooted human teeth. Ca(OH)₂ NPs were prepared by adding 17.40% of PLGA labelled with rhodamine 110 to the total concentration of PLGA (Gonzalez‐Pizarro et al, 2019). Moreover, free Ca(OH)₂ was mixed with rhodamine 6G as a control (Deniz et al, 2017; Pérez, 2016), in which the controls were prepared by adding 12.5% of rhodamine 6G to the same concentration of Ca(OH)₂ present in the NPs, after that the solution was dissolved in sterile saline.…”

Section: Methodsmentioning

confidence: 99%

Calcium hydroxide‐loaded PLGA biodegradable nanoparticles as an intracanal medicament

et al. 2021

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Aim To develop a formulation in which calcium hydroxide (Ca(OH)₂) was successfully loaded into poly(lactic‐co‐glycolic acid) (PLGA) biodegradable nanoparticles (NPs) to be used in the field of endodontics as an intracanal medicament, including NP optimization and characterization, plus drug release profile of the NPs compared with free Ca(OH)₂. Additionally, the depth and area of penetration of the NPs inside the dentinal tubules of extracted teeth were compared with those of the free Ca(OH)₂. Methodology Ca(OH)₂ NPs were prepared using the solvent displacement method. NPs was optimized with a central composite design to obtain a final optimized formulation. The morphology of the NPs was examined under transmission electron microscopy (TEM), and characterization was carried out using X‐ray diffraction (XRD), Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The drug release profile of the Ca(OH)₂ NPs and free Ca(OH)₂ was evaluated up to 48 h. Finally, the depth and area of penetration inside the dentinal tubules of extracted teeth were examined for both the Ca(OH)₂ NPs and free Ca(OH)₂ using the Mann–Whitney U test to determine any significant differences. Results Utilizing the optimized formulation, the Ca(OH)₂ NPs had an average size below 200 nm and polydispersity index lower than 0.2, along with a highly negative zeta potential and suitable entrapment efficiency percentage. The spherical morphology of the Ca(OH)₂ NPs was confirmed using TEM. The results of the XRD, FTIR and DSC revealed no interactions and confirmed that the drug was encapsulated inside the NPs. The drug release profile of the Ca(OH)₂ NPs exhibited a prolonged steady release that remained stable up to 48 h with higher concentrations than the free Ca(OH)₂. After examination by confocal laser scanning microscopy, Ca(OH)₂ NPs had a significantly greater depth and area of penetration inside dentinal tubules compared with the free drug. Conclusions Ca(OH)₂‐loaded PLGA NPs were successfully optimized and characterized. The NPs exhibited a prolonged drug release profile and superior penetration inside dentinal tubules of extracted teeth when compared to Ca(OH)2.

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“…Prior to the experiment, rhodamine-labelled PLGA (R-PLGA) was synthesized as described by Gonzalez-Pizarro et al [ 38 ] and used at 0.01% obtaining rhodamine labelled nanoparticles (R-TH-NPs). Skin penetration assay was executed using vertical diffusion Franz cells (FDC-400, Vidra-Foc, Barcelona, Spain) with a thermal bath set to 32 °C to mimic skin in vivo conditions, under constant stirring.…”

Section: Methodsmentioning

confidence: 99%

“…Cell nuclei were stained with 4′,6-diamidino-2-phenylindole (DAPI, Sigma Aldrich, Madrid, Spain) at 0.5 µg/mL for 15 min. Internalization of NPs in HaCaT cells was assessed by confocal microscopy (Leica TCS SPII), using the 63X oil immersion objective lens [ 38 ]. Images were processed using Fiji image software [ 38 ].…”

Section: Methodsmentioning

confidence: 99%

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Surface-Modified Multifunctional Thymol-Loaded Biodegradable Nanoparticles for Topical Acne Treatment

et al. 2021

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The present work is focused on the development of novel surface-functionalized poly(lactic-co-glycolic acid) nanoparticles loaded with thymol (TH-NPs) for topical administration enhancing thymol anti-inflammatory, antioxidant and wound healing activities against acne. TH-NPs were prepared by solvent evaporation method using different surface functionalization strategies and obtaining suitable physicochemical parameters and a good short-term stability at 4 °C. Moreover, TH-NPs skin penetration and antioxidant activity were assessed in ex vivo pig skin models. Skin penetration of TH-NPs followed the follicular route, independently of the surface charge and they were able to enhance antioxidant capacity. Furthermore, antimicrobial activity against Cutibacterium acnes was evaluated in vitro by the suspension test showing improved antibacterial performance. Using human keratinocyte cells (HaCat), cytotoxicity, cellular uptake, antioxidant, anti-inflammatory and wound healing activities were studied. TH-NPs were non-toxic and efficiently internalized inside the cells. In addition, TH-NPs displayed significant anti-inflammatory, antioxidant and wound healing activities, which were highly influenced by TH-NPs surface modifications. Moreover, a synergic activity between TH-NPs and their surface functionalization was demonstrated. To conclude, surface-modified TH-NPs had proven to be suitable to be used as anti-inflammatory, antioxidant and wound healing agents, constituting a promising therapy for treating acne infection and associated inflammation.

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Ocular Penetration of fluorometholone-loaded PEG-PLGA Nanoparticles Functionalized With cell-penetrating Peptides

Cited by 45 publications

References 48 publications

Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide

Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide

Calcium hydroxide‐loaded PLGA biodegradable nanoparticles as an intracanal medicament

Surface-Modified Multifunctional Thymol-Loaded Biodegradable Nanoparticles for Topical Acne Treatment

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