Freeze drying optimization of polymeric nanoparticles for ocular flurbiprofen delivery: effect of protectant agents and critical process parameters on long-term stability

Yacasi, Gladys Rosario Ramos; Calpena, Ana Cristina; Gras, María Antonia Egea; Espina, Marta; López, María Luisa García

doi:10.1080/03639045.2016.1275669

Cited by 26 publications

(19 citation statements)

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“…However, the ratio before and after was close to 1 in all cases. These results were in agreement with other authors that freeze dried PLGA NPs such as Ramos et al confirming that 25 KGy does not affect the physicochemical structure of DXI NPs [36].…”

Section: Sterilization Using Gamma Radiationsupporting

confidence: 94%

Dexibuprofen Biodegradable Nanoparticles: One Step Closer towards a Better Ocular Interaction Study

et al. 2020

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Ocular inflammation is one of the most prevalent diseases in ophthalmology, which can affect various parts of the eye or the surrounding tissues. Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, are commonly used to treat ocular inflammation in the form of eye-drops. However, their bioavailability in ocular tissues is very low (less than 5%). Therefore, drug delivery systems such as biodegradable polymeric PLGA nanoparticles constitute a suitable alternative to topical eye administration, as they can improve ocular bioavailability and simultaneously reduce drug induced side effects. Moreover, their prolonged drug release can enhance patient treatment adherence as they require fewer administrations. Therefore, several formulations of PLGA based nanoparticles encapsulating dexibuprofen (active enantiomer of Ibuprofen) were prepared using the solvent displacement method employing different surfactants. The formulations have been characterized and their interactions with a customized lipid corneal membrane model were studied. Ex vivo permeation through ocular tissues and in vivo anti-inflammatory efficacy have also been studied.

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Section: Sterilization Using Gamma Radiationsupporting

confidence: 94%

Dexibuprofen Biodegradable Nanoparticles: One Step Closer towards a Better Ocular Interaction Study

et al. 2020

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“…However, the signal intensity of F68 peaks were less pronounced on DLNs' diffractograms, and PVP-K25 maintained the amorphous state. These investigations support that the amorphous structure of DLNs, as demonstrated by the diffractograms, is related to the lower level of LOR's crystallinity rather than to the effects of the stabilizers used (Ramos Yacasi et al, 2017). To evaluate the thermal behavior of the nanoparticles prepared, DSC thermograms of the raw materials, PMs and DLNs were taken (Figure 4a).…”

Section: Structural Investigations (Xrpd Dsc and Ft-ir)mentioning

confidence: 56%

Design and characterization of loratadine nanosuspension prepared by ultrasonic-assisted precipitation

Alshweiat

Katona

Csóka

et al. 2018

European Journal of Pharmaceutical Sciences

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“…The increasing of T g of the polymer could be attributed to the incorporation of an alkaline drug, which causes interactions between the carboxylic groups of the polymer. In addition, results suggest that this formulation will be amenable to freeze‐dried . In vitro cell viability studies were performed demonstrating that MEM‐NPs were better tolerated than free memantine by epithelial and neuronal cultures.…”

Section: Discussionmentioning

confidence: 99%

Memantine‐Loaded PEGylated Biodegradable Nanoparticles for the Treatment of Glaucoma

Sánchez-López

Egea

Davis³

et al. 2017

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Glaucoma is a multifactorial neurodegenerative disease associated with retinal ganglion cells (RGC) loss. Increasing reports of similarities in glaucoma and other neurodegenerative conditions have led to speculation that therapies for brain neurodegenerative disorders may also have potential as glaucoma therapies. Memantine is an N-methyl-d-aspartate (NMDA) antagonist approved for Alzheimer's disease treatment. Glutamate-induced excitotoxicity is implicated in glaucoma and NMDA receptor antagonism is advocated as a potential strategy for RGC preservation. This study describes the development of a topical formulation of memantine-loaded PLGA-PEG nanoparticles (MEM-NP) and investigates the efficacy of this formulation using a well-established glaucoma model. MEM-NPs <200 nm in diameter and incorporating 4 mg mL of memantine were prepared with 0.35 mg mL localized to the aqueous interior. In vitro assessment indicated sustained release from MEM-NPs and ex vivo ocular permeation studies demonstrated enhanced delivery. MEM-NPs were additionally found to be well tolerated in vitro (human retinoblastoma cells) and in vivo (Draize test). Finally, when applied topically in a rodent model of ocular hypertension for three weeks, MEM-NP eye drops were found to significantly (p < 0.0001) reduce RGC loss. These results suggest that topical MEM-NP is safe, well tolerated, and, most promisingly, neuroprotective in an experimental glaucoma model.

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Freeze drying optimization of polymeric nanoparticles for ocular flurbiprofen delivery: effect of protectant agents and critical process parameters on long-term stability

Abstract: An optimal freeze dried ocular formulation was achieved. Evidently, the successful design of this promising colloidal system resulted from rational cooperation between a good formulation and the right conditions in the FD process.

Cited by 26 publications

References 50 publications

Dexibuprofen Biodegradable Nanoparticles: One Step Closer towards a Better Ocular Interaction Study

Dexibuprofen Biodegradable Nanoparticles: One Step Closer towards a Better Ocular Interaction Study

Design and characterization of loratadine nanosuspension prepared by ultrasonic-assisted precipitation

Memantine‐Loaded PEGylated Biodegradable Nanoparticles for the Treatment of Glaucoma

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