Triamcinolone acetonide-loaded lipid nanocapsules for ophthalmic applications

Formica, María Lina; Gamboa, Gabriela Verónica Ullio; Tártara, Luis Ignacio; Luna, José D.; Benoit, Jean‐Pierre; Palma, Santiago Daniel

doi:10.1016/j.ijpharm.2019.118795

Cited by 28 publications

(15 citation statements)

References 64 publications

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“…Similar results were previously reported by Sabzevari et al. where TA incorporated into PLGA nanoparticles and lipid nanocapsules had better anti-inflammatory effect compared with the drug suspension (Sabzevari et al., 2013b ; Guo et al., 2019 ; Formica et al., 2020 ). Group IV treated with TA-loaded PEG2- b -PLA1 micelles incorporated into chitosan hydrogel showed normal epithelial thickness of the corneal tissue and normal epithelial pattern.…”

Section: Resultssupporting

confidence: 89%

Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and in vivo evaluation in a rabbit ocular inflammatory model

et al. 2020

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The aim of this study was to prepare triamcinolone acetonide (TA)-loaded poly(ethylene glycol)-blockpoly(e-caprolactone) (PEG-b-PCL) and poly(ethylene glycol)-block-poly(lactic acid) (PEG-b-PLA) micelles as a potential treatment of ocular inflammation. The micelles were evaluated for particle size, drug loading capacity and drug release kinetics. Selected micellar formulations were dispersed into chitosan hydrogel and their anti-inflammatory properties were tested in rabbits using a carrageenan-induced ocular inflammatory model. Particle size ranged from 59.44 ± 0.15 to 64.26 ± 0.55 nm for PEG-b-PCL and from 136.10 ± 1.57 to 176.80 ± 2.25 nm for PEG-b-PLA micelles, respectively. The drug loading capacity was in the range of 6-12% and 15-25% for PEG-b-PCL and PEG-b-PLA micelles, respectively and was dependent on the drug/polymer weight ratio. TA aqueous solubility was increased by 5-and 10-fold after loading into PEG-b-PCL and PEG-b-PLA micelles at a polymer concentration as low as 0.5 mg/mL, respectively. PEG-b-PLA micelles suspended in chitosan hydrogel were able to sustain the drug release where only 42.8 ± 1.6% drug was released in one week. TA/PEG-b-PLA micelles suspended in chitosan hydrogel had better anti-inflammatory effects compared with the plain drug hydrogel or the drug micellar solution. Complete disappearance of the corneal inflammatory changes was observed for the micellar hydrogel. These results confirm the potential of PEG-b-PLA micelles suspended in chitosan hydrogel to enhance the anti-inflammatory properties of triamcinolone acetonide.

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Section: Resultssupporting

confidence: 89%

Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and in vivo evaluation in a rabbit ocular inflammatory model

et al. 2020

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“…129 Recently, a novel hybrid formulation based on lipid nanocapsules containing bevacizumab on the surface and triamcinolone acetonide in the inner core was developed to improve ocular therapy; taking into account the strong need to develop complementary and synergistic therapies to target other biomarkers involved in angiogenesis and the high efficacy presented by triamcinolone-loaded lipid nanocapsules in the endotoxin-induced uveitis rabbit model. 130 For this purpose, a phase inversion-insertion one-step method was developed for drug loading and surface modification in nanocapsules by post-inserting a bifunctional polymer, followed by antibody coupling using "click" chemistry. The novel hybrid lipid nanocapsule formulation presented nanometric size (102 nm), negative surface potential, and exhibited 56% of corticosteroid drug in the lipid core.…”

Section: Nanoparticles Based On Lipidsmentioning

confidence: 99%

Biological drug therapy for ocular angiogenesis: Anti‐VEGF agents and novel strategies based on nanotechnology

Formica

Alfonso

Palma

2021

Pharmacology Res & Perspec

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Currently, biological drug therapy for ocular angiogenesis treatment is based on the administration of anti‐VEGF agents via intravitreal route. The molecules approved with this purpose for ocular use include pegaptanib, ranibizumab, and aflibercept, whereas bevacizumab is commonly off‐label used in the clinical practice. The schedule dosage involves repeated intravitreal injections of anti‐VEGF agents to achieve and maintain effective concentrations in retina and choroids, which are administrated as solutions form. In this review article, we describe the features of different anti‐VEGF agents, major challenges for their ocular delivery and the nanoparticles in development as delivery system of them. In this way, several polymeric and lipid nanoparticles are explored to load anti‐VEGF agents with the aim of achieving sustained drug release and thus, minimize the number of intravitreal injections required. The main challenges were focused in the loading the molecules that maintain their bioactivity after their release from nanoparticulate system, followed the evaluation of them through studies of formulation stability, pharmacokinetic, and efficacy in in vitro and in vivo models. The analysis was based on the information published in peer‐reviewed published papers relevant to anti‐VEGF treatments and nanoparticles developed as ocular anti‐VEGF delivery system.

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“…The optimized TA-loaded LNC were tested for safety on human corneal epithelial cells and showed a high anti-inflammatory effect. This was confirmed by the reduction in interleukin-6 levels and the improvement of inflammatory signs in an endotoxin-induced uveitis rabbit model, hence suggesting its prospective applicability for the treatment of various eye diseases [62].…”

Section: Lipid Nanocapsules (Lnc)mentioning

confidence: 62%

“…The inflammation models were induced either in vitro or in vivo. In in vitro model, HCE cells were stimulated with TNF-α (25 ng/mL) for cellular inflammation, while the in vivo inflammation model is induced by treating the animal corneas with lipopolysaccharide (LPS) of E. Coli for 24 h. After that, the tested formulations were applied either to cells or viable corneas, and interleukin IL-6 and IL-8 concentrations were then quantified using ELISA (enzyme-linked immunosorbent assay) kit [29], [60], [62].…”

Section: Inflammation Modelsmentioning

confidence: 99%

Appraising the Competency of Lipid Nano-Platforms as Non-invasive Paradigms for the Treatment of Ocular Inflammations: A review

Shakshak

Ishak

Kamel

et al. 2021

Archives of Pharmaceutical Sciences Ain Shams University

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Ocular inflammation is one of the common ophthalmic disorders triggered by different underlying causes and affecting both anterior and posterior segments of the eye. The functional barriers within the eye greatly impede the efficient ocular drug delivery, and hence the efficient relief of inflammation. The conventional treatment approaches are often limited to the topical applications of eye solutions, suspensions, or ointments, in addition to the intravitreal injections in case of diffuse inflammatory conditions. These strategies suffer from poor patient acceptance and compliance because of their ineffectiveness and lack of safety. During the past few decades, research attention was focused on the development of innovative ophthalmic dosage forms. Lipid nano-platforms had particular importance in drug delivery in terms of safety, biocompatibility, sustainment of drug release, enhancement of drug bioavailability, and hence patient compliance. This review attempts to highlight the current state of lipid-based nanocarriers as a promising non-invasive approach in the management of superficial and diffuse ocular inflammations with special emphasis on their reported outcomes, and also to focus on future perspectives to fill the gaps in this area.

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Triamcinolone acetonide-loaded lipid nanocapsules for ophthalmic applications

Cited by 28 publications

References 64 publications

Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and in vivo evaluation in a rabbit ocular inflammatory model

Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and in vivo evaluation in a rabbit ocular inflammatory model

Biological drug therapy for ocular angiogenesis: Anti‐VEGF agents and novel strategies based on nanotechnology

Appraising the Competency of Lipid Nano-Platforms as Non-invasive Paradigms for the Treatment of Ocular Inflammations: A review

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