Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances

Đorđević, Sanela M.; Santrač, Anja; Cekić, Nebojša; Marković, Bojan; Divović, Branka; Ilić, Tanja; Savić, Miroslav M.; Savić, Snežana

doi:10.1016/j.ijpharm.2017.05.051

Cited by 40 publications

(18 citation statements)

References 27 publications

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“…NE technology has an increasing influence in every aspect of drug delivery (16)(17)(18), particularly in ophthalmic drug delivery (2,19). Physicochemical properties affecting in vivo performance of an ophthalmic NE include droplet size, size distribution and zeta-potential, formulation viscosity profile as a function of applied shear, pH, osmolarity, and surface tension (20,21).…”

Section: Resultsmentioning

confidence: 99%

In vitro evaluation of stearylamine cationic nanoemulsions for improved ocular drug delivery

et al. 2019

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Oil-in-water nanoemulsions (NEs) represent one of the formulation approaches to improve eye-related bio-availability of lipophilic drugs. The potential of cationic NEs is pronounced due to the electrostatic interaction of positively charged droplets with negatively charged mucins present in the tear film, providing prolonged formulation residence at the ocular surface. The aim of this study was to develop a cationic ophthalmic NE with cationic lipid stearylamine (SA) as a carrier of a positive charge. The addition of a nonionic surfactant provided the dual electro-steric stabilization of NEs and enabled tuning of SA concentration to achieve an optimal balance between its interaction with mucins and biocompatibility. Physicochemical characterization, stability profile, in vitro mucoadhesion study and biocompatibility study employing 3D HCE-T cell-based model of corneal epithelium pointed out the NE with 0.05 % (m/m) SA as the leading formulation. Minimizing SA content while retaining droplet/mucin interactions is of great importance for efficacy and safety of future ophthalmic drug products.

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Section: Resultsmentioning

confidence: 99%

In vitro evaluation of stearylamine cationic nanoemulsions for improved ocular drug delivery

et al. 2019

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“…The pharmacokinetic study revealed almost 8.30-fold increase in oral bioavailability of iloperidone NLCs as compared to the plain drug solution. The nanoemulsions of riperidone also showed improved bioavailability and brain uptake [147]. Intranasal administration of risperidone-loaded mucoadhesive nanoemulsion demonstrated higher efficacy, enhanced brain targeting and higher drug transport to the brain in Swiss albino rats, when compared with intranasal risperidone solution and risperidone nanoemulsion intravenously [105].…”

Section: Drug Delivery For Schizophrenia and Bipolar Disordersmentioning

confidence: 94%

Nano Carrier Drug Delivery Systems for the Treatment of Neuropsychiatric Disorders: Advantages and Limitations

et al. 2020

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Neuropsychiatric diseases are one of the main causes of disability, affecting millions of people. Various drugs are used for its treatment, although no effective therapy has been found yet. The blood brain barrier (BBB) significantly complicates drugs delivery to the target cells in the brain tissues. One of the problem-solving methods is the usage of nanocontainer systems. In this review we summarized the data about nanoparticles drug delivery systems and their application for the treatment of neuropsychiatric disorders. Firstly, we described and characterized types of nanocarriers: inorganic nanoparticles, polymeric and lipid nanocarriers, their advantages and disadvantages. We discussed ways to interact with nerve tissue and methods of BBB penetration. We provided a summary of nanotechnology-based pharmacotherapy of schizophrenia, bipolar disorder, depression, anxiety disorder and Alzheimer’s disease, where development of nanocontainer drugs derives the most active. We described various experimental drugs for the treatment of Alzheimer’s disease that include vector nanocontainers targeted on β-amyloid or tau-protein. Integrally, nanoparticles can substantially improve the drug delivery as its implication can increase BBB permeability, the pharmacodynamics and bioavailability of applied drugs. Thus, nanotechnology is anticipated to overcome the limitations of existing pharmacotherapy of psychiatric disorders and to effectively combine various treatment modalities in that direction.

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“…The autoclaved formulation remained stable at 4 and 25 • C; globule size (GS), polydispersity index (PDI), and zeta potential (ZP) did not show a significant change in comparison to pre-autoclaved formulation for one-month (last time-point tested). Sanela et al reported that the physical stability parameters such as GS, PDI, and ZP of risperidone-containing NE formulations did not change after autoclaving compared to 0.22 µm-filtered NE formula-tions, and no significant change in these parameters was observed after one year of storage at 25 • C [51]. Arjun et al also reported that there were no significant changes in GS, PDI, ZP, and drug content of the rebamipide containing NE formulation upon autoclaving [52].…”

Section: Autoclavability Of the Optimized Ne Formulationmentioning

confidence: 99%

Design of Topical Ocular Ciprofloxacin Nanoemulsion for the Management of Bacterial Keratitis

et al. 2021

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Bacterial keratitis (BK) is a critical ocular infection that can lead to serious visual disability. Ciprofloxacin (CIP), moxifloxacin (MOX), and levofloxacin (LFX) have been accepted as monotherapies by the US Food and Drug Administration for BK treatment. CIP is available commercially at 0.3% w/v concentration as an ophthalmic solution and as an ointment for ocular delivery. Because of solubility issues at physiological pH, CIP precipitation can occur at the corneal surface post instillation of the solution dosage form. Consequently, the ocular bioavailability of CIP is reduced. The ointment dosage form is associated with side effects such as blurred vision, itching, redness, eye discomfort, and eye dryness. This study aimed to design a CIP loaded nanoemulsion (NE; CIP-NE) to facilitate drug penetration into the corneal layers for improved therapeutic outcomes as well as to overcome the drawbacks of the current commercial ophthalmic formulations. CIP-NE formulations were prepared by hot homogenization and ultrasonication, using oleic acid (CIP-O-NE) and Labrafac® Lipophile WL 1349 (CIP-L-NE) as the oily phase, and Tween® 80 and Poloxamer 188 as surfactants. Optimized CIP-NE was further evaluated with respect to in vitro release, ex vivo transcorneal permeation, and moist heat sterilization process, using commercial CIP ophthalmic solution as a control. Optimized CIP-O-NE formulation showed a globule size, polydispersity index, and zeta potential of 121.6 ± 1.5 nm, 0.13 ± 0.01, and −35.1 ± 2.1 mV, respectively, with 100.1 ± 2.0 % drug content and was spherical in shape. In vitro release and ex vivo transcorneal permeation studies exhibited sustained release and a 2.1-fold permeation enhancement, respectively, compared with commercial CIP ophthalmic solution. Autoclaved CIP-O-NE formulation was found to be stable for one month (last time-point tested) at refrigerated and room temperature. Therefore, CIP-NE formulation could serve as an effective delivery system for CIP and could improve treatment outcomes in BK.

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Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances

Cited by 40 publications

References 27 publications

In vitro evaluation of stearylamine cationic nanoemulsions for improved ocular drug delivery

In vitro evaluation of stearylamine cationic nanoemulsions for improved ocular drug delivery

Nano Carrier Drug Delivery Systems for the Treatment of Neuropsychiatric Disorders: Advantages and Limitations

Design of Topical Ocular Ciprofloxacin Nanoemulsion for the Management of Bacterial Keratitis

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