Flurbiprofen sodium microparticles and soft pellets for nose-to-brain delivery: Serum and brain levels in rats after nasal insufflation

Fasiolo, Laura Tiozzo; Manniello, Michele Dario; Banella, Sabrina; Napoli, Laura; Bortolotti, Fabrizio; Quarta, Eride; Colombo, Paolo; Balafas, Evangelos; Kostomitsopoulos, Nikolaos; Rekkas, Dimitrios M.; Valsami, Georgia; Papakyriakopoulou, Paraskevi; Colombo, Gaia; Russo, Paola

doi:10.1016/j.ijpharm.2021.120827

Cited by 14 publications

(10 citation statements)

References 50 publications

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“…Although AUC plasma was considerably higher than AUC brain of CUR-LF NPs via IV administration, it was reassuring to observe that a significant proportion of CUR-LF NPs could still cross the BBB into the brain because LF receptors were highly expressed in the BBB ( Ye et al, 2013 ). The obtained results suggested that the brain accumulation of CUR via IN administration of CUR-LF NPs could be achieved mainly through two pathways: one was that CUR-LF NPs were absorbed into the peripheral circulation through the extensively vascularized respiratory area and then crossed the BBB via the LF receptor-mediated endocytic pathway, and the other was that CUR-LF NPs entered the brain via the direct nose-to-brain route ( Tiozzo Fasiolo et al, 2021 ). For further studies, we calculated the BTE and DTP of CUR-LF NPs via IN administration by Equations 6 , 7 , which were 248.1% and 59.7%, respectively.…”

Section: Resultsmentioning

confidence: 99%

Nose-to-brain delivery of self-assembled curcumin-lactoferrin nanoparticles: Characterization, neuroprotective effect and in vivo pharmacokinetic study

Tan

Zhang

et al. 2023

Front. Bioeng. Biotechnol.

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Curcumin (CUR) is a natural polyphenol extract with significant antioxidant and anti-inflammatory effects, which indicates its great potential for neuroprotection. Lactoferrin (LF), a commonly used oral carrier and targeting ligand, has not been reported as a multifunctional nanocarrier for nose-to-brain delivery. This study aims to develop a nose-to-brain delivery system of curcumin-lactoferrin nanoparticles (CUR-LF NPs) and to further evaluate the neuroprotective effects in vitro and brain accumulation in vivo. Herein, CUR-LF NPs were prepared by the desolvation method with a particle size of 84.8 ± 6.5 nm and a zeta potential of +22.8 ± 4.3 mV. The permeability coefficient of CUR-LF NPs (4.36 ± 0.79 × 10−6 cm/s) was 50 times higher than that of CUR suspension (0.09 ± 0.04 × 10−6 cm/s) on MDCK monolayer, indicating that the nanoparticles could improve the absorption efficiency of CUR in the nasal cavity. Moreover, CUR-LF NPs showed excellent protection against Aβ25-35-induced nerve damage in PC12 cells. In vivo pharmacokinetic studies showed that the brain-targeting efficiency of CUR-LF NPs via IN administration was 248.1%, and the nose-to-brain direct transport percentage was 59.7%. Collectively, nose-to-brain delivery of CUR-LF NPs is capable of achieving superior brain enrichment and potential neuroprotective effects.

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Section: Resultsmentioning

confidence: 99%

Nose-to-brain delivery of self-assembled curcumin-lactoferrin nanoparticles: Characterization, neuroprotective effect and in vivo pharmacokinetic study

Tan

Zhang

et al. 2023

Front. Bioeng. Biotechnol.

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“…The method of delivering aerogel to the rat’s nose is similar to the methods described in the works [ 38 , 39 , 40 ], but has several improvements. The powdered substance was placed in a cone-shaped tip, which was connected to a tube from a compressed air container.…”

Section: Resultsmentioning

confidence: 99%

Preparation of Protein Aerogel Particles for the Development of Innovative Drug Delivery Systems

Lovskaya

Bezchasnyuk

Mochalova

et al. 2022

Gels

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The research was oriented towards the preparation of aerogel particles based on egg white and whey protein isolate using various dispersion methods: dripping, spraying, and homogenization. Based on the results of analytical studies, the most appropriate samples were selected to obtain aerogels loaded with the drug. The results of the experimental research were used to study methods for obtaining nasal drug delivery systems based on aerogels. Protein aerogels were obtained by thermal gelation followed by supercritical drying. The obtained particles of protein aerogels have a specific surface area of up to 350 m2/g with a pore volume of up to 2.9 cm3/g, as well as a porosity of up to 95%. The results of experimental studies have shown that changing the dispersion method makes it possible to control the structural characteristics of protein aerogel particles. The results of the studies were applied to obtain innovative nasal drug delivery systems for the treatment of socially significant diseases. Analytical studies were conducted to determine the amount and state of adsorbed drugs in protein aerogel particles, as well as in vivo experiments on the distribution of clomipramine in blood plasma and brain tissue of rats to study the pharmacokinetics and bioavailability of the resulting drug-loaded protein aerogel.

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“…The oral administration was performed by gavage. For powder administration, the technique described by Tiozzo Fasiolo et al (2021) [ 34 ] was adopted. Briefly, the insufflator’s tip was inserted 1–2 mm into the nostril, and the powder was administered in a single shot by activating the pump.…”

Section: Methodsmentioning

confidence: 99%

“…In order to assess the IN administration of Que for brain targeting, various PK parameters such as the AUC (area under the concentration–time curve), C max (maximum observed concentration) and t max (time of maximum concentration) were determined. Additionally, the specific indexes [ 33 , 34 ] were calculated to evaluate the extent of the direct NTB delivery of Que.…”

Section: Introductionmentioning

confidence: 99%

Comparative Serum and Brain Pharmacokinetics of Quercetin after Oral and Nasal Administration to Rats as Lyophilized Complexes with β-Cyclodextrin Derivatives and Their Blends with Mannitol/Lecithin Microparticles

Manta,

Papakyriakopoulou,

Nikolidaki

et al. 2023

Pharmaceutics

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Quercetin (Que) is one of the most studied flavonoids with strong antioxidant properties ascribed to its ability to bind free radicals and inactivate them. However, the low solubility of the compound along with its inadequate absorption after oral administration limit its beneficial effects. Que’s complexation with two different cyclodextrin (CD) derivatives (hydroxypropyl-β-CD and methyl-β-CD) via the neutralization/lyophilization method has been found to improve its physicochemical properties. Moreover, blends of the lyophilized powders with mannitol/lecithin microparticles (MLMPs) have been proposed as candidates for intranasal (IN) administration after in vitro and ex vivo evaluations. In this context, a comparative pharmacokinetic (PK) study of the IN vs oral administration of Que lyophilized powders and their blends with MLMPs (75:25 w/w) was performed on Wistar rats. The PK parameters estimated by a non-compartmental analysis using the sparse data methodology in Phoenix® 8.3 (Certara, Princeton, NJ, USA) illustrated the effectiveness of IN administration either in brain targeting or in reaching the bloodstream. Significant levels of the compound were achieved at both sites, compared to those after oral delivery which were negligible. These results favor the potential application of the prepared Que nasal powders for systemic and nose-to-brain delivery for the prevention and/or treatment of neuroinflammatory degenerative conditions, such as Parkinson’s and Alzheimer’s disease.

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Flurbiprofen sodium microparticles and soft pellets for nose-to-brain delivery: Serum and brain levels in rats after nasal insufflation

Cited by 14 publications

References 50 publications

Nose-to-brain delivery of self-assembled curcumin-lactoferrin nanoparticles: Characterization, neuroprotective effect and in vivo pharmacokinetic study

Nose-to-brain delivery of self-assembled curcumin-lactoferrin nanoparticles: Characterization, neuroprotective effect and in vivo pharmacokinetic study

Preparation of Protein Aerogel Particles for the Development of Innovative Drug Delivery Systems

Comparative Serum and Brain Pharmacokinetics of Quercetin after Oral and Nasal Administration to Rats as Lyophilized Complexes with β-Cyclodextrin Derivatives and Their Blends with Mannitol/Lecithin Microparticles

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