Nose to brain delivery in rats: Effect of surface charge of rhodamine B labeled nanocarriers on brain subregion localization

Bonaccorso, Angela; Musumeci, Teresa; Serapide, Maria Francesca; Pellitteri, Rosalia; Uchegbu, Ijeoma F.; Puglisi, Giovanni

doi:10.1016/j.colsurfb.2017.03.035

Cited by 75 publications

(53 citation statements)

References 42 publications

(44 reference statements)

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“…At 48 h after their IN administration, PLGA 65/35-HPC-GAL-Rhod nanoparticles were detected in the hippocampus of all experimental rats. This was in full accordance with previous studies demonstrating that the uptake of PLGA nanoparticles in the rat brain is significantly increased 48 h after their IN administration [11]. No fluorescence was detected in the hippocampi of the IN saline-treated rats.…”

Section: Selection and Fluorescence Evaluation Of Rhodamine-treated Psupporting

confidence: 93%

“…More specifically, nanoparticle accumulations were detected in the cytoplasm of both pyramidal neurons (primary neurons of the CA fields) and granule cells (primary neurons of the DG). In a previous study by Bonaccorso et al [11], chitosan/PLGA nanoparticles were also detected in the cytoplasm of hippocampal neurons after their IN administration. Shang and colleagues [36] reported that not only the polymeric properties but also the size of polymeric nanoparticles determine their uptake efficiency and internalization when reacting with living cells, proposing that nanoparticles with an average size of 200-500 nm are capable to enter the cells via endocytosis, mostly involving a caveolae-mediated mechanism [37].…”

Section: Plga 65/35-hpc-gal Nanoparticles In the Hippocampus Of The Rmentioning

confidence: 78%

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Hierarchical Porous Carbon—PLLA and PLGA Hybrid Nanoparticles for Intranasal Delivery of Galantamine for Alzheimer’s Disease Therapy

et al. 2020

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In the present study, poly(l-lactic acid) (PLLA) and poly(lactide-co-glycolide) (PLGA) hybrid nanoparticles were developed for intranasal delivery of galantamine, a drug used in severe to moderate cases of Alzheimer's disease. Galantamine (GAL) was adsorbed first in hierarchical porous carbon (HPC). Formulations were characterized by FT-IR, which showed hydrogen bond formation between GAL and HPC. Furthermore, GAL became amorphous after adsorption, as confirmed by XRD and differential scanning calorimetry (DSC) studies. GAL was quantified to be 21.5% w/w by TGA study. Adsorbed GAL was nanoencapsulated in PLLA and PLGA, and prepared nanoparticles were characterized by several techniques. Their sizes varied between 182 and 394 nm, with an exception that was observed in nanoparticles that were prepared by PLLA and adsorbed GAL that was found to be 1302 nm in size. DSC thermographs showed that GAL was present in its crystalline state in nanoparticles before its adsorption to HPC, while it remained in its amorphous phase after its adsorption in the prepared nanoparticles. It was found that the polymers controlled the release of GAL both when it was encapsulated alone and when it was adsorbed on HPC. Lastly, PLGA hybrid nanoparticles were intranasally-administered in healthy, adult, male Wistar rats. Administration led to successful delivery to the hippocampus, the brain area that is primarily and severely harmed in Alzheimer's disease, just a few hours after a single dose.

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Section: Selection and Fluorescence Evaluation Of Rhodamine-treated Psupporting

confidence: 93%

Section: Plga 65/35-hpc-gal Nanoparticles In the Hippocampus Of The Rmentioning

confidence: 78%

Hierarchical Porous Carbon—PLLA and PLGA Hybrid Nanoparticles for Intranasal Delivery of Galantamine for Alzheimer’s Disease Therapy

et al. 2020

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“…Interestingly, although PLGA nanoparticles have not been reported to be mucoadhesive or penetration enhancers, drug delivery to the brain is still enhanced through the nasal route. In a trial to coat the PLGA nanoparticles with chitosan, it was observed that their brain transport was altered and positively charged chitosan-coated PLGA nanoparticles appeared to move slower than plain negatively charged PLGA nanoparticles from the caudal to the rostral regions of the brain [206]. Another study developed huperzine A-loaded, mucoadhesive, and targeted PLGA nanoparticles with surface modification by lactoferrin-conjugated N-trimethylated chitosan for efficient intranasal delivery of huperzine A to the brain for AD treatment.…”

Section: Nanoparticles Composed Of Chitosan and Chitosan Derivativesmentioning

confidence: 99%

Intranasal Delivery of Nanoformulations: A Potential Way of Treatment for Neurological Disorders

et al. 2020

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Although the global prevalence of neurological disorders such as Parkinson's disease, Alzheimer's disease, glioblastoma, epilepsy, and multiple sclerosis is steadily increasing, effective delivery of drug molecules in therapeutic quantities to the central nervous system (CNS) is still lacking. The blood brain barrier (BBB) is the major obstacle for the entry of drugs into the brain, as it comprises a tight layer of endothelial cells surrounded by astrocyte foot processes that limit drugs' entry. In recent times, intranasal drug delivery has emerged as a reliable method to bypass the BBB and treat neurological diseases. The intranasal route for drug delivery to the brain with both solution and particulate formulations has been demonstrated repeatedly in preclinical models, including in human trials. The key features determining the efficacy of drug delivery via the intranasal route include delivery to the olfactory area of the nares, a longer retention time at the nasal mucosal surface, enhanced penetration of the drugs through the nasal epithelia, and reduced drug metabolism in the nasal cavity. This review describes important neurological disorders, challenges in drug delivery to the disordered CNS, and new nasal delivery techniques designed to overcome these challenges and facilitate more efficient and targeted drug delivery. The potential for treatment possibilities with intranasal transfer of drugs will increase with the development of more effective formulations and delivery devices. Figure 1. Schematic demonstrating various transport systems that shuttle molecules across the BBB. Very small amount of water-soluble compounds cross through the tight junctions (paracellular), whereas lipid-soluble agents traverse via the transcellular lipophilic pathway. Selective transport systems exist for glucose, amino acids, nucleosides, and other substances, in addition to specific receptor-mediated endocytosis for certain proteins such as insulin and transferrin. (AZT = azathioprine). List of CNS Diseases Parkinson's Disease (PD)PD, occurring primarily in the substantia nigra, is the second-most common neurodegenerative disease, leading to the development of bradykinesia and tremors of cardinal motor functions ( Figure 2) [3]. PD models specifically show a decrease in dopamine transporters, which are responsible for dopamine uptake by dopaminergic neurons and progression of neuronal communications. Reduced Figure 1. Schematic demonstrating various transport systems that shuttle molecules across the BBB. Very small amount of water-soluble compounds cross through the tight junctions (paracellular), whereas lipid-soluble agents traverse via the transcellular lipophilic pathway. Selective transport systems exist for glucose, amino acids, nucleosides, and other substances, in addition to specific receptor-mediated endocytosis for certain proteins such as insulin and transferrin. (AZT = azathioprine). List of CNS Diseases Parkinson's Disease (PD)PD, occurring primarily in the substantia nigra, is the second-most common neuro...

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“…Surface charge of the nanoparticles could influence the mechanisms involved in their transport from the nasal cavity to the CNS. Indeed, the olfactory pathway is mainly responsible for the translocation of negatively charged nanoparticles, whereas the positively charged nanoparticles reach the brain more slowly, by involving the trigeminal pathway [50]. Intranasally applied nanoparticles have to penetrate the mucus layer covering nasal mucosa to reach the olfactory mucosa, and thus the CNS [51].…”

Section: Preparation Of Liposomesmentioning

confidence: 99%

Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

et al. 2020

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Direct nose-to-brain delivery has been raised as a non-invasive powerful strategy to deliver drugs to the brain bypassing the blood-brain barrier (BBB). This study aimed at preparing and characterizing an innovative composite formulation, associating the liposome and hydrogel approaches, suitable for intranasal administration. Thermosensitive gel formulations were obtained based on a mixture of two hydrophilic polymers (Poloxamer 407, P407 and Poloxamer 188, P188) for a controlled delivery through nasal route via liposomes of an active pharmaceutical ingredient (API) of potential interest for Alzheimer’s disease. The osmolarity and the gelation temperature (T° sol-gel) of formulations, defined in a ternary diagram, were investigated by rheometry and visual determination. Regarding the issue of assays, a mixture composed of P407/P188 (15/1%, w/w) was selected for intranasal administration in terms of T° sol-gel and for the compatibility with the olfactory mucosal (280 ± 20 mOsmol, pH 6). Liposomes of API were prepared by the thin film hydration method. Mucoadhesion studies were performed by using mucin disc, and they showed the good natural mucoadhesive characteristics of in situ gel formulations, which increased when liposomes were added. The study demonstrated successful pharmacotechnical development of a promising API-loaded liposomes in a thermosensitive hydrogel intended for nasal Alzheimer’s disease treatment.

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Nose to brain delivery in rats: Effect of surface charge of rhodamine B labeled nanocarriers on brain subregion localization

Cited by 75 publications

References 42 publications

Hierarchical Porous Carbon—PLLA and PLGA Hybrid Nanoparticles for Intranasal Delivery of Galantamine for Alzheimer’s Disease Therapy

Hierarchical Porous Carbon—PLLA and PLGA Hybrid Nanoparticles for Intranasal Delivery of Galantamine for Alzheimer’s Disease Therapy

Intranasal Delivery of Nanoformulations: A Potential Way of Treatment for Neurological Disorders

Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

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