scholarly journals Preparation and characterisation of PHT-loaded chitosan lecithin nanoparticles for intranasal drug delivery to the brain

RSC Advances ◽  
2020 ◽  
Vol 10 (48) ◽  
pp. 28992-29009
Author(s):  
Amal Yousfan ◽  
Noelia Rubio ◽  
Abdul Hakim Natouf ◽  
Aamal Daher ◽  
Nedal Al-Kafry ◽  
...  

The use of nanoparticles (NPs) for intranasal (IN) drug delivery to the brain represents a hopeful strategy to enhance brain targeting of anti-epileptic drugs.

2020 ◽  
Vol 26 (37) ◽  
pp. 4721-4737 ◽  
Author(s):  
Bhumika Kumar ◽  
Mukesh Pandey ◽  
Faheem H. Pottoo ◽  
Faizana Fayaz ◽  
Anjali Sharma ◽  
...  

Parkinson’s disease is one of the most severe progressive neurodegenerative disorders, having a mortifying effect on the health of millions of people around the globe. The neural cells producing dopamine in the substantia nigra of the brain die out. This leads to symptoms like hypokinesia, rigidity, bradykinesia, and rest tremor. Parkinsonism cannot be cured, but the symptoms can be reduced with the intervention of medicinal drugs, surgical treatments, and physical therapies. Delivering drugs to the brain for treating Parkinson’s disease is very challenging. The blood-brain barrier acts as a highly selective semi-permeable barrier, which refrains the drug from reaching the brain. Conventional drug delivery systems used for Parkinson’s disease do not readily cross the blood barrier and further lead to several side-effects. Recent advancements in drug delivery technologies have facilitated drug delivery to the brain without flooding the bloodstream and by directly targeting the neurons. In the era of Nanotherapeutics, liposomes are an efficient drug delivery option for brain targeting. Liposomes facilitate the passage of drugs across the blood-brain barrier, enhances the efficacy of the drugs, and minimize the side effects related to it. The review aims at providing a broad updated view of the liposomes, which can be used for targeting Parkinson’s disease.


2019 ◽  
Vol 9 (11) ◽  
pp. 2219 ◽  
Author(s):  
Blessing Atim Aderibigbe ◽  
Tobeka Naki

In the treatment of brain diseases, most potent drugs that have been developed exhibit poor therapeutic outcomes resulting from the inability of a therapeutic amount of the drug to reach the brain. These drugs do not exhibit targeted drug delivery mechanisms, resulting in a high concentration of the drugs in vital organs leading to drug toxicity. Chitosan (CS) is a natural-based polymer. It has unique properties such as good biodegradability, biocompatibility, mucoadhesive properties, and it has been approved for biomedical applications. It has been used to develop nanocarriers for brain targeting via intranasal administration. Nanocarriers such as nanoparticles, in situ gels, nanoemulsions, and liposomes have been developed. In vitro and in vivo studies revealed that these nanocarriers exhibited enhanced drug uptake to the brain with reduced side effects resulting from the prolonged contact time of the nanocarriers with the nasal mucosa, the surface charge of the nanocarriers, the nano size of the nanocarriers, and their capability to stretch the tight junctions within the nasal mucosa. The aforementioned unique properties make chitosan a potential material for the development of nanocarriers for targeted drug delivery to the brain. This review will focus on chitosan-based carriers for brain targeting.


Drug Delivery ◽  
2013 ◽  
Vol 21 (2) ◽  
pp. 148-154 ◽  
Author(s):  
Hitendra S. Mahajan ◽  
Milind S. Mahajan ◽  
Pankaj P. Nerkar ◽  
Anshuman Agrawal

2009 ◽  
Vol 29 (12) ◽  
pp. 1914-1923 ◽  
Author(s):  
Rongqin Huang ◽  
Weilun Ke ◽  
Liang Han ◽  
Yang Liu ◽  
Kun Shao ◽  
...  

Ligand-mediated brain-targeting drug delivery is one of the focuses at present. Elucidation of exact targeting mechanisms serves to efficiently design these drug delivery systems. In our previous studies, lactoferrin (Lf) was successfully exploited as a brain-targeting ligand to modify cationic dendrimer-based nanoparticles (NPs). The mechanisms of Lf-modified NPs to the brain were systematically investigated in this study for the first time. The uptake of Lf-modified vectors and NPs by brain capillary endothelial cells (BCECs) was related to clathrin-dependent endocytosis, caveolae-mediated endocytosis, and macropinocytosis. The intracellular trafficking results showed that Lf-modified NPs could rapidly enter the acidic endolysosomal compartments within 5 mins and then partly escape within 30 mins. Both Lf-modified vectors and NPs showed higher blood–brain barrier-crossing efficiency than unmodified counterparts. All the results suggest that both receptor- and adsorptive-mediated mechanisms contribute to the cellular uptake of Lf-modified vectors and NPs. Enhanced brain-targeting delivery could be achieved through the synergistic effect of the macromolecular polymers and the ligand.


2005 ◽  
Vol 2 (2) ◽  
pp. 165-175 ◽  
Author(s):  
Tushar Vyas ◽  
Aliasgar Shahiwala ◽  
Sudhanva Marathe ◽  
Ambikanandan Misra

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 680
Author(s):  
Sara Perteghella ◽  
Giovanna Rassu ◽  
Elisabetta Gavini ◽  
Antonella Obinu ◽  
Elia Bari ◽  
...  

The nose-to-brain delivery route is used to bypass the blood–brain barrier and deliver drugs directly into the brain. Over the years, significant signs of progress have been made in developing nano-drug delivery systems to address the very low drug transfer levels seen with conventional formulations (e.g., nasal solutions). In this paper, sericin nanoparticles were prepared using crocetin as a new bioactive natural cross-linker (NPc) and compared to sericin nanoparticles prepared with glutaraldehyde (NPg). The mean diameter of NPc and NPg was about 248 and 225 nm, respectively, and suitable for nose-to-brain delivery. The morphological investigation revealed that NPc are spherical-like particles with a smooth surface, whereas NPg seem small and rough. NPc remained stable at 4 °C for 28 days, and when freeze-dried with 0.1% w/v of trehalose, the aggregation was prevented. The use of crocetin as a natural cross-linker significantly improved the in vitro ROS-scavenging ability of NPc with respect to NPg. Both formulations were cytocompatible at all the concentrations tested on human fibroblasts and Caco-2 cells and protected them against oxidative stress damage. In detail, for NPc, the concentration of 400 µg/mL resulted in the most promising to maintain the cell metabolic activity of fibroblasts higher than 90%. Overall, the results reported in this paper support the employment of NPc as a nose-to-brain drug delivery system, as the brain targeting of antioxidants is a potential tool for the therapy of neurological diseases.


Pharmaceutics ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 38
Author(s):  
Gizem Rüya Topal ◽  
Mária Mészáros ◽  
Gergő Porkoláb ◽  
Anikó Szecskó ◽  
Tamás Ferenc Polgár ◽  
...  

Pharmacological treatment of central nervous system (CNS) disorders is difficult, because the blood–brain barrier (BBB) restricts the penetration of many drugs into the brain. To solve this unmet therapeutic need, nanosized drug carriers are the focus of research efforts to develop drug delivery systems for the CNS. For the successful delivery of nanoparticles (NPs) to the brain, targeting ligands on their surface is necessary. Our research aim was to design a nanoscale drug delivery system for a more efficient transfer of donepezil, an anticholinergic drug in the therapy of Alzheimer’s disease across the BBB. Rhodamine B-labeled solid lipid nanoparticles with donepezil cargo were prepared and targeted with apolipoprotein E (ApoE), a ligand of BBB receptors. Nanoparticles were characterized by measurement of size, polydispersity index, zeta potential, thermal analysis, Fourier-transform infrared spectroscopy, in vitro release, and stability. Cytotoxicity of nanoparticles were investigated by metabolic assay and impedance-based cell analysis. ApoE-targeting increased the uptake of lipid nanoparticles in cultured brain endothelial cells and neurons. Furthermore, the permeability of ApoE-targeted nanoparticles across a co-culture model of the BBB was also elevated. Our data indicate that ApoE, which binds BBB receptors, can potentially be exploited for successful CNS targeting of solid lipid nanoparticles.


2020 ◽  
Vol 20 (30) ◽  
pp. 2777-2788
Author(s):  
Bhumika Kumar ◽  
Mukesh Pandey ◽  
Faizana Fayaz ◽  
Tareq Abu Izneid ◽  
Faheem Hyder Pottoo ◽  
...  

Parkinson’s disease (PD) is one of the most prevalent and severe neurodegenerative disease affecting more than 6.1 million people globally. It is characterized by age-related progressive deterioration of neurological functions caused by neuronal damage or neuronal death. During PD, the dopamineproducing cells in the substantia nigra region of the brain degenerate, which leads to symptoms like resting tremors and rigidity. Treatment of PD is very challenging due to the blood-brain barrier, which restricts the drug from reaching the brain. Conventional drug delivery systems possess a limited capacity to cross the blood barrier, leading to low bioavailability and high toxicity (due to off-site drug release). Therefore, it becomes necessary to accelerate the development of novel drug delivery systems, including nanoparticles, microemulsions, matrix systems, solid dispersions, liposomes, and solid lipid nanoparticles for the treatment of PD. Exosomes are biological lipid bilayer membrane vesicles produced by nearly all mammalian cells. The characteristics of vesicles are unique to their cell of origin and are primarily involved in intracellular communication. Exosomes, due to their nanoscale size, could easily permeate across the central nervous system, which makes them ideal for targeting the neurons in the substantia nigra. Exosomes could be efficient drug carrier systems for brain targeting, which can increase the efficacy of the drug and minimize the side effects. The review aims at providing a broad updated view of exosomes and their application in the treatment of PD.


2020 ◽  
Vol 14 (3) ◽  
pp. 174-192 ◽  
Author(s):  
Ruchita Singh ◽  
Charles Brumlik ◽  
Mandar Vaidya ◽  
Abhishek Choudhury

Background: Current cerebral drug delivery to the brain and Cerebrospinal Fluid (CSF) is limited by the Blood-Brain Barrier (BBB) or the blood-blood Cerebrospinal Fluid (CSF) barrier. The popular, non-invasive, intranasal delivery provides an exciting route for topical and systemic applications. For example, intranasal drug delivery of Central Nervous System (CNS) drugs can be designed to pass the BBB barrier via the nose-to-brain pathways. Recent nanotechnology research and patenting focus mainly on overcoming typical limitations including bioavailability, transport, BBB penetration, targeted delivery, controlled release rate and controlled degradation. Objective: The aim of the present study was to assess the state-of-the-art of nose-to-brain drug delivery systems and the role of nanotechnology in targeted delivery for the treatment of CNS and related therapeutic conditions. Methods: Patent and related searches were made with analytics to explore and organize nanotech work in intranasal drug delivery to the brain. Technical advancements were mapped by API, formulation and performance criteria. Patents and published patent applications were searched with concept tables of keywords, metadata (e.g., assignee) and patent classes (e.g., International Patent Classes and Cooperative Patent Classes). Results: The reviewed patents and published applications show a focus on formulations and therapeutic indications related to the nano-based nose-to-brain drug delivery. The main patented materials were surface modifiers, delivery systems and excipients. Conclusion: Surface modified nanoparticles can greatly improve drug transport and bioavailability of drugs, particularly higher molecular weight drugs. The most commonly used surface modifiers were chitosan, lectin and cyclodextrin-cross-linker complex. Nanoformulations of herbal drugs could increase drug bioavailability and reduce toxicity. Biotechnology-related drug delivery approaches such as monoclonal antibodies and genetically engineered proteins (molecular Trojan horses) deliver large molecule therapeutics.


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