Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles

Silva, Sara; Marto, Joana; Gonçalves, Lídia; Almeida, António J.; Vale, Nuno

doi:10.3390/nano10102089

Cited by 22 publications

(11 citation statements)

References 47 publications

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“…Even though some toxicity was observed with a decrease of around 20% of cell viability, this value was expected from our previous studies. This experimental result is related to the use of Tween 80 as a surfactant in the NLC formulation [18,32,33]. After encapsulation of drug-MAP conjugates and Lys(N 3 )-MAP, the cytotoxic assays and microscope evaluation demonstrated a significant decrease in cell viability in both cell lines and severe cell morphological changes after treatment when compared with free drug-MAP and free Lys(N 3 )-MAP at the lowest concentration.…”

Section: Discussionmentioning

confidence: 81%

“…In a previous work conducted by our group, we demonstrated that conjugation of MAP with TAC resulted in increased toxicity against both MCF-7 and SH-SY5Y cell lines [17]. Moreover, this TAC-MAP conjugated activity was further studied with successful incorporation onto NLC [18]. Even though amphipathic peptides-drug conjugates can possibly form nanoobjects by self-assembly (developed in references [19][20][21]), we loaded them into nanoparticles to ensure increase systemic bioavailability, avoid protein adsorption to the conjugate, and increase efficacy.…”

Section: Introductionmentioning

confidence: 90%

“…TCP-loaded, TCP + MAP-loaded, and TCP-MAP-loaded NLC were prepared using a modification of a hot high-shear homogenization (HSH) method previously described in refs. [18,32]. Briefly, 300 mg of Compritol 888 ATO was melted at a temperature 10 • C above its melting point (80 • C).…”

Section: Preparation Of Nlcmentioning

confidence: 99%

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New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity

Silva

Marto

Gonçalves

et al. 2022

IJMS

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Nanoparticulate systems have been widely investigated as delivery vectors for efficient drug delivery in different diseases. Nanostructured lipid carriers (NLC) are composed of both solid and liquid lipids (glyceryl dibehenate and diethylene glycol monoethyl ether) and have demonstrated enhanced biological compatibility and increased drug loading capability. Furthermore, the use of peptides, in particular cell-penetrating peptides, to functionalize nanoparticles and enhance cell membrane permeation was explored in this paper. In this paper, we described the synthesis of a new conjugated of tranylcypromine with MAP. In addition, taking into consideration our previous results, this study developed different NLCs loaded with three central nervous system (CNS) drugs (tacrine (TAC), rasagiline (RAS), and tranylcypromine (TCP)) functionalized with model amphipathic peptide (MAP) and evaluated their activity against cancer cells. Particle size analysis demonstrated NLC presented less than 200 nm and a polydispersity index less than 0.3. Moreover, in vitro results showed that conjugation of MAP with drugs led to a higher decrease in cell viability of a neuroblastoma cell line and Caco-2 cell line, more than MAP alone. Furthermore, NLC encapsulation contributed to higher cellular delivery and enhanced toxic activity at lower concentrations when compared with free or co-administration drug-MAP conjugate.

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Section: Discussionmentioning

confidence: 81%

Section: Introductionmentioning

confidence: 90%

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New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity

Silva

Marto

Gonçalves

et al. 2022

IJMS

Self Cite

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“…The results showed that there was no significant change between the NLC formulation and the pure drug, indicating that pioglitazone-loaded NLC is safe for neuronal cells. In another study, Silva et al [ 73 ] evaluated the in vitro cytotoxicity of tacrine-loaded NLC and tacrine-loaded NLC conjugated to an amphipathic peptide in SH-SY5Y neuroblastoma cell lines. The formulation cytotoxicity was evaluated through the MTT assay and SBR assay.…”

Section: Solid Lipid Nanoparticles (Sln) and Nanostructured Lipid Carriers (Nlc) For Nasal Deliverymentioning

confidence: 99%

In Vitro Studies on Nasal Formulations of Nanostructured Lipid Carriers (NLC) and Solid Lipid Nanoparticles (SLN)

et al. 2021

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The nasal route has been used for many years for the local treatment of nasal diseases. More recently, this route has been gaining momentum, due to the possibility of targeting the central nervous system (CNS) from the nasal cavity, avoiding the blood−brain barrier (BBB). In this area, the use of lipid nanoparticles, such as nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN), in nasal formulations has shown promising outcomes on a wide array of indications such as brain diseases, including epilepsy, multiple sclerosis, Alzheimer’s disease, Parkinson’s disease and gliomas. Herein, the state of the art of the most recent literature available on in vitro studies with nasal formulations of lipid nanoparticles is discussed. Specific in vitro cell culture models are needed to assess the cytotoxicity of nasal formulations and to explore the underlying mechanism(s) of drug transport and absorption across the nasal mucosa. In addition, different studies with 3D nasal casts are reported, showing their ability to predict the drug deposition in the nasal cavity and evaluating the factors that interfere in this process, such as nasal cavity area, type of administration device and angle of application, inspiratory flow, presence of mucoadhesive agents, among others. Notwithstanding, they do not preclude the use of confirmatory in vivo studies, a significant impact on the 3R (replacement, reduction and refinement) principle within the scope of animal experiments is expected. The use of 3D nasal casts to test nasal formulations of lipid nanoparticles is still totally unexplored, to the authors best knowledge, thus constituting a wide open field of research.

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“…Nanoparticles have been tested with metabolic and impedance methods for cytotoxicity and cellular conductivity. By targeting apolipoprotein E (APOE) protein, the level of lipid nanoparticles increases in the brain of non-human primates [ 75 ]. There are many remarkable applications of SLNs and nanostructured lipid carriers (NLCs).…”

Section: Lipid Nanoparticles Effects On Amyloid Beta Peptidementioning

confidence: 99%

Potential Role of Nanoparticles in Treating the Accumulation of Amyloid-Beta Peptide in Alzheimer’s Patients

Abbas

2021

Polymers

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The disorder of Alzheimer’s is marked by progressive pathophysiological neurodegeneration. The amino acid peptides in the amyloid plaques found in the brains of people with Alzheimer’s disease (AD) are known as amyloid-beta (Aβ). Current treatments are not curative, and the effects associated with AD are reduced. Improving treatment results involved the targeting of drugs at optimum therapeutic concentration. Nanotechnology is seen as an unconventional, modern technology that plays a key role in the treatment of Alzheimer’s disease. Using nanoparticles, molecular detection, effective drug targeting, and their combination offer high sensitivity. The aim of this review is to shed light on the function and successful role of nanoparticles to resolve Aβ aggregation and thus to help cure Alzheimer’s disease. The analysis divides these nanoparticles into three categories: polymer, lipid, and gold nanoparticles. A thorough comparison was then made between the nanoparticles, which are used according to their role, properties, and size in the procedure. The nanoparticles can prevent the accumulation of Aβ during the efficient delivery of the drug to the cells to treat Alzheimer’s disease. Furthermore, this comparison demonstrated the ability of these nanoparticles to deal efficiently with Alzheimer’s disease. The role of these nanoparticles varied from delivering the drug to brain cells to dealing with the disease-causing peptide.

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Formulation, Characterization and Evaluation against SH-SY5Y Cells of New Tacrine and Tacrine-MAP Loaded with Lipid Nanoparticles

Cited by 22 publications

References 47 publications

New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity

New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity

In Vitro Studies on Nasal Formulations of Nanostructured Lipid Carriers (NLC) and Solid Lipid Nanoparticles (SLN)

Potential Role of Nanoparticles in Treating the Accumulation of Amyloid-Beta Peptide in Alzheimer’s Patients

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