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

ABSTRACT: 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.

SUBMITTER: Silva S

PROVIDER: S-EPMC9266917 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature

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

Silva Sara S Marto Joana J Gonçalves Lídia M LM Duarte Diana D Soares O Salomé G P OSGP Vasques-Nóvoa Francisco F Almeida António J AJ Vale Nuno N

International journal of molecular sciences 20220626 13

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 permeat ...[more]

PMID: 35806112

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Project description:Curcumin (Cur) and epigallocatechin gallate (EGCG), the primary active compounds in turmeric and green tea, respectively, have been investigated for their anti-aging potential. The Cur and EGCG combination was encapsulated in sustained-release nanostructured lipid carriers (NLCs) to enhance their bioactivities and pharmaceutical properties. A significant enhancement in the antioxidant activities of the Cur and EGCG combination was observed at an optimal ratio, as demonstrated by the 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay (118.83 ± 3.78 %), ferric ion reducing antioxidant power assay (217.25 ± 13.45 %), and lipid peroxidation inhibition assay (106.08 ± 12.93 %), compared to Cur alone without compromising the antioxidant activities and total phenolic content of EGCG. This is due to the enhancement of total phenolic content of the combination of 218.83 ± 10.57 %. For anti-aging activities, the combination exhibited stimulation of SIRT1 protein and inhibition of collagenase and elastase of 27.53 ± 0.73 %, 43.70 ± 1.05 % and 51.76 ± 6.52 % compared with that achieved with Cur alone, respectively. The incorporation of the Cur and EGCG combination into NLCs resulted in high entrapment efficiencies of 98.60 ± 0.05 % for Cur and 98.40 ± 0.08 % for EGCG, with corresponding loading capacities of 0.789 ± 0.001 % and 3.935 ± 0.003 %, respectively. When formulated NLCs into an emulgel base, the system demonstrated sustained release profiles over 48 h, with 12.82 ± 0.99 % release of Cur and 63.77 ± 5.76 % release of EGCG. Significant skin retention was also observed after 24 h, with 23.88 ± 1.71 % Cur and 22.79 ± 4.65 % EGCG retained in the skin. Therefore, Cur: EGCG-loaded NLCs in emulgel can deliver the active compounds into the dermis, enhancing skin penetration, sustained delivery, and anti-aging activity superior to each conventional single active compound in topical formulations.

Dataset Information

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

Publications

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

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