Natural product-based nanomedicine: recent advances and issues

Zielińska

et al. 2020

IJMS

In this work, we developed a solid lipid nanoparticle (SLN) formulation with (+)-limonene 1,2-epoxide and glycerol monostearate (Lim-SLNs), stabilized with Poloxamer® 188 in aqueous dispersion to modify the release profile of the loaded monoterpene derivative. We also evaluated the role of SLNs in lipid peroxidation and cytotoxicity in a spontaneously transformed aneuploid immortal keratinocyte cell line from adult human skin (the HaCaT cell line). For the cell viability assay, the colorimetric 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used. Lim-SLNs with a loading capacity and encapsulation efficiency of 0.39% and 63%, respectively, were produced by high pressure homogenization. A mean particle size of 194 ± 3.4 nm and polydispersity index of 0.244 were recorded for the loaded Lim-SLNs, as compared to 203 ± 1.5 nm (PI 0.213) for the non-loaded (blank) SLNs. The loading of the monoterpene derivative into glycerol monostearate SLNs fitted into the zero-order kinetics, and ameliorated both lipid peroxidation and cytotoxicity in a keratinocyte cell line. A promising formulation for antioxidant and anti-tumoral activities is here proposed.

Section: Introductionmentioning

confidence: 99%

(+)-Limonene 1,2-Epoxide-Loaded SLNs: Evaluation of Drug Release, Antioxidant Activity, and Cytotoxicity in an HaCaT Cell Line

Zielińska

et al. 2020

IJMS

“…They are placed in a gray area between pharmaceuticals and food, and have been recently named as: "the phytocomplex, if they derive from a food of vegetal origin, and as the pool of the secondary metabolites if they derive from a food of animal origin, concentrated and administered in the more suitable pharmaceutical form" [14,68]. This study addresses the emerging new branch of "Nanonutraceutical Science" [67,72]. Nanonutraceutical formulations are being exploited for their efficacy, safety, and effect, and could be another tool in the arsenal of strategies that are helpful in managing health conditions, especially in patients who are not eligible for a conventional pharmacological therapy.…”

Section: Resultsmentioning

confidence: 99%

Quantification of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles by a Validated Reverse-Phase HPLC Photodiode Array

Rigon

Fachinetti

Severino³

et al. 2019

Applied Sciences

A new method based on reverse-phase HPLC combined with photodiode array (PDA) was developed to quantify the release of trans-resveratrol (tRES) from solid lipid nanoparticles (SLN). The mobile phase was composed of 75:0:25 (V/V) water/methanol/acetonitrile at 0–3.5 min, 32.5:30.0:37.5 (V/V) water/methanol/acetonitrile at 3.6–5.8 min, and 75:0:25 (V/V) water/methanol/acetonitrile at 5.9–10 min. The flow rate was set at 1.0 mL/min, and tRES was detected at the wavelength of 306.6 nm. A concentration range of 1–100 µg/mL was used to obtain the linear calibration curve. SLN were produced by ultrasound technique to load 0.1% (wt/wt) of tRES, and the in vitro release of the drug was run in modified Franz diffusion cells. The mean recovery of tRES was found to be 96.84 ± 0.32%. The intra-assay and inter-assay coefficients of variation were less than 5%. The proposed method was applied to in vitro permeability studies, and the Weibull model was found to be the one that best fits the tRES release, which is characterized by a simultaneous lipid chain relaxation and erosion during drug release.

“…Nutraceutics, which derive from food matrices of vegetal or animal matrices, are a novel toolbox not yet completely explored for its full potential in medicine. Current research is looking towards several nanotechnological approaches to be exploited for the formulation of nutraceuticals [84][85][86][87][88][89][90][91][92][93], and to build up the emerging area of the nanonutraceutics [9,[94][95][96]. Nutraceutics, a portmanteau of the words 'nutrition' and 'pharmaceutical', have been recently defined as "the phytocomplex if they derive from a food of vegetal origin, and as the pool of the secondary metabolites if they derive from a food of animal origin, concentrated and administered in the more suitable pharmaceutical form" [84,97].…”

Section: From Nanopharmaceutics To Nanonutraceutics: a Bet For The Fumentioning

confidence: 99%

Nanopharmaceutics: Part II—Production Scales and Clinically Compliant Production Methods

et al. 2020

Due the implementation of nanotechnologies in the pharmaceutical industry over the last few decades, new type of cutting-edge formulations-nanopharmaceutics-have been proposed. These comprise pharmaceutical products at the nanoscale, developed from different types of materials with the purpose to, e.g., overcome solubility problems of poorly water-soluble drugs, the pharmacokinetic and pharmacodynamic profiles of known drugs but also of new biomolecules, to modify the release profile of loaded compounds, or to decrease the risk of toxicity by providing site-specific delivery reducing the systemic distribution and thus adverse side effects. To succeed with the development of a nanopharmaceutical formulation, it is first necessary to analyze the type of drug which is to be encapsulated, select the type matrix to load it (e.g., polymers, lipids, polysaccharides, proteins, metals), followed by the production procedure. Together these elements have to be compatible with the administration route. To be launched onto the market, the selected production method has to be scaled-up, and quality assurance implemented for the product to reach clinical trials, during which in vivo performance is evaluated. Regulatory issues concerning nanopharmaceutics still require expertise for harmonizing legislation and a clear understanding of clinically compliant production methods. The first part of this study addressing "Nanopharmaceutics: Part I-Clinical trials legislation and Good Manufacturing Practices (GMP) of nanotherapeutics in the EU" has been published in Pharmaceutics. This second part complements the study with the discussion about the production scales and clinically compliant production methods of nanopharmaceutics.Nanomaterials 2020, 10, 455 2 of 16 funding opportunities within Member States, Associated Countries and Third Countries. The strategic plan for the next Horizon Europe framework programme has clearly set nanomedicines and advanced therapies as priorities. To succeed, the nanoproduct needs to be manufacturable at large scale and its quality assured in order to reach clinical trials. The topic is indeed of high scientific interest considering the number of scientific papers dealing with clinical trials and nanoparticles over the last twenty years (Figure 1). Nanomaterials 2020, 10, x FOR PEER REVIEW 2 of 17European Commission aims to lead innovation towards the development of these nanopharmaceutics by launching several funding opportunities within Member States, Associated Countries and Third Countries. The strategic plan for the next Horizon Europe framework programme has clearly set nanomedicines and advanced therapies as priorities. To succeed, the nanoproduct needs to be manufacturable at large scale and its quality assured in order to reach clinical trials. The topic is indeed of high scientific interest considering the number of scientific papers dealing with clinical trials and nanoparticles over the last twenty years (Figure 1).