Ioana Lacatusu

The encapsulation effect of UV molecular absorbers into biocompatible lipid nanoparticles

The efficiency of a cosmetic product depends not only on the active ingredients, but also on the carrier system devoted to improve its bioavailability. This article aims to encapsulate two couples of UV molecular absorbers, with a blocking action on both UV-A and UV-B domains, into efficient lipid nanoparticles. The effect of encapsulation on the specific properties such as sun protection factor and photostability behaviour has been demonstrated. The lipid nanoparticles with size range 30-350 nm and a polydispersity index between 0.217 and 0.244 are obtained using a modified high shear homogenisation method. The nanoparticles had spherical shapes with a single crystallisation form of lipid matrices characteristic for the least ordered crystal structure (α-form). The in vitro determination of photoprotection has led to high SPF ratings, with values of about 20, which assure a good photoprotection and filtering about 95% of UV radiation. The photoprotection effect after irradiation stage was observed to be increased more than twice compared to initial samples as a result of isomerisation phenomena. All the results have shown that good photoprotection effect and improved photostability could be obtained using such sunscreen couples, thus demonstrating that UV absorbers-solid lipid nanoparticles are promising carriers for cosmetic formulations.

Novel bio-active lipid nanocarriers for the stabilization and sustained release of sitosterol.

In this work, new stable and efficiently bio-active lipid nanocarriers (NLCs) with antioxidant properties have been developed for the transport of active ingredients in food. The novel NLCs loaded with β-sitosterol/β-sitosterol and green tea extract (GTE) and prepared by a combination of natural oils (grape seed oil, fish oil and squalene) and biological lipids with food grade surfactants, were physico-chemically examined by DLS, TEM, electrokinetic potential, DSC and HPLC and found to have main diameters less than 200 nm, a spherical morphology, excellent physical stability, an imperfect crystalline lattice and high entrapment efficiency. The novel loaded-NLCs have demonstrated the potential to develop a high blocking action of chain reactions, trapping up to 92% of the free-oxygen radicals, as compared to the native β-sitosterol (AA%=36.5). Another advantage of this study is associated with the quality of bio-active NLCs based on grape seed oil and squalene to manifest a better sitosterol-sustained release behaviour as compared to their related nanoemulsions. By coupling both in vitro results, i.e. the enhanced antioxidant activity and superior release properties, this study emphasizes the sustainability of novel bio-active nanocarriers to gain specific bio-food features for development of functional foods with a high applicability spectrum.

Lipid nanoparticles based on butyl-methoxydibenzoylmethane: in vitro UVA blocking effect

The aim of the present study was to obtain efficient lipid nanoparticles loaded with butyl-methoxydibenzoylmethane (BMDBM) in order to develop cosmetic formulations with enhanced UVA blocking effect. For this purpose, two adequate liquid lipids (medium chain triglycerides and squalene) have been used in combination with two solid lipids (cetyl palmitate and glyceryl stearate) in order to create appropriate nanostructured carriers with a disordered lipid network able to accommodate up to 1.5% BMDBM. The lipid nanoparticles (LNs) were characterized in terms of particle size, zeta potential, entrapment efficiency, loading capacity and in vitro UVA blocking effect. The efficiency of lipid nanoparticles in developing some cosmetic formulations has been evaluated by determining the in vitro erythemal UVA protection factor. In order to quantify the photoprotective effect, some selected cream formulations based on BMDBM-LNs and a conventional emulsion were exposed to photochemical UV irradiation at a low energy to simulate the solar energy during the midday. The results obtained demonstrated the high ability of cream formulations based on BMDBM-LNs to absorb more than 96% of UVA radiation. Moreover, the developed cosmetic formulations manifest an enhanced UVA blocking effect, the erythemal UVA protection factor being four times higher than those specific to conventional emulsions.

Effect of UV Sunscreens Loaded in Solid Lipid Nanoparticles: A Combinated SPF Assay and Photostability

The aim of this investigation was to obtain lipid nanoparticles loaded with different sunscreen agents in order to achieve enhanced photoprotection and to decrease the amount of UV – absorbers, with preserving at the same time a high sun protection factor. The developed formulations combined different types of additives including a mixture of non-ionic surfactant and lechitine with two lipids as solid matrix to obtain favourable stable lipid formulations. The research work could be concluded as successefully production of lipid nanoparticles loaded with UV-A and UV-B absorbers (with average size less than 100 nm) that may represent useful UV-blocking systems in sunscreen products for cosmetical purpose.

Coencapsulation of Butyl-Methoxydibenzoylmethane and Octocrylene into Lipid Nanocarriers: UV Performance, Photostability and in vitro Release

The coencapsulation of two UV filters, butyl‐methoxydibenzoylmethane (BMDBM) and octocrylene (OCT), into lipid nanocarriers was explored to develop stable cosmetic formulations with broad‐spectrum photoprotection and slow release properties. Different types of nanocarriers in various concentrations of the two UV filters were tested to find the combination with the best absorption and release properties. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have been the two types of lipid nanocarriers used. The NLCs were based on either medium chain triglycerides (MCT) or squalene (Sq). The following physicochemical properties of the nanocarriers have been evaluated: particle size, morphology, zeta potential (ZP), entrapment efficiency, loading capacity, and thermal behavior. The nanocarriers have been formulated into creams containing low amounts of UV filters (2.5% BMDBM and 1% OCT). The best photoprotection results were obtained with the cream based on NLCs prepared with MCT, having a sun protection factor (SPF) of 17.2 and an erythemal UVA protection factor (EUVA–PF) of 50.8. The photostability of the encapsulated BMDBM filter was confirmed by subjecting the nanocarriers‐based creams to in vitro irradiation. The prolonged UV‐protection efficacy was coupled with a slow in vitro release of the synthetic UV filters, which followed the Higuchi release model.

Influence of vegetable oil on the synthesis of bioactive nanocarriers with broad spectrum photoprotection

Due to their unique features, most nanostructured lipid carriers (NLCs) in association with vegetable oils that exhibit UV filtering properties and bioactivity could be used in many cosmetic formulations. Therefore, in this work, a new application of pomegranate seed oil (PSO) in the cosmetic sector was developed, based on the synthesis of bioactive lipid nanocarriers loaded with various UV filters by the hot high pressure homogenization technique. To get broad spectrum photoprotection, different UVA and UVB filters have been used (Avobenzone — AVO, Octocrylen-OCT, Bemotrizinol — BEMT). The influence of the solid lipids combined with PSO on the particle size, physical stability and entrapment efficiency was investigated using 8 nanocarrier systems. An improved physical stability and an appropriate size were obtained for NLCs prepared with Emulgade, carnauba wax and PSO (e.g. −30.9÷-36.9 mV and 160÷185 nm). NLCs showed an entrapment efficiency above 90% and assured slow release rates of UV filters, especially for BEMT (5%). The developed nanocarriers have been formulated into safe and effective sunscreens containing low amounts of synthetic UV filters coupled with a high percent of natural ingredients. The highest SPF of 34.3 was obtained for a cream comprising of 11% PSO and 3.7% BEMT

Antioxidant Activity of Solid Lipid Nanoparticles Loaded with Umbelliferone

The objective of this investigation was to develop solid lipid nanoparticles (SLNs) of umbelliferone by means of a high shear homogenization technique and to evaluate the efficiency of SLN systems in preserving and enhancing antioxidant activity of the flavonoid active component. The aqueous SLN dispersions combine two structural types of lipid compounds and different types of emulsifiers including a mixture of monoalkyl polyoxyethylene sorbitan with a block copolymer and lecithin. The assessment of umbelliferone stability in aqueous SLN dispersions, the size distribution of lipid nanoparticles loaded with umbelliferone (by DLS technique), as well as the structural changes (FT-IR spectroscopy and differential scanning calorimetry) of these lipid nanomatrices have been investigated. Moreover, the influence of umbelliferone concentration onto entrapment efficiency and antioxidant properties were clearly evidenced on four kinds of lipid nanoparticles. The umbelliferone-loaded SLN prepared with polyethylene glycol sorbitan monostearate shown a mean particle size of 173.4 nm ± 3.279, as well as good entrapment efficiency (EE = 60.70%) and antioxidant properties (AA = 75%).

Lipid nanocarriers based on natural oils with high activity against oxygen free radicals and tumor cell proliferation

The development of nano-dosage forms of phytochemicals represents a significant progress of the scientific approach in the biomedical research. The aim of this study was to assess the effectiveness of lipid nanocarriers based on natural oils (grape seed oil, fish oil and laurel leaf oil) in counteracting free radicals and combating certain tumor cells. No drug was encapsulated in the nanocarriers. The cytotoxic effect exerted by bioactive nanocarriers against two tumor cells, MDA-MB 231 and HeLa cell lines, and two normal cells, L929 and B16 cell lines, was measured using the MTT assay, while oxidative damage was assessed by measuring the total antioxidant activity using chemiluminescence analysis. The best performance was obtained for nanocarriers based on an association of grape seed and laurel leaf oils, with a capacity to scavenge about 98% oxygen free radicals. A dose of nanocarriers of 5mg·mL(-1) has led to a drastic decrease in tumor cell proliferation even in the absence of an antitumor drug (e.g. about 50% viability for MDA-MB 231 cell line and 60% viability for HeLa cell line). A comparative survival profile of normal and tumor cells, which were exposed to an effective dose of 2.5mg·mL(-1) lipid nanocarriers, has revealed a death rate of 20% for normal B16 cells and of 40% death rate for MDA-MB 231 and HeLa tumor cells. The results in this study imply that lipid nanocarriers based on grape seed oil in association with laurel leaf oil could be a candidate to reduce the delivery system toxicity and may significantly improve the therapeutic efficacy of antitumor drugs in clinical applications.

Spectral Characterization of Model Systems Containing Lipids and Chlorophyll

The objective of the present work was to prove that the spectral features of chlorophyll a allow its use as a sensor for physical properties of liposomes. For this purpose, UV-VIS absorption, fluorescence emission and dynamic light scattering measurements were recorded and analyzed comparatively. Multilamellar and unilamellar vesicles with Chla have been prepared by a mechanical dispersion method and a further sonication treatment for obtaining unilamellar vesicles. The Chla – liposomes were prepared using an appropriate molar ratio and three types of lipids. It was confirmed that Chla – based model system can be used to assess specific molecular interactions in the liposome bilayer.

Phyto-mediated nanostructured carriers based on dual vegetable actives involved in the prevention of cellular damage.

The growing scientific interest in exploitation of vegetable bioactives has raised a number of questions regarding their imminent presence in pharmaceutical formulations. This study intends to demonstrate that a dual combination between vegetable oil (e.g. thistle oil, safflower oil, sea buckthorn oil) and a carrot extract represents an optimal approach to formulate safe carrier systems that manifest cell regeneration effect and promising antioxidant and anti-inflammatory activity. Inclusion of both natural actives into lipid carriers imparted a strong negative charge on the nanocarrier surface (up to -45mV) and displayed average sizes of 70nm to 140nm. The entrapment efficiency of carrot extract into nanostructured carriers ranged between 78.3 and 88.3%. The in vitro release study has demonstrated that the entrapment of the extract represents a viable way for an equilibrated release of carotenoids. Besides the excellent antioxidant properties (e.g. scavenging up to 98% of the free oxygen radicals), the results of cellular integrity (e.g. cell viability of 133%) recommend these nanocarriers based on dual carrot extract-bioactive oil as a promising trend for the treatment of certain disorders in which oxidative stress plays a prominent role. In addition, the lipid nanocarriers based on safflower oil and sea buckthorn oil demonstrated an anti-inflammatory effect on LPS induced THP-1 macrophages, by inhibiting the secretion of two pro-inflammatory cytokines, IL-6 and TNF-α.