Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence

Lipid-based nanocarriers (LNs) have made it po,ssible to prolong corneal residence time and improve the ocular bioavailability of ophthalmic drugs. In order to investigate how the LNs interact with the ocular mucosa and reach the posterior eye segment, we have formulated lipid nanocarriers that were designed to bear a traceable fluorescent probe in the present work. The chosen fluorescent probe was obtained by a conjugation reaction between fluoresceinamine and the solid lipid excipient stearic acid, forming a chemically synthesized adduct (ODAF, N-(3’,6’-dihydroxy-3-oxospiro [isobenzofuran-1(3H),9’-[9H] xanthen]-5-yl)-octadecanamide). The novel formulation (LN-ODAF) has been formulated and characterized in terms of its technological parameters (polydispersity index, mean particle size and zeta potential), while an in vivo study was carried out to assess the ability of LN-ODAF to diffuse through different ocular compartments. LN-ODAF were in nanometric range (112.7 nm ± 0.4), showing a good homogeneity and long-term stability. A TEM (transmission electron microscopy) study corroborated these results of characterization. In vivo results pointed out that after ocular instillation, LN ODAF were concentrated in the cornea (two hours), while at a longer time (from the second hour to the eighth hour), the fluorescent signals extended gradually towards the back of the eye. From the results obtained, LN-ODAF demonstrated a potential use of lipid-based nanoparticles as efficient carriers of an active pharmaceutical ingredient (API) involved in the management of retinal diseases.

Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization

Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of the folate receptor (FR) is overexpressed on a significant number of human cancers; therefore, folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with paclitaxel (PTX) have been prepared to maximize the proven antineoplastic activity of the drug against solid tumors. Nanometric-range-sized particles (169 ± 28 nm–296 ± 57 nm), with negative Z-potential values (between −0.12 ± 0.04 and −94.1± 0.4), were synthesized, and the loaded PTX (2.63 ± 0.19–3.56 ±0.13 µg PTX/mg Np) was sustainably released for 23 and 27 h. Three cell lines (MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded BSA/ALG nanocarriers. The presence of FR on the cell membrane led to a significantly larger uptake of BSA/ALG–Fol nanoparticles compared with the equivalent nanoparticles without folic acid on their surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle–Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticle–Fol due to the sustainable PTX release.

Non-Ionic Surfactants for Stabilization of Polymeric Nanoparticles for Biomedical Uses

Surfactants are essential in the manufacture of polymeric nanoparticles by emulsion formation methods and to preserve the stability of carriers in liquid media. The deposition of non-ionic surfactants at the interface allows a considerable reduction of the globule of the emulsion with high biocompatibility and the possibility of oscillating the final sizes in a wide nanometric range. Therefore, this review presents an analysis of the three principal non-ionic surfactants utilized in the manufacture of polymeric nanoparticles; polysorbates, poly(vinyl alcohol), and poloxamers. We included a section on general properties and uses and a comprehensive compilation of formulations with each principal non-ionic surfactant. Then, we highlight a section on the interaction of non-ionic surfactants with biological barriers to emphasize that the function of surfactants is not limited to stabilizing the dispersion of nanoparticles and has a broad impact on pharmacokinetics. Finally, the last section corresponds to a recommendation in the experimental approach for choosing a surfactant applying the systematic methodology of Quality by Design.

Nanoemulsions for the Encapsulation of Hydrophobic Actives

This work analyzes the dispersion of two highly hydrophobic actives, (9Z)-N-(1,3-dihydroxyoctadecan-2-yl)octadec-9-enamide (ceramidelike molecule) and 2,6-diamino-4-(piperidin-1-yl)pyrimidine 1-oxide (minoxidil), using oil-in-water nanoemulsions with the aim of preparing stable and safe aqueous-based formulations that can be exploited for enhancing the penetration of active compounds through cosmetic substrates. Stable nanoemulsions with a droplet size in the nanometric range (around 200 nm) and a negative surface charge were prepared. It was possible to prepare formulations containing up to 2 w/w% of ceramide-like molecules and more than 10 w/w% of minoxidil incorporated within the oil droplets. This emulsions evidenced a good long-term stability, without any apparent modification for several weeks. Despite the fact that this work is limited to optimize the incorporation of the actives within the nanoemulsion-like formulations, it demonstrated that nanoemulsions should be considered as a very promising tool for enhancing the distribution and availability of hydrophobic molecules with technological interest.

Application of Halloysite Nanotubes in Cancer Therapy—A Review

Halloysite, a nanoclay characterized by a unique, tubular structure, with oppositely charged interior and exterior, suitable, nanometric-range size, high biocompatibility, and low cost, is recently gaining more and more interest as an important and versatile component of various biomaterials and delivery systems of biomedical relevance. One of the most recent, significant, and intensely studied fields in which halloysite nanotubes (HNTs) found diverse applications is cancer therapy. Even though this particular direction is mentioned in several more general reviews, it has never so far been discussed in detail. In our review, we offer an extended survey of the literature on that particular aspect of the biomedical application of HNTs. While historical perspective is also given, our paper is focused on the most recent developments in this field, including controlled delivery and release of anticancer agents and nucleic acids by HNT-based systems, targeting cancer cells using HNT as a carrier, and the capture and analysis of circulating tumor cells (CTCs) with nanostructured or magnetic HNT surfaces. The overview of the most up-to-date knowledge on the HNT interactions with cancer cells is also given.

Paclitaxel-loaded Folate-targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization.

Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of folate receptor (FR) is overexpressed on a significant number of human cancers; therefore, folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with paclitaxel (PTX) have been prepared to maximizing the proven antineoplastic activity of the drug against solid tumors. Nanometric-range sized particles (169 ± 28nm - 296 ± 57nm), with negative Z-potential values (between -0.12 ± 0.04 and -94.1± 0.4), were synthesized. The loaded PTX (2.63±0.19 - 3.56 ±0.13 µg PTX/mg Np) was sustainably released along 23 and 27h. Three cell lines (MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded BSA/ALG nanocarriers. The presence of FR on cell membrane led to a significant larger uptake of BSA/ALG-Fol nanoparticles regarding to the equivalent nanoparticles without folic acid on its surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle-Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticles-Fol due to the sustainable PTX release.

Advanced Nanocellular Foams: Perspectives on the Current Knowledge and Challenges

Nanocellular polymers (i.e., cellular polymers with cells and walls in the nanometric range) were first produced in the early 2000s, with the works of [...]

Recent Progress in Synthesis and Application of Nanosized and Hierarchical Mordenite—A Short Review

Zeolites with their unique properties find applications in various fields, including medicine, agronomy, ecology, production of detergents and drying agents, and in a number of industrial processes. Among zeolites, mordenite is particularly widespread because of its high silica/alumina ratio, which allows it to resist exposure to high temperatures and to acidic gases and liquids. Mordenite is commercially available as a natural mineral and as a synthesized material. This zeolite is mostly used in its synthetic form as an acid catalyst in the petrochemical industry for the isomerization of alkanes and aromatics. In this review, we consider the scientific literature on the structure, synthesis, and two main types of modifications that solve the diffusion difficulties during catalytic processes. The first type of modifications is related to a reduction of the size of the mordenite crystals obtained to submicron or nanometric range, whereas the second ones aim to obtain hierarchical mordenite samples by appropriate post-synthetic treatments. Both types of modifications find many other applications besides solving diffusion constraints in catalytic processes. Attempts to fine-tune and control the particle size in the first type of modifications or the pore size in the second ones by adjusting various parameters during the synthesis are described.

New Mussel Inspired Polydopamine-Like Silica-Based Material for Dye Adsorption

A straightforward and economic procedure has been developed for the synthesis of a new polydopamine-like silica-based material that has been obtained by oxidation of catechol with KIO4 followed by reaction with 3-aminopropyltrimethoxysilane. All techniques adopted for characterization showed that the obtained material is rich in different functional groups and the morphological analyses revealed dimensions in the nanometric range. The hybrid material has been characterized by several techniques showing its polydopamine-like nature, and preliminary observations for dye adsorption have been reported.

STUDIES ON NANOLIPID EMULGEL OF NIMESULIDE FOR TRANSDERMAL DELIVERY

The objective of the present study was to develop and evaluate a nanolipid transdermal emulgel of Nimesulide. The nanolipid particles of Nimesulide were developed using Compritol 888 ATO and Labrafil M1944 as lipids, Polysorbate 80 as surfactant with Poloxamer 188 and Polyethylene Glycol 400 as stabilizer and cosolvent respectively. The nanoparticles were developed by Hot Nanoemulsification Low Temperature Solidification method and showed drug entrapment efficiency of 67 ± 2.316 % with particle size of 500 – 600 nm. TEM studies indicated presence of spherical particles in the nanometric range. The nanolipidic dispersions were suitably gelled to form emulgel. The in vitro release of the developed emulgel showed sustained drug release for 8 hours with no evidence of toxicity during histopathological testing after ex vivo permeation studies. The nanolipid emulgel of Nimesulide can thus provide sustained release action due to enhanced skin deposition for effective treatment of chronic arthritic conditions, thereby improving patient compliance.