Encapsulation of β-Carotene by Emulsion Electrospraying Using Deep Eutectic Solvents

The encapsulation β-carotene in whey protein concentrate (WPC) capsules through the emulsion electrospraying technique was studied, using deep eutectic solvents (DES) as solvents. These novel solvents are characterized by negligible volatility, a liquid state far below 0 °C, a broad range of polarity, high solubilization power strength for a wide range of compounds, especially poorly water-soluble compounds, high extraction ability, and high stabilization ability for some natural products. Four DES formulations were used, based on mixtures of choline chloride with water, propanediol, glucose, glycerol, or butanediol. β-Carotene was successfully encapsulated in a solubilized form within WPC capsules; as a DES formulation with choline chloride and butanediol, the formulation produced capsules with the highest carotenoid loading capacity. SEM micrographs demonstrated that round and smooth capsules with sizes around 2 µm were obtained. ATR-FTIR results showed the presence of DES in the WPC capsules, which indirectly anticipated the presence of β-carotene in the WPC capsules. Stability against photo-oxidation studies confirmed the expected presence of the bioactive and revealed that solubilized β-carotene loaded WPC capsules presented excellent photo-oxidation stability compared with free β-carotene. The capsules developed here clearly show the significant potential of the combination of DES and electrospraying for the encapsulation and stabilization of highly insoluble bioactive compounds.

A Highly Selective and Sensitive Fluorescent Chemosensor for Detecting Al3+ Ion in Aqueous Solution and Plant Systems

The solubilized form of aluminum, Al3+, is present under acid soil conditions and toxic to both animals and plants. Detecting and quantifying Al3+ is vital for both chemistry and biology. A new Schiff-based fluorescent turn-on sensor (probe L) for the selective detection of the Al3+ ion was synthesized by coupling 2-hydroxy-1-naphthaldehyde and 2-aminoisoindoline-1,3-dione, and the structure was characterized by nuclear magnetic resonance spectra. The probe L exhibited an excellent selective and sensitive response to the Al3+ ion over other metal ions in DMSO-H2O (1:9 v/v). Fluorescence quantification revealed that probe L was promising for the detection and accumulation of Al3+. Treating rice seedlings with Al3+ at 25–200 μM inhibited their growth. Al3+ treatment produced reactive oxygen species in rice roots. Practical applications of the fluorescent probe for the quantification of Al3+ in water samples and rice seedlings are demonstrated. Detecting the Al3+ ion with the probe L is easy and a potential alternative to existing analytical methods. The method can be used for detecting the Al3+ content of aqueous solution and plant systems. The novel fluorescent probe L has good potential for monitoring Al3+ content in the environment and biological systems.

Self-Microemulsifying Drug Delivery Systems: An Attractive Strategy for Enhanced Therapeutic Profile

Ease of administration and painless approach made oral route the most preferred. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs with minimum dose. Although many formulation approaches like solid dispersions, complexation, pH modification, and cocrystals exist, lipid based delivery systems finding increased appliance with the apparent increase in absorption of drug. Among lipid based formulations, self-microemulsifying formulations (droplet size < 100 nm) are evident to improve the oral bioavailability of hydrophobic drugs primarily due to their efficiency in facilitating solubilization and in presenting the hydrophobic drug in solubilized form whereby dissolution process can be circumvented. Various components that are used to formulate these dosage forms like surfactants and lipids contribute to the overall improvement in oral bioavailability via promoting the lymphatic transport; thereby hepatic first pass metabolism can be surmounted. The present paper gives exhaustive information on the formulation design and characterization of SMEDDS along with the probable mechanisms by which the bioavailability can be improved with SMEDDS.

Formulation and evaluation of colon targeted tablets containing simvastatin solid dispersion

Solid dispersions (SDs) of simvastatin with mannitol, Ineutic®, Pluronic® F-68, PEG 4000 and PVP K-30 were prepared and evaluated to deliver simvastatin to the colon in a pre-solubilized form. The formula of choice was compressed into fast disintegrating tablets using drug compatible excipients and was coated with Eudragit® S100 as a pH-responsive polymer. We investigated the effects of several variables related to both SD preparation (carrier type, combined carriers and drug to carrier ratio) and tablet coating (coat level and type of plasticizer) on drug dissolution. Differential scanning caloremitry (DSC) and scanning electron microscopy (SEM) proved drug amorphization in SDs. The 1:5 simvastatin/ Pluronic® SDs showed the greatest improvement in dissolution efficiency (12.2-fold) at the lowest carrier ratio. The coating level was critical for determining the duration of the lagphase. Best results were given by the 10% coat (20:2:1 w/w Eudragit S100/ triethylcitrate/ talc). This formula resisted pre-colonic pH values and showed an adequate lag time for the intended colonic targeting (4 h), followed by an immediate release phase (t50%=249 min) in pH 7.4. The proposed coated tablets may provide a colonic delivery system for simvastatin with improved bioavailability.

The Plasmodium falciparum Ca2+-ATPase PfATP6: insensitive to artemisinin, but a potential drug target

The disease malaria, caused by the parasite Plasmodium falciparum, remains one of the most important causes of morbidity and mortality in sub-Saharan Africa. In the absence of an efficient vaccine, the medical treatment of malaria is dependent on the use of drugs. Since artemisinin is a powerful anti-malarial drug which has been proposed to target a particular Ca2+-ATPase (PfATP6) in the parasite, it has been important to characterize the molecular properties of this enzyme. PfATP6 is a 139 kDa protein composed of 1228 amino acids with a 39% overall identity with rabbit SERCA1a (sarcoplasmic/endoplasmic reticulum Ca2+-ATPase 1a). PfATP6 conserves all sequences and motifs that are important for the function and/or structure of a SERCA, such as two high-affinity Ca2+-binding sites, a nucleotide-binding site and a phosphorylation site. We have been successful in isolating PfATP6 after heterologous expression in yeast and affinity chromatography in a pure, active and stable detergent-solubilized form. With this preparation, we have characterized and compared with the eukaryotic SERCA1a isoform the substrate (Ca2+ and ATP) -dependency for PfATP6 activity as well as the specific inhibition/interaction of the protein with drugs. Our data fully confirm that PfATP6 is a SERCA, but with a distinct pharmacological profile: compared with SERCA1a, it has a lower affinity for thapsigargin and much higher affinity for cyclopiazonic acid. On the other hand, we were not able to demonstrate any inhibition by artemisinin and were also not able to monitor any binding of the drug to the isolated enzyme. Thus it is unlikely that PfATP6 plays an important role as a target for artemisinin in the parasite P. falciparum.