Metoprolol Tartrate-Ethylcellulose Tabletted Microparticles: Development of a Validated Invitro In-vivo Correlation

This study describes the methodology for the development of a validated in-vitro in-vivo correlation (IVIVC) for metoprolol tartrate modified release dosage forms with distinctive release rate characteristics. Modified release dosage forms were formulated by microencapsulation of metoprolol tartrate into different amounts of ethylcellulose by non-solvent addition technique. Then in-vitro and in-vivo studies were conducted to develop and validate level A IVIVC for metoprolol tartrate. The values of regression co-efficient (R2-values) for IVIVC of T2 and T3 formulations were not significantly (p

Design of Salbutamol Sulphate Gastroretentive Nanoparticles via Surface Charge Manipulation

In the present study, development of salbutamol sulphate nanoparticles that adhere to gastric mucus was investigated. Salbutamol sulphate has low bioavailability due to short transit time in gastric. It also has a positive surface charge that provides hurdles to be encapsulated by the positively strong mucoadhesive polymer of chitosan. To overcome the difficulties, the surface charge of active ingredient was modified using several nonionic and anionic stomach-specific polymers. The nanoparticles were prepared using ionotropic gelation technique. The evaluation involved determination of particle size, zeta potential, entrapment efficiency, in vitro drug release and in vitro mucoadhesion test. Results exhibited that the use of anionic alginate polymer was more satisfactory than that of nonionic polymer. Characteristics of the particles was nano-size, high encapsulation efficiency, fulfilled the drug release requirements and adhesive towards stomach for around 11 hours. This result shows that the salbutamol sulphate nanoparticles can be utilized for improvement its delivery.

Topical Delivery of Thymidine Dinucleotide to Induce p53 Generation in the Skin by Elastic Liposome

Transcription factor p53 has a powerful tumor suppressing function that is associated with many cancers. However, p53 of the molecular weight was higher make the limitation across to skin or cell membrane. Thymidine dinucleotide (pTT), an oligonucleotide, can activate the p53 transcription factor. pTT is a hydrophilic and negative charge oligonucleotide, which delivery in to cell membrane need an appropriate carrier. The aim of this study was to improve the bioavailability of the nucleotide fragment, thymidine dinucleotide (pTT), using elasic liposome carriers to deliver the drug into the skin. The study demonstrate that dioleoylphosphocholine (DOPC) incorporated with sodium cholate at molar ratio 1:1 can archived the particle size about 220 nm. This elastic liposome could penetration through skin from stratum corneum to whole epidermis by confocal laser scanning microscopy (CLSM). Moreover, we observed the the slight increase in generation of p53 by western blot.

Biodegradable Surfactants for Advanced Drug Delivery Strategies

Oxidative stress makes up common incidents in eukaryotic metabolism. The presence of diverse components disturbing the equilibrium during oxygen metabolism increases oxidative damage unspecifically in living cells. Body´s own ubiquinone (Q10) seems to be a promising drug in defending the heightened appearance of reactive oxygen species (ROS). Though, its lipophilic properties require a new strategy in drug formulation to overcome their low bioavailability. Consequently, the manufacture of heterogeneous nanodispersions is in focus for medical applications. The composition of conventional nanodispersions is made up of a drug-consisting core and a surfactive agent, also named as surfactant. Long-termed encapsulation of the surfactive components into tissues might be the consequence of the use during medical therapeutics. The potential of provoking side-effects is given by their nonbiodegradable properties. Further improvements during fabrication process use the incorporation of biodegradable components such as modified γ-polyglutamic acid which decreases the potential of prospective side-effects.

The Effect of Compost Addition on Chemical and Nitrogen Characteristics, Respiration Activity and Biomass Production in Prepared Reclamation Substrates

Land degradation is of concern in many countries. People more and more must address the problems associated with the degradation of soil properties due to man. Increasingly, organic soil amendments, such as compost are being examined for their potential use in soil restoration and for preventing soil erosion. In the Czech Republic, compost is the most used to improve soil structure and increase the content of soil organic matter. Land reclamation / restoration is one of the ways to evaluate industrially produced compost because Czech farmers are not willing to use compost as organic fertilizer. The most common use of reclamation substrates in the Czech Republic is for the rehabilitation of landfills and contaminated sites. This paper deals with the influence of reclamation substrates (RS) with different proportions of compost and sand on selected soil properties–chemical characteristics, nitrogen bioavailability, leaching of mineral nitrogen, respiration activity and plant biomass production. Chemical properties vary proportionally with addition of compost and sand to the control variant (topsoil). The highest differences between the variants were recorded in leaching of mineral nitrogen (varies from 1.36mg dm-3 in C to 9.09mg dm-3). Addition of compost to soil improves conditions for plant growth in comparison with soil alone. However, too high addition of compost may have adverse effects on plant growth. In addition, high proportion of compost increases leaching of mineral N. Therefore, mixture of 70% of soil with 10% of compost and 20% of sand may be recommended as optimal composition of RS.

Biokinetics of Coping Mechanism of Freshwater tilapia following Exposure to Waterborne and Dietary Copper

The purpose of this study was to understand the main sources of copper (Cu) accumulation in target organs of tilapia (Oreochromis mossambicus) and to investigate how the organism mediate the process of Cu accumulation under prolonged conditions. By measuring both dietary and waterborne Cu accumulation and total concentrations in tilapia with biokinetic modeling approach, we were able to clarify the biokinetic coping mechanisms for the long term Cu accumulation. This study showed that water and food are both the major source of Cu for the muscle and liver of tilapia. This implied that control the Cu concentration in these two routes will be correlated to the Cu bioavailability for tilapia. We found that exposure duration and level of waterborne Cu drove the Cu accumulation in tilapia. The ability for Cu biouptake and depuration in organs of tilapia were actively mediated under prolonged exposure conditions. Generally, the uptake rate, depuration rate and net bioaccumulation ability in all selected organs decreased with the increasing level of waterborne Cu and extension of exposure duration.Muscle tissues accounted for over 50%of the total accumulated Cu and played a key role in buffering the Cu burden in the initial period of exposure, alternatively, the liver acted a more important role in the storage of Cu with the extension of exposures. We concluded that assumption of the constant biokinetic rates could lead to incorrect predictions with overestimating the long-term Cu accumulation in ecotoxicological risk assessments.

Development and in vitro Characterization of Self-nanoemulsifying Drug Delivery Systems of Valsartan

The present study is aim to prepare and evaluate the selfnanoemulsifying drug delivery (SNEDDS) system of a poorly water soluble drug valsartan in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. The present research work describes a SNEDDS of valsartan using labrafil M 1944 CS, Tween 80 and Transcutol HP. The pseudoternary phase diagrams with presence and absence of drug were plotted to check for the emulsification range and also to evaluate the effect of valsartan on the emulsification behavior of the phases. The mixtures consisting of oil (labrafil M 1944 CS) with surfactant (tween 80), co-surfactant (Transcutol HP) were found to be optimum formulations. Prepared formulations were evaluated for its particle size distribution, nanoemulsifying properties, robustness to dilution, self emulsication time, turbidity measurement, drug content and invitro dissolution. The optimized formulations are further evaluated for heating cooling cycle, centrifugation studies, freeze thaw cycling, particle size distribution and zeta potential were carried out to confirm the stability of the formed SNEDDS formulations. The prepared formulation revealed t a significant improvement in terms of the drug solubility as compared with marketed tablet and pure drug.

Effect of Ionic Strength on Mercury Adsorption on Contaminated Soil

Mercury adsorption on soil was investigated at different ionic strengths using Ca(NO3)2 as a background electrolyte. Results fitted the Langmuir equation and the adsorption isotherms reached a plateau at higher equilibrium concentrations. Increasing ionic strength decreased the sorption of mercury, due to the competition of Ca ions for the sorption sites in the soils. The influence of ionic strength was related to the mechanisms of heavy metal sorption by the soil. These results can be of practical importance both in the agriculture and contaminated soils since the solubility of mercury in soils are strictly dependent on the adsorption and release process.