Design and optimization of resveratrol-loaded porous calcium silicate powders for dissolution and photostability enhancement

In this study, resveratrol (RVT) was loaded onto porous calcium silicate (PCS) powders to improve its dissolution and photostability properties. The effects of RVT/PCS powders that included varying amounts of low-methoxyl pectin (LMP), ethyl acetate (EA) and PCS on drug loading capacity, encapsulation efficiency and drug dissolution at 5-min intervals (Q5) were investigated using a Box–Behnken design. The experimental results demonstrated that the EA and PCS amounts significantly influenced drug loading capacity. Encapsulation efficiency was affected by EA amount, whereas the amount of PCS had a significant effect on Q5. Empirical experiments demonstrated the reliability of mathematical models. A design space was established based on the criteria set for maximizing each response of the RVT/PCS powders. An optimized formulation containing 2.6% w/w LMP, 19% w/w EA and 13% w/w PCS prepared within the design space satisfied all criteria. The dissolution and photostability of RVT in the RVT/PCS powders were significantly improved. Further, the bulk density of the PCS powders in RVT/PCS was increased by LMP. The Box–Behnken design used in this study provided an improved understanding of the effects of formulation factors on RVT/PCS powder characteristics as well as the optimization of RVT/PCS powder formulations with the desired properties

Effect of high-pressure homogenization on stability of emulsions containing zein and pectin

The aim of this study was to investigate the effect of high-pressure homogenization on the droplet size and physical stability of different formulations of pectin–zein stabilized rice bran oil emulsions. The obtained emulsions, both before and after passing through high-pressure homogenizer, were subjected to stability test under environmental stress conditions, that is, temperature cycling at 4 °C/40 °C for 6 cycles and centrifugal test at 3000 rpm for 10 min. Applying high-pressure homogenization after mechanical homogenization caused only a small additional decrease in emulsion droplet size. The droplet size of emulsions was influenced by the type of pectin used; emulsions using high methoxy pectin (HMP) were smaller than that using low methoxy pectin (LMP). This is due to a greater emulsifying property of HMP than LMP. The emulsions stabilized by HMP–zein showed good physical stability with lower percent creaming index than those using LMP, both before and after passing through high-pressure homogenizer. The stability of emulsions after passing through high-pressure homogenizer was slightly higher when using higher zein concentration, resulting from stronger pectin–zein complexes that could rearrange and adsorb onto the emulsion droplets

A new self-emulsifying formulation of mefenamic acid with enhanced drug dissolution

To enhance the dissolution of poorly soluble mefenamic acid, self-emulsifying formulation (SEF), composing of oil, surfactant and co-surfactant, was formulated. Among the oils and surfactants studied, Imwitor® 742, Tween® 60, Cremophore® EL and Transcutol® HP were selected as they showed maximal solubility to mefenamic acid. The ternary phase diagram was constructed to find optimal concentration that provided the highest drug loading. The droplet size after dispersion and drug dissolution of selected formulations were investigated. The results showed that the formulation containing Imwitor® 742, Tween® 60 and Transcutol® HP (10:30:60) can encapsulate high amount of mefenamic acid. The dissolution study demonstrated that, in the medium containing surfactant, nearly 100% of mefenamic acid were dissolved from SEF within 5 min while 80% of drugs were dissolved from the commercial product in 45 min. In phosphate buffer (without surfactant), 80% of drug were dissolved from the developed SEF within 5 min while only about 13% of drug were dissolved in 45 min, from the commercial product. The results suggested that the SEF can enhance the dissolution of poorly soluble drug and has a potential to enhance drug absorption and improve bioavailability of drug

Design of Turmeric Rhizome Extract Nano-Formula for Delivery to Cancer Cells

Novel turmeric rhizome extract nanoparticles (TE-NPs) were developed from fractions of dried turmeric (Curcuma longa Linn.) rhizome. Phytochemical studies, by using HPLC and TLC, of the fractions obtained from ethanol extraction and solvent–solvent extraction showed that turmeric rhizome ethanol extract (EV) and chloroform fraction (CF) were composed mainly of three curcuminoids and turmeric oil. Hexane fraction (HE) was composed mainly of turmeric oil while ethyl acetate fraction (EA) was composed mainly of three curcuminoids. The optimal TE-NPs formulation with particle size of 159.6 ± 1.7 nm and curcumin content of 357.48 ± 8.39 µM was successfully developed from 47-run D-optimal mixture–process variables experimental design. Three regression models of z-average, d50, and d90 could be developed with a reasonable accuracy of prediction (predicted r2 values were in the range of 0.9120–0.9992). An in vitro cytotoxicity study using MTT assay demonstrated that the optimal TE-NPs remarkably exhibited the higher cytotoxic effect on human hepatoma cells, HepG2, when compared with free curcumin. This study is the first to report nanoparticles prepared from turmeric rhizome extract and their cytotoxic activity to hepatic cancer cells compared with pure curcumin. These nanoparticles might serve as a potential delivery system for cancer therapy