Enhancing the water-solubility of curcuminoids-rich extract using a ternary inclusion complex system: Preparation, characterization, and anti-cancer activity.

Curcuminoids are known to exert diverse pharmacological effects and used in some pharmaceutical formulations. This study describes the preparation, characterization, and enhancement in the solubility and anticancer activity of a curcuminoids-rich extract (CRE) using a ternary inclusion complex system. CRE containing 88.9% w/w curcuminoids was prepared using a 'green' microwave extraction coupled with fractionation on a column of hydrophobic adsorbent resin. The ternary complex consisting of CRE, hydroxylpropyl-ß-cyclodextrin and polyvinylpyrrolidone K30 was prepared using the solvent evaporation method and thoroughly characterized using Fourier-transform infrared spectroscopy, powder X-ray diffractograms, differential scanning calorimetry and scanning electron microscopy. The ternary complex of CRE improved the water-solubility of curcuminoids (up to 70.3 µg/mL) as well as the dissolution rate when compared to those of CRE (0 µg/mL). In addition, the ternary complex exhibited significantly stronger anticancer activity against human lung adenocarcinoma (A-549), human cervical adenocarcinoma (HeLa) and human colon adenocarcinoma (HT-29) cell lines than CRE.

Characterization, Antioxidant and Antibacterial Potentials of Tamarindus indica L. Fruit Pulp Extract Loaded O/W Nanoemulsions

Abstract The main purposes of the current study were to formulate o/w nanoemulsions as a carrier for Tamarindus indica (tamarind) fruit pulp extract and to study the antioxidant and antibacterial potentials of nanoemulsions containing tamarind extract, focusing on cosmetic/hygiene applications. The o/w nanoemulsions using a mixture of Tween 80 and Span 80 as an emulsifier (5%w/w) were prepared by a high pressure homogenization process. Two concentrations of sweet tamarind extract, 3.3 and 6.6%w/w, based on the bioactivity study, were incorporated into the blank nanoemulsions to produce loaded nanoemulsions, F1-3.3TE (3.3%) and F1- 6.6TE (6.6%). As compared with the unloaded nanoemulsion, both tamarind extract loaded nanoemulsions showed reduced pH and significantly increased viscosity. Overall, the loaded nanoemulsions had droplet sizes of approximately 130 nm, zeta potential around -38 mV and polydispersity index (PDI) values less than 0.2. The nanoemulsion F1-3.3TE had better stability (e.g. significantly greater % tartaric acid content and lesser PDI value) than the nanoemulsion F1-6.6TE did. The antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl assay revealed that the nanoemulsions F1-3.3TE and F1-6.6TE had scavenging activities of 81.66 ± 0.77% and 63.80 ± 0.79%, respectively. However, antioxidant activity of these two formulations decreased under stress conditions (heating-cooling cycles). Such incidence did not occur for their antibacterial properties investigated by agar well diffusion technique. The two formulations exhibited inhibition zones of approximately 24.0-27.7 mm against Staphylococcus aureus and Staphylococcus epidermidis, responsible for malodor of underarms. The results suggest the potential of using sweet tamarind pulp extract loaded nanoemulsions as hygiene products.

Influence of interfering co-appearing container peaks on the accuracy of direct quantitative Raman measurement of a sample in a plastic container.

The axially perpendicular offset (APO) scheme was previously demonstrated as a versatile scheme able to minimize or eliminate the glass background in the direct and non-sampling Raman measurement of an ethanol sample housed in a glass bottle. Alternatively, when directly analyzing a sample housed in a plastic container, another typical container yielding strong Raman peaks itself, the Raman peaks of both the container and the housed sample are unavoidably present together in a collected spectrum. Therefore, a crucial issue to investigate under this situation is how the magnitude of the co-appearing container peaks influences the accuracy for quantitative analysis of the housed sample. For the evaluation, a non-sampling Raman spectroscopic measurement of the urea concentration in a urea gel housed in a circular polypropylene (PP) container was attempted by employing two axially perpendicular offset (APO) schemes with detection windows of different sizes (25.4 and 10.0 mm, referred to as the wide-window APO (WW-APO) and narrow-window APO (NW-APO), respectively), and transmission and back-scattering schemes incorporating a 25.4 mm detection window. The intensity ratios between the container and urea peaks in the collected spectra were different depending on the adopted measurement scheme. The intensity ratio was greatest (smallest container peak) in the NW-APO measurement due to the narrowed detection window, making the generated container Raman photons at the side-wall less detectable to the bottom-positioned detector. A spectral acquisition scheme allowing the maximal suppression of the container peaks, while still maintaining the sample features, was a key requirement to secure an accurate measurement of the sample concentration. In addition, a Monte Carlo simulation was used to visualize the distributions of the container and urea photons inside the sample-housed container.

Characterization of a novel, co-processed bio-based polymer, and its effect on mucoadhesive strength.

In this study, a biological macromolecule obtained from seeds of Manilkara zapota was co-processed with hypromellose (cop-MPH)/sodium carboxymethylcellulose (cop-MPN)/polyvinylpyrrolidone (cop-MPP) in a 1:1 ratio and characterized for powder and mucoadhesive properties. The semi-crystalline nature of co-processed excipients and physical interaction between the component molecules were confirmed by X-ray diffraction and infrared spectroscopy analysis. The morphological study by scanning electron and atomic force microscopy showed spherical and polygonal-shaped particles with predominant smooth surfaces. Thermogravimetric analysis revealed thermal stability to a temperature of 200 °C followed by depolymerization. Zeta potential measurements showed that cop-MPP was anionic, whereas cop-MPH and MPN were non-ionic. Texture analysis revealed that work of adhesion (mN·s) for both cop-MPH (390 ± 0.0018) and MPN (304 ± 0.0024) enhanced the mucoadhesion compared with the un-processed hypromellose (300 ± 0.0019) and sodium carboxymethylcellulose (280 ± 0.0012), whereas cop-MPP (240 ± 0.0028) showed mucoadhesion similar to un-processed polyvinylpyrrolidone (250 ± 0.0022). In addition, the swelling studies showed enhancement in water absorbance for all co-processed excipients. Cytotoxicity against human cells revealed >99% of cell viability. These findings demonstrate that the co-processed biological macromolecule extracted from M. zapota seed could be further explored as an effective alternative drug delivery excipient for pharmaceutical applications.

A Cold Process Preparation of Vetiveria zizanioides (L.) Nash Oil Lotions using Simulgel FL as an Emulsifier.

Vetiveria zizanioides (vetiver) contains viscous volatile oil, which has the ability to repel mosquitoes similar to citronella oil, a well-known mosquito repellent in tropical countries, like Thailand. The objectives of the current study were to formulate the stable oil-in-water vetiver oil lotions using Simulgel FL as a liquid emulsifier, to investigate the physicochemical properties of the prepared lotions and to evaluate the in vitro release characteristics of the stable vetiver oil lotions. In this work, the concentrations of Simulgel FL ranged from 1% to 3% weight in weight, whereas the concentrations of vetiver oil were varied: 2.5%, 5%, and 10% weight in weight. The suitable concentration of Simulgel FL was found to be 3% weight in weight. For comparison purposes, oil-in-water citronella oil lotions (10% weightin- weight citronella oil) were also prepared with similar ingredients. A mixture of vetiver oil and citronella oil (1:1 by weight) was also used as an active ingredient. By using Simulgel FL, the lotions could be prepared using a cold process (without heat). The physicochemical properties (appearance, pH, viscosity) of the stable lotions were satisfactory. All prepared lotions possessed weak acidic pH values with pseudoplastic flows. Using modified Franz diffusion cell and synthetic membrane, the release rates of vetiver oil were relatively lower than those of citronella oil.

Topical anti-inflammatory and analgesic activities of standardized pomegranate rind extract in comparison with its marker compound ellagic acid in vivo.

ETHNOPHARMACOLOGICAL RELEVANCE: In Chinese traditional medicine, the peels of Punica granatum L. have been used to treat traumatic hemorrhage, burn, and ulcers. AIMS OF THE STUDY: This study aimed to assess the topical anti-inflammatory and analgesic activities of a standardized pomegranate rind extract (SPRE) of which ellagic acid (EA) was the major antioxidant constituent and the marker compound. MATERIAL AND METHODS: The topical anti-inflammatory effects of SPRE were evaluated against acute models (croton oil-induced mouse ear edema and carrageenan-induced rat paw edema) and chronic model (complete Freund's adjuvant (CFA)-induced polyarthritis). The topical analgesic activities of SPRE were investigated in the rat punctuate mechanical hyperalgesia test and in the mouse formalin test. All studies of SPRE were carried out in parallel with its marker compound EA. RESULTS: SPRE (5%, 2.5%, and 1%, w/w) and the equivalent EA (0.65%, 0.325%, and 0.13%, w/w) dose-dependently reduced the croton oil-induced mouse ear edema with a maximal inhibition of 86.30% and 80.82%, respectively. SPRE dose-dependently attenuated the inflammatory responses in the carrageenan-induced rat paw edema and in the CFA-induced polyarthritis but the equivalent EA were effective only at the doses of 0.65% and 0.325%. Both SPRE (5%) and EA (0.65%) showed significant topical analgesic activities in the rat punctuate mechanical hyperalgesia test and in the mouse formalin test. CONCLUSIONS: SPRE was more active as an anti-inflammatory agent than EA. The anti-inflammatory and analgesic effects of SPRE were achieved through inhibiting the leukocyte infiltration and modulating the pro-inflammatory cytokines IL-ß and TNF-α. These results clearly demonstrated that SPRE is a promising phytomedicine that could find use in the treatment of inflammatory diseases.

Effects of glucam P-20, vanillin, and fixolide on mosquito repellency of citronella oil lotions.

The objective of this study was to investigate the effects of three fragrance fixatives, Glucam P-20, Vanillin, and Fixolide, on the mosquito repellent property of citronella oil lotions. In the current study, two formulae (A and B) of oil-in-water citronella oil lotions were formulated using different ingredients (emulsifiers [Cremophors or Emulwax], stiffening agents, and emollients). Citronella oil was used at 10% wt:wt. The weight ratios tested between citronella oil and each fixative were 1:0.25, 1:0.5, and 1:1. Overall, 20 formulations, including one with no fixatives for both A and B, were produced, A1-A10 and B1-B10. The repellent activities of these 20 lotions against Aedes aegypti (L.) were tested using a human-bait technique. The types and concentrations of fixatives as well as the compositions of the formulations did affect the protection time of the citronella oil lotions. The lotion containing Emulwax and 5% vanillin (B6) was the most effective repellent. It provided the longest protection time of 4.8 h, which exceeded the minimum requirement of 2 h set by the National Institute of Health, Thailand. The shortest protection time (1 h) was observed in the lotion containing Emulwax and 2.5% Glucam P-20 (B2). It could be concluded that the tested fixatives affected the repellent activity of the citronella oil lotions.