Optimal Extraction Process and In Vivo Anti-Inflammatory Evaluation of High Purity Oily Capsicum Oleoresin for Pharmaceutical Applications.

Recently, plant-derived anti-inflammatory products have received an increasing attention from researchers due to their excellent in vivo activity with limited side effects. Therefore, the extraction of natural active compounds from the plant with high purity for use in anti-inflammatory formulations is required. In this study, oily Capsicum oleoresin (OCO) was extracted from Capsicum frutescens L. in ethanol by the ultrasound-assisted extraction technique, followed by a centrifugation step for a high purity OCO extract, which can be applied to develop anti-inflammatory formulations. The impact of various conditions (ethanol concentration, sonicating temperature, extraction time, solvent-to-sample ratio, and extraction repetition) on the efficiency of the extraction process was investigated. The results showed that the optimized conditions for the high yield of OCO were 95% ethanol, 50-60°C, 60 minutes, solvent-to-sample ratio of 5 : 1 ml/g, and one extraction repetition, followed by centrifuging at 5000 rpm in 2 hours. Then, the purity and in vivo anti-inflammatory activities of the obtained OCO was then determined by using the HPLC method and carrageenan-induced mice paw edema model, respectively. The purity of OCO was determined as 3.408 mg capsaicin per gram of Capsicum powder; meanwhile, its anti-inflammatory effect value was approximate to that of the commercial drug diclofenac after 48 hours of treatment. The high purity OCO prepared by this low-cost and ecofriendly extraction process would be a promising material for anti-inflammatory formulations.

A scalable process to produce lipid-based compartmented Janus nanoparticles with pharmaceutically approved excipients.

In the field of nanotechnologies, theranostic approaches and fixed-dose combination products require the development of innovative carriers able to co-encapsulate several entities of interest. This communication describes the preparation and characterization of lipid-based Janus compartmented nanoparticles. They were successfully prepared using a scalable process with pharmaceutically approved excipients. The analysis of the microscopic structure and supramolecular organization demonstrated the formation of two physico-chemically different compartments enabling the co-administration at once of both liposoluble and hydrosoluble active pharmaceutical ingredients.

Anti-inflammatory and wound healing activities of calophyllolide isolated from Calophyllum inophyllum Linn.

Due to the high-cost and limitations of current wound healing treatments, the search for alternative approaches or drugs, particularly from medicinal plants, is of key importance. In this study, we report anti-inflammatory and wound healing activities of the major calophyllolide (CP) compound isolated from Calophyllum inophyllum Linn. The results showed that CP had no effect on HaCaT cell viability over a range of concentrations. CP reduced fibrosis formation and effectively promoted wound closure in mouse model without causing body weight loss. The underlying molecular mechanisms of wound repair by CP was investigated. CP markedly reduced MPO activity, and increased M2 macrophage skewing, as shown by up-regulation of M2-related gene expression, which is beneficial to the wound healing process. CP treatment prevented a prolonged inflammatory process by down-regulation of the pro-inflammatory cytokines-IL-1ß, IL-6, TNF-α, but up-regulation of the anti-inflammatory cytokine, IL-10. This study is the first to indicate a plausible role for CP in accelerating the process of wound healing through anti-inflammatory activity mechanisms, namely, by regulation of inflammatory cytokines, reduction in MPO, and switching of macrophages to an M2 phenotype. These findings may enable the utilization of CP as a potent therapeutic for cutaneous wound healing.

Study on the hydatid cyst membrane: permeation of model molecules and interactions with drug-loaded nanoparticles.

The success of the chemotherapeutic treatment of hydatid disease is based upon the drug ability to operate on the germinal layer and on the protoscolices of the hydatid cyst interior at adequate concentrations for sufficient periods. The goal of this study was to evaluate the ability of the drug diffusion through the cyst membrane from sheep hydatid cysts and the increase of drug concentration in the cyst environment. In the first part of this work, the permeation behaviour through the hydatid cyst membrane was studied with five model molecules, having different molecular descriptors (logP, molecular weight, polar surface area ...) onto static Franz glass diffusion cells. A good correlation has been observed between the permeation coefficient and the partition coefficient, log P (r=0.951). In the second part, albendazole-loaded nanoparticles (about 300 nm) prepared by the emulsion solvent evaporation method have shown a sufficient entrapment efficiency (36.4 +/- 6.4%) to raise the apparent solubility of albendazole. The diffusion of drug from the nanoparticles across the hydatid cyst membrane was also improved compare to albendazole suspension. These results have shown the interest of the albendazole-loaded nanoparticles for the treatment of hydatid cysts in the future.