New ibuprofen derivatives with thiazolidine-4-one scaffold with improved pharmaco-toxicological profile.

BACKGROUND: Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an important heterocycle, which is associated with different biological effects such as anti-inflammatory and analgesic, antioxidant, antiviral, antiproliferative, antimicrobial etc. The present study aimed to evaluated the toxicity degree and the anti-inflammatory and analgesic effects of new 1,3-thiazolidine-4-one derivatives of ibuprofen. METHODS: For evaluation the toxicity degree, cell viability assay using MTT method and acute toxicity assay on rats were applied. The carrageenan-induced paw-edema in rat was used for evaluation of the anti-inflammatory effect while for analgesic effect the tail-flick test, as thermal nociception in rats and the writhing assay, as visceral pain in mice, were used. RESULTS: The toxicological screening, in terms of cytotoxicity and toxicity degree on mice, revealed that the ibuprofen derivatives (4a-n) are non-cytotoxic at 2 µg/ml. In addition, ibuprofen derivatives reduced carrageenan-induced paw edema in rats, for most of them the maximum effect was recorded at 4 h after administration which means they have medium action latency, similar to that of ibuprofen. Moreover, for compound 4d the effect was higher than that of ibuprofen, even after 24 h of administration. The analgesic effect evaluation highlighted that 4 h showed increased pain inhibition in reference to ibuprofen in thermal (tail-flick assay) and visceral (writhing assay) nociception models. CONCLUSIONS: The study revealed for ibuprofen derivatives, noted as 4 m, 4 k, 4e, 4d, a good anti-inflammatory and analgesic effect and also a safer profile compared with ibuprofen. These findings could suggest the promising potential use of them in the treatment of inflammatory pain conditions.

An Overview of Biopolymeric Electrospun Nanofibers Based on Polysaccharides for Wound Healing Management.

Currently, despite the thoroughgoing scientific research carried out in the area of wound healing management, the treatment of skin injuries, regardless of etiology remains a big provocation for health care professionals. An optimal wound dressing should be nontoxic, non-adherent, non-allergenic, should also maintain a humid medium at the wound interfacing, and be easily removed without trauma. For the development of functional and bioactive dressings, they must meet different conditions such as: The ability to remove excess exudates, to allow gaseous interchange, to behave as a barrier to microbes and to external physical or chemical aggressions, and at the same time to have the capacity of promoting the process of healing by stimulating other intricate processes such as differentiation, cell adhesion, and proliferation. Over the past several years, various types of wound dressings including hydrogels, hydrocolloids, films, foams, sponges, and micro/nanofibers have been formulated, and among them, the electrospun nanofibrous mats received an increased interest from researchers due to the numerous advantages and their intrinsic properties. The drug-embedded nanofibers are the potential candidates for wound dressing application by virtue of: Superior surface area-to volume ratio, enormous porosity (can allow oxy-permeability) or reticular nano-porosity (can inhibit the microorganisms'adhesion), structural similitude to the skin extracellular matrix, and progressive electrospinning methodology, which promotes a prolonged drug release. The reason that we chose to review the formulation of electrospun nanofibers based on polysaccharides as dressings useful in wound healing was based on the ever-growing research in this field, research that highlighted many advantages of the nanofibrillary network, but also a marked versatility in terms of numerous active substances that can be incorporated for rapid and infection-free tissue regeneration. In this review, we have extensively discussed the recent advancements performed on electrospun nanofibers (eNFs) formulation methodology as wound dressings, and we focused as well on the entrapment of different active biomolecules that have been incorporated on polysaccharides-based nanofibers, highlighting those bioagents capable of improving the healing process. In addition, in vivo tests performed to support their increased efficacy were also listed, and the advantages of the polysaccharide nanofiber-based wound dressings compared to the traditional ones were emphasized.