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.
In the past decades, the researchers have focused their attention on the synthesis of new polymeric nanoparticles as drug delivery systems based on their small particle size and large surface area. The aim of this study was to optimize the synthesis of chitosan-based nanoparticles (CSNPs) and to study the influence of different parameters on the formulation process. The CSNPs were prepared by the ionic gelation method using sodium tripolyphosphate (TPP) as cross-linking agent and two types of chitosan (CS) (low and medium molecular weight). In order to optimize the preparation method, several parameters, such as the CS and TPP concentration, the pH of CS solution, the stirring speed and the reticulation time have been varied. The CSNPs synthesis was monitored by dynamic light scattering (DLS) technique. The results showed that the optimized method use 0.1% TPP and 0.1% CS low molecular weight in ratio of 3:1, with pH ranking between 4.7 and 4.8 and stirring at 1000 rpm for 1 h. In these conditions the size of CSNPs was 208.8 ± 8.5 nm with 0.151 polydispersity index. Based on the obtained results it could be appreciated that optimized CSNPs could be further used as drug carriers. RezumatÎn ultimele decenii, cercetătorii și-au axat atenția pe sinteza de noi nanoparticule polimerice ca sisteme de eliberare a medicamentelor, datorită dimensiunii mici a particulelor și a suprafeței mari. Scopul acestui studiu a fost optimizarea metodei de sinteză pentru nanoparticule de chitosan (CSNPs) prin studierea influenței diferitelor parametrii asupra procesului de formulare. Nanoparticulele de chitosan au fost preparate prin metoda gelificării ionice folosind tripolifosfat de sodiu (TPP) ca agent de reticulare și două tipuri de chitosan (CS) (cu greutate moleculară mică și medie). În vederea optimizării metodei de preparare, s-au modificat diferiți parametri cum ar fi concentrația de CS și TPP, pH-ul soluției de CS, viteza de agitare a amestecului și timpul de reticulare. Sinteza nanoparticulelor a fost monitorizată prin tehnica de dispersie dinamică a luminii (DLS). Rezultatele au arătat că metoda optimizată implică folosirea solutiei de TPP 0,1%, de CS cu greutate moleculară mică 0,1%, în raport de 3:1, cu un pH cuprins între 4,7 -4,8 și viteză de agitare de 1000 rpm, timp de o oră. În aceste condiții, mărimea particulelor obținute a fost de 208,8 ± 8,5 nm, având un indice de polidispersie de 0,151. Pe baza rezultatelor obținute se poate aprecia că nanoparticulele de chitosan optimizate pot fi utilizate în continuare ca sisteme de transport a medicamentelor.
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.
Usually gastrointestinal discomfort is a very common complaint and most of the time it’s easy to manage in daily pharmaceutical practice. But some conditions can lead to further complications or become worse over time, so it’s really important that patients can access advice and support when they need it. Pharmacists are in the position to guide the selection of the best treatment by confirming the diagnosis, sending patients with alarm symptoms to physicians and educating patients on the proper use of their OTC medication. Gastrointestinal symptoms such as diarrhea and nausea/vomiting are often recognized among the patients with COVID-19. The impact of pharmacist intervention is needed in order to ensure reliable information for preventing, detecting, treating and managing coronavirus infection.
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