Optimizacija mikrokapsulacije aktivnog sastojka umrežavanjem i metodom premazivanja za liječenje bolesti debelog crijeva

The aim of this study was to prepare microcapsules based on a natural polymer chitosan solution (high degree of deacetylation (DDA), low molecular weight (MW), and low viscosity)/sodium alginate in the presence of a crosslinking agent (glutaraldehyde), in order to encapsulate and vectorise the active principle towards the diseased organ (colon), without being diffused into other levels of the digestive tract, to increase the therapeutic effectiveness of treatment by chemotherapy and to reduce undesirable effects. The method of preparation of the microcapsules obtained from the sodium alginate/chitosan solution/active ingredients system was examined by conventional optical microscopy. In addition, an in vitro study was carried out on the active ingredients’ release profiles, depending on the pH simulating the gastric and intestinal media for the seven systems proposed. It should be mentioned that, in the basic medium (pH(colon) = 8), the release of the active ingredients is of the utmost importance. Nevertheless, control of this release can be improved by a crosslinking agent and the coating method. The dry [sodium alginate / chitosan solution / active ingredients + crosslinking 2 %] formulation coated with non-crosslinked chitosan (Formulation 7) is the standard formula that meets all the criteria from our earlier work, with a core release rate of 67 %. The PSD was unimodal, with sizes ranging from 750 µm to 900 µm. This work is licensed under a Creative Commons Attribution 4.0 International License.Cilj ove studije bio je pripremiti mikrokapsule na bazi prirodne polimerne otopine kitozana (visokog stupnja deacetiliranja (DDA), niske molekulske mase (MW) i niske viskoznosti)/natrijeva alginata u prisutnosti umreženog agensa (glutaraldehida), za inkapsuliranje i vektoriziranje aktivnog sastojka prema bolesnom organu (debelom crijevu), bez difuzije u druge razine probavnog trakta, kako bi se povećala terapijska učinkovitost liječenja kemoterapijom i smanjili neželjeni učinci. Metoda pripreme mikrokapsula dobivenih iz sustava natrijeva alginata/otopine kitozana/aktivnih sastojaka ispitana je uobičajenom optičkom mikroskopijom. Uz to, provedeno je istraživanje in vitro na profilima oslobađanja aktivnih sastojaka, ovisno o pH koji simulira želučani i crijevni medij za sedam predloženih sustava. Treba napomenuti da je u osnovnom mediju (pH(debelog crijeva) = 8) oslobađanje aktivnih sastojaka od najveće važnosti. Ipak, kontrola tog ispuštanja može se poboljšati sredstvom za umrežavanje i metodom premazivanja. Suha formulacija [otopina natrijeva alginata/kitozana/aktivnih sastojaka + umreženog 2 %] presvučena neumreženim kitozanom (formulacija 7) standardna je formula koja udovoljava svim kriterijima iz našeg ranijeg rada s brzinom otpuštanja jezgre od 67 %. PSD je bio unimodalan s veličinama koje su se kretale od 750 µm do 900 µm. Ovo djelo je dano na korištenje pod licencom Creative Commons Imenovanje 4.0 međunarodna

Komparativna terapeutska svojstva ekstrakta češnjaka i metformina na hiperglikemiju, hiperkolesterolemiju i hipertrigliceridimiju kod štakora s dijabetesom tipa 1 induciranim aloksanom

The current pilot study was conducted to compare the triple effect of garlic extract and metformin on hyperglycaemia, hypercholesterolaemia, and hypertriglyceridaemia in alloxan-induced type 1-like diabetic rats. Wistar rats were randomly divided into four groups. Control group included normal rats. The second group included alloxan-induced type 1-like diabetic rats, receiving no treatment. The other two groups of diabetic rats were orally treated with 0.75 g of garlic extract per kg of body weight and 0.05 of metformin g per kg of body weight respectively for four weeks. The pharmacological impact of garlic compounds on serum glucose and lipids as opposed to the glucose-lowering and lipid-lowering was highlighted in these experiments. These results revealed that garlic extract has a triple action on hyperglycaemia, hypertriglyceridemia, and hypercholesterolemia. Its effect on hyperglycaemia is long lasting, and more pronounced compared to the metformin. Interestingly, it had a regulatory effect on glycaemia as highlighted in the control group. This work is licensed under a Creative Commons Attribution 4.0 International License.Ovo pilot-istraživanje provedeno je da bi se usporedio trostruki učinak ekstrakta češnjaka i metformina na hiperglikemiju, hiperkolesterolemiju i hipertrigliceridemiju kod štakora s dijabetesom tipa 1 induciranim aloksanom. Štakori Wistar nasumično su bili podijeljeni u četiri skupine. Kontrolna skupina sadržavala je normalne štakore. Druga skupina bili su netretirani štakori s dijabetesom (dijabetes tipa 1, induciran aloksanom). Preostale dvije skupine štakora s dijabetesom liječene su četiri tjedna ekstraktom češnjaka doziranim 75 g po kilogramu tjelesne težine, odnosno metforminom u dozi 0,05 g po kilogramu tjelesne težine. Navedeni spojevi unosili su se oralnim putem. U istraživanjima naglašen je farmakološki utjecaj spojeva iz češnjaka na glukozu i lipide u serumu. Dobiveni rezultati pokazali su da ekstrakt češnjaka ima trostruko djelovanje na: hiperglikemiju, hipertrigliceridemiju i hiperkolesterolemiju. Njegov učinak na hiperglikemiju dugotrajan je i izraženiji u usporedbi s metforminom. Zanimljivo je da je djelovao regulacijski na glikemiju. Ovo djelo je dano na korištenje pod licencom Creative Commons Imenovanje 4.0 međunarodna

Comparative Therapeutic Properties of Garlic Extract and Metformin on Hyperglycaemia, Hypercholesterolaemia, and Hypertriglyceridaemia in Alloxan-induced Type1-like Diabetic Rats

The current pilot study was conducted to compare the triple effect of garlic extract and metformin on hyperglycaemia, hypercholesterolaemia, and hypertriglyceridaemia in alloxan-induced type 1-like diabetic rats. Wistar rats were randomly divided into four groups. Control group included normal rats. The second group included alloxan-induced type 1-like diabetic rats, receiving no treatment. The other two groups of diabetic rats were orally treated with 0.75 g of garlic extract per kg of body weight and 0.05 of metformin g per kg of body weight respectively for four weeks. The pharmacological impact of garlic compounds on serum glucose and lipids as opposed to the glucose-lowering and lipid-lowering was highlighted in these experiments. These results revealed that garlic extract has a triple action on hyperglycaemia, hypertriglyceridemia, and hypercholesterolemia. Its effect on hyperglycaemia is long lasting, and more pronounced compared to the metformin. Interestingly, it had a regulatory effect on glycaemia as highlighted in the control group

Prediction of the antibacterial activity of garlic extract on E. coli, S. aureus and B. subtilis by determining the diameter of the inhibition zones using artificial neural networks

The aim of this study was to devise a model that predicts the inhibition zone diameter using artificial neural networks. The concentration, temperature and the exposure time of our extract were taken as input variables. The neural architecture model 3-13-3 and a learning algorithm Quasi-Newton (BFGS) revealed a positive correlation between the experimental results and those artificially predicted, which were measured according to a mean squared error (RMSE) and an R2 coefficient of E. coli (RMSE = 1.28; R2 = 0,96), S. aureus (RMSE = 1.46; R2 = 0,97) and B. subtilis (RMSE = 1.88; R2 = 0,96) respectively. Based on these results, an external and an internal model validation were attained. A neuronal mathematical equation was created to predict the inhibition diameters for experimental data not included in the basic learning. Consequently, a good correlation was observed between the values predicted by the equation and those obtained experimentally, as demonstrated by the R2 and RMSE values. The results regarding the sensitivity analysis showed that the concentration was the most determinant parameter compared to Temperature and Time variables. Ultimately, the model developed in this study will be used reliably to predict the variation of garlic extract's inhibition diameter