Flaxseed Lignans and Polyphenols Enhanced Activity in Streptozotocin-Induced Diabetic Rats.

Flaxseeds play an important role in human health due to their chemical composition and recognized beneficial outcomes. This study investigated the antidiabetic effects of present lignans and polyphenols found in the flaxseed extract on streptozotocin (STZ)-induced diabetic rats. The flaxseed administration produced favorable changes in body weight, food and water intake, and glycosylated hemoglobin and blood glucose quantities in the treated diabetic rats. Additionally, significant positive results were observed in the biochemical parameters, namely reduced plasma cholesterol, LDL cholesterol and triglycerides, plasma creatinine, and urea and uric acid levels, highlighting the seeds' use in traditional medicine. The results were sustained by histopathological observations that showed better tissue preservation following the flaxseed diet. Overall, the consumption of flaxseeds produced moderate reduction in glucose levels and hyperlipidemia, together with improvement in the impaired organs' function in diabetic rats. The daily administration of polyphenols and lignans compounds could impact therapeutic potential in diabetes management.

Chemical functionalization of hyaluronic acid for drug delivery applications.

Functionalized hyaluronic acid (HA) derivatives were obtained by ring opening mechanism of maleic anhydride (MA). FTIR and H(1) NMR spectroscopy were used to confirm the chemical linkage of MA on the hyaluronic acid chains. Thermal analysis (TG-DTG and DSC) and GPC data for the new products revealed the formation of new functional groups, without significant changes in molecular weight and thermal stability. New gels based on hyaluronic acid modified derivatives were obtained by acrylic acid copolymerization in the presence of a redox initiation system. The resulted circular and interconnected pores of the gels were visualized by SEM. The release profiles of an ophthalmic model drug, pilocarpine from tested gels were studied in simulated media. Evaluation of the cytotoxicity and cell proliferation properties indicates the potential of the new systems to be used in contact with biological media in drug delivery applications.

Poly(acrylic acid)-poly(ethylene glycol) nanoparticles designed for ophthalmic drug delivery.

Poly(acrylic acid) (PAA) and poly(ethylene glycol) (PEG), four-arm, amine-terminated particles with nanometer size and spherical shape were obtained by the polymers cross-linking, via activation with 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide hydrochloride, in a w/o emulsion. The morphology and surface charge of the final particles are strongly dependent on the molar ratio of PAA-PEG and the PAA concentration. The physicochemical characteristics correlated with the drug-loading capacity, in vitro and ex vivo release kinetics of pilocarpine hydrochloride and biocompatibility results indicate that these nanoparticles exhibit the prerequisite behavior for use as carriers of ophthalmic drugs.

In vitro and in vivo theophylline release from cellulose/chondroitin sulfate hydrogels.

In vitro and in vivo release of the theophylline, loaded in mixed polysaccharidic cellulose/chondroitin sulfate (C/CS) hydrogels has been evaluated. The C/CS hydrogels in various mixing ratios obtained by a crosslinking technique were supplementary characterized by swelling studies in a pH 2.2 acidic solution at 37 °C, simulating the gastrointestinal medium, as in vivo theophylline delivery was done by oral administration. The hydrogels loading degree with theophylline was evaluated by near infrared chemical imaging (NIR-CI) technique and confirmed also by FT-IR spectroscopy. Based on PLS-DA (partial least squares-discriminate analysis) prediction, the drug loading was found up to 92.5%. The in vitro release profiles of theophylline from C/CS hydrogels showed that an increase of chondroitin sulfate leads to a decreased theophylline percent released, increased half release time and time to reach maximum percent released. During in vivo test, the raw theophylline was rapidly, absorbed, distributed, and eliminated. Comparatively with raw drug administration, the t1/2 and AUC0-72 value were 4 times higher for theophylline loaded into 50/50 C/CS hydrogel. A good in vitro-in vivo correlation was found. A retarded release, controlled by CS content can be achieved by using mixed hydrogels as carriers.

Hydrogels based on chitosan-xanthan for controlled release of theophylline.

The aim of this paper is theophylline (THP) inclusion into xanthan-chitosan polyionic complex (Xa-CS) and the study of its in vitro and in vivo kinetic release. Xa-CS hydrogel was obtained by ionic complexation between two oppositely charged polysaccharides. THP was loaded into the Xa-CS matrix by diffusion of the drug solution. The obtained samples were characterized by FTIR spectroscopy, SEM microscopy and study of the swelling behavior. THP in vitro release experiments were carried out in conditions mimicking the gastrointestinal environment. The chosen drug dose for in vivo study was 15 mg THP/Kg body weight of THP powder or an equivalent dose in complex form. THP serum concentrations were determined by an HPLC assay. The THP peak serum concentration (C(max)) was 7.18 microg/ml for free THP and AUC(0-48) was 25.76 microg h/ml, while in the case of Xa-CS-THP, C(max) was of 5.72 microg/ml and AUC(0-48) = 45.72 microg h/ml. The in vivo study regarding the behaviour of the obtained formulation, showed an increase bioavailability of THP compared to the raw drug, suggesting the possible application of the complex Xa-CS as an oral controlled drug delivery system in the management of chronic pulmonary obstructive disease.

Tannic acid incorporation in chitosan-based microparticles and in vitro controlled release.

Chitosan, a natural polycationic polysaccharide, was coupled with two polyanionic polymers: Na-alginate and carboxymethylcellulose (CMC) and with tannic acid (TA) obtaining three species of self-assembled complexes: chitosan/alginate/TA (sample 1), chitosan/TA (sample 2) and chitosan/CMC/TA (sample 3). The microparticle formation was achieved by dropwise addition of one solution into other by using a coaxial airflow sprayer. These systems were characterized with regard to particle size distribution, thermal stability, tannic acid entrapment efficiency. Sample 2 showed quite a different behavior compared to the other two samples; the particle diameter is located in the nanometric region, the quantity of incorporated tannic acid is higher than in the other two samples and the material shows better thermal stability. The release of tannic acid from these complexes was studied in water (pH = 5.89), phosphates buffer (pH = 7.04) and acetate buffer (pH = 4.11). These studies revealed two distinct periods in tannic acid delivery process: an initial period, varying between 4 and 10 h, characterized by a high release rate with a delivered tannic acid amount of approximately 80% of the incorporated polyphenol and a second period, which starts after 20 to 30 h of delivery and it ends after approximately 120 h, when the release process takes place with low and constant rate and the kinetic curve is linear--characteristic for a zero order kinetic.