Thermal energy and tableting effects in benznidazole product: the impacts of industrial processing.

Objective: The investigation of benznidazole (BZN), excipients, and tablets aims to evaluate their thermal energy and tableting effects. They aim to understand better the molecular and pharmaceutical processing techniques of the formulation.

Significance: The Product Quality Review, part of Good Manufacturing Practices, is essential to highlight trends and identify product and process improvements.

Effect of polyvinyl alcohol and carboxymethylcellulose on the technological properties of fish gelatin films.

The objective of this work was to develop biodegradable films by mixing gelatin/carboxymethylcellulose (FG/CMC) and gelatin/polyvinyl alcohol (FG/PVOH) and to evaluate the effect of adding these polymers on the properties of fish gelatin films. The films FG/CMC and FG/PVOH were produced in the proportions 90/10, 80/20 and 70/30 and characterized their physical, chemical and functional properties. The addition of CMC and PVOH improved the mechanical strength, barrier property and water solubility of gelatin films.

Encapsulation of safflower oil in nanostructured lipid carriers for food application.

Unlabelled: Safflower oil (SO) is mainly rich in linoleic acid (ω-6), oleic acid (ω-9), and other bioactives with potential antioxidant, antidiabetic, thermogenic, anti-inflammatory, cardioprotective and anticancer activities. The reduced aqueous solubility and high susceptibility to oxidative degradation are undesirable for food applications and can be overcome by incorporation in lipid nanoparticles. Thus, the main goal was to develop and characterize SO-loaded nanostructured lipid carriers (NLC-SO) and to evaluate their potential for protection of the antioxidant activity of the bioactive.

Thermal Stability Kinetics and Shelf Life Estimation of the Redox-Active Therapeutic and Mimic of Superoxide Dismutase Enzyme, Mn(III) -Tetrakis(-ethylpyridinium-2-yl)porphyrin Chloride (MnTE-2-PyPCl, BMX-010).

Mn(III) -tetrakis(-ethylpyridinium-2-yl)porphyrin chloride (MnTE-2-PyPCl, BMX-010, and AEOL10113) is among the most studied superoxide dismutase (SOD) mimics and redox-active therapeutics, being currently tested as a drug candidate in a phase II clinical trial on atopic dermatitis and itch. The thermal stability of active pharmaceutical ingredients (API) is useful for estimating the expiration date and shelf life of pharmaceutical products under various storage and handling conditions. The thermal decomposition and kinetic parameters of MnTE-2-PyPCl were determined by thermogravimetry (TG) under nonisothermal and isothermal conditions.

Effect of the incorporation of lignin microparticles on the properties of the thermoplastic starch/pectin blend obtained by extrusion.

The present study aimed to produce thermoplastic starch films with different concentrations of thermoplastic pectin and the addition of 4% lignin microparticles as a reinforcing and active agent. The pectin improved the modulus of elasticity, and decreased the elongation at break. In addition, it improved the UV light protection to 100% at 320 nm and 95.

Novel self-nanoemulsifying drug-delivery system enhances antileukemic properties of all- retinoic acid.

All- retinoic acid (ATRA) shows erratic oral bioavailability when administered orally against leukemia, which can be solved through its incorporation in self-nanoemulsifying drug-delivery systems (SEDDS). The SEDDS developed contained a hydrophobic ion pair between benzathine (BZT) and ATRA and was enriched with tocotrienols by the input of a palm oil tocotrienol rich fraction (TRF) in its composition. SEDDS-TRF-ATRA-BZT allowed the formation of emulsions with nanometric size that retained ATRA within their core after dispersion.

Chitosan/hydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment: In vitro and in vivo evaluation.

Eye drops containing hydrophilic drugs are commonly used to reduce intraocular pressure (IOP) in glaucoma patients, but compliance to the treatement is commonly reduced by frequent dosing and eventual systemic side effects. Sustained-release drug delivery systems, such as ocular inserts, can reduce dosing, limit systemic exposure, reduce side effects, and, then, improve patient adherence to therapy. Here, we developed and evaluated chitosan/hydroxyethyl cellulose-based ocular inserts for sustained release of dorzolamide, a hydrophilic drug.

Sclareol is a potent enhancer of doxorubicin: Evaluation of the free combination and co-loaded nanostructured lipid carriers against breast cancer.

Aims: In this work, it was sought to determine if there was synergism between doxorubicin (DOX), a well-known antineoplastic, and sclareol (SC), a diterpene from natural origin, in breast cancer treatment. Moreover, it was investigated if their co-loading in the same nanocarrier would result in a gain of activity and/or a toxicity diminishment.

Main Methods: The synergism of the DOX:SC combination was evaluated in MDA-MB-231 and 4T1 cells.

β-Cyclodextrin inclusion complexes with essential oils: Obtention, characterization, antimicrobial activity and potential application for food preservative sachets.

The current study aimed obtaining antimicrobial sachets that could be used as preservatives for foods. Basil (BEO) and Pimenta dioica (PDEO) essential oils (EOs) were analyzed by GC-FID and GC-MS and tested against the foodborne bacteria S. aureus, E.

Polymorphic characterization and implications on biopharmaceutics properties of potential anti-inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica).

Objectives: To perform the polymorphic and physicochemical characterization of the potential anti-inflammatory drug, eremantholide C (EREC), as well as to evaluate the influence of these characteristics on its biopharmaceutics classification.

Methods: Eremantholide C was obtained from chloroformic extract of Lychnophora trichocarpha and crystallized in two distinct solvents: chloroform (EREC 1) and ethyl acetate (EREC 2). To evaluate the polymorphism, EREC samples were submitted to melting point, purity, infrared spectroscopy, differential scanning calorimetry (DSC), X-ray powder diffraction, optical microscopy and scanning electron microscopy analysis.

Polymorphic and Quantum Chemistry Characterization of Candesartan Cilexetil: Importance for the Correct Drug Classification According to Biopharmaceutics Classification System.

The recommended method for the biopharmaceutical evaluation of drug solubility is the shake flask; however, there are discrepancies reported about the solubility of certain compounds measured with this method, one of them is candesartan cilexetil. The present work aimed to elucidate the solubility of candesartan cilexetil by associating others assays such as stability determination, polymorphic characterization and in silico calculations of intrinsic solubility, ionized species, and electronic structures using quantum chemistry descriptors (frontier molecular orbitals and Fukui functions). For the complete biopharmaceutical classification, we also reviewed the permeability data available.

Physics, chemistry, and Hirshfeld surface analyses of gamma-irradiated thalidomide to evaluate behavior under sterilization doses.

Thalidomide was indicated as a sedative and antiemetic and prescribed for pregnant women. Its tragic teratogenic effects culminated in withdrawal from the market. Since the discovery of its anti-angiogenic and anti-inflammatory actions, thalidomide has been used in the treatment of leprosy and multiple myeloma, which justify studies of its stability.

Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples.

Meloxicam (MLX) is an anti-inflammatory drug susceptible to variations and crystalline transitions. In compounding pharmacies, the complete crystallographic evaluation of the raw material is not a routine procedure. We performed a complete crystallographic characterization of aleatory raw MLX samples from compounding pharmacies.

Properties of spray-dried fish oil with different carbohydrates as carriers.

This study evaluated the application of cashew gum, Arabic gum and starch on physical and thermal properties, and fatty acid profiles of spray-dried fish oil. A completely randomized design was used to evaluate the influence of the type of material on the properties of the microparticles. Hygroscopicity and solubility was higher for particles produced using cashew gum and reached 15 g/100 g and 85 g/100 g, respectively.

Drug-excipient compatibility assessment of solid formulations containing meloxicam.

Meloxicam (MLX) is a non-steroidal anti-inflammatory cyclooxygenase (COX) inhibitor that is used to relieve inflammation and pain. MLX has a preferential affinity for COX-2, which is associated with a lower incidence of gastrointestinal side effects. The drug belongs to Class II of the Biopharmaceutical Classification System (BCS) in which dissolution is the limiting step of its bioavailability.

Prebiotic Carbohydrates: Effect on Reconstitution, Storage, Release, and Antioxidant Properties of Lime Essential Oil Microparticles.

The aim of this study was to include prebiotic biopolymers as wall material in microparticles of lime essential oil. Whey protein isolate (WPI), inulin (IN), and oligofructose (OL) biopolymers were used in the following combinations: WPI, WPI/IN (4:1), and WPI/OL (4:1). The emulsion droplets in the presence of inulin and oligofructose showed larger sizes on reconstitution.

Effect of replacement of corn starch by whey protein isolate in biodegradable film blends obtained by extrusion.

The aim of this study was to evaluate the effect of replacing corn starch by whey protein isolated (WPI) in biodegradable polymer blends developed by extrusion. X-ray diffraction showed the presence of a Vh-type crystalline arrangement. The films were homogeneous, indicating strong interfacial adhesion between the protein and the thermoplastic starch matrix (TPS) as observed in scanning electron microscopy.

Cashew gum and inulin: New alternative for ginger essential oil microencapsulation.

This study aimed to evaluate the effect of partial replacement of cashew gum by inulin used as wall materials, on the characteristics of ginger essential oil microencapsulated by spray drying with ultrasound assisted emulsions. The characterization of particles was evaluated as encapsulation efficiency and particle size. In addition, the properties of the microcapsules were studied through FTIR analysis, adsorption isotherms, thermal gravimetric analysis, X-ray and scanning electron microscopy.

α-Tocopherol succinate improves encapsulation and anticancer activity of doxorubicin loaded in solid lipid nanoparticles.

This work aimed to develop solid lipid nanoparticles (SLN) co-loaded with doxorubicin and α-tocopheryl succinate (TS), a succinic acid ester of α-tocopherol that exhibits anticancer actions, evaluating the influence of TS on drug encapsulation efficiency. The SLN were characterized for size, zeta potential, entrapment efficiency (EE), and drug release. Studies of in vitro anticancer activity were also conducted.

Anti-Toxoplasma activity and impact evaluation of lyophilization, hot molding process, and gamma-irradiation techniques on CLH-PLGA intravitreal implants.

Intraocular delivery systems have been developed to treat many eye diseases, especially those affecting the posterior segment of the eye. However, ocular toxoplasmosis, the leading cause of infectious posterior uveitis in the world, still lacks an effective treatment. Therefore, our group developed an intravitreal polymeric implant to release clindamycin, a potent anti-Toxoplasma antibiotic.

Solid Lipid Nanoparticles Loaded with Retinoic Acid and Lauric Acid as an Alternative for Topical Treatment of Acne Vulgaris.

Topical therapy is the first choice for the treatment of mild to moderate acne and all-trans retinoic acid is one of the most used drugs. The combination of retinoids and antimicrobials is an innovative approach for acne therapy. Recently, lauric acid, a saturated fatty acid, has shown strong antimicrobial activity against Propionibacterium acnes.

Ocular Inserts for Sustained Release of the Angiotensin-Converting Enzyme 2 Activator, Diminazene Aceturate, to Treat Glaucoma in Rats.

The aim of this study was to develop and evaluate the effects of chitosan inserts for sustained release of the angiotensin-converting enzyme 2 (ACE2) activator, diminazene aceturate (DIZE), in experimental glaucoma. Monolayer DIZE loaded inserts (D+I) were prepared and characterized through swelling, attenuated total reflectance Fourier transformed infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and in vitro drug release. Functionally, the effects of D+I were tested in glaucomatous rats.

Accumulation and oxidation of elemental mercury in tropical soils.

The role of chemical and mineralogical soil properties in the retention and oxidation of atmospheric mercury in tropical soils is discussed based on thermal desorption analysis. The retention of gaseous mercury by tropical soils varied greatly both quantitatively and qualitatively with soil type. The average natural mercury content of soils was 0.

Quality evaluation of pharmaceutical formulations containing hydrochlorothiazide.

Hydrochlorothiazide is a diuretic used to treat hypertension that belongs to class IV of the Biopharmaceutics Classification System. The drug was evaluated by quality control, thermal characterization tests, and pharmaceutical formulation compatibility studies. It was concluded that the generic drug, Lab 2, was not a pharmaceutical equivalent.

Bimatoprost-loaded ocular inserts as sustained release drug delivery systems for glaucoma treatment: in vitro and in vivo evaluation.

The purpose of the present study was to develop and assess a novel sustained-release drug delivery system of Bimatoprost (BIM). Chitosan polymeric inserts were prepared using the solvent casting method and characterized by swelling studies, infrared spectroscopy, differential scanning calorimetry, drug content, scanning electron microscopy and in vitro drug release. Biodistribution of 99mTc-BIM eye drops and 99mTc-BIM-loaded inserts, after ocular administration in Wistar rats, was accessed by ex vivo radiation counting.