Co-Delivery of an Innovative Organoselenium Compound and Paclitaxel by pH-Responsive PCL Nanoparticles to Synergistically Overcome Multidrug Resistance in Cancer.

In this study, we designed the association of the organoselenium compound 5'-Seleno-(phenyl)-3'-(ferulic-amido)-thymidine (AFAT-Se), a promising innovative nucleoside analogue, with the antitumor drug paclitaxel, in poly(ε-caprolactone) (PCL)-based nanoparticles (NPs). The nanoprecipitation method was used, adding the lysine-based surfactant, 77KS, as a pH-responsive adjuvant. The physicochemical properties presented by the proposed NPs were consistent with expectations.

Transferrin-Decorated PLGA Nanoparticles Loaded with an Organoselenium Compound as an Innovative Approach to Sensitize MDR Tumor Cells: An In Vitro Study Using 2D and 3D Cell Models.

Multidrug resistance (MDR) is the main challenge in cancer treatment. In this sense, we designed transferrin (Tf)-conjugated PLGA nanoparticles (NPs) containing an organoselenium compound as an alternative to enhance the efficacy of cancer therapy and sensitize MDR tumor cells. Cytotoxicity studies were performed on different sensitive tumor cell lines and on an MDR tumor cell line, and the Tf-conjugated NPs presented significantly higher antiproliferative activity than the nontargeted counterparts in all tested cell lines.

In vivo and in vitro per se effect evaluation of Polycaprolactone and Eudragit® RS100-based nanoparticles.

Biodegradable polymeric nanocapsules (NC) present incredible characteristics as drug nanocarriers that optimize drug targeting. However, However, a more detailed isolated effect of polymer-based nanoparticles as drug carriers is required. This work aimed to evaluate the per se effect of blank-NC (NC-B) with different surface characteristics both in vitro and in vivo toxicity.

Effect of corn stigma extract on physical and antioxidant properties of biodegradable and edible gelatin and corn starch films.

The development of bio-based food packaging with antioxidant properties is an important research topic and has gained prominence these days. In this study, bioactive films were developed based gelatin-corn starch (GCS) incorporated with corn stigma extract (CSE) at different concentrations (15% and 25%; w/v). In preliminary tests, the extract maintained cell viability above 90% indicating that it is safe for application as an active ingredient.

Overcoming MDR by Associating Doxorubicin and pH-Sensitive PLGA Nanoparticles Containing a Novel Organoselenium Compound-An In Vitro Study.

In this study, we developed PLGA nanoparticles (NPs) as an effective carrier for 5'-Se-(phenyl)-3-(amino)-thymidine (ACAT-Se), an organoselenium compound, nucleoside analogue that showed promising antitumor activity in vitro. The PLGA NPs were prepared by the nanoprecipitation method and modified with a pH-responsive lysine-based surfactant (77KL). The ACAT-Se-PLGA-77KL-NPs presented nanometric size (around 120 nm), polydispersity index values < 0.

Comparative evaluation of the hepatotoxicity, phototoxicity and photosensitizing potential of dronedarone hydrochloride and its cyclodextrin-based inclusion complexes.

In this study, the hepatotoxicity, phototoxicity and photosensitizing potential of free dronedarone (DRO) and its inclusion complexes with β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), prepared by different methods, were investigated by using in vitro cell-based approaches. The results of the 3T3 NRU phototoxicity assay showed that free DRO and the CD-based inclusion complexes did not present any substantial phototoxic potential. The photosensitizing potential was assessed by using THP-1 cells and IL-8 as a biomarker, and the experimental data confirmed that both the free drug and the inclusion complexes are likely to cause skin photosensitization, as they were able to induce IL-8 release after irradiation.

Poly (ɛ-Caprolactone) Nanoparticles with pH-Responsive Behavior Improved the In Vitro Antitumor Activity of Methotrexate.

A promising approach to achieve a more efficient antitumor therapy is the conjugation of the active molecule to a nanostructured delivery system. Therefore, the main objective of this research was to prepare nanoparticles (NPs), with the polymer poly (ε-caprolactone) (PCL), as a carrier for the antitumor drug methotrexate (MTX). A pH-responsive behavior was obtained through conjugation of the amino acid-based amphiphile, 77KL, to the NP matrix.

Preparation, characterization and in vitro cytotoxicity study of dronedarone hydrochloride inclusion complexes.

Dronedarone is a new antiarrhythmic drug for the treatment of atrial fibrillation. This study investigated the complexation of dronedarone hydrochloride with β‑cyclodextrin (β-CD) and 2‑hydroxypropil‑β‑CD (HP-β-CD) using three different techniques. The complexes in the solid state were characterized by DSC, TGA, PXRD, FT-IR, SEM and H NMR, demonstrating the formation of the inclusion complexes and exhibiting different properties from the pure drug.

Investigation of the stabilizing effects of antioxidants and benzophenone-3 on desonide photostability.

Desonide is a topical corticoid used in the treatment of skin diseases and is marketed in different pharmaceutical dosage forms. Recently, the poor photostability of a commercially available hair solution after direct exposure to UVA light was verified. In this study, we investigated the ability of the antioxidants ascorbic acid, butylhydroxyanisole (BHA), butylhydroxytoluene (BHT), α-tocopherol, and the UV filter benzophenone-3 (BP-3) to prevent the photodegradation of desonide in hair solution (desonide 0.

Novel Pullulan-Eudragit® S100 blend microparticles for oral delivery of risedronate: formulation, in vitro evaluation and tableting of blend microparticles.

Polymer blends have been considered a promising strategy to tailor drug release. In order to achieve gastroresistance and controlled release, Pullulan, a polysaccharide, and Eudragit® S100, an enteric polymer were selected to prepare microparticles for oral delivery of risedronate, an antiresorptive drug associated with GI tract injuries. Blend microparticles were prepared by spray-drying technique at 3 Pullulan and Eudragit® S100 ratios (MP2:1, MP1:1 and MP1:2) and were characterized in terms of yield, particle size, encapsulation efficiency, morphology, moisture content, flowability and in vitro drug release profiles.

Development and validation of a stability-indicating LC method for the assay of lodenafil carbonate in tablets.

A stability-indicating liquid chromatographic method has been developed for the quantitative determination of lodenafil carbonate in tablets. The method employs a Synergi Fusion C18 column (250 × 4.6 mm, i.

HPLC determination of bezafibrate in human plasma and its application to pharmacokinetics studies.

An isocratic high-performance liquid chromatographic (HPLC) method was developed and validated for the determination of bezafibrate in biological fluids. Bezafibrate was separated on a C(18) analytical column (150 x 4.6 mm i.

A high-throughput liquid chromatography tandem mass spectrometry method for the comparative determination of fluticasone propionate by reversed-phase liquid chromatography and capillary electrophoresis methods in pharmaceutical nasal sprays.

A simple, specific, rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the analysis of fluticasone propionate (FP) in pharmaceutical formulations was developed and validated using deflazacort as internal standard (IS). The LC-MS/MS method was carried out on a C8 column (50 mm) with a mobile phase consisted of methanol : water (95 : 5, v/v) 100 mM formic acid-50 mM ammonium acetate (90 : 5 : 5, v/v/v). The mass spectrometry method was performed employing positive atmospheric pressure chemical ionization technique, operating in multiple reaction monitoring mode.

Quantitation of nimesulide in human plasma by high-performance liquid chromatography with ultraviolet absorbance detection and its application to a bioequivalence study.

A rapid and simple high-performance liquid chromatography-reversed phase (HPLC-RV) method with ultraviolet detection (258 nm) was developed and validated for the quantitation of nimesulide (CAS 51803-78-2) in human plasma. After the plasma samples were extracted with 6.0 ml of dichloromethane containing the internal standard phenacetin 2 microg/ml in methanol, the analysis of the nimesulide level in the plasma samples was carried out using a reverse phase Supelcosil LC-18 (15 cm x 4.

Validation of the anti-factor IIa assay and potency assessment of enoxaparin in pharmaceutical formulations.

The low molecular weight heparin enoxaparin sodium is used clinically for the prevention and treatment of venous and arterial thrombosis. An anti-factor IIa assay was applied and validated for the potency evaluation of the pharmaceutical formulations. Investigating the parameters of range, linearity (r(2)=0.