Preparation of PLGA/Rose Bengal colloidal particles by double emulsion and layer-by-layer for breast cancer treatment.

The use of colloidal particles (CPs) in the transport of drugs is developing rapidly thanks to its effectiveness and biosafety, especially in the treatment of various types of cancer. In this study Rose Bengal/PLGA CPs synthesized by double emulsion (W/O/W) and by electrostatic adsorption (layer-by-layer), were characterized and evaluated as potential breast cancer treatment. CPs were evaluated in terms of size, zeta potential, drug release kinetics and cell viability inhibition efficacy with the triple negative breast cancer cell line HCC70. The results showed that both types of CPs can be an excellent alternative to conventional cancer treatment by taking advantage of the enhanced permeation and retention (EPR) effect, manifested by solid tumors; however, the double emulsion CPs showed more suitable delivery times of up to 60% within two days, while layer-by-layer showed fast release of 50% in 90 min. Both types of CPs were capable to decrease cell viability, which encourage us to further testing in in vivo models to prove their efficacy and feasible use in the treatment of triple negative breast cancer.

Zidovudine-poly(L-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process.

A supercritical antisolvent (SAS) process for obtaining zidovudine-poly(L-lactic acid) (PLLA) solid dispersions (SDs) was used to attain a better intestinal permeation of this drug. A 3(2) factorial design was used, having as independent variables the ratio 3'-azido-2'3'-dideoxythymidine (AZT)-PLLA and temperature/pressure conditions, as dependent variables the process yield and particle macroscopic morphology. AZT-PLLA production batches were carried out by the SAS process, and the resulting products evaluated via scanning electron microscope, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared analyses. From the nine possible combinations of tests performed experimentally, only one combination did not produced a solid. The L3 batch of SD, produced with 1:2 (AZT-PLLA) ratio, resulted in a 91.54% yield, with 40% AZT content. Intestinal permeability studies using the AZT-PLLA from L3 batch led to an AZT permeability of approximately 9.87%, which was higher than that of pure AZT (∼3.84%). AZT remained in crystalline form, whereas PLLA remained in semicrystalline form. AZT release is controlled by a diffusion mechanism. It has been demonstrated that it is possible to use PLLA carrier and SAS process to obtain SD, in a single step.

Delivery of phytochemicals of tropical fruit by-products using poly (DL-lactide-co-glycolide) (PLGA) nanoparticles: synthesis, characterization, and antimicrobial activity.

Nanoencapsulation offers great potential in natural compounds delivery as it protects them from degradation, improves their aqueous solubility, and delivers active compounds to the action site. Poly (dl-lactide-co-glycolide) (PLGA) nanoparticles of acerola, guava, and passion fruit by-product extracts were synthesized using the emulsion-evaporation method. PLGA with different lactide to glycolide (50:50 and 65:35) ratios were used to determine how polymer composition affected nanoparticles properties and antimicrobial efficiency. Controlled release experiments showed an initial burst followed by a slower release rate for all encapsulated fruit by-products inside PLGA matrix. Nanoparticle properties were more dependent on by-product extract than on PLGA type. Fruit by-products and their nanoparticles were analyzed for antimicrobial activity against Listeria monocytogenes Scott A and Escherichia coli K12. All fruit by-products encapsulated in PLGA inhibited both bacteria at lower (P<0.05) concentration than corresponding unencapsulated fruit by-product. Both PLGA types improved fruit by-products delivery to pathogens and enhanced antimicrobial activity.

Development of biodegradable flexible films of starch and poly(lactic acid) plasticized with adipate or citrate esters.

Biodegradable films were produced from blends contained a high amount of thermoplastic starch (TPS) and poly(lactic acid) (PLA) plasticized with different adipate or citrate esters. It was not possible to obtain pellets for the production of films using only glycerol as a plasticizer. The plasticization of the PLA with the esters and mixture stages added through extrusion was critical to achieve a blend capable of producing films by blow extrusion. Adipate esters were the most effective plasticizers because they interacted best with the PLA and yielded films with appropriate mechanical properties.

Enzymatic synthesis of poly-L-lactide and poly-L-lactide-co-glycolide in an ionic liquid.

The syntheses of poly-L-lactide (PLLA) and poly-L-lactide-co-glycolide (PLLGA) is reported in the ionic liquid 1-hexyl-3-methylimidazolium hexafluorophosphate [HMIM][PF(6)] mediated by the enzyme lipase B from Candida antarctica (Novozyme 435). The highest PLLA yield (63%) was attained at 90 degrees C with a molecular weight (M(n)) of 37.8 x 10(3) g/mol determined by size exclusion chromatography. This procedure produced relatively high crystalline polymers (up to 85% PLLA) as determined by DSC. In experiments at 90 degrees C product synthesis also occurred without biocatalyst, however, PLLA synthesis in [HMIM][PF(6)] at 65 degrees C followed only the enzymatic mechanism as ring opening was not observed without the enzyme. In addition, the enzymatic synthesis of PLLGA is first reported here using Novozyme 435 biocatalyst with up to 19% of lactyl units in the resulting copolymer as determined by NMR. Materials were also characterized by TGA, MALDI-TOF-MS, X-ray diffraction, polarimetry and rheology.

Chemical synthesis and in vitro biocompatibility tests of poly (L-lactic acid).

Polylactic acid is a polymer of great technological interest, whose excellent mechanical properties, thermal plasticity, and bioresorbability render it potentially useful for environmental applications, as a biodegradable plastic and as a biocompatible material in biomedicine. This article discusses the synthesis and characterization of poly-L-lactic acid, obtained through two synthetic routes: direct polycondensation reactions without organic solvents, and in a supercritical medium. Tin complexes were used as catalysts in both polymerization reactions. The polymers were characterized by (1)HNMR, IR, GPC, DSC, and TGA techniques. In vitro biocompatibility tests were performed with human alveolar bone osteoblasts and there were assessed cell adhesion, proliferation and viability. The poly condensation reaction proved to be an excellent synthetic route to produce PLA polymers with different molar mass. The formation of polymers from lactic acid monomer was confirmed through techniques utilized. It was observed that cell adhesion and viability was not disturbed by the presence of the polymer, although the proliferation rate was decreased when compared to control.

Avaliaçäo da taxa de dissoluçäo de hidroxiapatias preparadas em diferentes condiçöes / Evaluation of dissolution rate of hidroxyapatite prepared in different conditions

A solubilidade dos vários compostos da família dos fosfatos de cálcio no meio fisiológico é uma das principais características utilizadas para a escolha do composto mais adequado para cada aplicação. Para um mesmo composto, entretanto, a solubilidade pode variar devido a variação da concentração de defeitos, a área superficial. a razão Ca/P, o tamanho de particulas, outros tipos e quantidade de fases presentes e porosidade. O objetivo do presente trabalho foi estudar um método que permite avaliar comparativamente a solubilidade de hidroxiapatitas com caracteristicas diferentes. Os resultados obtidos demonstram a eficácia do método proposto para avaliar a solubilidade da hidroxiapatita e confirmam a interrelação entre a solubilidade, a razão Ca/P e a presença de grupos CO3**-2 detectada pela espectroscopia de infravermelho

Abstract - The solubility of the various compounds of the calcium phosphate family in the physiological medium is one of the main characteristics used to identify the most suitable compound for each application. However. for one single compound the solubility may vary due to the concentration of defects. The objective of this work was to develop a method which would allow us to evaluate comparatively the solubility of hydroxyapatites with different characteristics. The results obtained have shown that the proposed method is suitable to evaluate the solubility of hydroxyapatite and have confirmed the relationship between solubility, the Ca/P ratio and the presence of CO/ groups detected by infrared spectroscopy