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This study aimed to encapsulate the novel synthetic naphthoquinone ENSJ39 in liposomes, characterize them, and evaluate their in vitro cytotoxic activity in different cancer cell lines. Liposomes were obtained by the dried-lipid film hydration method, and characterizations included thermogravimetric analysis, differential scanning calorimetry, dynamic light scattering technique, and atomic force microscopy. Simulation of storage conditions, in vitro cytotoxicity by MTT, Trypan blue exclusion assay, and evaluation of morphological changes in tumor cell lines were also analyzed. Liposomes containing ENSJ39 (LE39) exhibited an average size of 31 ± 5.81 nm, zeta potential of +53.5 mV, polydispersity index of 0.24, and high encapsulation efficiency (96.58 ± 0.09%). They were thermally stable up to 250 °C and able to preserve the mass loss of the free drug. After four months of storage, they maintained excellent physical-chemical characteristics. The encapsulated drug showed less cytotoxic activity than the free drug only in HCT-116 and SNB-19 cells and caused cytoplasmic vacuolization plus an increase in the number of non-viable HCT-116 cells. ENSJ39 encapsulation method was effective in obtaining stable liposomes that presented substantial cytotoxicity activity against tumor cell lines.

The strategy of antiangiogenic drugs is based on inhibiting formation of new blood vessels as alternative to limit cancer progression. In this work, we investigated the antitumor and antiangiogenic potential of eight thalidomide derivatives. Most of the molecules was not cytotoxic but 2a, 2d and 3d revealed weak antiproliferative activity on HL-60, Sarcoma 180 (S180) and normal peripheral blood mononuclear cells. Thalidomide, 2a and 2b were able to inhibit tumor growth (53.5%, 67.9% and 67.4%, respectively) in S180-bearing mice and presented moderate and reversible toxicity on liver, kidneys and spleens. Both analogs (2a and 2b) inhibited cell migration of endothelial (HUVEC) and melanoma cells (MDA/MB-435) at 50μg/mL. Immunohistochemistry labeling assays with CD-31 (PECAM-1) antibody showed microvascular density (MVD) was significantly reduced in thalidomide, 2a and 2b groups (30±4.9, 64.6±1.8 and 46.5±19.5%, respectively) (p

In this study, the cashew gum (Anacardium occidentale Linn) (GCa) and chicha gum (Sterculia striata) (GCh) were characterized and used in the development of tables and hydrogels. For this purpose, the gums were initially characterized by XRD, FTIR, TG, and DSC, and flow property. The tablets obtained were evaluated for hardness, swelling, and mucoadhesiveness, while the hydrogels developed were assessed by texturometric assays. The physicochemical analysis demonstrated that the GCa and GCh gums present microcrystalline and amorphous structures, respectively. Both were classified as fine powders and presented proper flowability and compressibility to the development of tables. The tablets containing GCa and GCh presented mucoadhesion strength of 2.10 ± 0.31 N and 1.72 ± 0.30 N, respectively. Both tablets exhibited similar mucoadhesion behavior to the polymers conventionally used for this purpose, such as the carbomers. However, there was an evident difference in the swelling process, in which the GCa table presented high erosion and low swelling, while the GCh tables presented a crescent and linear swelling behavior and no erosion process in the observed time. GCh hydrogel was the most easily obtained and presented the best thick consistency and adhesion compatible with topical formulations. Thus, based on the results found, we can conclude that both natural polymers are promising excipients in the development of adhesive and control drug delivery formulations.