pH-sensitive liposomes have been designed to deliver active compounds, specifically to acidic intracellular organelles, and to augment their cytoplasmic concentrations. These systems combine the protective effects of other liposomal formulations with specific environment-controlled drug release. They are stable at physiological pH, but abruptly discharge their contents when endocytosed into acidic compartments, allowing the drug to be released before it is exposed to the harsh environment of the lysosomes.
View Article and Find Full Text PDFIn this work, we propose pharmaceutical textiles imprinted with lipid microparticles of Econazole nitrate (ECN) as a mean to improve patient compliance while maintaining drug activity. Lipid microparticles were prepared and characterized by laser diffraction (3.5±0.
View Article and Find Full Text PDFThe purpose of this study was to evaluate in vivo a targeted pH-sensitive liposomal formulation tailored to promote the efficient intracellular delivery of 1-beta-d-arabinofuranosylcytosine (ara-C) to human myeloid leukemia cells. Specifically, pH-sensitive immunoliposomes were obtained by anchoring a copolymer of dioctadecyl, N-isopropylacrylamide and methacrylic acid in bilayers of PEGylated liposomes (LP) and by coupling the whole anti-CD33 monoclonal antibody (mAb) or its Fab' fragments. Their pharmacokinetic and biodistribution profiles were assessed in Balb/c and leukemic HL60-bearing immunodepressed (SCID) mice.
View Article and Find Full Text PDFpH-sensitive liposomes have been designed to deliver active compounds, specifically to acidic intracellular organelles and to augment their cytoplasmic concentrations. These systems combine the protective effects of other liposomal formulations with specific environment-controlled drug release. They are stable at physiological pH, but abruptly discharge their contents when endocytosed into acidic compartments, allowing the drug to be released before it is exposed to the harsh environment of lysosomes.
View Article and Find Full Text PDFA promising avenue in cancer therapy using liposomal formulations is the combination of site-specific delivery with triggered drug release. The use of trigger mechanisms in liposomes could be relevant for drugs susceptible to lysosomal hydrolytic/enzymatic degradation. Here, we propose a polymeric pH-sensitive liposome system that is designed to release its content inside the endosomes through a polymer structural change following receptor-mediated internalization.
View Article and Find Full Text PDFMethacrylic derivatives of bile acids have been synthesized for use as monomers in dental composites. Polymeric dental materials are known to leach cytotoxic unreacted monomers and degradation products. In this study, the in vitro cytotoxicity of bile acids and their derivatives towards 3T3 fibroblasts has been evaluated by colorimetric MTT assay and compared with that of the common dental monomers BisGMA, UDMA and TEGDMA.
View Article and Find Full Text PDFPurpose: The purpose of this study was to evaluate the ability of poly(ethylene glycol)-coated lipid nanocapsules (LN) to deliver the highly potent hydrophobic anticancer drug docetaxel to solid tumors.
Methods: Docetaxel-loaded nanocapsules (80-120 nm) were produced by a solvent-free phase inversion process and were coated with polyethylene glycol distearoylphosphatidylethanolamine conjugate by a postinsertion step. In vivo studies were conducted in mice bearing subcutaneously implanted C26 colon adenocarcinoma to assess the pharmacokinetics and biodistribution of both the drug and LN.
Spherulites are multilamellar vesicles obtained by shearing a lamellar phase of lipids and surfactants. They consist of concentric bilayers of amphiphiles alternating with layers of aqueous medium in which hydrophilic drugs can be sequestered with high yield. To be useful for drug targeting applications, spherulites should be small and long circulating.
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