NIPAAm-containing amphiphilic block copolymers with tailored LCST: Aggregation behavior,cytotoxicity and evaluation as carriers of indomethacin,tetracycline and doxorubicin |
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Authors: | Lorenzo A Picos-Corrales Melissa Garcia-Carrasco Rocio A Chavez-Santoscoy Sergio O Serna-Saldívar |
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Institution: | 1. Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Sinaloa, Culiacán, México;2. Centro de Graduados e Investigación en Química, Tecnológico Nacional de México/Instituto Tecnológico de Tijuana, Tijuana, México;3. Facultad de Ciencias Químicas e Ingeniería, Universidad Autónoma de Baja California-Campus Tijuana, Tijuana, México;4. Escuela de Biotecnología y Alimentos, Centro de Biotecnología FEMSA, Tecnológico de Monterrey-Campus Monterrey, Monterrey, México |
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Abstract: | Nanocarriers based on amphiphilic block copolymers, with tailored temperature and pH responsiveness, were prepared. The hydrophilic blocks consist of temperature-sensitive N-isopropylacrylamide (NIPAAm)] or NIPAAm plus pH-sensitive units 5-methacryloyloxy pentatonic acid (5MPA) or 4-methacryloyloxy benzoic acid (4MBA)], while the hydrophobic block is composed of n-hexyl acrylate (HA) or styrene (ST). Particle sizes were within the suitable range for the desired application (30–182?nm). Drug loading was achieved via an organic solvent-free method and a THF-buffer method leading to drug loadings of indomethacin, tetracycline and doxorubicin of up to 11, 11 and 60?wt%, respectively. In vitro release kinetics were performed under simulated physiological conditions (pH 7.4 and 37?°C; pH 6.0 and 40?°C) and show differences depending on the copolymer composition. The average kinetic data were well fitted to the mathematical model of Peppas. NIPAAm-containing copolymers were slight or non-cytotoxic for rat primary hepatocytes at concentrations less than 200?µg mL?1. Some of the polymeric aggregates prepared may find application as pharmaceutical carriers. |
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Keywords: | Polymeric drug delivery systems pH-sensitive cytotoxicity nanocapsules doxorubicin |
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