4.7 Article

Effect of some physiological and non-physiological compounds on the phase transition temperature of thermoresponsive polymers intended for oral controlled-drug delivery

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INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 222, 期 2, 页码 259-270

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ELSEVIER SCIENCE BV
DOI: 10.1016/S0378-5173(01)00716-5

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poly-N-isopropylacrylamide; thermoresponsive polymers; salts; surfactant; controlled-drug delivery; gastro-intestinal secretions

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Poly-N-isopropylacrylamide (PNIPAAm) thermosensibility makes this polymer a very attractive candidate for controlled drug delivery systems. The polymer possesses a lower critical solution temperature (LCST) which was found to be around 32 degreesC in pure water, but which can be affected by the medium composition, i.e. presence of salts or surfactants. The knowledge of the effects of such substances on the LCST is very important while using PNIPAAm as a controlled drug delivery agent. The influence of a number of physiological and non-physiological salts and surfactants has been studied. The results obtained show that the addition of salts provokes an important decrease of the LCST of the polymer (salting out effect). A strong influence of the valence and of the size of the anions of the halide group was found. As to the surfactants, according to their type and concentration, a decrease or an increase of the LCST or even no effect at all were found. The effect of the GI secretions on the PNIPAAm phase separation temperature is also discussed. (C) 2001 Elsevier Science B.V. All rights reserved.

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