Effect of neutralization degree of methacrylic acid on hydrogel swelling and drug release

Olga Pantic, R. Pjanovic, V. Panic, Sanja I. Savić, P. Spasojevic, Maja D. Markovic
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Abstract

Drug delivery system is an amazing tool which is widely used for drug protection and its controlled release in order to enhance drug bioavailability, reduce side effects and therefore to improve overall therapy. Hydrogels have been attracted great attention as drug carriers due to their great physicochemical properties, similarity to the living tissues and biocompatibility. One group of pH sensitive hydrogels are based on poly(methacrylic acid) (PMAA). These non-toxic hydrogels are used as drug delivery system because they swell as a response to the change in pH of external environment and drug is being released during the process. In present study, in order to improve the control of drug release rate, caffeine was encapsulated in liposomes which were further embedded into PMC hydrogel (PMCL). It was investigated how the change in neutralization degree of methacrylic acid affect the swelling degree of PMCL hydrogels and caffeine release in two environments at 37 °C for 24 h: 0.1 M hydrochloride acid (pH 1) and phosphate buffer with pH value of 6.8 (pH 6.8), as a simulation of pH environment in human stomach and intestines, respectively. Obtained results show that PMCL hydrogels have great potential for controlled release of poorly water-soluble drugs in human intestines.
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甲基丙烯酸中和度对水凝胶溶胀及药物释放的影响
药物传递系统是一种神奇的工具,广泛用于药物保护和控制释放,以提高药物的生物利用度,减少副作用,从而改善整体治疗。水凝胶由于具有良好的物理化学性质、与活体组织的相似性和生物相容性等优点,作为药物载体受到了广泛的关注。一组pH敏感的水凝胶是基于聚甲基丙烯酸(PMAA)。由于这些无毒的水凝胶会随着外界环境pH值的变化而膨胀,并在此过程中释放药物,因此被用作药物输送系统。本研究将咖啡因包封在脂质体中,脂质体再包埋在PMC水凝胶(PMCL)中,以提高对药物释放速度的控制。通过模拟人体胃和肠道的pH环境,研究了在0.1 M盐酸(pH值为1)和pH值为6.8的磷酸盐缓冲液(pH值为6.8)两种环境下,甲基丙烯酸中和度的变化如何影响PMCL水凝胶在37℃、24 h下的溶胀程度和咖啡因释放。所得结果表明,PMCL水凝胶具有很大的潜力,可以在人体肠道中控制低水溶性药物的释放。
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