Kulkarni Raghavendra V, Sa Biswanath
Department of Pharmaceutical Technology, Center for Advanced Research in Pharmaceutical Sciences, Jadavpur University, Kolkata, India.
Drug Dev Ind Pharm. 2008 Dec;34(12):1406-14. doi: 10.1080/03639040802130079.
Novel pH-sensitive interpenetrating network hydrogel beads of polyacrylamide-grafted-xanthan (PAAm-g-XG) and sodium carboxymethyl cellulose (NaCMC) loaded with ketoprofen were prepared and evaluated for pH sensitivity and drug release characteristics. The pH-sensitive PAAm-g-XG copolymer was synthesized by free radical polymerization under the nitrogen atmosphere followed by alkaline hydrolysis. The grafting and alkaline hydrolysis reactions were confirmed by Fourier transform infrared spectroscopy. Differential scanning calorimetry and X-ray diffraction studies were carried out to know the crystalline nature of encapsulated drug. Scanning electron microscopic study revealed that the interpenetrating polymer network (IPN) beads possess porous matrix structure in alkaline pH whereas nonporous matrix structure was observed in acidic pH. The swelling of the beads and drug release was significantly increased when pH of the medium was changed from acidic to alkaline. The results of pulsatile swelling study indicated that the IPN beads changed their swelling behavior when pH of the external medium was altered. As pH of the medium was changed from 1.2 to 7.4, a considerable increase in swelling was observed for all the beads. However, swelling process was slower than the deswelling. At higher pH values, the carboxyl functional groups of hydrogels undergo ionization and the osmotic pressure inside the beads increases resulting in higher swelling. Drug release followed case II transport mechanism in acidic medium whereas anomalous/non-Fickian transport mechanism was observed in alkaline medium.
制备了负载酮洛芬的新型聚丙烯酰胺接枝黄原胶(PAAm-g-XG)和羧甲基纤维素钠(NaCMC)的pH敏感互穿网络水凝胶珠,并对其pH敏感性和药物释放特性进行了评估。在氮气气氛下通过自由基聚合合成pH敏感的PAAm-g-XG共聚物,随后进行碱水解。通过傅里叶变换红外光谱证实了接枝和碱水解反应。进行差示扫描量热法和X射线衍射研究以了解包封药物的结晶性质。扫描电子显微镜研究表明,互穿聚合物网络(IPN)珠在碱性pH下具有多孔基质结构,而在酸性pH下观察到无孔基质结构。当介质的pH从酸性变为碱性时,珠的溶胀和药物释放显著增加。脉动溶胀研究结果表明,当外部介质的pH改变时,IPN珠改变了它们的溶胀行为。当介质的pH从1.2变为7.4时,所有珠的溶胀都有相当大的增加。然而,溶胀过程比消肿过程慢。在较高的pH值下,水凝胶的羧基官能团发生电离,珠内的渗透压增加,导致更高的溶胀。药物在酸性介质中遵循Ⅱ型转运机制释放,而在碱性介质中观察到异常/非菲克转运机制。