Preparation and characterization of novel semi-interpenetrating polymer network hydrogel microspheres of chitosan and hydroxypropyl cellulose for controlled release of chlorothiazide
Preparation and characterization of novel semi-interpenetrating polymer network hydrogel microspheres of chitosan and hydroxypropyl cellulose for controlled release of chlorothiazide
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DOI：
10.1080/02652040802109770
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发表时间：
2009-01-01
影响因子：
3.9
通讯作者：
Aminabhavi, T. M.
中科院分区：
文献类型：
--
作者：
Rokhade, A. P.;Kulkarni, P. V.;Aminabhavi, T. M.
以戊二醛（GA）为交联剂，采用乳液交联法制备了壳聚糖（CS）和羟丙基纤维素（HPC）半互穿聚合物网络（IPN）水凝胶微球。氯噻嗪（CT）是一种具有有限水溶性的利尿剂和降压药，成功地被包裹在IPN微球中。通过改变CS与HPC的比例、载药率和GA的用量，制备出不同的制剂。利用傅里叶红外光谱（FTIR）对微球进行了表征，研究了IPN结构的形成，并证实了药物、聚合物和交联剂之间没有化学相互作用。利用扫描电子显微镜（SEM）研究了微球的表面形貌。扫描电镜显示微球表面光滑。通过激光散射技术测量的颗粒大小平均在199-359米之间。用差示扫描量热法（DSC）了解IPN结构的形成。x射线衍射（X-RD）研究了解药物包封成IPN微球后的结晶性质。紫外光谱法测定药物包封率达76%。在0.1 N HCl中进行了平衡和动态膨胀实验。利用经验方程估计了水通过微球的扩散系数(D)。体外释放实验表明，释放速率与交联程度、载药量和制备微球的HPC用量有关；缓释时间延长至12 h。释放数据拟合经验方程，计算扩散指数(n)，表明释放符合非菲克趋势。
Novel semi-interpenetrating polymer network (IPN) hydrogel microspheres of chitosan (CS) and hydroxypropyl cellulose (HPC) were prepared by emulsion-cross-linking method using glutaraldehyde (GA) as a cross-linker. Chlorothiazide (CT), a diuretic and anti-hypertensive drug with limited water solubility, was successfully encapsulated into IPN microspheres. Various formulations were prepared by varying the ratio of CS and HPC, percentage drug loading and amount of GA. Microspheres were characterized by Fourier transform infrared (FTIR) spectroscopy to investigate the formation of IPN structure and to confirm the absence of chemical interactions between drug, polymer and cross-linking agent. Scanning electron microscopy (SEM) was performed to study the surface morphology of the microspheres. SEM showed that microspheres have smooth surfaces. Particle size, as measured by laser light scattering technique, gave an average size ranging from 199-359 m. Differential scanning calorimetry (DSC) was performed to know the formation of IPN structure. X-ray diffraction (X-RD) studies were performed to understand the crystalline nature of the drug after encapsulation into IPN microspheres. Encapsulation of drug up to 76% was achieved as measured by UV spectroscopy. Both equilibrium and dynamic swelling experiments were performed in 0.1 N HCl. Diffusion coefficients (D) for water transport through the microspheres were estimated using an empirical equation. In vitro release studies indicated the dependence of release rate on the extent of cross-linking, drug loading and the amount of HPC used to produce the microspheres; slow release was extended up to 12 h. The release data were also fitted to an empirical equation to compute the diffusional exponent (n), which indicated that the release followed the non-Fickian trend.