Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad, Pakistan.
Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad, Pakistan.
J Food Drug Anal. 2018 Apr;26(2):887-902. doi: 10.1016/j.jfda.2017.02.006. Epub 2017 Mar 21.
The purpose of this study was to fabricate a triple-component nanocomposite system consisting of chitosan, polyethylene glycol (PEG), and drug for assessing the application of chitosan-PEG nanocomposites in drug delivery and also to assess the effect of different molecular weights of PEG on nanocomposite characteristics. The casting/solvent evaporation method was used to prepare chitosan-PEG nanocomposite films incorporating piroxicam-β-cyclodextrin. In order to characterize the morphology and structure of nanocomposites, X-ray diffraction technique, scanning electron microscopy, thermogravimetric analysis, and Fourier transmission infrared spectroscopy were used. Drug content uniformity test, swelling studies, water content, erosion studies, dissolution studies, and anti-inflammatory activity were also performed. The permeation studies across rat skin were also performed on nanocomposite films using Franz diffusion cell. The release behavior of films was found to be sensitive to pH and ionic strength of release medium. The maximum swelling ratio and water content was found in HCl buffer pH 1.2 as compared to acetate buffer of pH 4.5 and phosphate buffer pH 7.4. The release rate constants obtained from kinetic modeling and flux values of ex vivo permeation studies showed that release of piroxicam-β-cyclodextrin increased with an increase in concentration of PEG. The formulation F10 containing 75% concentration of PEG showed the highest swelling ratio (3.42±0.02) in HCl buffer pH 1.2, water content (47.89±1.53%) in HCl buffer pH 1.2, maximum cumulative drug permeation through rat skin (2405.15±10.97 μg/cm) in phosphate buffer pH 7.4, and in vitro drug release (35.51±0.26%) in sequential pH change mediums, and showed a significantly (p<0.0001) higher anti-inflammatory effect (0.4 cm). It can be concluded from the results that film composition had a particular impact on drug release properties. The different molecular weights of PEG have a strong influence on swelling, drug release, and permeation rate. The developed films can act as successful drug delivery approach for localized drug delivery through the skin.
本研究的目的是制备由壳聚糖、聚乙二醇（PEG）和药物组成的三组分纳米复合体系，以评估壳聚糖-PEG 纳米复合材料在药物传递中的应用，并评估不同分子量的 PEG 对纳米复合材料特性的影响。采用浇铸/溶剂蒸发法制备了载有吡罗昔康-β-环糊精的壳聚糖-PEG 纳米复合薄膜。为了表征纳米复合材料的形貌和结构，采用 X 射线衍射技术、扫描电子显微镜、热重分析和傅里叶传输红外光谱。还进行了药物含量均匀度试验、溶胀研究、水分含量、侵蚀研究、溶解研究和抗炎活性。还通过 Franz 扩散池在纳米复合膜上进行了透皮研究。结果发现，薄膜的释放行为对释放介质的 pH 值和离子强度敏感。与 pH 值为 4.5 的醋酸盐缓冲液和 pH 值为 7.4 的磷酸盐缓冲液相比，在 pH 值为 1.2 的 HCl 缓冲液中，最大的溶胀比和水分含量。从动力学模型得到的释放速率常数和体外渗透研究的通量值表明，随着 PEG 浓度的增加，吡罗昔康-β-环糊精的释放增加。在 pH 值为 1.2 的 HCl 缓冲液中，含有 75%浓度 PEG 的配方 F10 表现出最大的溶胀比（3.42±0.02）、最大的水分含量（47.89±1.53%）、在 pH 值为 7.4 的磷酸盐缓冲液中，大鼠皮肤中最大的累积药物渗透量（2405.15±10.97μg/cm）和在连续 pH 变化介质中的体外药物释放（35.51±0.26%），并表现出显著（p<0.0001）更高的抗炎效果（0.4cm）。结果表明，薄膜组成对药物释放性质有特殊影响。不同分子量的 PEG 对溶胀、药物释放和渗透速率有很强的影响。所开发的薄膜可以作为通过皮肤局部给药的成功药物传递方法。
