G Dehghan Mohamed Hassan, Marzuka Marzuka
Department of Pharmaceutics, Maulana Azad Educational Trust's, Y. B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, Aurangabad-431001(M.S.), India.
Iran J Pharm Res. 2014 Summer;13(3):769-84.
The objective of this investigation was the development of chitosan/xanthan polyelectrolyte complex based mucoadhesive nasal insert of promethazine hydrochloride a drug used in the treatment of motion sickness. A 3(2) factorial design was applied for preparing chitosan/xanthan polyelectrolyte complex and to study the effect of independent variables i.e. concentration of xanthan [X1] and concentration of chitosan [X2] on various responses i.e. viscosity of polyelectrolyte complex solution, water uptake of nasal inserts (at pH 2, 5.5, 7.4), bioadhesion potential of nasal inserts and in-vitro drug release at Q6h through nasal inserts. FTIR and DSC analysis were carried out to confirm complex formation and on loaded and unloaded nasal insert to investigate any drug excipient interaction. The nasal inserts were also characterized by powder X-ray diffractometry (PXRD) and Scanning electron microscopy (SEM) and for ex-vivo permeation studies. The results show that higher amount of xanthan in polyelectrolyte complexes with respect to higher amount of chitosan retarded in-vitro drug release. The water uptake behaviour of nasal insert was strongly influenced by pH of the medium and by polycation/ polyanion concentration. The investigation verifies the formation of polyelectrolyte complexes formation between chitosan and xanthan at pH values in the vicinity of pKa intervals of the two polymers and confirms their potential for the nasal delivery of promethazine hydrochloride.
本研究的目的是开发一种基于壳聚糖/黄原胶聚电解质复合物的盐酸异丙嗪粘膜粘附性鼻腔插入剂，盐酸异丙嗪是一种用于治疗晕动病的药物。采用3(2)析因设计来制备壳聚糖/黄原胶聚电解质复合物，并研究自变量即黄原胶浓度[X1]和壳聚糖浓度[X2]对各种响应的影响，这些响应包括聚电解质复合物溶液的粘度、鼻腔插入剂的吸水率（在pH 2、5.5、7.4条件下）、鼻腔插入剂的生物粘附潜力以及在6小时时通过鼻腔插入剂的体外药物释放。进行傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）分析以确认复合物的形成，并对载药和未载药的鼻腔插入剂进行分析以研究药物与辅料之间的相互作用。还通过粉末X射线衍射（PXRD）和扫描电子显微镜（SEM）对鼻腔插入剂进行表征，并进行离体渗透研究。结果表明，在聚电解质复合物中，相对于较高含量的壳聚糖，较高含量的黄原胶会延迟体外药物释放。鼻腔插入剂的吸水行为受到介质pH值和聚阳离子/聚阴离子浓度的强烈影响。该研究验证了在两种聚合物的pKa区间附近的pH值下壳聚糖和黄原胶之间形成聚电解质复合物，并证实了它们用于鼻腔递送盐酸异丙嗪的潜力。
