Shastri D H, Prajapati S T, Patel L D
Department of Pharmaceutics, K. B. Institute of Pharmaceutical Education&Research, Plot No: 126/2, Sector-26, Kishaan Nagar, Gandhinagar, Gujarat, India-382028.
Curr Drug Deliv. 2010 Jul;7(3):238-43. doi: 10.2174/156720110791560928.
Conventional eye drops show relatively low bioavailability due to poor precorneal contact time. In situ hydrogels are of great importance in providing sustained ocular drug delivery. By exhibiting elastic properties they resist ocular drainage of the drug leading to longer contact times. In the present study an in situ gelling thermoreversible mucoadhesive gel was formulated of an antibacterial agent, Moxifloxacin HCl using a combination of poloxamer 407 and poloxamer 188 with different mucoadhesive polymers such as Xanthan gum and Sodium alginate with a view to increase gel strength and bioadhesion force and thereby increased precorneal contact time and bioavailability of the drug. Formulations were evaluated for physical parameters like clarity, pH, spreadability, drug content, gelation temperature, gel strength, bioadhesion force and in vitro drug release study. Formulations were found transparent, uniform in consistency and had good spreadability within a pH range of 6.8 to 7.4. A satisfactory bioadhesion (3298 to 4130 Dyne/cm2) on the sheeps corneal surface and good gel strength (95 to 128 sec) was also observed. As the concentration of mucoadhesive polymers in the gel formulation increased, the rate of drug release decreased. The order of drug release was in order: Xanthan gum > Sodium alginate. It was concluded that a thermoreversible in situ gel of Moxifloxacin HCl can be formulated by combining with mucoadhesive polymers and used effectively as safe and sustained ocular drug delivery. This combination provided greater bioadhesion force and gel strength as compared to the thermoreversible polymers i.e., poloxamer 407 (PF 127) or 188 (PF 68) when used alone.
由于角膜前接触时间短,传统眼药水的生物利用度相对较低。原位水凝胶在实现眼部药物的持续递送方面具有重要意义。通过展现弹性特性,它们能够阻止药物从眼部排出,从而延长接触时间。在本研究中,使用泊洛沙姆407和泊洛沙姆188与不同的粘膜粘附聚合物(如黄原胶和海藻酸钠)组合,制备了一种原位凝胶化的热可逆粘膜粘附凝胶,其含有抗菌剂盐酸莫西沙星,目的是提高凝胶强度和生物粘附力,从而延长角膜前接触时间并提高药物的生物利用度。对制剂的物理参数进行了评估,如澄清度、pH值、铺展性、药物含量、凝胶化温度、凝胶强度、生物粘附力和体外药物释放研究。发现制剂在pH值6.8至7.4范围内是透明的,质地均匀且具有良好的铺展性。在羊角膜表面也观察到了令人满意的生物粘附力(3298至4130达因/平方厘米)和良好的凝胶强度(95至128秒)。随着凝胶制剂中粘膜粘附聚合物浓度的增加,药物释放速率降低。药物释放顺序为:黄原胶>海藻酸钠。得出结论,盐酸莫西沙星的热可逆原位凝胶可通过与粘膜粘附聚合物组合来制备,并有效地用作安全的眼部持续药物递送。与单独使用的热可逆聚合物即泊洛沙姆407(PF 127)或188(PF 68)相比,这种组合提供了更大的生物粘附力和凝胶强度。
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