基于泊洛沙姆的盐酸莫西沙星粘膜粘附原位眼用水凝胶的研究

Studies on Poloxamer Based Mucoadhesive Insitu Ophthalmic Hydrogel of Moxifloxacin HCL.

作者信息

Shastri D H, Prajapati S T, Patel L D

机构信息

Department of Pharmaceutics, K. B. Institute of Pharmaceutical Education & Research, Plot No: 126/2, Sector-26, Kishaan Nagar, Gandhinagar, Gujarat, India.

出版信息

Curr Drug Deliv. 2010 Feb 17.

DOI:
Abstract

Conventional eye drops shows relatively low bioavailability due to poor precorneal contact time. In situ hydrogels are of great importance in providing sustained ocular drug delivery due to their elastic properties hydrogels resist ocular drainage 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 combination of poloxamer 407 and poloxamer 188 with different mucoadhesive polymers such as Xanthan gum and Sodium alginate with a view to increase in gel strength and bioadhesion force and thereby increase in precorneal contact time and there by increase in bioavailability of the drug. The formulations were evaluated for physical parameters like Clarity, pH, spreadability, drug content, gelation temperature, gel strength, bioadhesion force and in vitro drug release study. The formulated gels were transparent, uniform in consistency and had spreadability with a pH range of 6.8 to 7.4. A satisfactory bioadhesion (3298 to 4130 Dyne/cm(2)) on the sheep's corneal surface and good gel strength (95 to 128 sec) were also observed. As the concentration of mucoadhesive polymers in the gel formulation increases, the rate of drug release decreases. The order of drug release was Xanthan gum>Sodium alginate. It was concluded that a thermoreversible in situ gel formulation with Moxifloxacin HCl can be formulated by combining with mucoadhesive polymers and can effectively be used in safe and sustained ocular drug delivery with greater bioadhesion force and gel strength as compared to the thermoreversible polymers poloxamer 407 or 188 when used alone.

摘要

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持续递送方面具有重要意义,因为其弹性特性使水凝胶能够抵抗眼部引流,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,旨在提高凝胶强度和生物粘附力,从而增加角膜前接触时间,进而提高药物的生物利用度。对这些制剂进行了物理参数评估,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。所制备的凝胶是透明的,质地均匀,具有铺展性,pH值范围为6.8至7.4。在羊角膜表面还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。得出的结论是,通过与粘膜粘附聚合物组合,可以制备含盐酸莫西沙星的热可逆原位凝胶制剂,与单独使用热可逆聚合物泊洛沙姆407或188相比,该制剂具有更大的生物粘附力和凝胶强度,可有效用于安全、持续的眼部药物递送。

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