Preparation and Characterization of Natamycin Loaded Bioadhesive inSituOphthalmic Gel for Enhanced Bioavailability

P. Verma, Vandana Gupta, Ashish Manigauha
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Abstract

Natamycin, an antifungal agent that has been approved in the management of exteriorfungal infectionsof the oculus such asfungal keratitis,blepharitis, and conjunctivitis. The ophthalmic preparation needs frequent installation into the eye due to the quickprecorneldrugloss which may lead to poor bioavailability. The present investigation aimed at formulation development and characterization of in situophthalmic gel of natamycin by using a blend polymer of sodium alginate, ethylcellulose, and Xanthan gum for better residence time to improvethe bioavailability of the drug. The six different formulations (F1 to F6) of natamycin in situgel were prepared. All the formulations were evaluated for clarity, visual appearance, pH, gelling capacity, drug content, drug release, release kinetic, ocular irritancy, and in vitro stability. The results were found to have complied with the pharmacopoeial specification. The in vitrodrug releases of F3 formulation established maximum drug release for 8 h as compared to other formulations in sustained manner.Further, the F3 formulation was found to be stable, safe and innocuous. The studies suggested that prepared in situophthalmic gel of natamycin will be a valuable alternative to conventional eye drops to counter the precorneal loss.
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纳他霉素负载眼凝胶生物胶粘剂的制备及表征
纳他霉素,一种抗真菌药物,已被批准用于治疗眼膜外真菌感染,如真菌性角膜炎、眼咽炎和结膜炎。由于眼用制剂的药前光泽度快,需要频繁地植入眼内,导致生物利用度差。本研究采用海藻酸钠、乙基纤维素和黄原胶共混聚合物制备纳他霉素眼用凝胶,以延长其停留时间,提高药物的生物利用度。制备了纳他霉素在情境凝胶中的6种不同配方(F1 ~ F6)。对所有制剂进行清晰度、外观、pH、胶凝量、药物含量、药物释放、释放动力学、眼刺激性和体外稳定性评价。结果符合药典标准。与其他制剂相比,F3制剂的体外释药时间最长可达8 h。此外,F3配方稳定、安全、无害。研究表明,纳他霉素在眼内凝胶中的制备将是一种有价值的替代传统滴眼液来对抗角膜前缺损的方法。
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