利用天然渗透促进精油外用纳米凝胶作为非甾体抗炎药替诺昔康递送剂的研究进展

Swapnil S Chopade, Esther Gaikwad, N. Patil, A. Manjappa, J. Disouza
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引用次数: 1

摘要

替诺昔康(TNX)是一种有效的非甾体抗炎药(NSAIDs),用于治疗类风湿性关节炎。像其他非甾体抗炎药一样,替诺昔康的缺点是与胃肠道副作用有关。此外,该药物的透皮渗透性较弱,阻碍了经皮给药。本研究的目的是开发一种粒径更小的TNX纳米凝胶,以提高这种抗炎药物的生物利用度,并评估其治疗类风湿性关节炎的潜力。采用改性乳化扩散法制备TNX纳米级分散体,以noveon聚碳酸AA-1为胶凝剂。此外,精油通过与角质层(SC)相互作用增加皮肤渗透。他们被发现是成功地增加皮肤渗透的亲脂和亲水药物。对制备的TNX纳米凝胶进行了流变性、粒径、药物含量、药物释放率和体外扩散研究。通过对制剂流变学特性的研究发现,该制剂的粒径为125.05nm, zeta电位为-8.47mV,药物含量为97.05%,药物释放率为97.40%,药物扩散率为97.42%,pH值为6.2。以noveon多酚AA-1和桉树油为渗透促进剂制备了替诺昔康纳米凝胶,证明其适合作为治疗水肿和类风湿关节炎的典型外用凝胶配方。
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Development of Topical Nanogel as a Promising Delivery of NSAID’s Tenoxicam using Natural Permeation Enhancer Essential Oil (Euckolyptus)
Tenoxicam (TNX) is an effective non-steroidal anti-inflammatory drug (NSAIDs) used to treat rheumatoid arthritis. Like other NSAIDs, tenoxicam has the disadvantage of being linked to gastrointestinal side effects. Furthermore, this drug is having weak transdermal penetration, preventing transdermal administration. The goal of this study was to develop a TNX nanogel with a smaller particle size to improve the anti-inflammatory drug's bioavailability and assess its potential in rheumatoid arthritis. The modified emulsification-diffusion method is used to develop nanosized dispersion of TNX using noveon polycarbophil AA-1 as a gelling agent. Moreover, essential oils increase skin penetration by interacting with the stratum corneum (SC). They were found to be successful in increasing skin penetration of both lipophilic and hydrophilic drugs. The rheology, particle size, drug content, % drug release, and in-vitro diffusion study of prepared TNX nanogel were performed. Based on the rheological features of the formulations it was found to be substantial, with the particle size of 125.05nm and zeta potential -8.47mV, drug content of 97.05%, % drug release 97.40% drug diffusion of 97.42%, and pH of 6.2. Tenoxicam nanogel was prepared by using noveon polycarbophil AA-1 and eucalyptus oil as a permeation enhancer was proven to be suitable as a typical topical gel formulation for the treatment of edema and rheumatoid arthritis.
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