Dasgupta Sandipan, Ray Subhabrata, Dey Sanjay, Pal Paulami, Mazumder Bhaskar
Department of Pharmacology, NSHM College of Pharmaceutical Technology, Kolkata, 700053, West Bengal. India.
College of Pharmacy & AHS, Durgapur - 713206, West Bengal. India.
Pharm Nanotechnol. 2017;5(1):32-43. doi: 10.2174/2211738505666170105161336.
Lornoxicam, is a NSAID of the oxicam class. Its short duration of action owing to rapid elimination and gastrointestinal side effects limits its usefulness when administered orally.
The primary objective of the proposed work is to develop suitable lipid nanocarriers for transdermal delivery of Lornoxicam with increased drug residence time at local site of inflamation and in systemic circulation, overcoming undesired gastrointestinal side effects.
Lornoxicam loaded lipid nanocarriers like solid lipid nanocarriers (SLN), nano-structured lipid carriers (NLC) & nanoemulsions (NE) were prepared by high-speed homogenization technique.
The particle size, zeta potential, and polydispersity index as obtained, were in the range of 140- 193 nm, -22 to -32 mV, and 0.354-0.301 for SLN formulations and 146-201 nm, -23 to -30 mV, and 0.355-0.354 for NLC formulations respectively. Characterization of stable NE revealed that globule size, zeta potential and polydispersity index were within the range of 138 to 195 nm, -26.1±0.123 mV and 0.195 ± 1.231 respectively. It was also observed that entrapment efficacy and drug loading improved as the lipid concentration was increased. The results obtained from the in vitro permeation study and in vivo anti-inflammatory study showed controlled drug permeation, increased bioavailability, longer retention and better therapeutic potential of Lornoxicam after transdermal application of lipid nanoparticles as compared to conventional gel.
It can be concluded that the developed lipid nanoparticle loaded gel was found to be a suitable drug delivery carrier for transdermal delivery of Lornoxicam to increase the residence time of drug in systemic circulation and to combat the gastrointestinal side effects.
氯诺昔康是一种昔康类非甾体抗炎药。由于其快速消除导致作用时间短,且存在胃肠道副作用,口服给药时其用途受限。
本研究的主要目的是开发合适的脂质纳米载体用于氯诺昔康的经皮给药,以增加药物在炎症局部部位和体循环中的停留时间,克服不良的胃肠道副作用。
采用高速匀质技术制备了载氯诺昔康的脂质纳米载体,如固体脂质纳米粒(SLN)、纳米结构脂质载体(NLC)和纳米乳剂(NE)。
所制备的SLN制剂的粒径、zeta电位和多分散指数分别在140 - 193 nm、-22至-32 mV和0.354 - 0.301范围内;NLC制剂的粒径、zeta电位和多分散指数分别在146 - 201 nm、-23至-30 mV和0.355 - 0.354范围内。稳定的NE的表征显示,其球粒大小、zeta电位和多分散指数分别在138至195 nm、-26.1±0.123 mV和0.195±1.231范围内。还观察到随着脂质浓度的增加,包封率和载药量提高。体外渗透研究和体内抗炎研究结果表明,与传统凝胶相比,经皮应用脂质纳米粒后,氯诺昔康具有可控的药物渗透、提高的生物利用度、更长的滞留时间和更好的治疗潜力。
可以得出结论,所开发的载脂质纳米粒凝胶是氯诺昔康经皮给药的合适药物递送载体,可增加药物在体循环中的停留时间并对抗胃肠道副作用。