P.D.M. College of Pharmacy, Bahadurgarh, India.
Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.
Int J Pharm. 2014 Apr 25;465(1-2):175-86. doi: 10.1016/j.ijpharm.2014.02.023. Epub 2014 Feb 15.
The objective was to develop a stable, reproducible and patient non-infringing novel transdermal drug delivery system "nano-carrier transdermal gel" (NCTG) in combination of partial dose replacement of diclofenac diethylamine (DDEA) by curcumin (CRM). The drug content of gel was 99.30 and 97.57% for DDEA and CRM. Plasma samples were analyzed by liquid chromatography with triple-quadrupole tandem mass spectrometer (LC-MS/MS). Data were integrated with Analyst™ and analyzed by WinNonlin; stability parameters were analyzed using Tukey-Kramer multiple comparison test. Its average skin irritation scored 0.49 concluded to be non-irritant, safe for human use and in vivo studies revealed significantly greater extent of absorption and highly significant inhibition (%) of carrageenan induced paw edema. The results also demonstrated that encapsulation of drugs in nano-carrier increases its biological activity due to superior skin penetration potential. Hence, a novel once day transdermal gel of nano-carrier (nano-transfersomes; deformable vesicular) is achieved, to increase systemic availability, subsequent reduction in dose and toxicity of DDEA was developed for the treatment of inflammation.
目的是开发一种稳定、可重现且不会对患者造成侵犯的新型经皮药物传递系统“纳米载体透皮凝胶”（NCTG），该系统将部分剂量的双氯芬酸二乙胺（DDEA）由姜黄素（CRM）替代。凝胶的药物含量为 99.30%和 97.57%，分别为 DDEA 和 CRM。采用液相色谱-三重四极杆串联质谱法（LC-MS/MS）对血浆样品进行分析。数据使用 Analyst™进行整合，并通过 WinNonlin 进行分析；使用 Tukey-Kramer 多重比较检验分析稳定性参数。其平均皮肤刺激评分为 0.49，表明无刺激性，对人体安全，体内研究显示其吸收程度显著增加，对卡拉胶诱导的爪肿胀有高度显著的抑制（%）作用。结果还表明，由于具有卓越的皮肤渗透潜力，将药物封装在纳米载体中可提高其生物活性。因此，为了提高系统可用性，减少 DDEA 的剂量和毒性，我们开发了一种新型的每日一次经皮纳米载体（纳米传递体；变形囊泡）凝胶，用于治疗炎症。
