Londhe Vaishali Y, Bhasin Bhavya
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle [W], Mumbai 400056, Maharashtra, India.
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle [W], Mumbai 400056, Maharashtra, India.
Colloids Surf B Biointerfaces. 2019 Nov 1;183:110409. doi: 10.1016/j.colsurfb.2019.110409. Epub 2019 Jul 30.
The objective of present study was to develop and evaluate lipid vesicular transdermal system of iloperidone. Liposomes were prepared successfully using thin film hydration method. With aim of enhancing permeation, cholesterol from liposomes was replaced with transcutol to give PEVs. Liposomes and PEVs were evaluated for particle size, shape, entrapment efficiency, viscosity and release study. The vesicles were incorporated in 0.5% of Carbopol gel and evaluated. Particle size of liposomes and PEVs was found between 200-300 nm and entrapment efficiency was found 80-90%w/w. The transdermal gels were homogeneous, spreadable having acceptable pH and drug content between 90-100%.In ex vivo studies, both liposomes and PEVs showed relatively higher skin deposition and permeation of Iloperidone than the plain drug without vesicles. The in vivo pharmacokinetics studies showed relative bioavailability of the PEV loaded gel as 62% and 166% when compared to the oral drug and gel without vesicles respectively. Pharmacodynamic studies showed FRT and HRT delay responses of the transdermal gel systems were significant[p < 0.05] as compared to control at the end of 24 hs. Thus, it can be concluded that transdermal delivery system can be a promising approach for sustained delivery of Iloperidone.
本研究的目的是开发并评估齐拉西酮脂质囊泡经皮给药系统。采用薄膜水化法成功制备了脂质体。为提高渗透性，用肉豆蔻酸异丙酯取代脂质体中的胆固醇以得到渗透促进型脂质体（PEVs）。对脂质体和渗透促进型脂质体的粒径、形态、包封率、黏度及释放情况进行了评估。将这些囊泡加入0.5%的卡波姆凝胶中并进行评估。发现脂质体和渗透促进型脂质体的粒径在200 - 300纳米之间，包封率为80 - 90%（w/w）。经皮凝胶均匀、可涂抹，pH值可接受，药物含量在90 - 100%之间。在体外研究中，与不含囊泡的普通药物相比，脂质体和渗透促进型脂质体均显示出相对较高的齐拉西酮皮肤沉积和渗透。体内药代动力学研究表明，与口服药物和不含囊泡的凝胶相比，载有渗透促进型脂质体的凝胶的相对生物利用度分别为62%和166%。药效学研究表明，在24小时结束时，与对照组相比，经皮凝胶系统的FRT和HRT延迟反应具有显著性差异（p < 0.05）。因此，可以得出结论，经皮给药系统可能是齐拉西酮持续给药的一种有前景的方法。
