Somagoni Jaganmohan, Boakye Cedar H A, Godugu Chandraiah, Patel Apurva R, Mendonca Faria Henrique Antonio, Zucolotto Valtencir, Singh Mandip
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, United States of America.
Nanomedicine and Nanotoxicology Group, Physics Institute of São Carlos, USP, 13566-590, São Carlos, SP, Brazil.
PLoS One. 2014 Dec 29;9(12):e115952. doi: 10.1371/journal.pone.0115952. eCollection 2014.
The objective of this study was to formulate and evaluate a unique matrix mixture (nanomiemgel) of nanomicelle and nanoemulsion containing aceclofenac and capsaicin using in vitro and in vivo analyses and to compare it to a marketed formulation (Aceproxyvon).
Nanomicelles were prepared using Vitamin E TPGS by solvent evaporation method and nanoemulsion was prepared by high-pressure homogenization method. In vitro drug release and human skin permeation studies were performed and analyzed using HPLC. The efficiency of nanomiemgel as a delivery system was investigated using an imiquimod-induced psoriatic like plaque model developed in C57BL/6 mice.
Atomic Force Microscopy images of the samples exhibited a globular morphology with an average diameter of 200, 250 and 220 nm for NMI, NEM and NMG, respectively. Nanomiemgel demonstrated a controlled release drug pattern and induced 2.02 and 1.97-fold more permeation of aceclofenac and capsaicin, respectively than Aceproxyvon through dermatomed human skin. Nanomiemgel also showed 2.94 and 2.09-fold greater Cmax of aceclofenac and capsaicin, respectively than Aceproxyvon in skin microdialysis study in rats. The PASI score, ear thickness and spleen weight of the imiquimod-induced psoriatic-like plaque model were significantly (p<0.05) reduced in NMG treated mice compared to free drug, NEM, NMI & Aceproxyvon.
Using a new combination of two different drug delivery systems (NEM+NMI), the absorption of the combined system (NMG) was found to be better than either of the individual drug delivery systems due to the utilization of the maximum possible paths of absorption available for that particular drug.
本研究的目的是通过体外和体内分析来制备和评估一种含有醋氯芬酸和辣椒素的纳米胶束与纳米乳剂的独特基质混合物(纳米混合凝胶),并将其与市售制剂(Aceproxyvon)进行比较。
采用溶剂蒸发法用维生素E TPGS制备纳米胶束,采用高压均质法制备纳米乳剂。进行体外药物释放和人体皮肤渗透研究,并使用高效液相色谱法进行分析。使用在C57BL/6小鼠中建立的咪喹莫特诱导的银屑病样斑块模型研究纳米混合凝胶作为给药系统的效率。
样品的原子力显微镜图像显示出球形形态,NMI、NEM和NMG的平均直径分别为200、250和220 nm。纳米混合凝胶表现出控释药物模式,通过离体人皮肤,醋氯芬酸和辣椒素的渗透分别比Aceproxyvon高2.02倍和1.97倍。在大鼠皮肤微透析研究中,纳米混合凝胶中醋氯芬酸和辣椒素的Cmax也分别比Aceproxyvon高2.94倍和2.09倍。与游离药物、NEM、NMI和Aceproxyvon相比,纳米混合凝胶治疗的小鼠中咪喹莫特诱导的银屑病样斑块模型的PASI评分、耳厚度和脾脏重量显著降低(p<0.05)。
使用两种不同给药系统(NEM+NMI)的新组合,发现联合系统(NMG)的吸收优于任何一种单独的给药系统,这是因为利用了该特定药物可用的最大可能吸收途径。