Gaur Praveen Kumar, Mishra Shikha, Aeri Vidhu
Department of Pharmaceutics, I.T.S. Paramedical (Pharmacy) College, Muradnagar, Ghaziabad 201206, India.
Department of Pharmacognosy & Phytochemistry, Jamia Hamdard, New Delhi 110062, India.
ScientificWorldJournal. 2014 Feb 6;2014:534210. doi: 10.1155/2014/534210. eCollection 2014.
Most new drugs have low water solubility and liposome is an important formulation to administer such drugs; however, it is quite unstable and has negligible systemic absorption.
Aceclofenac nanovesicles were made using guggul lipid for formulating stable transdermal formulation.
Guggul lipid was formulated into vesicles along with cholesterol and dicetyl phosphate using film hydration method. The formulations were analyzed for physicochemical properties and stability. Then its skin permeation and anti-inflammatory activity were determined.
Both categories of vesicles (PC and GL) showed optimum physicochemical properties; however, accelerated stability study showed considerable differences. GL-1 was appreciably stable for over 6 months at 4 °C. Corresponding gels (PCG-1 and GLG-1) showed C max values at 4.98 and 7.32 μg/mL along with the Tmax values at 4 and 8 hours, respectively. GLG-1 inhibited edema production by 90.81% in 6 hours. Discussion. PC liposomes are unstable at higher temperature and upon longer storage. The formulation with higher lipid content (GL-1) showed good drug retention after 24 hours and appreciable stability both at higher temperature and for longer duration. Guggul lipid being a planar molecule might be stacked in vesicle wall with cholesterol.
The composition of the nanovesicle played an important role in stability and drug permeation. Guggul lipid is suitable for producing stable vesicles.
大多数新药的水溶性较低，脂质体是这类药物给药的重要剂型；然而，它相当不稳定，全身吸收可忽略不计。
使用古古勒脂制备醋氯芬酸纳米囊泡，以配制稳定的透皮制剂。
采用薄膜水化法将古古勒脂与胆固醇和磷酸二鲸蜡酯一起制成囊泡。对制剂的理化性质和稳定性进行分析。然后测定其皮肤渗透性和抗炎活性。
两类囊泡（PC和GL）均表现出最佳的理化性质；然而，加速稳定性研究显示出相当大的差异。GL-1在4℃下6个月以上相当稳定。相应的凝胶（PCG-1和GLG-1）的Cmax值分别为4.98和7.32μg/mL，Tmax值分别为4和8小时。GLG-1在6小时内抑制水肿产生90.81%。讨论。PC脂质体在较高温度和较长储存时间下不稳定。脂质含量较高的制剂（GL-1）在24小时后显示出良好的药物保留率，在较高温度和较长时间内均具有相当的稳定性。古古勒脂作为平面分子可能与胆固醇堆叠在囊泡壁中。
纳米囊泡的组成在稳定性和药物渗透中起重要作用。古古勒脂适合制备稳定的囊泡。
