Ramreddy Srividya, Kandadi Prabhakar, Veerabrahma Kishan
Nanotechnology Research Lab, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh, India-506009.
PDA J Pharm Sci Technol. 2012 Jan-Feb;66(1):28-37. doi: 10.5731/pdajpst.2012.00735.
The objective of the present study was to formulate and determine the pharmacokinetics of stable o/w parenteral lipid nanoemulsions (LNEs) of diclofenac acid used to treat arthritic conditions. The LNEs of diclofenac acid with a mean size ranging from 200 to 240 nm and a zeta potential of -29.4 ± 1.04 mV (negatively charged LNEs) and 62.1 ± 3.5 (positively charged LNEs) emulsions were prepared by hot homogenization and ultrasonication process. The influence of formulation variables, such as the change in proportion of cholesterol, was studied, and optimized formulations were developed. The optimized formulations were relatively stable during centrifugal stress, dilution stress, and storage. The drug content and entrapment efficiency were determined using high-performance liquid chromatography. The in vitro drug release was carried out in phosphate-buffered saline pH 7.4 and cumulative amount of drug released was estimated using a UV-visible spectro-photometer. During in vivo pharmacokinetic studies in male Wistar rats, diclofenac serum concentration from LNEs was higher than that of Voveran injection and was detectable up to 12 h. Diclofenac in LNEs showed improved pharmacokinetic profile with increase in area under the curve, elimination half-life and mean residence time in comparison to Voveran.
Our aim was to prepare and determine the pharmacokinetics of injectable lipid nanoemulsions of diclofenac acid for treating arthritic conditions by reducing the frequency of dosing and pain at site of injection. The nanoemulsions of diclofenac acid were prepared by homogenization and ultrasonication process. The sizes and charges of oil globules were determined. The effect of cholesterol on stability of emulsion was studied, and an optimized preparation was developed. The optimized formulations were stable during centrifugation, dilution, and storage. The total amount of drug in emulsion and percentage amount of drug present in emulsion globules were determined using high-performance liquid chromatography. The drug release from preparation was carried out in phosphate-buffered saline pH 7.4. The cumulative amount of drug released was estimated using a spectrophotometer. The time course of the released drug in rat serum was determined. Diclofenac concentrations from lipid nanoemulsions were higher than that of Voveran injection (solution form) in serum.
本研究的目的是制备用于治疗关节炎的双氯芬酸稳定的油包水型肠胃外脂质纳米乳剂（LNE）并确定其药代动力学。通过热均质化和超声处理过程制备了平均粒径在200至240nm范围内、ζ电位为-29.4±1.04mV（带负电荷的LNE）和62.1±3.5（带正电荷的LNE）乳液的双氯芬酸LNE。研究了配方变量的影响，如胆固醇比例的变化，并开发了优化配方。优化后的配方在离心应力、稀释应力和储存过程中相对稳定。使用高效液相色谱法测定药物含量和包封率。在pH7.4的磷酸盐缓冲盐水中进行体外药物释放，并使用紫外可见分光光度计估计药物释放的累积量。在雄性Wistar大鼠体内药代动力学研究期间，LNE中的双氯芬酸血清浓度高于扶他林注射剂，并且在12小时内均可检测到。与扶他林相比，LNE中的双氯芬酸显示出改善的药代动力学特征，曲线下面积、消除半衰期和平均驻留时间增加。
我们的目的是通过减少给药频率和注射部位疼痛来制备用于治疗关节炎的双氯芬酸注射用脂质纳米乳剂并确定其药代动力学。通过均质化和超声处理过程制备双氯芬酸纳米乳剂。测定油滴的大小和电荷。研究了胆固醇对乳液稳定性的影响，并开发了优化制剂。优化后的配方在离心、稀释和储存过程中稳定。使用高效液相色谱法测定乳液中药物的总量和乳液小球中药物的百分比量。在pH7.4的磷酸盐缓冲盐水中进行制剂的药物释放。使用分光光度计估计药物释放的累积量。测定大鼠血清中释放药物的时间过程。脂质纳米乳剂中的双氯芬酸浓度高于血清中扶他林注射剂（溶液形式）的浓度。
