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泊洛沙姆磷脂有机凝胶作为一种局部药物传递系统。

Pluronic lecithin organogel as a topical drug delivery system.

机构信息

Department of Pharmaceutics, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, India.

出版信息

Drug Deliv. 2010 Jan;17(1):38-47. doi: 10.3109/10717540903508961.

DOI:10.3109/10717540903508961
PMID:22747074
Abstract

The objective of this study was to formulate and evaluate the pluronic lecithin organogel containing flurbiprofen for topical application. Different formulations of pluronic lecithin organogels were prepared by using pluronic F127, lecithin, flurbiprofen, isopropyl palmitate, water, sorbic acid, and potassium sorbate. To study the in vitro potential of these formulations, permeation studies were performed with Keshary-Chien diffusion cells. The results of the in vitro permeation studies found that release of flurbiprofen from dialysis membrane-70 was more than excised dorsal rat skin. Gelation temperature study was carried out to determine the temperature where sol-gel transformation takes place. The viscosities of different formulations were determined by using Brookfield Viscometer at 25°C, the viscosity of formulations increases as the lecithin concentration increases. Also the formulations were tested for appearance and feel psychorheologically, pH, and drug content. Interactions between the components of the gel have been investigated by differential scanning calorimetry and X-ray powder diffractometry. The optimized formulation subjected to differential scanning calorimetry shows no drug-polymer interaction. To investigate the in vivo performance of the formulations, a carrageenan-induced rat paw edema model and skin irritation study was used. The stability studies and freeze-thaw thermal cyclic test were carried out, showing no phase separation of gel, and representing gel stability. Statistical analysis of the data of animal study (anti-inflammatory activity) was done by using one way analysis of variance (ANOVA) followed by Dunnett's test. The formulation shows a statistically significant anti-inflammatory activity and is non-irritant to skin.

摘要

本研究的目的是制备和评价含有氟比洛芬的泊洛沙姆-卵磷脂组织凝胶剂用于局部应用。通过使用泊洛沙姆 F127、卵磷脂、氟比洛芬、异丙基棕榈酸酯、水、山梨酸和山梨酸钾,制备了不同配方的泊洛沙姆-卵磷脂组织凝胶剂。为了研究这些配方的体外潜力,采用 Keshary-Chien 扩散池进行了渗透研究。体外渗透研究的结果发现,从透析膜-70 释放的氟比洛芬多于切除的大鼠背部皮肤。凝胶化温度研究是为了确定发生溶胶-凝胶转变的温度。在 25°C 下使用 Brookfield 粘度计测定了不同配方的粘度,随着卵磷脂浓度的增加,配方的粘度增加。还对制剂的外观和感觉、pH 值和药物含量进行了测试。通过差示扫描量热法和 X 射线粉末衍射法研究了凝胶中各成分之间的相互作用。优化的配方进行差示扫描量热法分析显示没有药物-聚合物相互作用。为了研究制剂的体内性能,采用角叉菜胶诱导的大鼠足肿胀模型和皮肤刺激性研究。进行了稳定性研究和冻融热循环试验,结果表明凝胶没有相分离,代表凝胶稳定性。动物研究(抗炎活性)数据的统计分析采用单因素方差分析(ANOVA),然后进行 Dunnett 检验。该配方具有统计学显著的抗炎活性,对皮肤无刺激性。

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