Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
Eur J Pharm Sci. 2019 Apr 1;131:23-38. doi: 10.1016/j.ejps.2019.02.006. Epub 2019 Feb 5.
In the present study, umbelliferone - phospholipids complex - loaded matrix film (UPLC - MF) was developed with a goal of improving transdermal permeation and anti-inflammatory potential of umbelliferone (UMB). Umbelliferone - phospholipids complex (UPLC) was prepared using solvent evaporation method. UPLC-MF was prepared by simple and reproducible solvent casting method. Prepared UPLC and UPLC-MF were both physico-chemically characterized by Fourier transforms infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), proton nuclear magnetic resonance spectroscopy (H NMR), weight variation, thickness, tensile strength, folding endurance, % elongation, moisture content and uptake Functional characterization of UPLC and UPLC-MF was carried out by solubility analysis, in vitro dissolution, diffusion, and ex vivo permeation via dialysis and biological membrane. UPLC - MF was also evaluated for in vivo anti-inflammatory activity using carrageenan-induced Albino rat paw model. Design-based optimal values for formulation and process variables of UPLC were observed to be 1:1.78, 50 °C and 2 h, respectively. Physico-chemical characterization confirmed the formation of the complex and the film. UPLC demonstrated a higher aqueous solubility (~11-fold), compared to pure UMB. Rate and extent of dissolution of UMB from UPLC was enhanced significantly to that of pure UMB. Compared to UMB-MF, the diffusion and permeation rate of UMB from UPLC-MF enhanced significantly. The UPLC - MF improved the anti-inflammatory potential of UMB by significant enhancement of edema inhibition (%), compared to UMB-MF. The obtained results showed that the present combined formulation system could be employed as a promising strategy for improving transdermal permeation of UMB.
在本研究中，开发了一种含有伞形酮-磷脂复合物的基质膜（UPLC-MF），旨在提高伞形酮（UMB）的透皮渗透和抗炎潜力。伞形酮-磷脂复合物（UPLC）是通过溶剂蒸发法制备的。UPLC-MF 是通过简单且可重复的溶剂浇铸法制备的。所制备的 UPLC 和 UPLC-MF 均通过傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DSC）、粉末 X 射线衍射（PXRD）、质子核磁共振光谱（H NMR）、重量变化、厚度、拉伸强度、耐折性、伸长率、水分含量和吸收来进行物理化学性质表征。通过溶解度分析、体外溶解、扩散和通过透析和生物膜的体外渗透对 UPLC 和 UPLC-MF 的功能进行了表征。还通过角叉菜胶诱导的白化大鼠足爪模型评估了 UPLC-MF 的体内抗炎活性。观察到 UPLC 的配方和工艺变量的基于设计的最佳值分别为 1:1.78、50°C 和 2 h。物理化学特性证实了复合物和膜的形成。UPLC 表现出比纯 UMB 更高的水溶解度（~11 倍）。与纯 UMB 相比，UMB 的溶解速率和程度显著提高。与 UMB-MF 相比，UMB 从 UPLC-MF 的扩散和渗透速率显著提高。与 UMB-MF 相比，UPLC-MF 显著提高了 UMB 的抗炎潜力，抑制水肿（%）的效果明显增强。结果表明，这种联合制剂系统可作为提高 UMB 透皮渗透的有前途的策略。
