Fadel Maha, Kassab Kawser, Abdel Fadeel Doaa A, Farag Maha A
Pharmaceutical Technology Unit, Department of Medical Applications of Laser, National Institute of Laser Enhanced Sciences, Cairo University, Giza 12613, Egypt.
Photobiology and Cell Photosensitization Lab, National Institute of Laser Enhanced Sciences, Cairo University, Giza 12613, Egypt.
Photodiagnosis Photodyn Ther. 2020 Jun;30:101789. doi: 10.1016/j.pdpdt.2020.101789. Epub 2020 Apr 30.
Photodynamic therapy is a clinically approved procedure for the treatment of neoplastic and other non-malignant diseases. Meso-tetrakis(N-methyl-4-pyridyl)porphyrin (TMPyP) is a photosensitizing agent which has been used in many applications. However, the use of TMPyP topically is limited due to its hydrophilicity. To overcome this problem, TMPyP was loaded in ethosomes. Three ethosomal formulae (A), (B) and (C) were prepared and characterized. Preparation (A) was chosen to be used in the in vitro and in vivo study, having the greatest encapsulation efficiency, the smallest size and the highest cumulative release percentage. The results of in vitro permeation study revealed that the ethosomal TMPyP was superior to the drug in the free form with permeation flux (3.92 μg cm h). In the in vivo animal study done on Swiss albino mice, after 19 days of Ehrlich tumor implantation, the group treated with the ethosomal preparation showed significantly smaller tumor size (143.28 ± 13.2 mm) compared to the group treated with the free TMPyP (219 ± 11.9 mm). It showed also significant longer survival time (21 days) compared to that treated with the free drug (18.2 ± 1.2 days). Based on the obtained results, transdermal delivery of TMPyP was potentiated by incorporating it in ethosomes.
光动力疗法是一种临床上已获批准用于治疗肿瘤及其他非恶性疾病的方法。中-四（N-甲基-4-吡啶基）卟啉（TMPyP）是一种已在许多应用中使用的光敏剂。然而，由于其亲水性，TMPyP的局部应用受到限制。为克服这一问题，将TMPyP载入醇质体中。制备了三种醇质体配方（A）、（B）和（C）并进行了表征。配方（A）具有最高的包封率、最小的粒径和最高的累积释放率，因此被选用于体外和体内研究。体外渗透研究结果表明，醇质体包载的TMPyP的渗透通量（3.92μg·cm·h）优于游离形式的药物。在对瑞士白化小鼠进行的体内动物研究中，接种艾氏腹水瘤19天后，与游离TMPyP治疗组（219±11.9mm）相比，醇质体制剂治疗组的肿瘤尺寸明显更小（143.28±13.2mm）。与游离药物治疗组（18.2±1.2天）相比，其存活时间也显著延长（21天）。基于所获得的结果，将TMPyP载入醇质体可增强其经皮递送效果。
