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Topical photodynamic therapy of tumor bearingmice with meso-tetrakis (N- methyl-4-pyridyl) porphyrin loaded in ethosomes

机译:常规光动力学治疗肿瘤upersoome - 四甲基-4-吡啶基)卟啉在乙烯体中加载

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摘要

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 mu g cm(-2) h(-1)). 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(3)) compared to the group treated with the free TMPyP (219 +/- 11.9 mm(3)). 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.
机译:光动力疗法是一种临床批准的治疗肿瘤和其他非恶性疾病的程序。中核 - 四甲基-4-吡啶基)卟啉(Tmpyp)是一种光敏剂,其已用于许多应用中。然而,由于其亲水性,使用TMPYP局部的限制。为了克服这个问题,TMPYP被加载在祖传群中。制备三种原料公式(A),(B)和(C)。选择制备(A)在体外和体内研究中使用,具有最大的封装效率,最小尺寸和最高的累积释放百分比。体外渗透研究的结果表明,乙染粒子Tmpyp在渗透通量(3.92μgcm(-2)h(-1))中的自由形式中的药物优于药物。在体内动物研究中对瑞士白化小鼠进行的,在19天的EHRLICH肿瘤植入后,与用细胞处理的基团相比,用乙染蛋白制剂处理的基团显示出明显较小的肿瘤大小(143.28 +/- 13.2mm(3))免费TMPYP(219 +/- 11.9 mm(3))。它表现出显着的生存时间(21天)与用自由药物治疗(18.2 +/- 1.2天)。基于所得的结果,通过将其掺入归因组中来激增Tmpyp的透皮递送。

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