Prasanthi D, Lakshmi P K
Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Osmania University, Hyderabad, Andhra Pradesh 500 028, India.
ISRN Pharm. 2012;2012:965280. doi: 10.5402/2012/965280. Epub 2012 Dec 20.
The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q(24)) of 702.28 ± 6.97 μg/cm(2) and 702.74 ± 7.49 μg/cm(2), respectively. A flux rate of 31.08 ± 0.21 μg/cm(2)/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm(2)/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.
本研究的目的是在多种可用的渗透促进剂中，探索能有效克服盐酸阿夫唑嗪（AH）经皮给药时角质层屏障的化学渗透促进剂。将不同的渗透促进剂加入2%的卡波姆凝胶中，该凝胶被选为对照，并通过透析膜进行体外扩散研究以及使用Keshary-Chien扩散池对大鼠腹部皮肤的渗透进行评估。与对照相比，除油酸降低了释放速率但显示出药物的最大溶解度外，所有渗透促进剂均增加了通过透析膜的释放速率。在各种渗透促进剂中，20%的二甲基亚砜和吐温-20（2%）分别显示出最高的累积量（Q(24)），即702.28±6.97μg/cm²和702.74±7.49μg/cm²。20%的二甲基亚砜获得的通量率为31.08±0.21μg/cm²/小时，吐温-20（2%）为30.38±0.18μg/cm²/小时。20%的二甲基亚砜显示滞后时间缩短至0.13±0.05小时。2.5%的油酸的皮肤含量最低，为342.33±5.30μg/gm。20%的二甲基亚砜使通量最大增强了3.94倍。用兔子进行了原发性皮肤刺激性研究。20%的二甲基亚砜的组织病理学研究显示出明显变化，如真皮中单核细胞的变性和浸润，表明二甲基亚砜对皮肤的作用。在不同的渗透促进剂中，二甲基亚砜在增强AH的经皮给药方面是有效的。
