Transfollicular drug delivery:: Penetration of drugs through human scalp skin and comparison of penetration between scalp and abdominal skins in vitro
Transfollicular drug delivery:: Penetration of drugs through human scalp skin and comparison of penetration between scalp and abdominal skins in vitro
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DOI：
10.1080/1061186021000001814
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发表时间：
2002-08-01
影响因子：
4.5
通讯作者：
Wada, T
中科院分区：
文献类型：
--
作者：
Ogiso, T;Shiraki, T;Wada, T
为了定量研究药物传递的重要性，通过人头皮皮肤的药物渗透进行了研究，在体外使用含有亲脂性和亲水性药物的液体制剂。用荧光探针检测药物通过头皮皮肤的渗透途径，并将药物通过头皮皮肤的渗透与通过人腹部皮肤的渗透进行比较，以阐明毛囊内给药的有效性。亲脂性褪黑激素（MT）和酮洛芬（KP）通过头皮皮肤显示出高渗透性，尽管KP的通量要高得多。吸收促进剂，N-甲基-2-吡咯烷酮和肉豆蔻酸异丙酯，只有轻微增加的通量。亲水性氟尿嘧啶（5 FU）和阿昔洛韦（ACV）通过头皮皮肤渗透相对较大的通量。然而，这些药物在不同来源的头皮皮肤中的通量存在很大的差异。当对毛囊密度与流量的关系进行估计时，两者之间具有良好的相关性（MT和ACV的r = 0.651和r = 0.666，P < 0.05）。在应用具有尼罗红或荧光素钠的制剂后，头皮皮肤的组织学检查表明，探针渗透到毛囊的内根鞘和外根鞘的连接处，并在初始时间通过外根鞘扩散到真皮中。亲脂性探针尼罗红经头皮角质层的渗透晚于经毛囊的渗透。MT和5 FU经头皮皮肤的渗透量远高于经腹部皮肤的渗透量，分别为腹部皮肤的27倍和48倍。这些结果表明，通过头皮皮肤的药物递送将提供一个可用的药物，特别是亲水性药物的传递手段。
In order to quantitatively investigate the importance of transfollicular pathway for drug delivery, drug penetration through human scalp skin was investigated using liquid formulations containing lipophilic and hydrophilic drugs in vitro. The penetration pathway for drugs through the scalp skin was examined using fluorescent probes, Additionally, the drug penetration through the scalp skin was compared with that via human abdominal skin to clarify the usefulness of intrafollicular delivery. Lipophilic melatonin (MT) and ketoprofen (KP) showed high permeabilities through the scalp skin, although the flux of KP was much higher. Absorption enhancers, N-methyl-2-pyrrolidone and isopropylmyristate, only slightly increased the fluxes. Hydrophilic fluorouracil (5FU) and acyclovir (ACV) penetrated through the scalp skin with relatively large fluxes. However, there was large variability in the fluxes of these drugs across scalp skin from different sources. When the relationship between the flux and hair follicle density was estimated, there was good correlation between the two (r = 0.651 for MT and r = 0.666 for ACV, P < 0.05). The histologic examination of the scalp skin, following application of the formulation with nile red or sodium fluorescein, indicated that the probes permeated into the junction of the internal and external root sheath of follicles and diffused into the dermis via the outer root sheath at the initial times. The penetration of nile red, a lipophilic probe, via the stratum corneum of scalp skin was later than that via the follicles. The permeation of MT and 5FU through the scalp skin was much higher than that via the abdominal skin, being 27 and 48 times as high as the abdominal skin, respectively. These results indicate that the drug delivery through the scalp skin will offer an available delivery means for drugs, particularly for hydrophilic drugs.