Dave Kaushalkumar, Averineni Ranjith, Sahdev Preety, Perumal Omathanu
Department of Pharmaceutical Sciences, South Dakota State University, Brookings, South Dakota, 57007, United States of America.
PLoS One. 2014 Dec 29;9(12):e115712. doi: 10.1371/journal.pone.0115712. eCollection 2014.
The study was aimed at investigating localized topical drug delivery to the breast via mammary papilla (nipple). 5-fluorouracil (5-FU) and estradiol (EST) were used as model hydrophilic and hydrophobic compounds respectively. Porcine and human nipple were used for in-vitro penetration studies. The removal of keratin plug enhanced the drug transport through the nipple. The drug penetration was significantly higher through the nipple compared to breast skin. The drug's lipophilicity had a significant influence on drug penetration through nipple. The ducts in the nipple served as a major transport pathway to the underlying breast tissue. Results showed that porcine nipple could be a potential model for human nipple. The topical application of 5-FU on the rat nipple resulted in high drug concentration in the breast and minimal drug levels in plasma and other organs. Overall, the findings from this study demonstrate the feasibility of localized drug delivery to the breast through nipple.
该研究旨在调查通过乳头将局部外用药物递送至乳房。分别使用5-氟尿嘧啶(5-FU)和雌二醇(EST)作为亲水性和疏水性化合物模型。使用猪乳头和人乳头进行体外渗透研究。去除角质栓可增强药物通过乳头的转运。与乳房皮肤相比,药物通过乳头的渗透明显更高。药物的亲脂性对药物通过乳头的渗透有显著影响。乳头中的导管是通向其下方乳房组织的主要转运途径。结果表明,猪乳头可能是人类乳头的潜在模型。在大鼠乳头上局部应用5-FU可使乳房中的药物浓度升高,而血浆和其他器官中的药物水平最低。总体而言,本研究的结果证明了通过乳头向乳房局部给药的可行性。