In Situ Gel Formation in Microporated Skin for Enhanced Topical Delivery of Niacinamide
In Situ Gel Formation in Microporated Skin for Enhanced Topical Delivery of Niacinamide
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DOI：
10.3390/pharmaceutics12050472
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发表时间：
2020-05-01
期刊：
影响因子：
5.4
通讯作者：
Banga, Ajay K.
中科院分区：
文献类型：
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作者：
Bhattaccharjee, Sonalika;Beck-Broichsitter, Moritz;Banga, Ajay K.
尽管广泛用于化妆品制剂中，但通过常规手段局部递送烟酰胺（LogP = -0.35）是不利的。聚（丙交酯-共-乙交酯）（PLGA）制剂可以经历由溶剂交换引发的溶胶-凝胶转变，捕获分子并维持其释放。目前的研究旨在利用PLGA原位凝胶化的能力，并增强烟酰胺在微孔皮肤中的局部递送。使用垂直Franz扩散池进行体外药物渗透研究。使用Dr. Pen（TM）Ultima A6进行微孔化，其中比较了以13，000次插入/分钟的1 mm针长10秒和0.5mm针长5秒的预处理。还测定了不同等级的PLGA、EXPANSORB（R）DLG 50-2A（“低”分子量）和EXPANSORB（R）DLG 50-8A（“高”分子量）对局部递送的影响。含有PLGA的制剂在微孔皮肤上应用时成功地原位凝胶化。用0.5 mm处理5 s（892 +/- 36 μ g/cm（2））的皮肤中发现的药物量明显高于用1 mm处理10 s（167 +/- 16 μ g/cm（2））的皮肤。因此，用0.5 mm，5 s处理评价不同等级的PLGA，在皮肤中观察到较高分子量聚合物而不是较低分子量聚合物（172 +/- 53 μ g/cm（2））的显著更大的量。
Although used widely in cosmetic formulations, topical delivery of niacinamide (LogP = -0.35) is unfavorable by conventional means. Poly(lactide-co-glycolide) (PLGA) formulations, can undergo a sol-gel transition triggered by solvent exchange, entrapping molecules and sustaining their release. The current study aims to exploit the ability of PLGA to gel in situ and enhance the topical delivery of niacinamide in microporated skin. In vitro drug permeation studies were performed using vertical Franz diffusion cells. Microporation was performed using Dr. Pen(TM)Ultima A6, where pre-treatment with a 1 mm needle-length for 10 s and a 0.5 mm needle-length for 5 s, both at 13,000 insertions/min were compared. The effect of different grades of PLGA, EXPANSORB(R)DLG 50-2A ("low" molecular weight), and EXPANSORB(R)DLG 50-8A ("high" molecular weight) on topical delivery was also deter mined. Formulations containing PLGA resulted in successful gelation in situ on application over microporated skin. A significantly higher amount of drug was found in the skin with the 0.5 mm treatment for 5 s (892 +/- 36 mu g/cm(2)) than with 1 mm for 10 s (167 +/- 16 mu g/cm(2)). Hence, the different grades of PLGA were evaluated with 0.5 mm, 5 s treatment, and a significantly larger amount was seen in skin with the higher rather than the lower molecular weight polymer (172 +/- 53 mu g/cm(2)).