In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions.
In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions.
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DOI：
10.1007/s11095-018-2495-1
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发表时间：
2018-10-09
影响因子：
3.7
通讯作者：
Brogden NK
中科院分区：
文献类型：
--
作者：
Kelchen MN;Brogden NK
局部β受体阻滞剂对治疗婴儿血管瘤有效，但没有针对皮肤给药专门优化的制剂。我们的目的是定量皮肤浓度和普萘洛尔（一种非选择性β-受体阻滞剂）后，应用微乳液完整和微针预处理的皮肤药物渗透。四普萘洛尔加载微乳的特点是液滴大小，表面电荷，电导率，pH值，药物溶解度，和药物释放。使用LC-MS定量皮肤浓度和药物通过皮肤的渗透。皮肤-受体比用于比较微乳液制剂与药物-PBS溶液。普萘洛尔在微乳剂中的溶解度显著高于PBS。在24小时内从微乳中的累积药物释放范围为13%至26%。皮肤浓度和药物渗透通过完整的皮肤是从PBS显着更高，但是，皮肤-接收器比显着更高的富水微乳液相比，PBS或表面活性剂丰富的微乳液。针头预处理显著增加所有制剂的皮肤浓度。微针预处理富含表面活性剂的微乳剂后，皮肤与受体的比例显著增加。可以改变微乳制剂以通过MN处理的皮肤引起不同的药物递送曲线。这可能有利于最大限度地提高局部皮肤药物浓度和改善婴儿血管瘤治疗的给药方案。
Topical beta-blockers are efficacious for treating infantile hemangiomas, but no formulations have been specifically optimized for skin delivery. Our objective was to quantify skin concentrations and drug permeation of propranolol (a nonselective beta-blocker) after application of microemulsions to intact and microneedle pretreated skin. Four propranolol-loaded microemulsions were characterized for droplet size, surface charge, conductivity, pH, drug solubility, and drug release. Skin concentrations and drug permeation through skin were quantified using LC-MS. Skin-to-receiver ratios were used to compare the microemulsion formulations to a drug-in-PBS solution. Propranolol solubility was significantly greater in microemulsions vs PBS. Cumulative drug release from the microemulsions over 24 h ranged from 13 to 26%. Skin concentrations and drug permeation through intact skin was significantly higher from PBS; however, the skin-to-receiver ratios were significantly higher for water-rich microemulsions compared to PBS or surfactant-rich microemulsions. Microneedle pretreatment significantly increased skin concentrations for all formulations. Skin-to-receiver ratios significantly increased after microneedle pretreatment for surfactant-rich microemulsions. Microemulsion formulation can be altered to elicit different drug delivery profiles through MN-treated skin. This could be advantageous for maximizing local skin drug concentrations and improving dosing schedules for infantile hemangioma treatment.
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影响因子：
5.8
作者：
Djordjevic, L;Primorac, M;Stupar, M
通讯作者：
Stupar, M
影响因子：
10.8
作者：
Kreilgaard, M;Pedersen, EJ;Jaroszewski, JW
通讯作者：
Jaroszewski, JW
影响因子：
3.8
作者：
Ren, Qiuyue;Deng, Chunli;Fang, Xiaoling
通讯作者：
Fang, Xiaoling
DOI：
10.1111/bjd.12804
发表时间：
2014-04
期刊：
The British journal of dermatology
影响因子：
--
作者：
Munden A;Butschek R;Tom WL;Marshall JS;Poeltler DM;Krohne SE;Alió AB;Ritter M;Friedlander DF;Catanzarite V;Mendoza A;Smith L;Friedlander M;Friedlander SF
通讯作者：
Friedlander SF
影响因子：
46.9
作者：
Prausnitz, Mark R.;Langer, Robert
通讯作者：
Langer, Robert