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经激光微穿孔透皮给药用肝素凝胶的研制与评价。

Development and evaluation of a heparin gel for transdermal delivery via laser-generated micropores.

机构信息

Department of Pharmaceutical Sciences, Center for Drug Delivery Research, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.

出版信息

Ther Deliv. 2021 Feb;12(2):133-144. doi: 10.4155/tde-2020-0024. Epub 2021 Jan 26.

Abstract

Our study investigated the feasibility of transdermal delivery of heparin, an anticoagulant used against venous thromboembolism, as an alternative to intravenous administration. Skin was pretreated using ablative laser (Precise Laser Epidermal System [P.L.E.A.S.E.] technology) for enhanced delivery of heparin. permeation studies using static Franz diffusion cells provided a comparison between delivery from 0.3% w/v heparin-loaded poloxamer gel and solution across untreated and laser-treated dermatomed porcine ear skin. No passive delivery of heparin was observed. Laser-assisted delivery from solution (26.07 ± 1.82 μg/cm) was higher (p < 0.05) than delivery from heparin gel (11.28 ± 5.32 μg/cm). However, gel is likely to sustain the delivery over prolonged periods like a maintenance dose via continuous intravenous infusion. Thus, ablative laser pretreatment successfully delivered heparin, establishing the feasibility of delivering hydrophilic macromolecules using the transdermal route.

摘要

我们的研究调查了肝素(一种用于对抗静脉血栓栓塞的抗凝剂)经皮给药的可行性,作为静脉给药的替代方法。皮肤先用激光(Precise Laser Epidermal System [P.L.E.A.S.E.] 技术)预处理,以增强肝素的传递。使用静态 Franz 扩散细胞进行渗透研究,比较了未经处理和激光处理的去皮猪耳皮肤从 0.3%w/v 肝素负载泊洛沙姆凝胶和溶液中的传递。未观察到肝素的被动传递。从溶液中(26.07 ± 1.82 μg/cm)的激光辅助传递(26.07 ± 1.82 μg/cm)高于从肝素凝胶(11.28 ± 5.32 μg/cm)的传递(p < 0.05)。然而,凝胶可能会像通过连续静脉输注的维持剂量一样,在较长时间内持续输送。因此,激光预处理成功地传递了肝素,证明了经皮途径传递亲水性大分子的可行性。

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