卟啉和卟啉前体的新给药策略

D. I. Morrow, R. Donnelly
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引用次数: 3

摘要

浅表病变,如光化性角化病。此外,光动力抗微生物化疗(PACT)正在引起越来越多的兴趣,用于治疗感染。然而,局部PDT和PACT的给药策略仍然基于相当简单的乳膏和溶液配方的应用,很少考虑活性剂的热力学、靶向性或物理化学性质。专为局部递送氨基乙酰丙酸或其酯类而设计的剂型包括含有渗透增强剂和/或铁螯合剂的药膏、压敏贴剂和生物粘合剂贴剂。这种系统旨在增强药物在角质层和肿瘤病变上的角化碎片上的传递,并改善随后的原卟啉IX (PpIX)的产生。使用卟啉前体的替代方法是使用预成型光敏剂。然而,由于其相对较高的分子量,传统的局部应用是不合适的。创新的策略,如使用无针注射和微针阵列,绕过角质层,不仅可以快速和有针对性地递送卟啉前体,还可以预先形成光敏剂。本报告将回顾迄今为止在PDT和PACT领域发表的给药工作。此外,还将强调采用最新制药技术的好处。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel drug delivery strategies for porphyrins and porphyrin precursors
superficial lesions, such as actinic keratosis. In addition, photodynamic antimicrobial chemotherapy (PACT) is attracting increasing interest for the treatment of infection. However, delivery strategies for topical PDT and PACT are still based on application of rather simplistic cream and solution formulations, with little consideration given to thermodynamics, targeting or the physicochemical properties of the active agent. Purpose-designed dosage forms for topical delivery of aminolevulinic acid or its esters include creams containing penetration enhancers and/or iron chelators, pressure sensitive patches and bioadhesive patches. Such systems aim to enhance drug delivery across the stratum corneum and keratinised debris overlying neoplastic lesions and improve subsequent protoporphyrin IX (PpIX) production. The alternative to using porphyrin precursors is the use of pre-formed photosensitisers. However, owing to their relatively high molecular weights, conventional topical application is not appropriate. Innovative strategies, such as the use of needle-free injections and microneedle arrays, bypass the stratum corneum, enabling rapid and targeted delivery not only porphyrin precursors but also pre-formed photosensitisers. This presentation will review drug delivery work published to date in the fields of PDT and PACT. In addition, the benefits of employing the latest advances in pharmaceutical technology will be highlighted.
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