Sanz Roser, Calpena Ana C, Mallandrich Mireia, Clares Beatriz
Faculty of Pharmacy, University of Granada, Campus Universitario de Cartuja, 18071 Granada, Spain.
Curr Pharm Des. 2015;21(20):2867-82. doi: 10.2174/1381612821666150428145627.
Topical administration is an appealing method for drug delivery due to its non-invasiveness, self-controlled application, avoidance of first-pass metabolism in the liver and reduction of systemic side effects compared to other conventional routes such as oral and parenteral. However, topical administration must overcome the permeable barriers that skin and mucosa represent for the drug to achieve its desired therapeutic effect. Penetration of drugs through human skin is mainly impaired by the stratum corneum- the uppermost keratinized skin layer. In contrast, the stratified squamous epithelium (a nonkeratinized tissue) represents the major physical barrier for transbuccal drug administration in humans. Different technologies have been studied to enhance the bioavailability or local effects of drugs administered through skin and buccal mucosa. Those technologies involve the use of physical or chemical enhancers and new dosage forms such as vesicles, cyclodextrins, nanoparticles and other complex systems. Combinations of these technologies may further increase drug delivery in some cases. As analgesia is one of the main therapeutic effects sought through topical administration, this paper focuses on the review of drug delivery systems to improve the topical and transdermal/transbuccal drug delivery of substances with known analgesic action. A discussion of their possibilities and limitations is also included.
与口服和注射等其他传统给药途径相比，局部给药因其无创性、可自我控制给药、避免肝脏首过代谢以及减少全身副作用，是一种具有吸引力的给药方法。然而，局部给药必须克服皮肤和黏膜对药物形成的渗透屏障，才能达到预期的治疗效果。药物透过人体皮肤的主要障碍是角质层——皮肤最上层的角质化层。相比之下，复层鳞状上皮（一种非角质化组织）是人类经颊给药的主要物理屏障。人们研究了不同技术来提高通过皮肤和颊黏膜给药的药物的生物利用度或局部效果。这些技术包括使用物理或化学增强剂以及新剂型，如囊泡、环糊精、纳米颗粒和其他复杂系统。在某些情况下，这些技术的组合可能会进一步提高药物递送效率。由于镇痛是局部给药追求的主要治疗效果之一，本文重点综述了药物递送系统，以改善具有已知镇痛作用的物质的局部和经皮/经颊给药。文中还讨论了它们的可能性和局限性。
