Azeem Adnan, Khan Zeenat Iqbal, Aqil M, Ahmad Farhan Jalees, Khar Roop Kishan, Talegaonkar Sushama
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.
Drug Dev Ind Pharm. 2009 May;35(5):525-47. doi: 10.1080/03639040802448646.
Microemulsions are isotropic, thermodynamically stable transparent (or translucent) systems of oil, water, and surfactant, frequently in combination with a cosurfactant with a droplet size usually in the range of 20-200 nm. Since their discovery, they have attained increasing significance both in basic research and in industry. Due to their distinct advantages such as enhanced drug solubility, thermodynamic stability, facile preparation, and low cost, uses and applications of microemulsions have been numerous. Recently, there is a surge in the exploration of microemulsion for transdermal drug delivery for their ability to incorporate both hydrophilic (5-fluorouracil, apomorphine hydrochloride, diphenhydramine hydrochloride, tetracaine hydrochloride, and methotrexate) and lipophilic drugs (estradiol, finasteride, ketoprofen, meloxicam, felodipine, and triptolide) and enhance their permeation. Very low surface tension in conjunction with enormous increase in the interfacial area due to nanosized droplets of the microemulsion influences the drug permeation across the skin. A large number of oils and surfactants are available, which can be used as components of microemulsion systems for transdermal delivery but their toxicity, irritation potential, and unclear mechanism of action limit their use. Besides surfactants, oils can also act as penetration enhancers (oleic acid, linoleic acid, isopropyl myristate, isopropyl palmitate, etc.). The transdermal drug delivery potential of microemulsions is dependent not only on the applied constituents of the vehicle but also drastically on the composition/internal structure of the phases which may promote or hamper the drug distribution in the vehicles. This article explores microemulsion as transdermal drug delivery vehicles with emphasis on components selection for enhanced drug permeation and skin tolerability of these systems and further future directions.
微乳剂是由油、水和表面活性剂组成的各向同性、热力学稳定的透明(或半透明)体系,通常还会与助表面活性剂结合使用,其液滴尺寸通常在20-200nm范围内。自被发现以来,它们在基础研究和工业领域都变得越来越重要。由于微乳剂具有诸如提高药物溶解度、热力学稳定性、制备简便和成本低等显著优点,其用途和应用非常广泛。最近,由于微乳剂能够同时包载亲水性药物(5-氟尿嘧啶、盐酸阿扑吗啡、盐酸苯海拉明、盐酸丁卡因和甲氨蝶呤)和亲脂性药物(雌二醇、非那雄胺、酮洛芬、美洛昔康、非洛地平和雷公藤内酯醇)并增强它们的渗透能力,因此在经皮给药方面对微乳剂的探索激增。微乳剂纳米级液滴极低的表面张力以及界面面积的大幅增加影响药物透过皮肤。有大量的油和表面活性剂可供使用,它们可作为经皮给药微乳剂系统的成分,但它们的毒性、刺激潜力和作用机制不明确限制了它们的使用。除了表面活性剂外,油也可作为渗透促进剂(油酸、亚油酸、肉豆蔻酸异丙酯、棕榈酸异丙酯等)。微乳剂的经皮给药潜力不仅取决于载体中所使用的成分,还极大地取决于各相的组成/内部结构,这可能会促进或阻碍药物在载体中的分布。本文探讨了微乳剂作为经皮给药载体,重点关注用于增强药物渗透和这些系统的皮肤耐受性的成分选择以及未来进一步的发展方向。