Polymethacrylate Microparticles Gel for Topical Drug Delivery
Polymethacrylate Microparticles Gel for Topical Drug Delivery
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DOI：
10.1007/s11095-010-0212-9
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发表时间：
2010-07-24
影响因子：
4.300
通讯作者：
Labiba K. El-Khordagui
中科院分区：
文献类型：
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作者：
Hagar Ibrahim Labouta;Labiba K. El-Khordagui
评价微粒给药系统在局部给药中的潜力：以具有局部应用潜力的亲水性药物盐酸维拉帕米（VRP）为模型药物，采用Eudragit RS 100和Eudragit L 100制备了聚甲基丙烯酸酯微粒（MP），用于制备复合局部凝胶。研究了初始载药量、聚合物组成，特别是作为相互作用聚合物组分的Eudragit L100的比例和分散剂的HLB对MP特性的影响。将测试MP制剂掺入凝胶中并评价药物释放和人皮肤渗透性。混合聚合物基质的组成是MP特性，特别是药物释放的主要决定因素。已知影响药物释放的因素，如MP大小和高药物溶解度，被强大的VRP-Eudragit L100相互作用所超过。与游离药物凝胶相比，所开发的MPs凝胶显示出受控的VRP释放和减少的皮肤滞留。局部药物递送和皮肤滞留可以使用微粒递送系统来调节。从实用的角度来看，开发的VRP凝胶可以在一系列皮肤病条件下提供优势，以应对日益增长的VRP标签外局部使用。
Evaluating the potentials of particulate delivery systems in topical drug delivery.Polymethacrylate microparticles (MPs) incorporating verapamil hydrochloride (VRP) as a model hydrophilic drug with potential topical clinical uses, using Eudragit RS100 and Eudragit L100 were prepared for the formulation of a composite topical gel. The effect of initial drug loading, polymer composition, particularly the proportion of Eudragit L100 as an interacting polymer component and the HLB of the dispersing agent on MPs characteristics was investigated. A test MPs formulation was incorporated in gel and evaluated for drug release and human skin permeation.MPs showed high % incorporation efficiency and % yield. Composition of the hybrid polymer matrix was a main determinant of MPs characteristics, particularly drug release. Factors known to influence drug release such as MPs size and high drug solubility were outweighed by strong VRP-Eudragit L100 interaction. The developed MPs gel showed controlled VRP release and reduced skin retention compared to a free drug gel.Topical drug delivery and skin retention could be modulated using particulate delivery systems. From a practical standpoint, the VRP gel developed may offer advantage in a range of dermatological conditions, in response to the growing off-label topical use of VRP.