Graduate Institute of Clinical Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan, Republic of China.
J Pharm Sci. 2011 Jun;100(6):2358-65. doi: 10.1002/jps.22474. Epub 2011 Jan 18.
The aim of this study was to evaluate the influence of components such as type, level, and hydrophilic-lipophilic balance (HLB) value of surfactant, type and amount of cosurfactant, and drug concentration on the permeability of buspirone hydrochloride microemulsions through rat skin. The cumulative amount at 24 h ranged from 502.2 ± 57.8 to 1754.3 ± 616.6 μg/cm(2), flux ranged from 23.03 ± 1.84 to 83.36 ± 25.08 μg/(cm(2)/h), and lag time ranged from 3.0 to 4.7 h, indicating that the permeation parameters of buspirone from microemulsions were markedly influenced by the composition of microemulsions. In comparison with the effect of composition of microemulsions on the buspirone permeation capacity, it was found that microemulsions containing surfactant with HLB value of 11.16 possessed higher flux. The viscosity of microemulsions increased, flux decreased, and lag time was prolonged when amount of surfactant in microemulsions increased. The various cosurfactants can also influence the microemulsion formation and drug permeability. The microemulsion with ethanol as cosurfactant had higher permeation rate. However, the buspirone microemulsion with higher flux can provide the therapeutic minimum effective concentration, at workable administrated area about 3.3-5.8 cm(2), demonstrating microemulsions could be a promising drug carrier for transdermal delivery systems.
本研究旨在评估表面活性剂的类型、浓度和亲水亲油平衡值（HLB）、助表面活性剂的类型和用量以及药物浓度等因素对盐酸丁螺环酮微乳经皮渗透的影响。24 小时累积渗透量在 502.2±57.8μg/cm(2)至 1754.3±616.6μg/cm(2)之间，渗透通量在 23.03±1.84μg/(cm(2)/h)至 83.36±25.08μg/(cm(2)/h)之间，滞后时间在 3.0 至 4.7 小时之间，表明微乳的组成对丁螺环酮的渗透参数有显著影响。与微乳组成对丁螺环酮渗透能力的影响相比，发现 HLB 值为 11.16 的表面活性剂的微乳具有更高的通量。当微乳中表面活性剂的用量增加时，微乳的粘度增加，通量降低，滞后时间延长。各种助表面活性剂也可以影响微乳的形成和药物的渗透性。含有乙醇作为助表面活性剂的微乳具有更高的渗透速率。然而，具有更高通量的丁螺环酮微乳可以提供治疗的最低有效浓度，在可管理的给药面积约为 3.3-5.8cm(2)，表明微乳可以作为一种有前途的经皮给药系统的药物载体。
