The effect of component of microemulsions on transdermal delivery of buspirone hydrochloride.
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.
Graduate Institute of Clinical Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan, Republic of China.
Yi-Hung
YH
Tsai
Jung Tzu
JT
Chang
Jui-Sheng
JS
Chang
Chi-Te
CT
Huang
Yaw-Bin
YB
Huang
Pao-Chu
PC
Wu
D000279:Administration, Cutaneous; D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage*; D002065:Buspirone / Q000008:administration & dosage*; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions; D005260:Female; D057927:Hydrophobic and Hydrophilic Interactions; D066298:In Vitro Techniques; D010316:Particle Size; D010539:Permeability; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects; D012995:Solubility; D013997:Time Factors; D014783:Viscosity
D014151:Anti-Anxiety Agents; D004337:Drug Carriers; D004655:Emulsions; D002065:Buspirone