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http://dx.doi.org/10.4333/KPS.2005.35.4.233

Formulation Design and Evaluation of Ursolic Acid Microemulsion Delivery System for Topical Formulation  

Park, Jong-Hee (College of Pharmacy, Chungnam National University)
Kyong, Kee-Yeol (College of Pharmacy, Chungnam National University)
Lee, Gye-Won (Dept. of Pharmaceutical Engineering, Konyang University)
Jee, Ung-Kil (College of Pharmacy, Chungnam National University)
Publication Information
Journal of Pharmaceutical Investigation / v.35, no.4, 2005 , pp. 233-241 More about this Journal
Abstract
Ursolic acid (UA), a bioactive triterpene acid, has been known to increase collagen content in human skin in addition to other actions such as anti-inflammatory, skin-tumor prevention and anti-invasion. However, it is poorly soluble in water. Therefore, we firstly prepared microemulsion system with benzyl alcohol, ethanol and Cremophor EL, RH 40 and Brij 35 as surfactant in order to increase solubility of UA and then prepared microemulsion was dispersed in o/w cream base for the topical delivery of UA in an effort to improve anti-wrinkle effect. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using benzyl alcohol as an oil, Cremophor EL, RH 40 and Brij 35 as a surfactant. The droplet size of microemulsions was characterized by dynamic light scattering. The accumulation of VA in the skin from topical cream was evaluated in vitro using hairless mouse skins. The mean droplet size was $26.8{\pm}6.6$ nm for microemulsions II with Cremophor EL. All UA creams showed pseudoplastic flow and hysterisis loop in their rheogram, depending on the type of materials added in topical creams. The in vitro accumulation data demonstrated the UA topical cream prepared with the combination of Poloxamer 407 and Xanthan gum as a copolymer showed higher accumulation percentage than those prepared with either Poloxamer 407 or Xanthan gum. These results suggest that UA topical cream using microemulsion systems may be promising for the topical delivery of UA.
Keywords
Microemulsion; Cream; Ursolic acid; Cremophor EL;
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