Lamellar Liquid Crystal Improves the Skin Retention of 3-O-Ethyl-Ascorbic Acid and Potassium 4-Methoxysalicylate In Vitro and In Vivo for Topical Preparation.
The study aimed at increasing the skin retention of 3-O-ethyl-ascorbic acid (EA) and potassium 4-methoxysalicylate (4-MSK) via topical administration for effective skin-whitening. To achieve this goal, EA and 4-MSK were formulated into lamellar liquid crystalline (LLC) cream, and response surface methodology (RSM) was employed to optimize the formulation. Polarized light microscopy (PLM), differential scanning calorimetry (DSC), and rheological experiments were performed to confirm the presence of the LLC structure in the base of cream. In addition, a comparison analysis of the skin retention of the two drugs between the LLC cream and the common o/w (COW) cream was made through in vitro permeation and in vivo drug distribution experiments. As a result, the optimal formulation was defined as 1.2% of EA, 1.48% of 4-MSK, 14.05% of Schercemol™ DISM Ester (DISM) as the oil, 4.0% of Emulium® Delta as the emulsifier, and 3.0% of stearyl alcohol as the co-emulsifier. In comparison with the COW cream, the LLC cream significantly increased the skin retention of EA and 4-MSK both in vitro and in vivo. In conclusion, the LLC carrier serves as a promising choice for topical preparation by enhancing skin retention and providing desirable rheological characteristics.
Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
Yuanru
Y
Li
Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
Cuilian
C
Dong
Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
Dongmei
D
Cun
Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
Jie
J
Liu
School of Medical Instrument, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Rongwu
R
Xiang
Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China. fangliangspu@aliyun.com.
Liang
L
Fang
D000287:Administration, Topical; D000818:Animals; D001205:Ascorbic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D050866:Liquid Crystals; D008297:Male; D051379:Mice; D011817:Rabbits; D012459:Salicylates / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology; D063465:Skin Cream / Q000008:administration & dosage / Q000493:pharmacokinetics*
D045703:Emulsifying Agents; D012459:Salicylates; C000594008:3-O-ethylascorbic acid; D001205:Ascorbic Acid
3-O-ethyl-ascorbic acid; lamellar liquid crystal; potassium 4-methoxysalicylate; response surface methodology; rheology