Night-use and day-use nanoemulsions as passive targeted transdermal drug delivery system for whitening skin and inhibiting pigmentation, and their preparation methods.

Abstract

The invention relates to night-use and day-use nanoemulsions as passive targeted transdermal drug delivery system (TDDS) for whitening skin and inhibiting pigmentation, and their prepn. methods. The night-use nanoemulsion is prepd. from (by g) iso-Pr myristate 2.0-8.0, labrasol 10-50, plurol oleique 2-20, triple distd. water 20-50, flavor 0.01-0.05, tocopheryl ferulate 1.0-6.0, kojic acid dipalmitate 0.5-5.0, asiaticoside 0.1-3.0, coenzyme Q10 0.1-5.0, L-ascorbic acid-2-glucoside 1.0-6.0, nicotinamide 1.0-6.0, β-raspberry ketone glucoside 1.0-6.0, α-arbutin 1.0-7.0, β-arbutin 1.0-7.0, cysteine 0.1-5.0, AR grade sodium hydroxide 0.2-1.0, and citric acid 0.2-2.0. The day-use whitening nanoemulsion is prepd. from (by g) iso-Pr myristate 5.0-20.0, labrasol 15.0-40.0, plurol oleique 5.0-15.0, triple distd. water 20.0-45.0, vitamin E 1.5-5.5, isooctyl ferulate 1.5-5.5, baicalin 0.2-2.0, glabridin soln. 3.0-8.0, L-ascorbic acid-2-glucoside 2.0-6.0, vitamin PP factor 2.0-6.0, N-acetylglucosamine 1.0-6.0, β-raspberry ketone glucoside 2.0-6.0, SymWhite 377 0.1-1.5, disodium ethylenediaminetetraacetate 0.1-1.5, citric acid 0.1-1.5 and sodium hydroxide 0.1-1.5. The night-use whitening nanoemulsion is prepd. by dissolving NaOH and citric acid with triple distd. water, adding L-ascorbic acid-2-glucoside, dissolving and adding β-raspberry ketone glucoside, nicotinamide, α-arbutin, β-arbutin and cysteine, ultrasonic shaking, detg. pH, and marking it for water phase (I); dissolving iso-Pr myristate, tocopheryl ferulate, kojic acid dipalmitate, asiaticoside, coenzyme Q10 and flavor, and marking it for oil phase (II); mixing labrasol (S) and plurol oleique (C), and marking it for S/C mixt. (III); placing water phase (I) and S/C (III) in a container; ultrasonic shaking for about 2 min or stirring for 2 min, adding oil phase (II), and ultrasonic shaking or stirring for 20 min; observing extrinsic feature; and filling in glass container, covering, sterilizing, packaging, and storing. The nanoemulsion has the advantages of good passive targeted action, good transdermal absorption performance, strong penetrability, even texture, good stability, etc. [on SciFinder(R)]