Preparation of nanosuspension-based gel of Ganoderma lucidum triterpenoids and its in vitro transdermal diffusion characteristics / 中草药

Objective: To prepare the nanosuspension-based gel of Ganoderma lucidum triterpenoids (GT-NS-gel) and investigate the in vitro transdermal diffusion characteristics. Methods: GT-NS was prepared by high pressure homogenization and then transformed into gel. The formulation of GT-NS-gel was optimized by response surface method with cumulative release of drug from the GT-NS-gel within 24 h, and the amount of drug in the skin after applying GT-NS-gel for 24 h was used as indexes. In vitro percutaneous permeation and skin deposition of GT-NS-gel were studied and compared with those of GT-gel. Results: The GT-NS-gel prepared by optimal formulation (5 mg/g Carbomer 940, 30 mg/g GT, and 47.2 mg/g lecithin) could release in vitro at 24 h to (56.28±2.16)%, and the amount of drug in the skin after applying GT-NS-gel for 24 h was (472.89±8.74) μg/cm2. There was a little deviation between the theoretically predicted value and the measured value. It showed that this model had a good prediction. The amounts of GT penetrating through the skin and in the skin after applying GT-NS-gel for 24 h were (50.73±4.97) and (475.89±10.74) μg/cm2, which were significantly higher than GT-gel (P<0.05). Conclusion: The GT-NS-gel has the ability to increase drug concentration in the skin, which can improve the bioavailability of the local skin.

Enhanced In Vitro Skin Deposition Properties of Retinyl Palmitate through Its Stabilization by Pectin

The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin demonstrated significantly increased RP distributions in the epidermis. Furthermore, it was found that skin distribution of RP could be further improved by combined use of pectin and ascorbyl palmitate (AP), due largely to their anti-oxidative effect. These results clearly demonstrate that the skin deposition properties of RP can be improved by stabilizing RP with pectin. Therefore, it is strongly suggested that pectin could be used in the pharmaceutical and cosmetic formulations as an efficient stabilizing agent and as skin penetration modulator.

Enhanced In Vitro Skin Deposition Properties of Retinyl Palmitate through Its Stabilization by Pectin

The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin demonstrated significantly increased RP distributions in the epidermis. Furthermore, it was found that skin distribution of RP could be further improved by combined use of pectin and ascorbyl palmitate (AP), due largely to their anti-oxidative effect. These results clearly demonstrate that the skin deposition properties of RP can be improved by stabilizing RP with pectin. Therefore, it is strongly suggested that pectin could be used in the pharmaceutical and cosmetic formulations as an efficient stabilizing agent and as skin penetration modulator.