Abstract
Purpose: To enhance the stability and reduce photo-degradation of phenylethyl resorcinol (PR) by elastic vesicle formation.Methods: PR solution was stored at different temperatures, pH conditions, and under protected and unprotected natural light. The color of the solution and total active content were investigated. Three types of elastic vesicles, viz, ethosomes, transfersomes and invasomes, were prepared and their sedimentation in formulations and total active content were investigated before and after storage under various conditions for 4 months. The stability of the solutions and vesicular formulations were assessed.Results: PR solution was unstable at pH 9, higher temperature (70 ± 1 oC) and under natural light. The color of PR solution changed from colorless to orange tone and the PR content decreased. On the other hand, PR entrapped within ethosome, tranfersome and invasome vesicles showed better stability, color change was not observed in the formulations, and PR content remained > 90 %.Conclusion: All the vesicles display reduced degradation of PR under thermal and natural light. Thus, PR vesicular formulation enhances stability and improves the quality of the product for use in topical administration.Keywords: Phenylethyl resorcinol, Degradation, Ethosomes, Transfersomes, Invasomes, Topical administration
Highlights
Phenylethyl Resorcinol (4 - (1- Phenylethyl) 1, 3Benzenediol, phenylethyl resorcinol (PR)) is a recently introduced skinlightening agent that can interrupt tyrosinase activity by obstructing tyrosine being converted to L-3,4-dihydroxyphenylalanine (L-DOPA) [1]
It served as an antioxidant, which is more effective than butylated hydroxytoluene (BHT), ascorbic acid, and alpha tocopherol [3]
In this study, elastic vesicle carriers such as PR-loaded ethosomes, transfersomes and invasomes were assessed for overcoming the limitation of using PR for topical products
Summary
Phenylethyl Resorcinol (4 - (1- Phenylethyl) 1, 3Benzenediol, PR) is a recently introduced skinlightening agent that can interrupt tyrosinase activity by obstructing tyrosine being converted to L-3,4-dihydroxyphenylalanine (L-DOPA) [1]. An excess amount of PR was added in glass vials holding 5 ml hydrochloric acid buffer having pH 2.0, acetate buffer having pH 5.5, and phosphate buffer having pH 7.4 and 9.0 which was prepared in consonance with USP 30 [12] These samples were first sonicated for 30 minutes, preserved at room temperature (30 ± 1 oC) for 48 and 72 hours to determine if the solubility of PR has reached equilibrium. On study day 0, 0.5, 1, 3, 5, 7, 14 and 30 days, the 500 μl of sample was collected, filtered using a 0.45 μm syringe filter membrane and analyzed using HPLC to determine the concentration of PR These experiments were reciprocated for 3 times, and all the samples were examined in triplicate. The statistically significant value was considered at P < 0.05
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