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Preparation And Properties Studies Of Nanoliposomes/lipid Nanovesicles Loaded Phenylethyl Resorcinol

Posted on:2023-02-10Degree:MasterType:Thesis
Country:ChinaCandidate:H XiaFull Text:PDF
GTID:2531307046994249Subject:Biological engineering
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Phenylethyl resorcinol(PR)is a new type of high-efficiency tyrosinase inhibitor discovered in recent years,which can effectively inhibit tyrosinase activity and reduce the production of melanin,and has been used as an effective whitening and brightening active ingredient in skin whitening cosmetics.However,PR has problems such as poor water solubility,unstable light,strong skin irritation and poor transdermal absorption,which greatly affects its whitening and skin care effect.In the study,nanocarrier technology was used to prepare and optimize PR-loaded nanoliposomes(PR-NLPs)and PR-loaded lipid nanovesicles(PR-LNVs)to solve problems of poor water solubility,light instability,low bioavailability and poor transdermal absorption performance of PR in practical applications.Firstly,PR-NLPs were prepared by ethanol injection method,and the optimal formulation was optimized by single-factor investigation experiment and Box-Behnken response surface design,and determined as follows: lecithin concentration of 50 mg/m L,cholesterol content of 17.5%,PR content of 10% and 0.5% Tween?80 aqueous solution.The prepared PR-NLPs were spherical vesicles with a bilayer membrane structure,with the mean size of 130.1±3.5 nm,good dispersibility(polydispersity index of 0.23±0.02 and Zeta potential of-43.9±3.4 m V),and loading content(LC)and encapsulation efficiency(EE)of 8.8±0.6% and 96.81±3.46%,respectively.The results of the stability investigation showed that PR-NLPs had good photostability to PR and could be stored stably for at least 3 months at 4°C and 25°C under dark conditions.Secondly,PR-LNVs were prepared by high pressure homogenization,and the formulation and preparation process was optimized by the single factor method.The optimal preparation process was determined as follows: lecithin content of 6%,GTCC content of 5%,PR content of 3%,glycerol content of 40%,and the high-pressure homogenization pressure was 1100 bar,and the number of homogenization cycles was 3 times.The results showed that the optimized PR-LNVs were spherical vesicles with a single-layer membrane structure,with the mean size of 132.4±1.4nm,good dispersibility(polydispersity index of 0.14±0.01),and EE of 97.37±6.14%,the load of PR was 3%.By examining the stability of PR-LNVs,the results showed that PR-LNVs had good freeze-thaw stability and thermal stability,and could be stored stably for at least 3 months at 4°C and 25°C.Finally,through the biocompatibility evaluation of PR-NLPs and PR-LNVs in three aspects:blood compatibility,skin irritation,and cytotoxicity,it was proved that the prepared PR-NLPs and PR-LNVs had good properties of biological safety.The delivery properties of PR-NLPs and PRLNVs were evaluated by in vitro release,cellular uptake behavior,and in vitro and in vivo transdermal absorption experiments.Experiments showed that both PR-NLPs and PR-LNVs had sustained release ability,which could enhance the uptake efficiency of cells and improve the transdermal absorption capacity of PR.Compared with free PR,PR-NLPs and PR-LNVs significantly inhibited the activity and content of tyrosinase,reduced the production of melanin,and improved the whitening effect of PR.The above research results showed that PR-NLPs and PR-LNVs were used as nano-delivery carriers of PR,which could improve the water solubility and photostability of PR,enhance the transdermal absorption of PR,improve the whitening effect of PR,which was expected to provide a specific reference and theoretical basis for the practical application of PR in the field of cosmetics.
Keywords/Search Tags:Phenethyl Resorcinol, nanoliposomes, lipid nanovesicles, transdermal absorption, skin whitening
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