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用于增强对苯乙基间苯二酚包封的杂化聚合物微球。

Hybrid polymeric microspheres for enhancing the encapsulation of phenylethyl resorcinol.

机构信息

a College of Pharmacy and Institute of Drug Research and Development , Chungnam National University , Daejeon , Korea.

出版信息

J Microencapsul. 2019 Mar;36(2):130-139. doi: 10.1080/02652048.2019.1607598. Epub 2019 May 14.

DOI:10.1080/02652048.2019.1607598
PMID:30982372
Abstract

Phenylethyl resorcinol (PR) has been known to allow the whitening effect by inhibiting formation of tyrosinase. PR has solubility of 4.05 ± 0.02 mg/g for water and log of 3.017, proposed an amphiphilic substance. Hybrid PLGA microspheres with oil (HPMSs) have been used to improve encapsulation efficiency (EE) of hydrophilic molecules and control the release of them. The solubility (618.3 ± 22.29 mg/g) of PR was the highest in Capryol 90. The formulations (F6 and F`6) were selected after evaluation with EE and the released % (w/w) at 8 h. HPMSs showed 40% (w/w) increase of EE compared to that in CPMSs. Retention study on rat skin at 12 h resulted in that PR of HPMSs was remained more than that of CPMSs in dermal layer forming the melanin. HPMSs showed 1.4-fold increase of tyrosinase inhibition significantly in melanoma cells than that of the PR solution at 24 h.

摘要

苯乙基间苯二酚(PR)通过抑制酪氨酸酶的形成而具有美白效果。PR 在水中的溶解度为 4.05±0.02mg/g,log 为 3.017,是一种两亲性物质。油相混合 PLGA 微球(HPMSs)已被用于提高亲水分子的包封效率(EE)并控制其释放。PR 在 Capryol 90 中的溶解度(618.3±22.29mg/g)最高。在通过 EE 和 8 小时释放的%(w/w)进行评估后,选择了配方(F6 和 F`6)。与 CPMSs 相比,HPMSs 的 EE 增加了 40%(w/w)。在 12 小时的大鼠皮肤保留研究中,HPMSs 在真皮层形成黑色素中保留的 PR 多于 CPMSs。与 24 小时的 PR 溶液相比,HPMSs 在黑素瘤细胞中对酪氨酸酶的抑制作用增加了 1.4 倍。

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