|
|
|
| Effect of different penetration enhancers on the transdermal absorption of phloretin |
| GUAN Bo1 HUANGFU Junru2 XU Yuan1 ZHOU Xuejiao3 LIU Xueying4 WANG Qingwei1 |
1.Department of Pharmacy, the Second Affiliated Hospital of Air Force Medical University, Shaanxi Province, Xi′an 710038, China;
2.Product Department, Ginwa Pharmaceutical Factory, Shaanxi Province, Xi′an 710065, China;
3.Department of Pharmacy, Xi′an Chest Hospital, Shaanxi Province, Xi′an 710075, China;
4.Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Air Force Medical University, Shaanxi Province, Xi′an 710032, China |
|
|
|
Abstract Objective To investigate the effect of azone, menthol, borneol and muscone on the transdermal promotion of phloretin in order to provide basis for the research and development of external preparations of phloretin. Methods The skin of 18 male SD rats with 2-month-old as the permeation barrier, the Franz diffusion cell was used to conduct the in vitro transdermal absorption experiment. The content of phloretin was determined by HPLC, the permeation kinetic parameters were calculated, and the permeation promoting effect of different transdermal enhancers on phloretin was evaluated. HPLC method for the determination of phloretin was as followed, chromatographic column: Inertsil ODS-3 (150 mm×4.6 mm, 5 μm); mobile phase: acetonitrile water (45:55); flow rate: 1.0 mL/min; detection wavelength: 280 nm; injection volume: 20 μL; column temperature: 25℃. Results The regression equation of phloretin in the concentration range of 0.1030-51.48 μg/mL was Y = 86.45C+3.901 (r = 0.9999). RSD of intraday and intraday precision was less than 2.0%. When the concentrations of azone, menthol, borneol and muscone were 4.0%, ER was 8.825, 13.561, 6.540 and 3.466 respectively. Conclusion Azone, menthol, borneol and muscone can enhance the transdermal effect of phloretin in a concentration-dependent manner. 4.0% penetration enhancer has the best promoting effect. The better transdermal enhancer for phloretin is menthol.
|
|
|
|
|
|
[1] Bentsáth A，Szentgy?觟rgyi A. Vitamin P [J]. Nature，1937， 140（3540）：426.
[2] Rusznyák S，Szent-Gy?觟rgyi A. Vitamin P：flavonols as vitamins [J]. Nature，1936，138（3479）：27.
[3] Heim KE，Tagliaferro AR，Bobilya DJ. Flavonoid antioxidants：chemistry，metabolism and structure-activity relationships [J]. J Nutr Biochem，2002，13（10）：572-584.
[4] 陆晓宇，曾耀英，叶燕霞，等.根皮素的抗炎和免疫抑制作用[J].药学学报，2009（5）：480-485.
[5] Rezk BM，Haenen GR，van der Vijgh WJ，et al. The antioxidant activity of phloretin：the disclosure of a new antioxidant pharmacophore in flavonoids [J]. Biochem Biophys Res Commun，2002，295（1）：9-13.
[6] 王会，吴汉东，刘政.根皮素对胃癌细胞SGC-7901凋亡的影响及可能机制[J].中国生化药物杂志，2015，35（8）：34-37.
[7] 单良，肖建英.根皮素对人卵巢癌细胞增殖的影响及虚拟筛选研究[J].中药材，2018，41（6）：1480-1486.
[8] 李岷，甄雅贤.外用含维生素C、阿魏酸和根皮素的抗氧化制剂对紫外线诱导的皮肤光损伤的保护功效[J].中华皮肤科杂志，2010，43（6）：447.
[9] 焦鹏飞.根皮素的心血管保护作用研究[J].现代医药卫生，2012，28（9）：1284-1286.
[10] Lee EJ，Kim JL，Kim YH，et al. Phloretin promotes osteoclast apoptosis in murine macrophages and inhibits estrogen deficiency-induced osteoporosis in mice [J]. Phytomedicine，2014，21（10）：1208-1211.
[11] Vasantha Rupasinghe HP，Yasmin A. Inhibition of oxidation of aqueous emulsions of omega-3 fatty acids and fish oil by phloretin and phloridzin [J]. Molecules，2010， 15（1）：251-257.
[12] 刘斌，王红，韩俊泉，等.中药经皮给药及透皮吸收研究进展[J].中国中西医结合外科杂志，2012，18（6）：641-643.
[13] 张红，张华，张伟.促进药物透皮吸收方法研究进展[J].辽宁中医药大学学报，2015，17（8）：101-104.
[14] 畅敏，王庆伟，刘新友，等.反相高效液相色谱法测定根皮素溶解度[J].中国医药导报，2011，8（32）：33-34.
[15] 冯鑫.挥发油促透作用适用性研究进展[J].中成药，2013， 35（1）：157-161.
[16] 冯甜，王力彬，周楠，等.根皮素的研究进展[J].转化医学杂志，2017，6（1）：42-46.
[17] 黄钊.薄荷醇通过影响皮肤KC内PLC活性而产生促透作用的研究[D].广州：广东药学院，2013.
[18] 林桂涛，刘新.氮酮对痹舒巴布剂体外透皮吸收影响的研究[J].山东中医药大学学报，2007（4）：326-328.
[19] 郭淑娟，杨畅，陈丽萍，等.不同基源冰片促透效果的差异研究[J].环球中医药，2019，12（3）：348-352.
[20] 党学良，赵军，李晰，等.不同促透剂对Ex-RAD凝胶体外透皮吸收的影响[J].医药导报，2016，35（10）：1050-1054. |
|
|
|
