药物—油相性质对药物纳米晶自稳定Pickering乳液构建的影响研究(1)
[摘要] 探究药物及油相性质对药物纳米晶自稳定Pickering乳液(nanocrystalline self-stabilized Pickering emulsions，NSSPE)成型与稳定的影响。分别以葛根素、丹参酮ⅡA和阿魏酸3种难溶性中药成分自身纳米晶为固体微粒，以Capmul C8、Fabrafil M 1944 CS、肉豆蔻酸异丙酯、川芎油、橄榄油为油相，高压匀质法制备NSSPE。以室温静置14 d 后NSSPE的外观、离心稳定性、乳滴粒径变化以及乳液层药物含量变化为指标对NSSPE进行评价。分析油相的性质(表面张力、黏度)、药物的性质(表面能、油水分配系数、纳米晶粒径、Zeta电位及药物-水-油的三相接触角)等对NSSPE成型与稳定的影响。以阿魏酸纳米晶为固体微粒制备的5种油相的样品，成乳性和稳定性均明显差于葛根素和丹参酮ⅡA；阿魏酸纳米晶的粒径高达3.90 μm，极显著高于葛根素的305 nm和丹参酮ⅡA的406 nm(P<0.05)；阿魏酸纳米晶的Zeta电位为-0.018 0 mV，极显著低于葛根素的-29.1 mV和丹参酮ⅡA的-42.6 mV(P<0.05)。以肉豆蔻酸異丙酯为油相制备的3种药物的样品均不成乳状；肉豆蔻酸异丙酯的黏度为4.67 mPa·s，极显著低于其余各油(P<0.01)。以川芎油为油相制备的葛根素-NSSPE成乳性和稳定性最好；葛根素在川芎油-水中的接触角为69.7°，接近90°，且显著高于其余各接触角。药物为丹参酮ⅡA时，Capmul C8和Labrafil M 1944 CS制备的NSSPE稳定性最好，其接触角分别为99.2°和112°，较其余油相更近接90°。油相的黏度、药物纳米晶粒径、Zeta电位及三相接触角对NSSPE成型与稳定有较大影响；而油相的表面张力、药物的表面能和油水分配系数可能与NSSPE的构建不相关。
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[关键词] Pickering乳液； 葛根素； 丹参酮ⅡA； 阿魏酸； 纳米晶； 自稳定
[Abstract] To investigate the effects of drug and oil properties on the formation and stability of drug nanocrystalline self-stabilizied Pickering emulsions (NSSPE). Three insoluble Chinese medicine components (puerarin， tanshinone ⅡA and ferulic acid) were selected as model drugs， and Capmul C8， Fabrafil M 1944 CS， isopropyl myristate， Pzechwan Lovage Rhizome oil， and olive oil were used as oil phase. NSSPEs were developed by high pressure homogenization method and were evaluated for their appearance， centrifugal stability， droplet size and drug content changes in emulsion layer after storing at room temperature for 14 d. Then the properties of the oil (surface tension and viscosity) and properties of the drugs (surface energy， oil-water partition coefficient， size and Zeta potential of nanocrystalline and drug-water-oil contact angle) on the formation and stability of NSSPE were analyzed. The emulsification property and stability of five samples prepared with ferulic acid nanocrystals and different oils were significantly lower than those of puerarin and tanshinone ⅡA； the particle size of ferulic acid nanocrystals was 3.90 μm， extremely higher than 305 nm of puerarin and 406 nm of tanshinone ⅡA (P<0.05)； the zeta potential of ferulic acid nanocrystals was -0.018 0 mV， significantly lower than -29.1 mV of puerarin and -42.6 mV of tanshinone ⅡA (P<0.05). Three samples prepared with isopropyl myristate and different drugs were not emulsions and the viscosity of isopropyl myristate was 4.67 mPa·s， significantly lower than that of the other oils (P<0.01). Puerarin-NSSPEs prepared with Pzechwan Lovage Rhizome oil showed best emulsification property and stability； the contact angle of puerarin in Pzechwan Lovage Rhizome oil-water was 69.7°， close to 90°， significantly higher than other contact angles. NSSPEs made by tanshinone ⅡA-Capmul C8-water， tanshinone ⅡA-Labrafil M 1944 CS-water showed highest stability， with a contact angle of 99.2° and 112° respectively， more close to 90° than other oils. The results indicated that viscosity， size and Zeta potential of nanocrystalline and three-phase contact angle had great influence on the formation and stability of NSSPE； surface tension of oil， surface energy of drug and oil-water partition coefficient may not be related to the construction of NSSPE., 百拇医药(王帆 王帅 易涛 张继芬)
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[关键词] Pickering乳液； 葛根素； 丹参酮ⅡA； 阿魏酸； 纳米晶； 自稳定
[Abstract] To investigate the effects of drug and oil properties on the formation and stability of drug nanocrystalline self-stabilizied Pickering emulsions (NSSPE). Three insoluble Chinese medicine components (puerarin， tanshinone ⅡA and ferulic acid) were selected as model drugs， and Capmul C8， Fabrafil M 1944 CS， isopropyl myristate， Pzechwan Lovage Rhizome oil， and olive oil were used as oil phase. NSSPEs were developed by high pressure homogenization method and were evaluated for their appearance， centrifugal stability， droplet size and drug content changes in emulsion layer after storing at room temperature for 14 d. Then the properties of the oil (surface tension and viscosity) and properties of the drugs (surface energy， oil-water partition coefficient， size and Zeta potential of nanocrystalline and drug-water-oil contact angle) on the formation and stability of NSSPE were analyzed. The emulsification property and stability of five samples prepared with ferulic acid nanocrystals and different oils were significantly lower than those of puerarin and tanshinone ⅡA； the particle size of ferulic acid nanocrystals was 3.90 μm， extremely higher than 305 nm of puerarin and 406 nm of tanshinone ⅡA (P<0.05)； the zeta potential of ferulic acid nanocrystals was -0.018 0 mV， significantly lower than -29.1 mV of puerarin and -42.6 mV of tanshinone ⅡA (P<0.05). Three samples prepared with isopropyl myristate and different drugs were not emulsions and the viscosity of isopropyl myristate was 4.67 mPa·s， significantly lower than that of the other oils (P<0.01). Puerarin-NSSPEs prepared with Pzechwan Lovage Rhizome oil showed best emulsification property and stability； the contact angle of puerarin in Pzechwan Lovage Rhizome oil-water was 69.7°， close to 90°， significantly higher than other contact angles. NSSPEs made by tanshinone ⅡA-Capmul C8-water， tanshinone ⅡA-Labrafil M 1944 CS-water showed highest stability， with a contact angle of 99.2° and 112° respectively， more close to 90° than other oils. The results indicated that viscosity， size and Zeta potential of nanocrystalline and three-phase contact angle had great influence on the formation and stability of NSSPE； surface tension of oil， surface energy of drug and oil-water partition coefficient may not be related to the construction of NSSPE., 百拇医药(王帆 王帅 易涛 张继芬)