Synthesis and characterization of surface-active compounds derived from cholesterol derivatives and glucose

The synthesis and characterization of surface-active compounds based on various steroid derivatives and glucose are presented. The hydrophobic and hydrophilic parts of the compounds were linked via glucosidic bonds. All compounds were found to have very low water solubility and only limited solubility in various organic solvents. The compounds were investigated according to their ability to interact with an anionic surfactant, sodium dodecylsulfate (SDS), in order to induce a decrease in the critical micelle concentration (CMC) of the surfactants. This synergistic effect was pronounced for cholestanol-6-on-β-D-glucopyranoside and for cholestan-3,6-diol-β-D-glucopyranoside. These two compounds lowered the CMC from 8 to 6 and 0.6 mM, respectively, for water solutions of SDS/glucoside with a molar ratio of 92∶8. Furthermore, the ability of the compounds to stabilize lipid membranes, in liposomes, at varying concentrations of Ca²⁺, was studied. The compounds were, as expected, found to induced stabilization similar to that of cholesterol.     

Adaptation of a Biomineralization Strategy for Remineralization of Enamel and Dentin

1Introduction Theextra cellularphospholipidshavebeendetectedmainlyattheperipheryofthecalcifyingnodules.Matrix vesicles,whichareconsideredapossiblesourceofextra cellularphospholipids[1].Electronmicroscopystudiesofmineralizingtissueshaverevealedthattheiniti…     

Permeability changes caused by surfactants in liposomes that model the stratum corneum lipid composition

The alterations caused by different surfactants in the permeability of liposomes formed by a lipid mixture that models the stratum corneum (SC) composition (40% ceramides, 25% cholesterol, 25% palmitic acid, and 10% cholesteryl sulfate) were investigated. The surfactant/lipid molar ratios (Re) and the bilayer/aqueous phase surfactant partition coefficients (K) were determined at two sublytic levels. The selected surfactant were sodium dodecyl sulfate (SDS); sodium dodecyl ether sulfate (SDES) to assess the influence of the ethylene oxide groups on the anionic surfactant’s behavior; Triton X-100 (OP-10EO) and dodecyl betaine (D-Bet) as representatives of nonionic and amphoteric surfactants. Permeability alterations were determined by monitoring the increase in the fluorescence intensity of liposomes due to the 5(6) carboxyfluorescein (CF) released from the interior of vesicles. The SC liposomes/surfactant sublytic interactions were mainly ruled by the action of surfactant monomers. OP-10EO showed the highest ability to alter the permeability of bilayers and the highest affinity with these structures, whereas D-Bet showed the lowest tendencies. Although SDS and SDES exhibited similar activity at 50% CF release (similar Re values), SDES appeared to be more active at 100% CF release, its affinity with bilayers being also increased. The different ability exhibited by SDS, SDES, and D-Bet (same alkyl chainlength) to alter the permeability of SC liposomes emphasizes the role played by the polar part of these surfactants in this interaction. Different trends in the evolution of Re and K were observed when comparing the results with those reported for phosphatidylcholine (PC) liposomes. Thus, whereas SC liposomes appeared to be more resistant to the action of surfactants, the surfactant affinity with SC bilayers was always greater than that reported for PC bilayers.     

神经酰胺及其脂质体技术的国内外研究动态

介绍了Ceramides（神经酰胺）及其脂质体技术在化妆品、食品和药品等方面的应用，以及最新的研究进展。     

熊果苷脂质体的制备研究

采用逆相蒸发制备熊果苷脂质体,研究了熊果苷脂质体配方中不同成分的比例、水合介质及高压挤压工艺对脂质体包封率的影响。结果表明:较佳的配方组成为大豆磷脂PC、胆固醇、熊果苷的质量比为400∶34∶136;投药比越大,包封率越低;较佳的水合介质是葡萄糖溶液。高压挤压工艺不利于得到较高包封率的熊果苷脂质体。     

溶胶-凝胶法固定化木瓜蛋白酶的活性保护

选择糖和脂质体作为溶胶-凝胶法固定木瓜蛋白酶(Papain)过程中的保护剂. 研究了蔗糖、葡萄糖、海藻糖、木糖、麦芽糖及构成脂质体的正癸烷溶液中胆固醇含量、卵/胆比等因素对固定化酶活性的影响. 结果表明,80 mL 20 mg/mL Papain溶液与15 mg木糖、500 mL正癸烷溶液[溶有1.5%(w)胆固醇,卵磷脂/胆固醇质量比为4.5:1]充分混合后制备的固定化酶活性最高. 在优化条件下制备的固定化酶包封率为42.0%,活力回收率为61.2%. SEM分析表明,固定化酶形态呈球状且大小均匀,内孔分布呈蜂窝状. 破膜剂对固定化酶活性发挥的影响研究表明,TritonX-100的效果最好.     

全新的化妆品活性成份的稳定超微载体Nanotope~(TM)——纳能托~[注]及其与普通脂质体的性能比较

介绍了一种全新的平均粒径为２５ｎｍ左右的化妆品活性物的超微载体系统ＮａｎｏｔｏｐｅＴＭ（纳能托［注］）。它对皮肤具有高覆盖率和强渗透性。它比普通脂质体更耐表面活性剂,并具有良好的ｐＨ值和离子强度的适应性,是一种比脂质体、纳球、纳颗粒以及纳乳液都稳定且粒径分布均匀的纳胶体。运用动态光散射法及浊度法研究了ＮａｎｏｔｏｐｅＴＭ（纳能托［注］）及脂质体在一系列不同表面活性剂中的稳定性及其粒径分布。讨论了该超微载体系统的应用前景。     

佛手精油脂质体的制备及其抗氧化活性

以大豆卵磷脂和胆固醇作为壁材,采用薄膜分散-高压均质法制备佛手精油脂质体。以脂质体粒径、Zeta电位和包封率为指标筛选工艺参数和配方参数,确定脂质体最佳制备工艺,并对脂质体的形貌、稳定性进行考察,同时研究其抗氧化活性。结果表明,佛手精油脂质体的最佳制备工艺参数为:均质压力120 MPa、均质次数5次、磷脂/胆固醇比例5:1、精油添加量3.5 mg/mL。在此条件下制备的脂质体粒径为183.53 nm,PDI多分散指数为0.147,Zeta电位值为38.75 mV,包封率为47.23%,载药量为1.67 mg/mL。所制备的脂质体具有良好的离心稳定性、贮藏稳定性4℃贮藏30 d,精油保留率为85.03%,对DPPH、ABTS、羟基自由基的清除率分别为82.58%、78.02%、70.89%。结论:在均质压力120MPa、均质次数5次、磷脂/胆固醇比例5:1、精油添加量3.5mg/m L的条件下,制备的脂质体粒径适中、稳定性良好,具有良好的抗氧化活性。     

硫酸头孢喹肟脂质体的制备工艺

采用固体分散技术结合泡腾技术制备硫酸头孢喹肟脂质体,考察了减压旋转蒸发温度、氯仿用量、大豆卵磷脂/胆固醇质量比、吐温-80用量、药/脂质量比、柠檬酸与NaHCO3用量对脂质体外观形态和包封率的影响. 通过正交实验优化制备条件,并探讨了脂质体的形成机制. 结果表明,制备硫酸头孢喹肟脂质体的优化条件为：大豆卵磷脂/胆固醇/吐温-80/柠檬酸/NaHCO3的质量比为37:18:5:33:7,药/脂质量比1:10. 该条件下所制脂质体外观形态良好,粒径分布均匀,平均粒径为(203±5) nm,平均包封率为55.17%±0.44%,平均载药量为5.04%±0.02%.     

降温速率对脂质体冻干品质量影响的实验研究

脂质体冻结过程中形成的冰晶不仅会对脂质体囊泡造成损伤,而且会影响热量的传递和水蒸气的逸出。研究了含有海藻糖的脂质体悬浮液在不同的降温速率下的冻干品质量,比较了不同降温速率下冻干脂质体的温度变化曲线和含水量变化曲线,及冻干脂质体复水后的囊泡粒径变化。结果表明,对于脂质体快速冻结后得到的冻干品质量优于慢速冻结。