双连续相微乳液制备连续孔聚丙烯酰胺凝胶

以十二烷基硫酸钠/甲苯/2-丁醇/盐水双连续微乳液相为模板,制备了3种组分双连续有机凝胶,水凝胶和有机/水杂化凝胶.12-羟基硬脂酸(12-HA)为有机凝胶剂.它们固定了水和油并使水和油微相共存于凝胶中.以静态光散射(SLS)测定了各双连续相微乳液的粒径,结果显示值在8～80nm.扫描电子显微镜观察了各凝胶的形貌,表明...     

双连续相微乳液制备多孔聚合物与表征

双连续相乳液制备多孔聚合物是以甲基丙烯酸丁酯单体(BMA),甲基丙烯酸甲酯单体(MMA)为油相,十二烷基硫酸钠(质量分数20%)水溶液为水相,丙烯酸(AA)为助乳化剂,偶氮二异丁腈(AIBN)为引发剂,在60℃聚合制备得到。利用扫描电镜和热重分析仪对产物的多孔结构进行表征,利用红外光谱和万能拉力机表征产物结构组成和拉伸性能等。研究了水相含量不同对聚合产物形貌的影响,扫描电镜和热重分析结果表明水相比例为40%和50%时,聚合产物为呈开孔结构的多孔聚合物。当水相比例30%时,其拉伸强度最大。     

聚苯乙烯/二乙烯基苯多孔材料的制备工艺研究

以高内相比乳液模板法制备了PS/DVB(聚苯乙烯/二乙烯基苯)多孔材料,研究了连续相的性质、致孔剂和乳化剂对PS/DVB多孔材料表面结构的影响.结果表明,连续相疏水性的提高有助于提高乳液的稳定性,致孔剂与PS之间良好的相容性有利于提高多孔材料的比表面积;复合乳化体系更能有效地降低乳液的界面张力,增加多孔材料的比表面积.     

双连续相微乳液聚合制备L-色氨酸分子印迹膜

以L-色氨酸(L-Trp)为模板分子,丙烯酸(AA)为功能单体,同时作为双连续相微乳液的乳化剂,采用光引发无皂双连续相微乳液聚合制备L-色氨酸分子印迹膜。考察了丙烯酸、L-色氨酸、骨架单体比例对印迹膜分离性能的影响,结果表明印迹膜对L-Trp具有良好的选择吸附性和优先渗透性,相比于结构类似物L-酪氨酸其分离因子可达1.97,具有良好的应用前景。     

聚丙烯/线型低密度聚乙烯开孔泡沫的制备及吸油性能

以超临界二氧化碳为发泡剂,通过连续挤出发泡法制备聚丙烯/线型低密度聚乙烯(PP/LLDPE)共混物开孔泡沫,并用于吸油性能研究。文中系统研究了发泡温度、原料配比和口模直径对PP/LLDPE泡沫开孔结构和吸油倍率的影响,并研究了泡沫的亲油疏水性和吸油的重复使用性。结果表明,当发泡温度为170℃,LLDPE的含量为10%,口模直径为0.5 mm时,发泡样品的密度低、开孔率高、吸油倍率高;PP/LLDPE泡沫对水的接触角为137.8°,疏水性能好;对机油10次重复使用后仍具有很高的吸油倍率。因此,该复合开孔泡沫在污水处理、溢油事故和环境保护中具有潜在的应用价值。     

可降解功能性聚合物多孔材料的制备与表征EI北大核心CSCD

通过己内酯(CL)和甲基丙烯酸缩水甘油酯(GMA)共聚合成可降解大分子交联剂,将其应用于高内相乳液聚合制备可降解聚合物多孔材料。在此基础上,引入端双键的聚甲基丙烯酸二甲氨基乙酯(PDMAEMA)大分子单体共聚,制备含功能链段的可降解聚合物多孔材料。用核磁共振、傅里叶变换红外光谱和扫描电镜等对大分子交联剂、大分子单体及多孔材料进行分析和表征。结果表明,合成的大分子交联剂相对分子质量为8100,残留双键含量为GMA结构单元的20%。当大分子交联剂含量为单体质量的1/10时,体系可以形成稳定的高内相乳液,经聚合可得到内部孔洞丰富、泡孔直径为20~22μm的可降解聚合物多孔材料。引入端双键的PDMAEMA大分子单体后,所得聚合物多孔材料孔壁泡孔直径为10~15μm,微孔尺寸为5~8μm,其可在碱性溶液中水解。     

可降解功能性聚合物多孔材料的制备与表征

通过己内酯(CL)和甲基丙烯酸缩水甘油酯(GMA)共聚合成可降解大分子交联剂,将其应用于高内相乳液聚合制备可降解聚合物多孔材料。在此基础上,引入端双键的聚甲基丙烯酸二甲氨基乙酯(PDMAEMA)大分子单体共聚,制备含功能链段的可降解聚合物多孔材料。用核磁共振、傅里叶变换红外光谱和扫描电镜等对大分子交联剂、大分子单体及多孔材料进行分析和表征。结果表明,合成的大分子交联剂相对分子质量为8100,残留双键含量为GMA结构单元的20%。当大分子交联剂含量为单体质量的1/10时,体系可以形成稳定的高内相乳液,经聚合可得到内部孔洞丰富、泡孔直径为20~22μm的可降解聚合物多孔材料。引入端双键的PDMAEMA大分子单体后,所得聚合物多孔材料孔壁泡孔直径为10~15μm,微孔尺寸为5~8μm,其可在碱性溶液中水解。     

蔗糖模板法制备PDMS多孔材料及其吸油性能研究

以聚二甲基硅氧烷(PDMS)、环己烷为原料,蔗糖为模板,采用模板滤取法简单安全地制备出PDMS三维多孔材料。采用扫描电子显微镜、接触角测试、万能力学试验机对PDMS多孔材料的结构形貌及性能进行表征,并考察了蔗糖粒径和环己烷用量对PDMS多孔材料吸油性能的影响。结果表明:采用不同粒径的蔗糖混合物作为模板、环己烷用量为6g制得的PDMS多孔材料的吸油性能最佳,吸油率最高达到1521%。此外,PDMS多孔材料可通过机械挤压的方式循环使用20次以上,且不引起力学强度和吸油性能的下降。     

多孔氧化锆块体材料的水热处理

以无机锆盐氧氯化锆(ZrOCl2·8H2O)为前驱体,聚氧乙烯(PEO,Mv=106)为相分离诱导剂,环氧丙烷(PO)为凝胶促进剂,采用溶胶-凝胶伴随相分离制备孔径尺寸可控、骨架连续的多孔氧化锆块体材料,并对所制备的多孔块体材料进行水热处理,考察了水热溶剂体系、氨水浓度、水热温度和时间对多孔氧化锆块体结晶特性和孔结构特征的影响。结果表明,在氨水/乙醇溶液中进行水热处理时,形成了四方相的氧化锆晶粒,同时块体骨架变得光滑均匀,内部构造出了发达的介孔结构,其比表面积从172m2/g增加至584m2/g,平均孔径从27.7nm增加至58.3nm;增大氨水的浓度、延长水热处理时间、增加水热温度都能提高块体骨架的修饰效果和结晶性。     

聚丙烯酸/聚乳酸复合多孔pH响应水凝胶的制备及性能

利用电纺制备直径为(2.69±0.63)μm,孔径大小为150 nm×120 nm聚乳酸(PLLA)纳米孔超细纤维。以丙烯酸(AA)为单体,N,N-亚甲基双丙烯酰胺为交联剂,过硫酸钾为引发剂,通过自由基聚合制备聚丙烯酸(PAA)水凝胶。将PLLA纳米孔超细纤维浸泡在上述体系中,通过原位聚合制备PAA/PLLA复合水凝胶,并研究m(AA)∶m(PLLA)对复合水凝胶形貌的影响。致孔剂聚乙二醇(PEG)加入,明显提高纤维孔隙率。与PAA水凝胶相比,PAA/PLLA复合水凝胶pH响应时间大大缩短,且拉伸强度由1.9 MPa增加到5.2 MPa,弹性模量从90.4 MPa增加到108.2 MPa。     

反应性反相微乳液体系的构建

以可聚合的甲基丙烯酸甲酯代替传统微乳液中非反应性的油相,采用反应性表面活性剂SE-10N及助表面活性剂丙烯酸构建了反应性反相微乳液体系.通过滴定法描绘出微乳液体系的拟三元相图,并用电导率测量分析微乳液体系的相结构.利用紫外光低温引发微乳液体系聚合制得透明的聚合物.     

电导法对CTAB／正丁醇／环己烷／水四组分微乳体系的研究

利用电导率（K）-增溶水量（ml）关系曲线研究了CTAB／正丁醇／环己烷／水四组分微乳体系在不同增溶水量时的3种结构，即油包水（W／O）、油水双连续（BC）、水包油（O／W）。讨论了表面活性剂CTAB与助表面活性剂正丁醇不同浓度时对微乳液稳定性的影响，得出了微乳液稳定时CTAB和正丁醇的合适配比。     

可聚合阴离子表面活性剂微乳液聚合制备多孔高分子材料

利用易于合成的马来酸单十二醇酯钠盐为可聚合表面活性剂,以甲基丙烯酸羟乙酯为助表面活性剂,研究了甲基丙烯酸甲酯的微乳液聚合,制得了具有连续孔结构(即开孔结构)的高分子材料,孔的尺寸为100 nm至数微米,材料呈半透明至白色不透明状。用场发射扫描电镜对材料的微观结构进行表征;考察了表面活性剂浓度以及表面活性剂水溶液(水相)的含量对材料结构的影响。     

Enhanced Oral Bioavailability of Puerarin Using Microemulsion Vehicle

The main purpose of this study was to prepare puerarin microemulsion system to improve oral bioavailability of puerarin. The microemulsion formulations were prepared using soybean oil, soybean lecithin/ethyl lactate (1:1), and 1,2-propanediol/water. The presence of microemulsion regions were investigated by pseudo-ternary phase diagrams. The droplet size of microemulsion was characterized by photo-correlation spectroscopy. In vivo pharmacokinetic study was conducted in mice, and the results indicated that AUC_0→∞ was 15.82-fold higher than that of puerarin suspension upon oral administration. Particles of puerarin microemulsion were round and homogeneous. Puerarin microemulsion also showed good stability. These studies showed that microemulsion system of puerarin might be promising vehicles for the peroral delivery of puerarin.     

纳米级两性聚丙烯酰胺微乳胶的合成

绘制了以丙烯酰胺、(2-甲基丙烯酰氧乙基)三甲基氯化铵、2-丙烯酰胺基-2-甲基丙磺酸钠为单体,环己烷为油相,Span 20和Tw een80为复配乳化剂体系的拟三元相图,并结合电导率将透明区划分为水/油、双连续和油/水三个区域;采用氧化还原引发体系,通过反相微乳液聚合法合成了两性聚丙烯酰胺微胶乳,并研究了乳化剂质量百分含量对产物特性黏度、粒径和透光率,聚合时间对单体转化率和粒径的影响;对不同类型微乳液中的聚合进行了简单比较。     

Microemulsion for simultaneous transdermal delivery of benzocaine and indomethacin: in vitro and in vivo evaluation

This study investigated simultaneous transdermal delivery of indomethacin and benzocaine from microemulsion. Eucalyptus oil based microemulsion was used with Tween 80 and ethanol being employed as surfactant and cosurfactant, respectively. A microemulsion formulation comprising eucalyptus oil, polyoxyethylene sorbitan momooleate (Tween 80), ethanol and water (20:30:30:20) was selected. Indomethacin (1% w/w) and benzocaine (20% w/w) were incorporated separately or combined into this formulation before in vitro and in vivo evaluation. Application of indomethacin microemulsion enhanced the transdermal flux and reduced the lag time compared to saturated aqueous control. The same trend was evident for benzocaine microemulsion. Simultaneous application of the two drugs in microemulsion provided similar enhancement pattern. The in vivo evaluation employed the pinprick method and revealed rapid anesthesia after application of benzocaine microemulsion with the onset being 10?min and the action lasting for 50?min. For indomethacin microemulsion, the analgesic effect was recorded after 34.5?min and lasted for 70.5?min. Simultaneous application of benzocaine and indomethacin provided synergistic effect. The onset of action was achieved after 10?min and lasted for 95?min. The study highlighted the potential of microemulsion formulation in simultaneous transdermal delivery of two drugs.     

醇对微乳化金属切削液增溶水量的影响研究

醇是微乳化金属切削液中常用的一种助表面活性剂。主要探讨了不同种类和含量的醇对微乳液增溶水量的影响,结合相图研究了具有较大增溶水量的乙醇和带有支链的异戊醇分别与表面活性剂脂肪醇聚氧乙烯醚(EM)复配对微乳液的形成及微乳区面积的影响,并研究了微乳体系形成过程的热力学。结果表明,当乙醇添加量为1.0%时有最大的增溶水量。m(乙醇)∶m(EM)=1∶3,m(异戊醇)∶m(EM)=1∶5时单相微乳区面积最大,增溶的水量最多;通过热力学研究发现乙醇和异戊醇影响此过程热力学函数的变化。在微乳液形成过程中,乙醇和异戊醇从连续相油相进入微乳液界面层的标准自由能变化ΔGs0;标准焓变ΔHs=0,为无热效应过程;ΔGs由醇分子的混乱度熵变ΔSs决定。     

Enhanced percutaneous permeability of diclofenac using a new U-type dilutable microemulsion

Enhanced systemic absorption in vivo and percutaneous penetration in vitro was demonstrated after transdermal administration of diclofenac sodium formulated in U-type microemulsion. Diclofenac sodium was solubilized in a typical four-component system consisting of an oil, polyoxyethylene-10EO-oleyl alcohol (Brij 96V) as the surfactant, and 1-hexanol along water dilution line W46 (40 wt % surfactant and 60 wt % oil phase before water titration).Viscosity and small angle X-ray scattering measurements have evidenced bicontinuous structures within water fractions of 0.25 and 0.5 along the dilution line. Self-diffusion NMR studies showed that drug molecules accumulated in the interfacial film and, to some extent, dissolved in the oil. Relative to a commercial macro-emulsion cream (Voltaren® Emulgel®), microemulsions containing paraffin oil or isopropyl myristate increased the in vivo transdermal penetration rate of diclofenac by two order of magnitude, whereas the rat plasma levels were increased by one order of magnitude. The in vitro data obtained from excised rat skin were comparable to the in vivo results, but suffered from discrepancies from the ideal in vivo-in vitro correlation, which might be explained by optimal in vitro conditions of perfusion and hydration. It has also been found that when jojoba oil is formulated as the oil phase in the microemulsion, the penetration rate of the drug decreases significantly. Based on the three-dimensional structure of jojoba oil, the wax is presumed to prevent the drug from being freely diffused into the skin while migrating from the interfacial film into the continuous oil phase.     

W/O微乳液制备纳米羟基磷灰石的影响因素研究

W/O微乳液制备的纳米羟基磷灰石粉体具有颗粒细小、团聚度低、分散性好、表面活性高等优点。综述了W/O微乳液制备纳米羟基磷灰石的原理;重点论述了影响粉体粒径和形貌的水油比、表面活性剂与助表面活性剂类型、前驱物浓度、反应温度等因素;并初步展望了该领域的研究发展趋势。     

Optimizing the dermal accumulation of a tazarotene microemulsion using skin deposition modeling

Abstract

Context: It is well known that microemulsions are mainly utilized for their transdermal rather than their dermal drug delivery potential due to their low viscosity, and the presence of penetration enhancing surfactants and co-surfactants.

Objective: Applying quality by design (QbD) principles, a tazarotene microemulsion formulation for local skin delivery was optimized by creating a control space.

Materials and methods: Critical formulation factors (CFF) were oil, surfactant/co-surfactant (SAA/CoS), and water percentages. Critical quality attributes (CQA) were globular size, microemulsion viscosity, tazarotene skin deposition, permeation, and local accumulation efficiency index.

Results and discussion: Increasing oil percentage increased globular size, while the opposite occurred regarding SAA/CoS, (p?=?0.001). Microemulsion viscosity was reduced by increasing oil and water percentages (p?<?0.05), due to the inherent high viscosity of the utilized SAA/CoS. Drug deposition in the skin was reduced by increasing SAA/CoS due to the increased hydrophilicity and viscosity of the system, but increased by increasing water due to hydration effect (p?=?0.009). Models with very good fit were generated, predicting the effect of CFF on globular size, microemulsion viscosity, and drug deposition. A combination of 40% oil and 45% SAA/CoS showed the maximum drug deposition of 75.1%. Clinical skin irritation study showed that the aforementioned formula was safe for topical use.

Conclusion: This article suggests that applying QbD tools such as experimental design is an efficient tool for drug product design.