芹菜素固体脂质纳米粒的制备

目的为芹菜素新型制剂的研究和开发提供实验基础。方法采用热熔超声法制备芹菜素固体脂质纳米粒;以包封率为指标,通过正交试验对处方进行优化。结果制备的纳米粒为类球形,包封率为63.11%,平均粒径为(135±18)nm,zeta电位为-18.90 mV,36 h体外累积释放95.74%。结论热熔超声法可用于制备芹菜素固体脂质纳米粒。     

乳化蒸发法制备固体脂质纳米粒

目的：采用乳化蒸发法制备固体脂质纳米粒,并考察其载药性能。方法：对影响固体脂质纳米粒质量的工艺因素和处方因素进行考察和优化设计,得到最优处方。选用模型药物酮洛芬制备载药固体脂质纳米粒,考察其包封率和体外释放行为。结果：所得固体脂质纳米粒平均粒径为（228.2±18.1）nm,多分散系数为（0.217±0.022）,ξ电位为-（21.4±0.6）mV。载药固体脂质纳米粒最佳包封率为（64.1±3.3）%,体外释放行为符合Weibull模型。结论：采用乳化蒸发法制备固体脂质纳米粒是可行的。     

不同粒径多西他赛固体脂质纳米粒制剂及其细胞毒活性

目的制备不同粒径的多西他赛(docetaxel,DTX)固体脂质纳米粒,考察多西他赛固体脂质纳米粒理化性质,研究粒径对体外释放行为以及细胞毒作用的影响。方法通过热熔超声法制备不同粒径多西他赛固体脂质纳米粒,观察纳米粒形态,测定其包封率、粒径、Zeta电位。考察粒径因素对固体脂质纳米粒体外释放行为、体外细胞毒性的影响。结果制备的纳米粒均为球形及类球形,3种粒径的多西他赛固体脂质纳米粒平均粒径分别为(83.7±8.4)、(162.7±11.9)、(232.1±26.4)nm;Zeta电位分别为-24.19、-23.67、-23.19 mV;包封率分别为98.03%、97.84%、97.92%。60 h粒径分别为83、16、232 nm的多西他赛固体脂质纳米粒在释放介质中分别累计释放86.34%、76.98%、67.14%。3种不同粒径多西他赛固体脂质纳米粒(DTX-SLN-83,DTX-SLN-162,DTX-SLN-232),多西他赛原料药(DTX solutions)以及空白SLN溶液与多西他赛的混合溶液(physi-calm ixture)对MCF-7细胞作用24 h的IC50值分别为3.36、6.20、9.74、13.15、12.92 mg.L-1;48 h的IC50值分别为0.93、2.01、4.35、9.48、9.21 mg.L-1;72 h的IC50值分别为0.30、0.91、1.67、7.36、7.82 mg.L-1。随着多西他赛固体脂质纳米粒粒径的减小,其肿瘤细胞杀伤力逐渐增强。结论热熔超声法可用于制备不同粒径多西他赛固体脂质纳米粒。降低固体脂质纳米粒粒径有利于药物更完全地释放,同时增强其对肿瘤细胞的杀伤能力。     

黄芩素固体脂质纳米粒包封率测定及体外释放度考察

目的测定黄芩素固体脂质纳米粒的包封率,并考察其体外释放规律。方法溶剂扩散法制备脂质纳米粒,高速离心法分离纳米粒和游离药物,HPLC法测定包封率并考察其体外释放规律。结果测得纳米粒的平均包封率为60.73%,其体外释放规律符合H iguch i动力学方程。结论黄芩素固体脂质纳米粒有较高的包封率,在体外具有良好的缓释作用。     

薄膜-超声法制备芦丁固体脂质纳米粒的研究

目的优化薄膜-超声法制备芦丁固体脂质纳米粒的处方。方法以包封率为指标,采用正交设计优化法考察硬脂酸和大豆卵磷脂的用量、吐温-80和聚乙二醇-400的体积分数对包封率的影响,优选最佳处方。用透射电镜观察外观形态,用电位/纳米粒度分析仪分析纳米粒的粒径及Zeta电位,用透析法评价体外释药特征。结果以最佳处方制备的芦丁固体脂质纳米粒呈类球形,平均粒径为195.8±11nm,Zeta电位为-20.65±0.6mV,平均包封率为86.31%,72h体外累积释放87.32%。结论按最佳处方工艺制备的芦丁固体脂质纳米粒具有较高的包封率和较好的缓释效果。     

吡喹酮-硬脂酸固体脂质纳米粒的制备及性能评价

目的：制备吡喹酮-固体脂质纳米粒,考察其理化性质和体外释放度。方法：以硬脂酸为脂质材料,聚乙烯吡咯烷酮为乳化剂,利用热熔乳化超声法制备吡喹酮-固体脂质纳米粒,扫描电镜观察纳米粒形态和均匀度,纳米粒度仪测定其粒径、分散指数、Zeta电位、包封率和载药量,并进行体外释放试验。结果：制备的固体脂质纳米粒为类圆球状,粒径分布较均匀、表面光滑。纳米的平均粒径、分散指数、电位、包封率和载药量分别为（316.5±22.8）nm、0.23±0.05、（-25.3±0.7）mV,（92.64±5.12）%和（18.45±1.34）%。药物在制剂的过程中稳定性良好。体外释放表明吡喹酮-硬脂酸固体脂质纳米粒在生理盐水中具有一定程度的突释和显著的缓释效果。结论：本试验制备的吡喹酮-硬脂酸固体脂质纳米粒具有较好的均匀度和高载药量,并具有良好的缓释性能。     

全反式维甲酸固体脂质纳米粒的制备及体内外评价

目的以山嵛酸甘油酯(Compritol 888 ATO)为脂质材料，采用超声分散法制备维甲酸固体脂质纳米粒，并考察其体内外性质。方法选用脂溶性较高的维甲酸作为模型药物，采用超声分散法制备固体脂质纳米粒，并对其各种理化性质进行研究。考察了纳米粒的体外释放，以维甲酸溶液剂为对照，测定了两种纳米粒在大鼠体内的药代动力学参数。结果采用超声分散法可以简便、快速制备得到两种维甲酸固体脂质纳米粒，透射电镜测得纳米粒为圆球状，大小均匀。动态光散射法测得平均粒径分别为(158±9) nm和(89±11) nm。于4 ℃放置1年粒径无明显变化，载药量为3.3%，包封率大于95%。药物体外释放符合Weibull方程。与对照组相比，两种维甲酸固体脂质纳米粒静脉注射后药物在血液中的滞留时间显著延长。结论超声分散法适用于固体脂质纳米粒的制备。     

汉黄芩素固体脂质纳米粒的制备及体外释放度考察

目的:制备汉黄芩素固体脂质纳米粒并对其体外释放度进行考察.方法:采用乳化分散-超声法制备汉黄芩素固体脂质纳米粒,以包封率和载药量为评价指标,进行正交试验筛选最优处方,并对最优处方的外观、粒径和体外释放度进行考察.结果:制得的纳米粒为均一球形,平均粒径为(153 ±34)nm,其平均载药量为(60.53±2.17)％,平均包封率为(85.54±4.16)％,48 h累积释放达80％.结论:本试验获得了较理想的汉黄芩素固体脂质纳米粒,其体外释放具有缓释作用.     

非洛地平-硬脂酸固体脂质纳米粒的制备及其体外透皮吸收研究

目的:以固体脂质纳米粒为栽体,通过透皮给药达到提高非洛地平透皮吸收及缓释长效的目的.方法:采用溶剂挥发-超声法制备非洛地平固体脂质纳米粒水分散体,以大鼠皮肤为渗透屏障对非洛地平固体脂质纳米粒的经皮渗透进行研究.结果:非洛地平-硬脂酸固体脂质纳米粒为类球形实体粒子,平均粒径范围在50～150 nm,包封率大于85%,栽药量大于7%,药物体外释放符合一级动力学过程.体外经皮渗透速率显著高于空白对照组.结论:非洛地平固体脂质纳米粒处方设计合理,制备工艺可靠,以纳米粒作为透皮给药载体具有广阔的发展前景.     

固体脂质纳米粒作为维A酸经皮给药载体的研究

目的:采用固体脂质纳米粒作为维A酸载体以提高其稳定性,增加经皮给药时的局部药物浓度。方法:采用纳米乳法制备维A酸固体脂质纳米粒,通过相图研究确定处方组成并通过单因素试验进行优化,采用葡聚糖G50微型凝胶柱测定包封率。对维A酸固体脂质纳米粒稳定性、释放度、经皮渗透性和皮肤贮留量进行评价。结果:制得的固体脂质纳米粒为球形或类球形粒子,平均粒径为83.2 nm,包封率>95%。4℃,25℃和40℃避光贮存3个月,含量和包封率均无明显变化。其体外释放速率和经皮渗透速率较市售乳膏慢,皮肤贮留量大于市售乳膏。结论:固体脂质纳米粒作为维A酸载体有助于提高其稳定性,增加局部药物浓度。     

长春西汀固体分散体的制备及体外溶出特性

目的:制备长春西汀固体分散体,提高其溶出速度和程度。方法:以泊洛沙姆188(F68)为载体,用溶剂-熔融法制备固体分散体;差热分析、X-射线粉末衍射分析以鉴别药物在载体中的存在状态;并考察载体的用量、溶出介质和转速对药物体外溶出特性的影响。结果:长春西汀的固体分散体中药物部分以分子状态分散,部分以微晶分散。固体分散体VIN-F68(1∶6,w/w)的溶出参数t50t、d与相应物理混合物、原料药粉末和市售片剂间差异存在显著性(P<0.01),溶出介质和转速的选择对药物的溶出有一定影响。结论:长春西汀的固体分散体能显著提高药物的溶出速度和程度。     

固体脂质纳米粒和纳米结构脂质载体在经皮给药系统中的研究进展

目的介绍固体脂质纳米粒和纳米结构脂质载体在经皮给药系统中的应用与优势,为其开发利用提供参考。方法查阅国内外相关文献共30余篇,从固体脂质纳米粒和纳米结构脂质载体用于经皮给药系统的优势、药物在固体脂质纳米粒和纳米结构脂质载体中的分布形式及固体脂质纳米粒和纳米结构脂质载体在经皮给药领域中的应用等方面进行综述。结果固体脂质纳米粒和纳米结构脂质载体可以增强药物稳定性,能在皮肤表面产生包封效应,增加皮肤水合作用,具有药物靶向性。结论固体脂质纳米粒和纳米结构脂质载体是极有发展前景的新型经皮给药系统。     

HPLC法测定马钱子碱固脂纳米粒冻干粉的包封率和载药量

目的：测定马钱子碱固脂纳米粒冻干粉的包封率和载药量。方法：采用SephadexG-50凝胶柱分离固脂纳米粒和游离马钱子碱,高效液相色谱法测定包封率和载药量,并进行方法学考察。结果：葡聚糖凝胶柱能有效分离固脂纳米粒与游离马钱子碱,平均柱回收率和平均柱加样回收率分别为97．2％和96．4％。马钱子碱固脂纳米粒冻干粉的平均包封率为50．18％,平均载药量为2．11％。结论：该方法简便易行,准确可靠,重复性好,可用于马钱子碱田脂纳米粒冻千粉的载药量和包封率的测定。     

香叶木素固体脂质纳米粒的制备及质量评价

目的 制备香叶木素固体脂质纳米粒并对其进行质量评价。方法 采用溶剂注入法制备香叶木素固体脂质纳米粒,用 Box-Benhnken效应面法优化处方,并通过包封率、微观形态、粒径分布和Zeta电位对香叶木素固体脂质纳米粒的质量进行评价。 结果 香叶木素固体脂质纳米粒最优处方组成：表面活性剂浓度3.39%,棕榈酸浓度0.116%,脂药质比为21:100,制备的香叶木素 固体脂质纳米粒外观澄清透明,带淡蓝色乳光;平均粒径为(91.73±3.18)nm(n=3),PDI为0.228,电位为(-11.46±0.74)mV(n=3);包 封率为95.13%,载药量为9.04%;透射电镜照片显示纳米粒大小均一,呈球形或类球形。 结论 该处方可用于香叶木素固体脂 质纳米粒的制备,工艺简单,稳定可行。     

长春西汀自乳化固体分散体的研究

目的：制备长春西汀自乳化固体分散体,并测定其体外特性.方法：以自乳化辅料和泊洛沙姆188（F68）为栽体制备长春西汀自乳化固体分散体,考察不同自乳化辅料及用量、不同制备方法、投药量和溶出介质对自乳化固体分散体溶出特性的影响,并采用差热分析、X-射线粉末衍射分析鉴别药物在载体中的存在状态.结果：与普通固体分散体（F1）相比,自乳化固体分散体（F8）的溶出度显著提高,药物主要以分子状态存在;自乳化辅料的种类、用量的不同对药物溶出有显著差异;溶剂法和溶剂熔融法好于熔融法;投药量和介质的不同对溶出也有一定影响.结论：与普通固体分散体相比,自乳化固体分散体能进一步提高长春西汀的溶解度和溶出度.     

Simvastatin Solid Lipid Nanoparticles for Oral Delivery: Formulation Development and In vivo Evaluation

Solid lipid nanoparticles have been increasingly utilised for improving oral bioavailability of drugs. Simvastatin is biopharmaceutical class 2 drug with poor oral bioavailability of 5%. In the present study, simvastatin solid lipid nanoparticles were successfully prepared by hot melt emulsification process and optimised with respect to surfactant and lipid concentration, and drug loading. The nanoparticles were characterised for entrapment efficiency, particle size, morphology, crystallinity and thermal behavior. Optimised formulations prepared from solid lipids glyceryl behenate and glyceryl palmitostearate containing Tween 80 as surfactant exhibited satisfactory entrapment efficiencies above 96% and mean particle size below 200 nm. The electron micrographs indicated that lipid nanocarriers were almost spherical in appearance. X-ray diffraction and differential calorimetric studies proved that the drug was amorphised in the lipid matrix and did not crystallise out. To improve the physical as well as chemical stability of formulations, dry adsorbed nanoparticles were prepared by evaporative drying method using a carrier. The adsorbed nanoparticles demonstrated good flow properties and satisfactory reconstitution properties. Pharmacodynamic studies of simvastatin solid lipid nanoparticles revealed improved reduction in total cholesterol values as compared to pure drug powder indicating improved bioavailability.     

Solid lipid nanoparticles for targeted brain drug delivery

The present review discusses the potential use of solid lipid nanoparticles for brain drug targeting purposes. The state of the art on surfactant-coated poly(alkylcyanoacrylate) nanoparticles specifically designed for brain targeting is given by emphasizing the transfer of this technology to solid lipid matrices. The available literature on solid lipid nanoparticles and related carriers for brain drug targeting is revised as well. The potential advantages of the use of solid lipid nanoparticles over polymeric nanoparticles are accounted on the bases of a lower cytotoxicity, higher drug loading capacity, and best production scalability. Solid lipid nanoparticles physicochemical characteristics are also particularly regarded in order to address the critical issues related to the development of suitable brain targeting formulations. A critical consideration on the potential application of such technology as related to the current status of brain drug development is also given.     

Fabrication and Evaluation of Curcumin-loaded Nanoparticles Based on Solid Lipid as a New Type of Colloidal Drug Delivery System

Curcumin has very broad spectrum of biological activities; however, photodegradation, short half-life and low bioavailability have limited its clinical application. Curcumin-loaded solid lipid nanoparticles were studied to overcome these problems. The aim of this study was to optimize the best formulation on curcumin-loaded solid lipid nanoparticles. Emulsion-evaporation and low temperature-solidification technique was applied with monostearin as lipid carriers. The single factor analysis and orthogonal design were used to optimize formulation and various parameters were investigate. By the optimisation of a single factor analysis and orthogonal test, the particles size, polydispersity index, zeta potential, encapsulation efficiency and drug loading capacity of the optimised formulation were 99.99 nm, 0.158, −19.9 mV, 97.86%, and 4.35%, respectively. The differential scanning calorimetry and X-ray diffraction analysis results demonstrated new structure was formed in nanoparticles. The release kinetics in vitro demonstrated curcumin-loaded solid lipid nanoparticles can control drug release. These studies confirmed that curcumin-loaded solid lipid nanoparticles could be prepared successfully with high drug entrapment efficiency and loading capacity. Curcumin-loaded solid lipid nanoparticles may be a promising drug delivery system to control drug release and improve bioavailability.     

Preparation and characteristics of oridonin-loaded nanostructured lipid carriers as a controlled-release delivery system

In order to improve drug entrapment efficiency and loading capacity, nanostructured lipid carriers consisting of solid lipid and liquid lipid as a new type of colloidal drug delivery system were prepared. The dispersions of oridonin-loaded solid lipid nanoparticles and nanostructured lipid carriers were successfully prepared by the emulsion-evaporation and low temperature-solidification technique using monostearin as the solid lipid, caprylic/capric triglycerides as the liquid lipid and oridonin as the model drug. Their physicochemical properties of oridonin-loaded nanostructured lipid carriers and release behaviours were investigated and compared with those of solid lipid nanoparticles. As a result, the mean particle size was ～200 nm with narrow polydispersity index lower than 0.4 for all developed formulations. Zeta potential values were in the range ?35 mV ～ ?50 mV, providing good physical stability of all formulations. The differential scanning calorimetry and X-ray diffraction analysis results demonstrated lipid nanoparticles exhibited crystal order disturbance and thus left more space to accommodate drug molecules. The improved drug entrapment efficiency and loading capacity were observed for nanostructured lipid carriers and they enhanced with increasing the caprylic/capric triglycerides content. In vitro drug release experiments exhibited biphasic drug release patterns with burst release initially and prolonged release afterwards. These results indicated that nanostructured lipid carriers could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release.     

黄芩苷固体脂质纳米粒体外释放研究

目的:研究黄芩苷固体脂质纳米粒的体外释药规律。方法:采用动态透析技术研究黄芩苷固体脂质纳米粒的体外释药性能,并用高效液相色谱法测定黄芩苷含量,以累积释药百分率进行不同模型的拟合。结果:黄芩苷固体脂质纳米粒的释放曲线符合Hixon-crowell方程,t≈3h。结论:黄芩苷固体脂质纳米粒具有良好的缓释作用。