固体脂质纳米粒的研究进展

目的综述固体脂质纳米粒的最新研究进展。方法以国内外大量有代表性的论文为依据,将固体脂质纳米粒的制备方法、特性分析、药物载入、药物释放及应用情况进行了概括,指出了发展前景和尚待解决的问题。结果固体脂质纳米粒的多种制备方法各有优、缺点,调整制备参数可调整药物的包封率和释药曲线。结论固体脂质纳米粒可供多途径给药,是极有发展前景的新型给药系统。     

单唾液酸四己糖神经节苷脂固体脂质纳米粒的制备方法及性质考查

目的：建立适用于生产的单唾液酸四己糖神经节苷脂（GM1）固体脂质纳米粒的制备方法。方法：分别采用溶剂乳化法和高压乳匀法制备GM1固体脂质纳米粒,并将制备结果进行比较。结果：通过比较两种制备方法制得的GM1固体脂质纳米粒进行外观及稳定性、形态学考查、包封率等指标,同时比较以该固体脂质纳米粒制备的冻干粉针剂性状,发现高压乳匀法获得的固体脂质纳米粒性质较佳。结论：高压乳匀法可作为实际GM1固体脂质纳米粒冻干粉针剂中间体的制备方法。     

酮洛芬固体脂质纳米粒的制备

目的：微乳法制备固体脂质纳米粒,以酮洛芬作为模型药物,考查其载药性能。方法：通过对空白微乳粒径和稳定性考查,确定优化处方,将其保温分散于冷水中制备固体脂质纳米粒。对影响其质量的工艺因素和处方因素进行考查和优化设计,筛选最优处方。结果：制备固体脂质纳米粒的直接影响因素包括脂质用量、药物的用量、冷水相温度和微乳保温温度等,所得固体脂质纳米粒的平均粒径（143.9±1.2）nm,多分散系数为0.443。载药固体脂质纳米粒包封率为81.47%,载药量为8.16%。结论：该法稳定可靠,可用于酮洛芬固体脂质纳米粒的制备。     

固体脂质纳米粒的研究概述

目的：从固体脂质纳米载体的制备和剂型应用等方面阐述其研究进展情况。方法：以国内外大量有代表性的论文为依据进行分析、归纳整理。结果：固体脂质纳米粒的多种制备方法各有优缺点，以高压乳化法、微乳法较好，其低毒、靶向性好、缓控释药物能力强等优点决定其在剂型应用方面有很大潜力。结论：固体脂质纳米粒是一种有巨大发展前景的新型给药系统。     

固体脂质纳米粒的研究进展

固体脂质纳米粒的制备方法有熔融 匀质法、冷却 匀质法和微乳法等，所制备的固体脂质纳米粒的稳定性和释放机制与粒子大小、δ电位、结晶度、脂类的修饰、多种交替结构共存的特性以及药物的药动学等因素有关。目前固体脂质纳米粒可通过静脉注射、口服、肺部、经皮、经眼部以及疫苗佐剂等途径给药。限制固体脂质纳米粒临床应用的因素包括物理稳定性差、对脂溶性差的药物包封率低等，一般可通过加入离子对试剂、对药物进行PEG衍生化、β-环糊精包合等方法解决。     

固体脂质纳米粒的研究进展

目的 介绍固体脂质纳米粒的制备方法及物理化学性质等的研究概况及展望。方法 以国内外发表的文献为依据,总结归纳了固体脂质纳米粒的制备方法及物理化学性质等的研究进展。结果和结论 固体脂质纳米粒是一种十分有发展前景的给药系统。     

固体脂质纳米粒的制备和载体结构的研究进展及其应用

目的:从固体脂质纳米载体的制备和结构特征方面介绍其研究进展.方法:以国内外大量有代表性的论文为依据进行分析、归纳整理.结果:固体脂质纳米粒的多种制备方法各有优缺点,其中以高压乳化法和微乳化法被推崇.以固体和液体的混合脂质为基材,制备出O/F/W结构的纳米粒,不但能够有较好的载药能力,还可以拥有优异的缓控释功能.结论:固体脂质纳米粒是一种性能优异、有发展前景的新型给药系统.     

蓝萼甲素固体脂质纳米粒的制备工艺研究

目的以固体脂质纳米粒作为蓝萼甲素新型缓释给药系统,进行蓝萼甲素固体脂质纳米粒的制备工艺研究。方法采用乳化蒸发-低温固化法,均匀设计优化处方,按照优化工艺条件,以硬脂酸作为蓝萼甲素模型药物载体,制备得到蓝萼甲素固体脂质纳米粒,并对其包封率进行考察。结果本研究制得的蓝萼甲素固体脂质纳米粒的包封率达到80.4%。结论本研究方法可以作为蓝萼甲素固体脂质纳米粒的制备方法。     

人参皂苷Rd固体脂质纳米粒的制备

目的:制备人参皂苷Rd固体脂质纳米粒,并考察其理化性质。方法:从旋转薄膜-超声分散法、乳化蒸发-低温固化法、高剪切乳化超声法和高压乳匀法中优选出制备方法;在脂质、表面活性剂等辅料和主药用量的单因素考察基础上,采用正交试验设计,确定最佳处方组成和制备工艺条件;用凝胶柱色谱和HPLC法测定包封率,透射电镜观察形态,激光粒径分析仪测定粒径和Zeta电位。结果:脂质、表面活性剂、助表面活性剂和主药的用量对Rd固体脂质纳米粒的粒径、Zeta电位和包封率均有不同程度的影响。高压乳匀法适合制备Rd固体脂质纳米粒。纳米粒表面呈圆整的球状,大小相近,分散均匀;平均粒径为(102.7±27.0)nm,Zeta电位为(-44.9±9.5)mV,包封率和载药量分别为(81.8±2.6)%和(6.37±0.21)%(n=3)。纳米粒稳定性良好,在4℃下保存4周后,粒径和包封率变化不明显。结论:高压乳匀法适合制备人参皂苷Rd固体脂质纳米粒,工艺稳定可行。     

降香挥发油固体脂质纳米粒的制备工艺研究

目的研究降香挥发油固体脂质纳米粒制备中的主要影响因素。方法分别采用高压乳匀法和熔融 超声法制备了降香挥发油固体脂质纳米粒混悬液。以单因素考察和正交设计法研究制备工艺中影响降香挥发油固体脂质纳米粒质量的主要因素 ,筛选出较理想的处方和工艺。结果所得纳米粒为圆整的类球形实体粒子 ,表面光滑 ,平均粒径为 4 0 0nm和 34 5nm ,含药量为 72 11%和71 5 4 % ,包封率为 91 2 7%和 92 36 %。结论采用熔融 超声法制备降香挥发油固体脂质纳米粒实用性更强。     

Solid Lipid Nanoparticles of a Water Soluble Drug,Ciprofloxacin Hydrochloride

The aim of this study was to understand and investigate the relationship between experimental factors and their responses in the preparation of ciprofloxacin hydrochloride based solid lipid nanoparticles. A quadratic relationship was studied by developing central composite rotatable design. Amount of lipid and drug, stirring speed and stirring time were selected as experimental factors while particle size, zeta potential and drug entrapment were used as responses. Prior to the experimental design, a qualitative prescreening study was performed to check the effect of various solid lipids and their combinations. Results showed that changing the amount of lipid, stirring speed and stirring time had a noticeable influence on the entrapment efficiencies and particle size of the prepared solid lipid nanoparticles. The particle size of a solid lipid nanoparticle was in the range of 159-246 nm and drug encapsulation efficiencies were marginally improved by choosing a binary mixture of physically incompatible solid lipids. Release of ciprofloxacin hydrochloride from solid lipid nanoparticle was considerably slow, and it shows Higuchi matrix model as the best fitted model. Study of solid lipid nanoparticle suggested that the lipid based carrier system could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release for water soluble actives.     

Formulation and in vitro-in vivo evaluation of piribedil solid lipid micro- and nanoparticles

Modification of the dissolution rate and, thus, the enhancement of the bioavailability of a dopaminergic drug, piribedil, which has a low aqueous solubility and short elimination half-life have been the aim in this study. Preparations of micron and submicron particles using solid lipid carriers have been performed for this purpose. For the avoidance of solvent residues resulting from the preparation technique, cold and hot homogenization methods have been used to prepare solid lipid particles. After obtaining an appropriate particle size, piribedil loading and preparation yield by the use of those two methods, various formulations have been prepared with different lipid, drug and surfactant materials. The factors mentioned were found to affect properties of the particles, and the release rate was found to be the fastest in acidic medium. Suspensions of pure piribedil and a formulation, selected according to the results obtained from in vitro dissolution and particle size experiments, were compared using tremor tests in mice. The same suspensions were applied perorally to rabbits and bioavailability of the solid lipid particle was found to be higher than the pure piribedil. After an in vitro-in vivo evaluation of piribedil solid lipid particles developed for Parkinson's disease therapy, it has been determined that release rate could be controlled and piribedil bioavailability could be improved.     

Formulation and in vitro-in vivo evaluation of piribedil solid lipid micro- and nanoparticles

Modification of the dissolution rate and, thus, the enhancement of the bioavailability of a dopaminergic drug, piribedil, which has a low aqueous solubility and short elimination half-life have been the aim in this study. Preparations of micron and submicron particles using solid lipid carriers have been performed for this purpose. For the avoidance of solvent residues resulting from the preparation technique, cold and hot homogenization methods have been used to prepare solid lipid particles. After obtaining an appropriate particle size, piribedil loading and preparation yield by the use of those two methods, various formulations have been prepared with different lipid, drug and surfactant materials. The factors mentioned were found to affect properties of the particles, and the release rate was found to be the fastest in acidic medium. Suspensions of pure piribedil and a formulation, selected according to the results obtained from in vitro dissolution and particle size experiments, were compared using tremor tests in mice. The same suspensions were applied perorally to rabbits and bioavailability of the solid lipid particle was found to be higher than the pure piribedil. After an in vitro-in vivo evaluation of piribedil solid lipid particles developed for Parkinson's disease therapy, it has been determined that release rate could be controlled and piribedil bioavailability could be improved.     

Nimodipine loaded lipid nanospheres prepared by solvent diffusion method in a drug saturated aqueous system

To overcome the disadvantages such as lower drug entrapment efficiency (EE) of lipid nanospheres prepared by conventional solvent diffusion method, a solvent diffusion method in drug saturated aqueous system was developed. Nimodipine was used as a model drug to incorporate into lipid nanospheres. The monostearin (MS) solid lipid nanoparticles (SLN) produced by conventional method under different production temperature only showed 24.40-30.21wt% EE, and relatively higher EE was achieved when the production temperature was 0 degrees C. The EE could be enhanced by the incorporation of liquid lipid (caprylic/capric triglycerides, CT) into SLN and the employing of drug saturated dispersion medium. The nanostructured lipid carrier (NLC) with higher CT content indicated the highest EE as the drug saturated aqueous solution was used as dispersion medium. The differential scanning calorimetry (DSC) results demonstrated the present method could improve the drug encapsulation into lipid nanospheres. In vitro drug release experiments indicated the present preparation method could delay the drug release rate from lipid nanospheres, and the drug release rate could adjust by the CT content in lipid nanospheres. The highest drug loading (DL) was reached up to 4.22wt% when 8wt% drug was charged in the preparation of lipid nanospheres.     

新藤黄酸固体脂质纳米粒的制备与质量评价

目的制备新藤黄酸固体脂质纳米粒并进行质量考察。方法采用正交试验设计优化处方,以高温乳化-低温固化的方法制备新藤黄酸固体脂质纳米粒。并对其包封率、形态等进行研究。结果所制得的新藤黄酸固体脂质纳米粒外观形态圆整,粒度分布均匀,平均粒径为163.3 nm,包封率为(60.1±1.1)%。结论高温乳化-低温固化的方法适用于新藤黄酸-固体脂质纳米粒的制备。     

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。     

Preparation and characteristics of monostearin nanostructured lipid carriers

Nanostuctured lipid carriers (NLC) consisted of solid lipid and liquid lipid are a new type of lipid nanoparticles, which offer the advantage of improved drug loading capacity and release properties. In this study, solvent diffusion method was employed to produce NLC. Monostearin (MS) and caprylic/capric triglycerides (CT) were chosen as the solid lipid and liquid lipid. Clobetasol propionate used as a model drug was incorporated into the NLC. The influences of preparation temperature and CT content on physicochemical properties of the NLC were characterized. As a result, monostearin solid lipid nanoparticles (without CT content, SLN) obtained at higher temperature (70 degrees C) exhibited slightly higher drug loading capacity than that of 0 degrees C (P < 0.05). In contrast, the production temperature made little effect on NLC drug loading capacity (P > 0.05). The improved drug loading capacity was observed for NLC and it enhanced with increasing the CT content in NLC. The results were explained by differential scanning calorimetry (DSC) measurement for NLC. The incorporation of CT to NLC led to crystal order disturbance and thus left more space to accommodate drug molecules. NLC displayed a good ability to reduce the drug expulsion in storage compared to SLN. The in vitro release behaviors of NLC were dependent on the production temperature and CT content. NLC obtained at 70 degrees C exhibited biphasic drug release pattern with burst release at the initial 8h and prolonged release afterwards, whereas NLC obtained at 0 degrees C showed basically sustained drug release throughout the release time. The drug release rates were increased with increasing the CT content. These results indicated that the NLC produced by solvent diffusion method could potentially be exploited as a carrier with improved drug loading capacity and controlled drug release.     

维生素E脂质纳米粒的制备与表征

目的寻找合适的脂溶性药物载体。方法采用高压均质法制备3种不同类型的纳米脂质载体体系,分别为纳米乳液（NM）、固体脂质纳米粒（SLN）和纳米结构脂质载体（NLC）,并用透射电镜（TEM）、粒度分析仪（PCS）和高效液相色谱（HPLC）仪对其进行表征。结果3种不同类型的脂质载体在合适的配比情况下均有较好的稳定性。载药固体脂质纳米粒其微观形貌呈球形,表明其未结晶,具有较好的载药能力。于4℃、以10000r／min冷冻离心30min或避光保存4个月后粒径分布仍然基本不变,且可冷冻干燥（-40℃,0．01Pa）后长期保存。结论3种体系制备工艺简单,适合于大规模生产。     

固体脂质纳米粒研究新进展

综述固体脂质纳米粒(SLN)的制备方法、应用、存在的问题和解决方法以及发展前景，介绍基于SLN而开发的新型载体——纳米脂质载体和药脂结合物纳米粒。     

A controlled-release ocular delivery system for ibuprofen based on nanostructured lipid carriers

The objective of this study was to develop an ocular drug delivery system based on nanostructured lipid carrier and investigate its in vitro and in vivo characteristics. Ibuprofen was chosen as the model drug. Four different formulations of Ibuprofen nanostructured lipid carriers were prepared by melted-ultrasonic methods; Gelucire 44/14 was screened as one of the solid lipid matrix materials due to the good particle size dispersion and excellent contribution to the corneal permeability of the model drug. The modified Franz-type diffusion cells and isolated corneas were used in the test of drug corneal permeability and the in vivo releasing tests were carried out using microdialysis method. Gelucire 44/14 and Transcutol P could enhance the corneal permeability by different mechanisms. The corresponding apparent permeability coefficients (P(app)) were 1.28 and 1.36 times more than that of the control preparation. Stearylamine could prolong the pre-cornea retention time of the model drug to some extent. Ibuprofen nanostructured lipid carriers displayed controlled-release property. The AUC of the optimized formulation of Ibuprofen nanostuctured lipid carriers was 3.99 times more than that of Ibuprofen eye drops).