In situ Localization of Molecules in Crosslinked Particles during Electrohydrodynamic Process: Simple Route to Produce Microcapsules and Fibers with Controlled Release

This study reports a spontaneous selective localization of molecules in crosslinked particles during electrospraying and electrospinning polymer solutions containing the particles. It provides a facile way of preparing microcapsules and fibers with controlled release. The dye molecules were phase separated from the crystalline polymer matrix during the electrohydrodynamic process and moved to the solvent‐rich crosslinked particles. The position of the particles in the microcapsules and fibers could be controlled by adjusting compatibility of the particles with the matrix polymer. The microcapsules and fibers did not show the initial burst release of the molecules and gave considerably prolonged release behavior.

     

石蜡相变微胶囊的制备与表征

采用复乳交联法制备了以相变石蜡为芯材、壳聚糖为壁材的新型储能相变微胶囊。 此相变微胶囊具有很高的相变焓值（可达110 J/g以上）,并且可以根据具体需要改变芯材的温度;TGA研究表明,该相变微胶囊具有很好的热稳定性,在150 ℃以下可以稳定存在;由于壳材料进行了化学交联反应,使得该相变微胶囊具有很好溶剂稳定性,可以在水、乙醇和乙醚等常见溶剂中稳定存在。     

A controlled-release anti-inflammatory drug

A procedure to obtain a controlled-release microencapsulated anti-inflammatory drug based on a solvent evaporation method is described. The present method makes use of ethylcellulose as the polymer and methylene chloride as solvent. The evaporation of solvent is controlled by means of an air stream. Variations in the preparative procedure and their effects on capsule dimensions and permeabilities were studied. The release behavior of the drug is determined, and two different diffusion constants are also determined: 7.0×10⁻¹⁰ cm²/s and 1.2×10⁻¹⁰ cm²/s, corresponding to low and high release time. Based on these results it is proposed that these microcapsules have a nonhomogeneous polymeric wall, and are more porous in the outer surface. This model might be applicable to the microcapsules obtained by means of the solvent evaporation method.     

Tramadol Release from a Delivery System Based on Alginate‐Chitosan Microcapsules

Alginate‐chitosan microcapsules to control the release of Tramadol‐HCl were prepared using two different methods. In the two‐stage procedure (Variant I) alginate was first pumped into a CaCl₂/NaCl solution and then transferred into a chitosan solution. In the one‐stage procedure (Variant II) alginate was directly pumped into a chitosan/CaCl₂ solution, and different behavior could be noted in each case. The microcapsules were spherical in both variants and they swelled to a greater extent in a basic medium as compared to an acid one. The drug release profile of Tramadol from microcapsules in simulated gastric fluid and simulated intestinal fluid was also studied. The maximum release of Tramadol at 24 h was 64% and 86% for Variant I and II, respectively, in simulated intestinal fluid. Release was adjusted using the power law of the semi‐empirical Peppas equation in order to gain information about the release mechanism. In both cases the values of the exponent were found to be between 0.53 and 0.84 for swellable microcapsules in simulated gastric and intestinal fluids, respectively, indicating anomalous drug transport for both variants. The good results obtained with alginate‐chitosan microcapsules are comparable to those of the best products so far described in the scientific bibliography and in addition, chitosan is useful in pharmacy.

Surface morphology of Tramadol‐loaded microcapsule.     

光致变色微胶囊的制备与性能

以蜜胺树脂为壁材、光致变色材料为芯材,采用原位聚合法制备了具有光致变色性能的微胶囊.研究了三聚氰胺/甲醛摩尔比、壁材与芯材的用量比、乳化剂浓度等因素对微胶囊形貌及性能的影响.在最佳工艺条件下制备的变色微胶囊,在日光和紫外光下具有快速、可逆的光致变色性能.     

Assembly of MOF Microcapsules with Size‐Selective Permeability on Cell Walls

The assembly of metal–organic frameworks (MOFs) into microcapsules has attracted great interest because of their unique properties. However, it remains a challenge to obtain MOF microcapsules with size selectivity at the molecular scale. In this report, we used cell walls from natural biomaterials as non‐toxic, stable, and inexpensive support materials to assemble MOF/cell wall (CW) microcapsules with size‐selective permeability. By making use of the hollow structure, small pores, and high density of heterogeneous nucleation sites of the cell walls, uniform and continuous MOF layers could be easily obtained by inside/outside interfacial crystallization. The prepared MOF/CW microcapsules have excellent stability and enable the steady, slow, and size‐selective release of small molecules. Moreover, the size selectivity of the microcapsules can be adjusted by changing the type of deposited MOF.     

Self-assembly of human serum albumin (HSA) and L-alpha-dimyristoylphosphatidic acid (DMPA) microcapsules for controlled drug release

Human serum albumin (HSA) and L-alpha-dimyristoylphosphatidic acid (DMPA) were applied as a pair to encapsulate ibuprofen microcrystals by means of a technique based on the layer-by-layer (LbL) assembly of oppositely charged species, for the purpose of controlling drug release. The successful adsorption of HSA and DMPA multilayers onto ibuprofen crystals was confirmed by optical microscopy. The drug release process, in a solution of pH 7.4, was monitored by optical microscopy and UV spectroscopy. The results revealed that the rate of release of ibuprofen from HSA/DMPA microcapsules decreased as the capsule wall thickness and drug crystal size increased, indicating that the permeability of the microcapsules can be controlled by simply varying the number of HSA/DMPA deposition cycles.     

Effects of protective colloids on the preparation of poly(l-lactide)/poly(butylene succinate) microcapsules

Poly(l-lactide)/poly(butylene succinate) microcapsules containing an aqueous solution of sodium(+)-tartrate dihydrate were prepared by the interfacial precipitation method through solvent evaporation from (w/o)/w emulsion. The effects of poly(vinyl alcohol) used as a protective colloid in the microencapsulation were investigated regarding thermal properties, particle size distributions, surface morphologies, and release behaviors of the biodegradable microcapsules. It was concluded that encapsulation efficiency, surface morphologies, thermal properties, and releasing speed were closely related to the particle size distributions of microcapsules under different conditions of the protective colloid.     

硬脂酸丁酯微胶囊的制备与表征

采用原位聚合法用脲醛树脂包覆硬脂酸丁酯,制得相变储热微胶囊.利用激光粒径分布仪、扫描电镜、差示扫描量热仪(DSC)和傅立叶转换红外光谱仪分别研究了微胶囊的粒径分布、表面形态、热性能和壳结构.结果表明,所得微胶囊粒径分布均匀,表面光洁,具有良好的韧性和致密性.不同的制备工艺对微胶囊粒径分布有一定的影响,其中在28 000 r/m in下乳化5 m in时,所得微胶囊的粒径分布集中在1~4μm.DSC测定结果显示硬脂酸丁酯微胶囊的最大相变焓为68 J/g.     

Microencapsulation of astiban acid for the treatment ofSchistosomiasis mansoni

Schistosomiasis is among the top five diseases in the world in terms of morbidity, affecting perhaps 200 million people in tropical and subtropical countries. Antischistosomal drugs are toxic and rapidly metabolized. Hence, they must be given in a number of spaced doses. In spite of this there are severe side effects leading to poor patient compliance. This is an ideal situation for the application of sustained drug release to avoid the toxic peak concentration of drug. This study was carried out using Astiban acid, an antimonial drug that is effective againstS. mansoni. Unfortunately, the drug is sufficiently soluble that 50 mg will dissolve in 100 mL water in less than a minute. To permit sustained release of intramuscularly injected drug, microcapsules of astiban acid in poly(d,l-lactic acid) were formed by coacervation. Release studies show that an appreciable fraction of the drug is available at the surface for rapid solution. After this surface drug dissolves, the remaining drug is released slowly with half-times of many hours. After the initial burst, the release of drug follows Higuchi’s equation up to approximately 80% release, with exponentially decreasing release rates thereafter.     

Formulation and In Vitro Evaluation of Sustained Release Microspheres of Diltiazem Hydrochloride Prepared by Emulsification-Internal Gelation Method

The present work describes the formulation of alginate microspheres containing diltiazem hydrochloride by the emulsification-internal gelation method with the use of barium carbonate as a cross-linking agent. The effect of various factors (the concentration of alginate and barium chloride) on the drug loading efficiency and in vitro release were investigated. Fourier transform infrared microscopy (FTIR) and differential scanninig calorimetry (DSC) analysis confirmed the absence of any drug polymer interaction. X-ray diffraction (XRD) pattern showed that there is a decrease crystallinity of the drug. The in vitro drug release profile could be altered significantly by changing various processing parameters to give a controlled release of drug from microcapsules. The stability studies of drug-loaded microcapsules showed that the drug was stable at different storage conditions.     

甲胺基阿维菌素苯甲酸盐微胶囊的制备与表征

以三聚氰胺-甲醛树脂为壁材,采用原位聚合法制备了甲胺基阿维菌素苯甲酸盐微胶囊,研究了三聚氰胺与甲醛的质量比、芯壁比、乳化剂、搅拌速度与时间、pH值、温度等因素对微胶囊形成的影响,对制备的微胶囊进行了表征,测定了甲维盐微胶囊化前后的光解率。结果表明,三聚氰胺与甲醛质量比为1∶2、芯材与壁材质量比为3∶2、以质量分数1%羟乙基纤维素(HEC)为乳化剂、在1000r/min搅拌速度下、pH=5.0和50℃保温2h可制备出形貌较好、平均粒径4.4μm的甲维盐微胶囊。红外光谱分析证明,甲维盐已完全被包覆在微胶囊中。紫外分光光度法测定其缓释性能良好。光解实验表明,微胶囊化可有效降低甲维盐原药的光解。     

Synthesis and Spectrophotometric Analysis of Microcapsules Containing Immortelle Essential Oil

In this study, microcapsules were prepared by solvent evaporation technique using ethyl cellulose component as wall and essential oil as core material. The synthesis of microcapsules was carried out using different oil masses. The analysis of the microcapsules was carried out using field emission scanning electron microscope (FE-SEM) and UV spectrophotometric analysis using absorption spectrophotometer. The obtained results confirm the regular spherical shape and size of the synthesized microcapsules. The qualitative and quantitative spectrophotometric analysis of the microencapsulated immortelle oil was measured at the wavelength of 265 nm. The calibration diagram was used to calculate the unknown concentrations of the microencapsulated oil. The obtained results confirm the application of the presented method as relevant for the possible determination of microencapsulated oil on textile materials.     

Preparation and Characterization of Oil Containing Microcapsules Obtained by an Interaction Induced Coacervation

A novel method for microencapsulation of oil by coacervation is presented. The method employs segregative phase separation between sodium carboxymethyl cellulose (NaCMC) and a complex of hydroxypropylmethyl cellulose (HPMC) and sodium dodecylsulfate (SDS), which results in coacervate formation. Microstructural properties of the coacervate can be varied by tuning NaCMC-HPMC/SDS interaction, which is achieved by changing SDS concentration. Microcapsules preparation route is presented. Encapsulation efficiency and dispersion properties of microcapsules with coacervate shell of different properties and different oil content were tested. Microcapsules with smallest droplet size, the narrowest droplet size distribution, and with lowest extractability of encapsulated oil were obtained when NaCMC-HPMC/SDS interaction results in formation of the most compact coacervate shell, no matter of the encapsulated oil.     

Effect of drug-loading methods on drug load, encapsulation efficiency and release properties of alginate/poly-L-arginine/chitosan ternary complex microcapsules

The drug-loaded alginate/poly-L-arginine/chitosan ternary complex microcapsules were prepared by mixing method, absorption method and the combined method of mixing and absorption, respectively. The effect of drug-loading methods on drug load, the encapsulation efficiency and the release properties of the complex microcapsules were investigated. The results showed that the absorption process is a dominating factor to greatly increase the drug load of Hb into microcapsules. Upon loading Hb into microcapsules by combined method of mixing and absorption, the drug load (19.9%) is up to the maximum value, and the encapsulation efficiency is 93.8%. Moreover, the drug release is a zero-order kinetics process for the ternary complex microcapsules made by mixing. For the complex microcapsules made by absorption, the drug release is a first-order kinetics. However, for the complex microcapsules made by combining the mixing and the absorption, the drug release obeys a first-order kinetics during the first eighteen hours, changing afterwards to a zero-order kinetics process. Effect of drug-loading methods on drug load and encapsulation efficiency of alginate/poly-L-arginine/chitosan ternary complex microcapsules.     

十八烷/聚(St-MMA)相变微胶囊制备及表征

采用乳液聚合的方法,分别选取聚苯乙烯(PS)、聚甲基丙烯酸甲酯(PMMA)或苯乙烯和甲基丙烯酸甲酯的共聚物为壁材,正十八烷为芯材,十二烷基苯磺酸钠(SDBS)为乳化剂,制作相变储能微胶囊。用粒径分析仪、透射电子显微镜(TEM)、热重分析仪(TG)和示差扫描量热测试仪(DSC)对微胶囊的形貌、相变热性能和热稳定性分别进行表征。结果表明:壁材选取两者共聚物,当两种单体的比例为St∶MMA=1∶5,SDBS用量为1.5g(总质量的3%)时,微胶囊粒径大小均匀,粒子分散性好,壁材的包裹性好。微胶囊的放热峰为起始温度为27.3℃,终止温度为31.9℃,相变温度为28.9℃,相变焓为48.4J/g。TG表明长期使用温度不能超过131℃。IR分析微胶囊中含有芯材和壁材。这种十八烷/聚(St-MMA)相变微胶囊可以用于诸能材料。     

Preparation of poly(butylene-co-ε-caprolactone carbonate) and their use as drug carriers for a controlled delivery system

Poly(butylene-co-ε-caprolactone carbonate) (PBCCL) was successfully synthesized via terpolymerization of carbon dioxide, 1,2-butylene oxide (BO), and ε-caprolactone (ε-CL). ε-CL was inserted into the backbone of BO-CO₂. The glass transition temperature (T_g) and the decomposition temperature (T_d) of PBCCL were much higher than those of poly(butylene carbonate) (PBC). The degradation rate of PBCCL was higher than that of PBC in a pH 7.4 phosphate-buffered solution. ε-CL offered an ester structural unit that gave the terpolymers remarkable degradability. PBC and PBCCL microcapsules containing a hydrophilic antibiotic drug pazufloxacin mesilate (PZFX) were elaborated by solvent evaporation method based on the formation of double W/O/W emulsion. Microcapsules were characterized in terms of the morphology, size, amount of encapsulated, and encapsulation efficiency. The results showed that the microcapsules had smooth and spherical surfaces, and the mean diameter of the microcapsules was in the range of 0.5–1 μm. Of all, 87.90% drug encapsulation efficiency has been achieved for microcapsules of 38.21% drug loading. In vitro drug release of these microcapsules was performed in a pH 7.4 phosphate-buffered solution. The release profiles were investigated from the measurement of PZFX presented in the release medium at various intervals. The release profiles of PZFX from PBC and PBCL microcapsules were found to be biphasic with a burst release followed by a gradual release phase. The release rate of PZFX from the microcapsules increased with increasing the content of ε-CL inserted into the copolymers. It showed that the release profiles of PZFX were highly polymer-dependent. © 2007 Wiley Periodicals, Inc. JPolym Sci Part A: Polym Chem 45: 2152–2160, 2007     

Characterization of ovalbumin-containing polyurethane microcapsules with different structures

Ovalbumin (OVA)-containing polyurethane microcapsules were successfully prepared by a reaction between toluene diisocyanate (TDI) and different polyols such as glycerol, ethane diol, and propylene glycol. The structural and thermal properties of the resultant microcapsules and the release profile of the OVA from the wall membranes were studied. In conclusion, the microcapsules from the glycerol showed the highest thermal stability, with the formation of many hydrogen bonds. From the data of release profiles, it was confirmed that the particle size distribution and morphologies of microcapsules determined the release profiles of the OVA from the wall membranes.     

丁烯氟虫腈缓释微胶囊的制备及其性能

以丁烯氟虫腈为囊芯化合物,带有相反电性的壳聚糖和海藻酸钠为囊壁材料,采用层层自组装技术制备了丁烯氟虫腈微胶囊,通过流点法筛选出十二烷基苯磺酸钠为丁烯氟虫腈的分散稳定剂。 对制备的微胶囊进行了表征,系统研究了丁烯氟虫腈微胶囊的载药量、包封率、缓释性能和抗光解性能随着组装层数增加的变化规律。 结果表明,组装层数为6~8层的丁烯氟虫腈微胶囊的包封率达到80%以上,达最高释放量所需要的时间为60 h,光解率降到20%以下,综合效果最好。     

The Role of Microencapsulation in Food Application

Modern microencapsulation techniques are employed to protect active molecules or substances such as vitamins, pigments, antimicrobials, and flavorings, among others, from the environment. Microencapsulation offers advantages such as facilitating handling and control of the release and solubilization of active substances, thus offering a great area for food science and processing development. For instance, the development of functional food products, fat reduction, sensory improvement, preservation, and other areas may involve the use of microcapsules in various food matrices such as meat products, dairy products, cereals, and fruits, as well as in their derivatives, with good results. The versatility of applications arises from the diversity of techniques and materials used in the process of microencapsulation. The objective of this review is to report the state of the art in the application and evaluation of microcapsules in various food matrices, as a one-microcapsule-core system may offer different results according to the medium in which it is used. The inclusion of microcapsules produces functional products that include probiotics and prebiotics, as well as antioxidants, fatty acids, and minerals. Our main finding was that the microencapsulation of polyphenolic extracts, bacteriocins, and other natural antimicrobials from various sources that inhibit microbial growth could be used for food preservation. Finally, in terms of sensory aspects, microcapsules that mimic fat can function as fat replacers, reducing the textural changes in the product as well as ensuring flavor stability.