叶面亲和型阿维菌素微胶囊的制备及pH响应性释放性能

为减少农药流失，设计了一种叶面亲和型缓释微胶囊。以甲基丙烯酸甲酯（MMA）接枝改性羧甲基纤维素（CMC）得到羧甲基纤维素-聚甲基丙烯酸甲酯（CMC-g-PMMA），然后利用自组装负载阿维菌素（AVM）形成载药微胶囊（CMC-g-PMMA@AVM），通过多巴胺（DA）包覆提高CMC-g-PMMA@AVM的叶面亲和性。采用扫描电镜、红外光谱、热重分析等对其结构和形貌进行表征，研究了微胶囊的载药性能、叶面亲和性及响应释放性能。结果显示，DA/CMC-g-PMMA@AVM为平均粒径126nm的球形粒子，多巴胺的包覆可有效提高微胶囊的载药性能，包封率可达88.56%；增强AVM的叶面亲和性，使其叶面滞留量相对于阿维菌素水乳液提升30.56%；赋予AVM优异的抗紫外光分解性能，强紫外光照射60min后，由AVM水乳液中AVM的残留率14.03%提高到DA/CMC-g-PMMA@AVM中的59.55%。载药微胶囊中药物释放具有pH响应，在pH=5条件下出现爆释，药物释放过程符合Weibull模型，受Fick扩散控制。     

羧甲基壳聚糖-蓖麻油基聚氨酯农药缓释微球的制备及性能

以羧甲基壳聚糖（CMCS）、蓖麻油（CO）和异佛尔酮二异氰酸酯（IPDI）为原料，自乳化法制备了羧甲基壳聚糖-蓖麻油基聚氨酯微球（CO-CMCS-PU），通过分子自组装法负载阿维菌素（AVM）得到载药微球（CO-CMCS-PU@AVM）。采用FTIR、1HNMR、SEM、TGA等对产品结构及形貌进行表征，并探究了不同药量载药微球的包封率、缓释性能、抗紫外性能、叶面接触角和黏附性能。结果表明，相比AVM分散液，紫外照射后载药微球中AVM的保留率提高到43%，说明CO-CMCS-PU载体的抗紫外性能良好；载药微球比AVM分散液在黄瓜叶面上的接触角降低了20%以上，滞留量提高了40%以上，说明其在叶面上有较好的黏附性和润湿性；载药微球包封率可达80%以上，具有良好的缓释和pH响应释放性能，释药行为符合First-order动力学模型，药物释放受Fickian扩散控制。     

木质素季铵盐-海藻酸钠聚合物负载阿维菌素粉体的制备及抗紫外光性能分析

以三甲基木质素季铵盐-海藻酸钠(QL-SA)为载体,用物理混合法制备了阿维菌素缓释聚合物(AVM-QL-SA),利用FT-IR对其结构进行了表征,探讨了交联剂用量、药物加入量、体系pH值等因素对载药量和包封率的影响,并对其缓释性能和抗紫外光降解进行了研究。结果表明:阿维菌素(AVM)均匀的混合在QL-SA载体中,主要以物理混合为主;最佳制备条件为:戊二醛为5%(以单体质量分数计)、药物加入量为1%(以单体质量分数计)、体系pH值为8.5,载药量和包封率分别达到1.36%和73.36%;阿维菌素缓释聚合物粒径符合正态分布,平均粒径为83.90 μm;阿维菌素缓释聚合物具有很好的缓释性能,在乙醇/水(体积比1:1)中释放30 h,累计释放率为88.97%;经8 h紫外光照射,阿维菌素原药中AVM残留量为6.24%,阿维菌素缓释聚合物中AVM残留量为37.75%,具有良好的抗紫外分解性能。     

硅烷化聚琥珀酰亚胺负载阿维菌素的制备与性能

为了减少农药的流失和降解,采用纳米材料与技术开发新型纳米剂型具有巨大潜力。本文以3-氨丙基三乙氧基硅烷（APTES）和丁二胺（DBA）为改性单体,采用胺解开环反应制备了硅烷化聚琥珀酰亚胺（PDSi）,并通过自组装方式负载阿维菌素（AVM）得到AVM@PDSi纳米体系。结果表明,相较于原药,AVM@PDSi对叶面的黏附性明显提升,叶面滞留量提高了56.50%。PDSi材料具有良好的抗氧化活性,PDSi对1,1-二苯基-2-苦基肼（DPPH）自由基的清除率最高可达41.88%。AVM@PDSi具有良好的抗紫外性能,在相同的紫外强度照射下（E_max=365nm）,AVM@PDSi半衰期比原药AVM延长了近一半。AVM@PDSi具有良好的缓释性能和pH响应释放性能,在pH=9时释放最快;在pH=7时,AVM@PDSi-3在72h后累积释放量为67%。研究表明,AVM@PDSi具有良好的储存稳定性,并且保留了AVM的杀虫活性。     

pH响应性阿维菌素/介孔硅的一步合成与释放

以三嵌段共聚物F127（(EO)106(PO)70(EO)106）为模板剂,正硅酸甲酯（TMOS）为硅源,阿维菌素(AVM)为模型药物,通过一步法合成载药介孔硅材料(HOMS),采用铜、锌、锰3种金属离子改性,形成具有pH响应性的缓释材料AVM/Zn-HOMS、AVM/Cu-HOMS和AVM/Mn-HOMS,借助FTIR、SEM、N2吸附-脱附法和TGA表征了缓释材料,并研究了其在不同pH下的释放行为。结果表明,AVM/Zn-HOMS、AVM/Cu-HOMS和AVM/Mn-HOMS材料表面分别呈现层状、疏松多孔状以及气泡状结构,比表面积分别为308.581、101.218和318.011 m2/g,氮气吸附-脱附等温线类型为具有H2型滞后环的Langmuir Ⅳ型。AVM/Zn-HOMS和AVM/Cu-HOMS呈现良好的pH响应性,AVM/Mn-HOMS则未表现出明显的pH响应性,3种材料的缓释行为均可用Higuchi动力学模型描述,释放过程受扩散机制控制。     

海藻酸钙/埃洛石载药微球的制备与缓释盐酸二甲双胍性能

缓释可提高药物利用率,降低其毒副作用。采用交联法制备了海藻酸钙/埃洛石载药微球,以载药微球对盐酸二甲双胍（MH）药物的包封率和缓释效果为考察对象,研究了载药微球的制备工艺和缓释性能,并通过SEM、FTIR和TGA对其结构进行了表征。结果表明：在交联温度为0℃、海藻酸钠用量为1g、埃洛石添加量为2g时,能得到较优的载药微球包封率（79.23%）。上述条件下制得的复合载药微球在pH=6.8的磷酸盐缓冲液中能有效缓释,且720min后缓释度可达85.83%,说明其具有较好的pH敏感性和缓释效果。SEM表明海藻酸钙颗粒与埃洛石在载药微球内部形成复合结构,FTIR表明MH主要以物理包埋的形式于载药微球中,TGA表明添加埃洛石可以提高复合材料在200℃以上的热稳定性。     

载阿霉素聚乳酸多孔微球的表征及释药性能

以阿霉素（DOX）为小分子化学药物模型,采用吸附法对聚乳酸（poly-L-lactide,PLLA）多孔微球进行载药,采用场发射扫描电子显微镜（FE-SEM）、傅里叶变换红外光谱（FTIR）、X射线衍射（XRPD）及差示扫描量热（DSC）对DOX-PLLA复合微球的形貌粒径及空气动力学性能、药物及材料的理化性能、载药性能进行表征,并且研究了其载药量、包封率和体外释放性能。结果表明,不同载药量之间的PLLA多孔微球粒径并无显著差异,均具有良好的空气动力学性能,适合肺部可吸入给药的条件;化学组成未见明显改变,物理结构由结晶态变为无定形态;随载药量的增加（2.9%,4.0%,4.6%）,包封率逐渐降低（56%,51%,44%）;药物的体外释放与原料药相比具有一定的缓释效果,最长释放时间可达5天,表明DOX-PLLA复合微球有望作为缓释制剂用于肺部给药。     

氧化石墨烯对盐酸四环素的缓释性能研究

本文以氧化石墨烯为药物载体,承载盐酸四环素,探究不同的载药量、pH值、温度的装载率和缓释性能。结果表明,氧化石墨烯的载药率为81.5%,包封率为16.3%。且在pH为5的条件下药物缓释性能最佳,24小时后累计释放率为72.89%;在一定温度范围内,温度越高其药物累积释放率越多。当温度为60℃时,8小时后药物累计释放率为58.59%。     

pH响应性阿维菌素/介孔硅的一步合成与释药性能

以三嵌段共聚物F127[(EO)_(106)(PO)_(70)(EO)_(106)]为模板剂,正硅酸甲酯(TMOS)为硅源,阿维菌素(AVM)为模型药物,通过一步法合成了载药介孔硅材料(AVM/HOMS),采用铜、锌、锰3种金属离子改性,制备了具有pH响应性的缓释材料AVM/Zn-HOMS、AVM/Cu-HOMS和AVM/Mn-HOMS,借助FTIR、SEM、N2吸附-脱附法和TGA表征了缓释材料,并研究了其在不同pH下的释放行为。结果表明:AVM/Zn-HOMS、AVM/Cu-HOMS和AVM/Mn-HOMS材料表面分别呈现层状、疏松多孔状以及气泡状结构,比表面积分别为308.581、101.218和318.011 m2/g,氮气吸附-脱附等温线类型为具有H2型滞后环的LangmuirⅣ型。AVM/Zn-HOMS和AVM/Cu-HOMS呈现良好的pH响应性,AVM/Mn-HOMS则未表现出明显的pH响应性,3种材料的缓释行为均可用Higuchi动力学模型描述,释放过程受扩散机制控制。     

O-季铵化改性壳聚糖固载环糊精的制备及其载药性能

对壳聚糖进行O-季铵化改性,并与羧甲基-β-环糊精在均相条件下进行缩合反应,制得O-季铵化壳聚糖固载环糊精(QCSCD),用FTIR、EA和SEM对产物进行表征。以酮洛芬为模型药物,研究其载药及药物释放行为。结果表明,季铵盐基团的引入提高了QCSCD的载药量,为3.97mg/mg,并且改变了QCSCD的pH响应性能。与壳聚糖固载环糊精相反,QCSCD在模拟胃液中的释放速率很快,而在模拟肠液中具有缓释性能。     

Elaboration of a feather keratin/carboxymethyl cellulose complex exhibiting pH sensitivity for sustained pesticide release

Feather keratin (FK) and carboxymethyl cellulose (CMC) were used as raw materials to prepare a FK/CMC polyelectrolyte complex via electrostatic interactions. Using avermectin (AVM) as a model drug and elevated temperature, an FK/CMC@AVM drug-carrying complex was obtained. The structure and morphology of FK/CMC@AVM were both analyzed by Fourier transform infrared spectroscopy, dynamic light scattering, and scanning electron microscopy (SEM). Furthermore, the encapsulation efficiency, anti-ultraviolet, sustained release, and toxicity properties of FK/CMC@AVM were studied. The results showed that the average particle size of FK/CMC@AVM was 386.57 nm and the encapsulation efficiency was 67.06%. Under UV light irradiation, FK/CMC@AVM significantly improved the stability of AVM and the half-life of AVM was found to be delayed from 354 to 1800 min. Moreover, the sustained release of AVM featured pH sensitivity and was consistent with the Korsmeyer–Peppas model. Upon increasing the pH from 1.5 to 9.5, the release mechanism of AVM changed from Fick diffusion to non-Fick diffusion. Finally, the toxicity characteristics of FK/CMC@AVM were not significantly different from those of nonmodified AVM. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 47160.     

Avermectin/polyacrylate nanoparticles: preparation,characterization, anti-UV and sustained release properties

In an effort to reduce the dose of drugs and in order to improve drug efficacy, avermectin (AVM) was encapsulated by amphipathic polyacrylic ester (PAE) via self-assembly. The experimental results indicated that the AVM/PAE nanoparticles were spherical in shape, homogeneous dispersion, and had a core-shell structure, the particle size ranged from 172.7?nm to 337.8?nm, the highest encapsulation efficiency and loading capacity were 62.11 and 25.65%. The anti-UV property has been significantly improved. Consistent with the Korsmeyer–Peppas model, the release rate was observed to be higher upon decreasing Tg and increasing the core-shell ratio.     

基于静电纺丝技术的农药传递体系的制备与性能表征

为获得一种新型高载药量、易分散型农药制剂,基于药物传递理论,以阿维菌素（AVM）为农药模型,以乙基纤维素（EC）为主要农药载体,以卡波姆（CB）为改性材料,利用静电纺纳米纤维载药技术构建一种具有微纳结构的农药传递体系。通过对复配比例、溶解参数及纺丝条件的探索,结果表明：采用N,N-二甲基乙酰胺与乙醇以体积比3∶1的混合溶剂对载体材料EC与CB分别进行溶解,EC与CB纺丝液的体积复配比为1∶1时,农药传递体系的载药量可高达35.7%,包封率接近100%,耐光解性大幅提升。并且,该农药传递体系的水分散性非常优异,具有长效释药性。     

Carboxymethyl chitosan-graft-phosphatidylethanolamine: Amphiphilic matrices for controlled drug delivery

Modified carboxymethyl chitosan (CMC) containing phosphatidylethanolamine (PEA) groups were synthesized by a 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC)-mediated coupling reaction. The structure of the modified CMC exhibiting an amphiphilic character was analysed by FT-IR and ¹H NMR. CMC-g-PEA beads were prepared with sodium tripolyphosphate (TPP) by ionic-crosslinking. The beads sizes were in range from 800 to 1200 μm and encapsulation efficiencies of drug were more than 68%. The morphologies of CMC-g-PEA beads were examined with scanning electron microscopy (SEM). The release experiments were performed using ketoprofen as an hydrophobic model drug. The drug dissolution kinetics showed longer release times for CMC-g-PEA beads: 20 h (at pH 1.4) and 45 h (at pH 7.4). The amount of the drug release was much higher in acidic solution than in basic solution due to the swelling properties of the matrix at acidic pH. These results suggest that modified CMC with PEA may become a potential delivery system to control the release of hydrophobic drugs.     

Structure and control release of chitosan/carboxymethyl cellulose microcapsules

Microcapsules of chitosan/sodium carboxymethyl cellulose (NaCMC) were successfully prepared using a novel method of emulation phase separation. Their structure and morphology were characterized by infrared spectroscopy (IR), scanning electron microscopy (SEM), and X-ray diffraction. Bovine serum albumin (BSA) was encapsulated in the microcapsules to test their release behavior. The swelling behavior, encapsulation efficiency, and release behavior of the microcapsules with different chitosan contents and pH conditions were investigated. The results indicated that the microcapsules have a high encapsulation efficiency (75%) and a suitable size (20–50 μm). The BSA in the microcapsules was speedily released at pH 7.2, namely, in intestinal fluid. The BSA release was reduced with increase of the chitosan content from 17 to 38% in the microcapsules. Acid-treated microcapsules have a compact structure, owing to a strong electrostatic interaction caused by —NH₂ groups of chitosan and —COOH groups of CMC, and the encapsulated BSA was hardly released at pH 1.0, namely, in gastric juice. © 2001 John Wiley & Sons, Inc. J Appl Polym Sci 82: 584–592, 2001     

Preparation and properties of physically crosslinked sodium carboxymethylcellulose/poly(vinyl alcohol) complex hydrogels

A series of physically crosslinked complex hydrogels of poly(vinyl alcohol) (PVA) and sodium carboxymethylcellulose (CMC) were prepared via physical mixing and a freeze/thaw technique. The morphology of the CMC/PVA complex gels was analyzed with differential scanning calorimetry and wide‐angle X‐ray diffraction. It was found that the crystallinity and melting temperature of the complex gels decreased, whereas the glass‐transition temperature increased, with an increase in the content of CMC. The reswelling of the complex gels was pH‐responsive and relied on the content of CMC and the freeze/thaw cycles. A network structure model of the complex gel was presented. PVA crystalline regions served as physical crosslinks; the interaction between CMC and PVA resulted in intramolecular entanglements. It was also found that the model drug hemoglobin was released completely from the complex hydrogels in 4 h, and its release rate increased with an increase in the content of CMC. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008     

Smart carboxymethylchitosan hydrogels that have thermo‐ and pH‐responsive properties

Thermo‐responsive poly(N‐isopropylacrylamide) (poly(NIPAAm)) and pH‐responsive poly(N,N′‐diethylaminoethyl methacrylate) (poly(DEAEMA)) polymers were grafted to carboxymethylchitosan (CMC) via radical polymerization to form highly water swellable hydrogels with dual responsive properties. Ratios of CMC, NIPAAm to DEAEMA used in the reactions were finely adjusted such that the thermo and pH responsiveness of the hydrogels was retained. Scanning electron microscopy (SEM) indicated the formation of an internal porous structure for the swollen CMC hydrogels upon incorporation of poly(NIPAAm) and poly(DEAEMA). Effect of temperature and pH changes on water swelling properties of the hydrogels was investigated. It was found that the water swelling of the hydrogels was enhanced when the solution pH was under basic conditions (pH 11) or the temperature was below its lower critical solution temperature (LCST). These responsive properties can be used to regulate releasing rate of an entrapped drug from the hydrogels, a model drug, indomethacin was used to demonstrate the release. These smart and nontoxic CMC‐based hydrogels show great potential for use in controlled drug release applications with controllable on‐off switch properties. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41505.     

Synthesis and evaluating of carbon nanoallotrope-biomacromolecule gel composites as drug delivery systems

This work was done to assess the role of precursors (agro and graphite) on performance of carbon nanoallotropes-biomacromolecules composite as drug delivery for controlling the release of niacin. In this respect graphene oxide and bagasse-based carbon oxide were synthesized and chelated with chitosan (Cs-GO and Cs-Co). These gel composites were characterized by many techniques [morphology, differential scanning calorimetry, Fourier-transform infrared spectroscopy, swelling, encapsulation efficiency (EE) and loading (L) % of niacin. Another series of experiments was carried out for studying the role of replacing part of carbon nanoallotrope by carboxymethyl cellulose (CMC) on performance of produced drug carries, these systems were coded as Cs-GO-CMC and Cs-Co-CMC. The data showed that, the Cs-GO gel composite provided maximum release of NA, at 5 h, for pH's simulated gastric and intestinal fluids; pH. 2.1 and pH 7.4 (1120 mg/L and 757 mg/L). The incorporation of CMC is not acceptable as it provided low drug release together with burst release of NA-drug, and consequently possible caused tissue irritation or toxicity in the human body. The Cs-GO and Cs-CO systems with relatively low drug loading were recommended for their better controllability system to NA release, which prolonging benefit of human with niacin. The NA release from all investigated gels followed Fickian and non-Fickian diffusion mechanisms.