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Impact of formulation design and lyophilisation on the physicochemical characteristics of finasteride nanosystems. 配方设计和冻干对非那雄胺纳米系统理化特性的影响。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-03-01 DOI: 10.1080/02652048.2023.2178537
Malik Muhammad Irfan, Shefaat Ullah Shah, Kifayat Ullah Shah, Nicolas Anton, Idoux-Gillet Ysia, Guillaume Conzatti, Kifayat Ullah Shah, Perennes Elise, Thierry Vandamme

The fundamental purpose of this study was to develop a stable lyophilised finasteride nanosystem (FNS-NS) for topical delivery. The FNS-NS was fabricated using an ultrasonication technique. The impact of two different cryoprotectants on the physicochemical characteristics of FNS-NS before and after lyophilisation was thoroughly investigated. The lyophilised FNS-NS had spherical shape with particle size lied between 188.6 nm ± 4.4 and 298.7 nm ± 4.7, low PDI values (0.26 ± 0.02 to 0.32 ± 0.02) and zeta potential ranging from -38.3 to +53.3 mV. The confocal laser microscopy depicted a comparatively higher cellular internalisation achieved for undecorated FNS-NS with respect to its chitosan-decorated counterpart. The lyophilised FNS-NS was stable for 90 days at proper storage conditions. The FNS-NS with 15% trehalose had appropriate physicochemical attributes that could be a promising carrier for topical delivery to treat androgenic alopecia.

本研究的基本目的是开发一种稳定的冻干非那雄胺纳米系统(FNS-NS)用于局部给药。利用超声技术制备了FNS-NS。研究了两种不同的冷冻保护剂对FNS-NS冻干前后理化特性的影响。冻干后的FNS-NS呈球形,粒径在188.6 nm±4.4 ~ 298.7 nm±4.7之间,PDI值较低(0.26±0.02 ~ 0.32±0.02),zeta电位在-38.3 ~ +53.3 mV之间。共聚焦激光显微镜描绘了相对较高的细胞内化实现了未修饰的FNS-NS相对于其壳聚糖修饰的对应物。冻干后的FNS-NS在适当的保存条件下可稳定保存90天。添加15%海藻糖的FNS-NS具有良好的理化特性,是治疗雄激素性脱发的理想载体。
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引用次数: 0
Design, development and characterisation of an optimised scaffold to enhance cell proliferation for tissue repair. 优化支架的设计,开发和特性,以促进组织修复的细胞增殖。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-03-01 DOI: 10.1080/02652048.2023.2175922
Subodh Kumar, Chanakya Lahiri, Somya Chaaudhary, Prateek Paul, Yogesh Kumar Verma

Scaffolds are implanted to spur the regeneration of damaged tissues. The inappropriate construction of scaffolds laden with cells is not efficient. The optimisation of the scaffolds' constituents is essential for tissue repair. In this study, a scaffold embedded with Raloxifene drug was optimised via Response Surface Methodology (RSM), targeting controlled cell proliferation. The independent variables for RSM (fibronectin, collagen I, glutaraldehyde, and Raloxifene) were screened in Swiss target prediction software (probability ≥99%) to optimise dependent variables (porosity, cell viability, degradation, and swelling) by ANOVA and characterised with FTIR, SEM and contact angle measurement. The scaffold was tested for antimicrobial property, and proliferation and attachment of mouse mesenchymal stem cells. The ANOVA analysis with p value ≤ 0.0001 suggested the optimal concentration of biomaterials and drugs. The optimised scaffold displayed 80% porosity with pore size 33 ± 3 µm. We also observed significant cell attachment and proliferation (p value ≤ 0.05) in optimised scaffold. The scaffold may be further evaluated for its potential for tissue repair.

植入支架来刺激受损组织的再生。不适当的细胞支架结构是没有效率的。支架成分的优化对组织修复至关重要。在本研究中,通过响应面法(Response Surface Methodology, RSM)优化了雷洛昔芬药物包埋支架,以控制细胞增殖。RSM的自变量(纤维连接蛋白、ⅰ型胶原、戊二醛和雷洛昔芬)在瑞士靶标预测软件中筛选(概率≥99%),通过方差分析优化因变量(孔隙度、细胞活力、降解和肿胀),并用FTIR、SEM和接触角测量进行表征。对该支架进行了抗菌性能和小鼠间充质干细胞的增殖和附着试验。p值≤0.0001的方差分析提示生物材料和药物的最佳浓度。优化后的支架孔隙率为80%,孔径为33±3µm。我们还观察到优化后的支架有显著的细胞附着和增殖(p值≤0.05)。该支架的组织修复潜力有待进一步评估。
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引用次数: 0
Microencapsulation of n-tetradecane with poly (methyl methacrylate-co-methacrylic acid) shell by seeded emulsion polymerisation and its thermal energy storage characteristics. 种子乳液聚合法制备正十四烷与聚甲基丙烯酸甲酯-共甲基丙烯酸壳的微胶囊化及其储热特性
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-03-01 DOI: 10.1080/02652048.2023.2175923
U R Mahajan, I Emmanuel, A Shrinivasa Rao, S T Mhaske

This study aims to enhance the latent heat storage properties of the microcapsules by altering the amount of crosslinking agent from 3 to 20%w/w, the core-to-shell ratio from 1:1 to 2:1, and the amount of initiator from 1 to 3%. The phase change material n-tetradecane (C-14) was microencapsulated by using poly (methyl methacrylate -co- methacrylic acid) as a shell material through an oil by water-seeded emulsion polymerisation technique. The structural, morphological, and thermal properties of microcapsules were evaluated by using Fourier transform infrared spectroscopy, optical microscopy, scanning electron microscopy, differential scanning calorimetry analysis, and thermogravimetric analysis. The average particle size of the microcapsules ranges from 01 to 15 µm. The results showed that the microcapsules have a higher melting enthalpy value of 127.3 ± 0.06 J/g with a microencapsulation efficiency of 66.72% when a 20% w/w crosslinker was used. The thermal stability of the phase change material (PCM) was increased by ∼30 ± 2 °C by encapsulation.

通过将交联剂用量从3%提高到20%w/w,核壳比从1:1提高到2:1,引发剂用量从1%提高到3%,提高微胶囊的潜热储存性能。以聚甲基丙烯酸甲酯-co-甲基丙烯酸为包壳材料,采用油水种子乳液聚合技术对相变材料正十四烷(C-14)进行了微囊化。采用傅里叶变换红外光谱、光学显微镜、扫描电镜、差示扫描量热分析和热重分析对微胶囊的结构、形态和热性能进行了评价。微胶囊的平均粒径为01 ~ 15µm。结果表明,当交联剂用量为20% w/w时,微胶囊的熔融焓值为127.3±0.06 J/g,微胶囊化效率为66.72%。通过封装,相变材料(PCM)的热稳定性提高了~ 30±2°C。
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引用次数: 2
Poly(lactic acid)/β-cyclodextrin based nanoparticles bearing ruthenium(II)-arene naproxen complex: preparation and characterisation. Analytical validation for metal determination by microwave-induced plasma optical emission spectrometry. 含钌(II)-芳烃萘普生配合物的聚乳酸/β-环糊精纳米颗粒:制备和表征。微波诱导等离子体发射光谱法测定金属的分析验证。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-03-01 DOI: 10.1080/02652048.2023.2172469
Ruan Reis Nascimento, Julie Pauline Gaitan Tabares, Paulo Neilson Marques Dos Anjos, Luana Novaes Santos, Denise de Oliveira Silva, Rodrigo Luis Silva Ribeiro Santos

The objectives of this work are to develop nanocarrier systems for the Ru(II)-p-cymene naproxen antitumor metallodrug, [Ru(η6-p-cymene)(npx)Cl] or Rupcy, based on polymeric nanoparticles (NPs) composed by the biodegradable poly(lactic acid) (PLA) and the hydrophilic polymerised β-cyclodextrin (PolyCD); to validate an analytical method for determination of Ru incorporated into the metallodrug loaded-NPs. The PolyCD was prepared by single step condensation and polymerisation reaction and incorporated as a polymer blend during the fabrication of PLA/PolyCD blends NPs and also as a core/shell structure built by adsorption of the PolyCD onto the surface of PLA NPs to give PLA(core)/PolyCD(shell) NPs. Three different loaded-systems incorporating the metallodrug (Rupcy-PLA NPs (1), Rupcy-PLA/PolyCD blends (2), and Rupcy-PLA(core)/PolyCD(shell) NPs (3)) were prepared by nanoprecipitation. The characterisation was performed by Proton Nuclear Magnetic Resonance, Matrix Assisted Laser Desorption/Ionization Time-of-Flight, Fourier-Transform Infra-red and UV-VIS Electronic Absorption Spectroscopies, Thermogravimetric Analysis, Differential Scanning Calorimetry, Dynamic Light Scattering, and Electrophoretic Light Scattering. Ru was determined by Microwave Induced Plasma Optical Emission Spectrometry (MIP-OES) with validation of the method. The metallodrug entrapment efficiency was around 90% (w/w) and drug loading was at 3-4% (w/w). The characterised metallodrug-loaded systems exhibited monomodal size distributions and appropriate hydrodynamic diameters [218.3 ± 13.5 (1), 205.4 ± 14.4 (2), 231.5 ± 22.0 (3) nm] and zeta potential values [-31.5 ± 2.2 (1), -26.1 ± 4.5 (2), -28.8 ± 6.1 (3) mV]. The validation of the MIP-OES method by evaluating selectivity, linearity, precision, accuracy, and limits of detection and quantification succeeded. The NPs parameters are compatible with colloidally stable systems. The MIP-OES method showed to be simple, reliable, and feasible to quantify indirectly the amount of the metallodrug-loaded into the PLA NPs.

本研究的目的是基于由可生物降解的聚乳酸(PLA)和亲水性聚合的β-环糊精(PolyCD)组成的聚合物纳米颗粒(NPs),开发Ru(II)-对伞花烯萘普生抗肿瘤金属药物[Ru(η - 6-对伞花烯)(npx)Cl]或Rupcy的纳米载体体系;验证了金属药物负载nps中Ru含量的分析方法。PolyCD通过单步缩合和聚合反应制备,并在PLA/PolyCD共混NPs制备过程中作为聚合物共混物加入,同时通过将PolyCD吸附在PLA NPs表面形成PLA(核)/PolyCD(壳)NPs。采用纳米沉淀法制备了三种不同的金属药物负载体系(Rupcy-PLA NPs(1)、Rupcy-PLA/PolyCD共混物(2)和Rupcy-PLA(核)/PolyCD(壳)NPs(3))。通过质子核磁共振、矩阵辅助激光解吸/电离飞行时间、傅里叶变换红外和紫外可见电子吸收光谱、热重分析、差示扫描量热法、动态光散射和电泳光散射进行表征。采用微波诱导等离子体发射光谱法(MIP-OES)测定钌,并对方法进行了验证。金属药物包封效率约为90% (w/w),载药量为3 ~ 4% (w/w)。所表征的金属药物负载体系具有单峰尺寸分布和合适的流体动力直径[218.3±13.5(1),205.4±14.4(2),231.5±22.0 (3)nm]和zeta电位值[-31.5±2.2(1),-26.1±4.5(2),-28.8±6.1 (3)mV]。通过评价选择性、线性度、精密度、准确度、检出限和定量限对MIP-OES方法进行了验证。NPs参数与胶体稳定体系兼容。MIP-OES方法简便、可靠、可行,可间接定量金属药物在PLA NPs中的负载量。
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引用次数: 1
Preparation and characterisation of self-emulsifying drug delivery system (SEDDS) for enhancing oral bioavailability of metformin hydrochloride using hydrophobic ion pairing complexation. 疏水离子对络合提高盐酸二甲双胍口服生物利用度的自乳化给药系统(SEDDS)的制备与表征。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-01-01 DOI: 10.1080/02652048.2023.2170488
Seyedeh Nika Rezvanjou, Mohammad Reza Niavand, Omid Heydari Shayesteh, Ehsan Mehrani Yeganeh, Davood Ahmadi Moghadam, Katayoun Derakhshandeh, Reza Mahjub

Aim: The aim of this study was preparation of a self-emulsifying drug delivery system (SEEDS) containing metformin hydrochloride.

Methods: Hydrophobic ion paired complexes were prepared by electrostatic interaction between metformin and sodium lauryl sulphate (SLS). The nanodroplets were optimised using two-level full factorial methodology and their morphology were examined. In vitro release of metformin from SEDDS was evaluated in simulated gastric and intestinal fluids. Finally, the ex-vivo efficacy of the optimised formulation in enhancing the intestinal permeability of metformin was evaluated using non-everted intestinal sac.

Results: The data revealed that in weight ratio 1:4(metformin: SLS), the highest recovery was achieved. The physico-chemical properties of the optimised nano-droplets including size, polydispersity index (PdI), zeta potential, and loading efficiency (%) were 192.33 ± 9.9 nm, 0.275 ± 0.051; -1.52 mV, and 93.75 ± 0.77% (w/w), respectively.

Conclusions: The data obtained from the intestinal transport study demonstrated that SEDDS can significantly enhance the oral permeability of the compound.

目的:制备盐酸二甲双胍自乳化给药系统。方法:二甲双胍与十二烷基硫酸钠(SLS)静电相互作用制备疏水离子配对配合物。采用两水平全因子方法对纳米液滴进行优化,并对其形态进行了检测。在模拟胃液和肠液中评估了SEDDS中二甲双胍的体外释放。最后,采用非外翻肠囊评价优化后的配方提高二甲双胍肠通透性的体外疗效。结果:二甲双胍:SLS质量比为1:4时,回收率最高。优化后的纳米液滴的理化性质包括粒径、PdI、zeta电位和负载效率(%)分别为192.33±9.9 nm、0.275±0.051 nm;分别为-1.52 mV和93.75±0.77% (w/w)。结论:肠道转运研究数据表明,SEDDS可显著提高化合物的口服通透性。
{"title":"Preparation and characterisation of self-emulsifying drug delivery system (SEDDS) for enhancing oral bioavailability of metformin hydrochloride using hydrophobic ion pairing complexation.","authors":"Seyedeh Nika Rezvanjou,&nbsp;Mohammad Reza Niavand,&nbsp;Omid Heydari Shayesteh,&nbsp;Ehsan Mehrani Yeganeh,&nbsp;Davood Ahmadi Moghadam,&nbsp;Katayoun Derakhshandeh,&nbsp;Reza Mahjub","doi":"10.1080/02652048.2023.2170488","DOIUrl":"https://doi.org/10.1080/02652048.2023.2170488","url":null,"abstract":"<p><strong>Aim: </strong>The aim of this study was preparation of a self-emulsifying drug delivery system (SEEDS) containing metformin hydrochloride.</p><p><strong>Methods: </strong>Hydrophobic ion paired complexes were prepared by electrostatic interaction between metformin and sodium lauryl sulphate (SLS). The nanodroplets were optimised using two-level full factorial methodology and their morphology were examined. <i>In vitro</i> release of metformin from SEDDS was evaluated in simulated gastric and intestinal fluids. Finally, the ex<i>-vivo</i> efficacy of the optimised formulation in enhancing the intestinal permeability of metformin was evaluated using non-everted intestinal sac.</p><p><strong>Results: </strong>The data revealed that in weight ratio 1:4(metformin: SLS), the highest recovery was achieved. The physico-chemical properties of the optimised nano-droplets including size, polydispersity index (PdI), zeta potential, and loading efficiency (%) were 192.33 ± 9.9 nm, 0.275 ± 0.051; -1.52 mV, and 93.75 ± 0.77% (w/w), respectively.</p><p><strong>Conclusions: </strong>The data obtained from the intestinal transport study demonstrated that SEDDS can significantly enhance the oral permeability of the compound.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"53-66"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10746231","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Polymer drug conjugates containing memantine, tacrine and cinnamic acid: promising nanotherapeutics for the treatment of Alzheimer's disease. 含有美金刚、他克林和肉桂酸的聚合物药物偶联物:治疗阿尔茨海默病的有前途的纳米疗法。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-01-01 DOI: 10.1080/02652048.2023.2167011
Tobeka Naki, William Morwa Reagile Matshe, Mohammed Olusegun Balogun, Suprakas Sinha Ray, Samuel Ayodele Egieyeh, Blessing Atim Aderibigbe

Aim: To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders.

Methods: The conjugates were characterised by 1HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by in vitro anti-acetylcholinesterase and drug release studies.

Results: 1H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC50 values in the range of 13-44.4 µm which was more effective than tacrine (IC50 =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity.

Conclusion: The drug release profile, particle sizes, and in vitro studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.

目的:制备含有美金刚、他卡因和E)- n -(3-氨基丙基)肉桂酸的聚合物-药物偶联物,这是一种治疗神经退行性疾病的有前景的药物。方法:采用1HNMR、粒度分析、SEM、LC-MS、TEM/EDX、XRD等方法对其进行表征,并进行体外抗乙酰胆碱酯酶和药物释放研究。结果:1H NMR分析显示药物偶联成功,药物质量百分比在1.3 ~ 6.0% w/w范围内。药物在20-36%范围内持续释放10 h。结合物对乙酰胆碱酯酶(AChE)活性的抑制作用显著,IC50值在13 ~ 44.4µm范围内,优于他克林(IC50 =1698.8µm)。对接研究进一步证实,将药物偶联到聚合物中可以提高其抗乙酰胆碱酯酶活性。结论:药物释放谱、颗粒大小和体外研究表明,缀合物是治疗神经退行性疾病的有希望的治疗药物。
{"title":"Polymer drug conjugates containing memantine, tacrine and cinnamic acid: promising nanotherapeutics for the treatment of Alzheimer's disease.","authors":"Tobeka Naki,&nbsp;William Morwa Reagile Matshe,&nbsp;Mohammed Olusegun Balogun,&nbsp;Suprakas Sinha Ray,&nbsp;Samuel Ayodele Egieyeh,&nbsp;Blessing Atim Aderibigbe","doi":"10.1080/02652048.2023.2167011","DOIUrl":"https://doi.org/10.1080/02652048.2023.2167011","url":null,"abstract":"<p><strong>Aim: </strong>To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and <i>E</i>)-<i>N</i>-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders.</p><p><strong>Methods: </strong>The conjugates were characterised by <sup>1</sup>HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by <i>in vitro</i> anti-acetylcholinesterase and drug release studies.</p><p><strong>Results: </strong><sup>1</sup>H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC<sub>50</sub> values in the range of 13-44.4 µm which was more effective than tacrine (IC<sub>50</sub> =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity.</p><p><strong>Conclusion: </strong>The drug release profile, particle sizes, and <i>in vitro</i> studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":"40 1","pages":"15-28"},"PeriodicalIF":3.9,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10780347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nanoencapsulation of R-phycoerytrin extracted from Solieria filiformis improves protein stability and enables its biological application as a fluorescent dye. 从丝状梭菌中提取的r -植红蛋白的纳米胶囊化提高了蛋白质的稳定性,使其作为荧光染料的生物学应用成为可能。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-01-01 DOI: 10.1080/02652048.2023.2168081
Jéssica Roberta Pereira Martins, Antonia Livânia Linhares de Aguiar, Karina Alexandre Barros Nogueira, Acrisio José Uchôa Bastos Filho, Thais da Silva Moreira, Márjory Lima Holanda Araújo, Claudia Pessoa, Josimar O Eloy, Ivanildo José da Silva Junior, Raquel Petrilli

We aimed to encapsulate R-PE to improve its stability for use as a fluorescent probe for cancer cells. Purified R-PE from the algae Solieria filiformis was encapsulated in polymeric nanoparticles using PCL. Nanoparticles were characterised and R-PE release was evaluated. Also, cellular uptake using breast and prostate cancer cells were performed. Nanoparticles presented nanometric particle size (198.8 ± 0.06 nm) with low polydispersity (0.13 ± 0.022), negative zeta potential (-18.7 ± 1.10 mV), and 50.0 ± 7.3% encapsulation. FTIR revealed that R-PE is molecularly dispersed in PCL. DSC peak at 307 °C indicates the presence of R-PE in the nanoparticle. Also, in vitro, it was demonstrated low release for nanoparticles and degradation for the free R-PE. Finally, cellular uptake demonstrated the potential of R-PE/PCL nanoparticles for cancer cell detection. Nanoparticles loaded with R-PE can overcome instability and allow application as a fluorescent probe for cancer cells.

我们的目的是封装R-PE,以提高其作为癌细胞荧光探针的稳定性。从丝状水藻中纯化的R-PE用PCL包封在聚合物纳米颗粒中。对纳米颗粒进行表征,并评价其R-PE释放度。此外,使用乳腺癌和前列腺癌细胞进行细胞摄取。纳米颗粒粒径为纳米级(198.8±0.06 nm),多分散性低(0.13±0.022),zeta电位为负(-18.7±1.10 mV),包封率为50.0±7.3%。FTIR显示R-PE分子分散在PCL中。307℃时的DSC峰表明纳米颗粒中存在R-PE。此外,在体外,它对纳米颗粒具有低释放性,对游离R-PE具有降解性。最后,细胞摄取证明了R-PE/PCL纳米颗粒用于癌细胞检测的潜力。携带R-PE的纳米颗粒可以克服不稳定性,并允许作为癌细胞的荧光探针应用。
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引用次数: 2
Synthesis characterisation and neuroprotectivity of Silybum marianum extract loaded chitosan nanoparticles. 水飞蓟提取物负载壳聚糖纳米颗粒的合成特征和神经保护作用
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-01-01 Epub Date: 2023-01-25 DOI: 10.1080/02652048.2023.2167012
Hatice Feyzan Ay, Serap Yesilkir-Baydar, Rabia Cakir-Koc

Aim: Silybum marianum extract (SME) possesses neuroprotective potency through its high antioxidant content. We attempted to increase the effectiveness of SME by encapsulating them in chitosan. Neuroprotective potency of SME and SME-loaded chitosan nanoparticles (SME-CNPs) were shown in SH-SY5Y cell line against H2O2-induced oxidative stress.

Methods: We produced CNPs and SME-CNPs by ionic gelation method and properly determined their physical characteristics. Encapsulation efficiency, loading capacity, and in vitro release tests were performed for SME-CNPs. The neurotoxicity and neuroprotective efficiency in SH-SY5Y cell line against H2O2 was also investigated.

Results: The size of SME-CNPs was 168.2 ± 11.12 nm with zeta potential 10.6 ± 1.0 mV. The encapsulation efficiency and loading capacity were successfully achieved at 96.6% and 1.89% respectively. SME and SME-CNPs improved cell viability higher than 80%, and SME-CNPs exhibited significant neuroprotective effects against H2O2 damage.

Conclusions: It was concluded that SME and SME-CNPs highly prevent damage caused by H2O2 and reduce cell damage in vitro by their neuroprotective effects.

目的:水飞蓟提取物(SME)具有很高的抗氧化剂含量,因而具有保护神经的功效。我们试图通过将 SME 包裹在壳聚糖中来提高其功效。在 SH-SY5Y 细胞系中显示了 SME 和 SME 负载壳聚糖纳米颗粒(SME-CNPs)对 H2O2 诱导的氧化应激的神经保护效力:方法:我们采用离子凝胶法制备了 CNPs 和 SME-CNPs,并正确测定了它们的物理特性。对 SME-CNPs 进行了包封效率、负载能力和体外释放试验。此外,还研究了 SME-CNPs 在 SH-SY5Y 细胞系中对 H2O2 的神经毒性和神经保护作用:结果:SME-CNPs 的尺寸为 168.2 ± 11.12 nm,zeta 电位为 10.6 ± 1.0 mV。封装效率和负载能力分别达到 96.6% 和 1.89%。SME和SME-CNPs对细胞活力的改善超过80%,SME-CNPs对H2O2损伤具有显著的神经保护作用:结论:SME 和 SME-CNPs 可有效防止 H2O2 造成的损伤,并通过其神经保护作用减少体外细胞损伤。
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引用次数: 0
L-Ascorbic acid and phosphatidylcholine complex vesicles: formation and elucidation of their biological activities, and their molecular interactions. l -抗坏血酸和磷脂酰胆碱复合物囊泡:其生物活性的形成和阐明及其分子相互作用。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2023-01-01 DOI: 10.1080/02652048.2022.2160845
Thapakorn Tree-Udom, Chalermrat Simavong, Prapasiri Phetklung, Kanjanaporn Chompoonuch, Sagaw Prateepchinda, Supatchaya Jaemsai, Andrew William King, Oraphan King

The aim is to prepare, characterise, and evaluate the biological activities and key molecular interactions of L-ascorbic acid and phosphatidylcholine (PC-AA) complex vesicles. PC-AA complexes were prepared and characterised using DLS, TEM, FTIR, UV-Vis, in-vitro release, bioactivities, and cytotoxicity. The key interactions of the AA with the PC were studied with MD simulations. PC-AA complex provides improved stability towards the degradation of AA in aqueous solutions while also slowing its release profile. The PC-AA complexes with an optimal molar ratio of PC: AA = 2.5:1 was shown to have a hydrodynamic diameter of 368.67 ± 4.65 nm and an EE of 68.16 ± 0.23%. At low concentration, the PC-AA complexes have no toxicity towards human dermal fibroblast cells over 48 h. Importantly, MD suggests that AA only forms the PC-AA complex when in its neutral form which is the desired active form. PC-AA complex could be a potential active to use in medicinal and cosmeceutical applications.

目的是制备、表征和评价l -抗坏血酸和磷脂酰胆碱(PC-AA)复合物囊泡的生物活性和关键的分子相互作用。制备了PC-AA配合物,并用DLS、TEM、FTIR、UV-Vis、体外释放度、生物活性和细胞毒性对其进行了表征。通过MD模拟研究了AA与PC的关键相互作用。PC-AA配合物提高了AA在水溶液中降解的稳定性,同时也减缓了其释放。以PC: AA = 2.5:1为最佳摩尔比的PC-AA配合物的水动力直径为368.67±4.65 nm, EE为68.16±0.23%。在低浓度下,PC-AA复合物对人真皮成纤维细胞在48小时内无毒性。重要的是,MD表明AA仅在中性形式下形成PC-AA复合物,而中性形式是期望的活性形式。PC-AA配合物在医药和药妆领域具有潜在的应用价值。
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引用次数: 0
The preparation and characterisation of tasteless core-shell clarithromycin microcapsules. 无味核壳克拉霉素微胶囊的制备与表征。
IF 3.9 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2022-11-01 DOI: 10.1080/02652048.2022.2146221
Yu Fu, Yunjing Zhu, Xue Liang, Yihan Kong, Xiaolin Wang, Anan Zhang, Zhiqing Zhao, Jingxin Gou, Yanjiao Wang, Tian Yin, Yu Zhang, Haibing He, Xing Tang

This study aims to fabricate core-shell clarithromycin (CAM) microcapsules to cover up the bitter taste of CAM by spray drying with aqueous polymer dispersion. Water dispersion of Eudragit EPO and Surelease® were innovatively used to encapsulate CAM into microcapsules via a one-step spray-drying method. The inlet air temperature, airflow rate, CAM-polymer ratio, and particle size of CAM were optimised based on drug content and T6% (the time taken for the drug to release equal to 6% w/w). The powder properties were assessed by measuring particle size and microstructure using SEM, FT-IR, and PXRD. Furthermore, selected batch was assessed for their drug content, encapsulation efficiency, in vitro release, bitterness, and stability studies. EPO-Surelease® (1: 4) microcapsules had an average diameter (D50) of 37.69 ± 3.61 μm with a span of 2.395. The drug contents and encapsulation efficiency of EPO-Surelease®(1:4) were 10.89% and 63.7%, respectively. EPO-Surelease® (1:4) microcapsules prepared by spray drying with aqueous polymer dispersion can effectively mask the bitter taste of CAM.

本研究的目的是利用聚合物水分散体喷雾干燥的方法制备芯壳型克拉霉素微胶囊,以掩盖克拉霉素的苦味。创新地使用Eudragit EPO和Surelease®的水分散液,通过一步喷雾干燥方法将CAM封装成微胶囊。以药物含量和T6%(药物释放时间等于6% w/w)为指标,优化进风温度、气流速率、CAM-聚合物比和CAM粒径。采用扫描电镜(SEM)、红外光谱(FT-IR)和PXRD对粉末的粒径和微观结构进行了表征。此外,还对所选批次进行了药物含量、包封效率、体外释放度、苦味和稳定性研究。EPO-Surelease®(1:4)微胶囊的平均直径(D50)为37.69±3.61 μm,直径跨度为2.395。EPO-Surelease®(1:4)的药含量和包封率分别为10.89%和63.7%。EPO-Surelease®(1:4)微胶囊采用水性聚合物分散体喷雾干燥制备,可有效掩盖CAM的苦味。
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Journal of microencapsulation
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