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Formulation and Evaluation of Liposomal Drug Delivery System for Sulfasalazine 磺胺嘧啶脂质体给药系统的研制与评价
Q3 Medicine Pub Date : 2021-12-17 DOI: 10.2174/2468187312666211217100726
S. P., A. Sailaja
Aim of the current study is to prepare and characterize sulfasalazine-loaded liposomes to improve the bioavailability of the drug and to lessen the adverse effects of the drug. Diseases like inflammatory bowel disease can be treated by anti-inflammatory agents like “Sulfasalazine,” It can also be used to treat ulcerative colitis and Crohn’s disease. The biological half-life of sulfasalazine is 5-10hr; as in the case of conventional therapy, there is a chance of missing the dose. Therefore, frequent administration of drugs is essential to maintain the desired steady-state level. The side effects are thrombocytopenia, megaloblastic anemia, bone marrow depression, folic acid deficiency, impairment of male fertility (Oligospermia), intestinal nephritis due to 5-ASA, diarrhoea, headache, and skin rashes. The bioavailability of sulfasalazine is 15%. This work was undertaken to enhance bioavailability and decrease the side effects.The main objective of the study is to improve the solubility of sulfasalazine by formulating a liposomal drug delivery system. The major objective is to develop a liposomal formulation with good stability and the highest entrapment efficiency.Liposomes were produced by the thin-film hydration method. Nine formulations of liposomes were prepared by varying the concentrations of soya lecithin and cholesterol and changing the drug ratio. The obtained liposomes were characterized for surface morphology, FTIR, particle size, zeta potential, drug content, entrapment efficiency, and in-vitro diffusion studies.Among the nine formulations of liposomes, F3 was found to be the best formulation with an entrapment efficiency of 97.8% and a zeta potential value of -37.2mV. Liposomes followed first-order kinetics with a non-fickian diffusion pathway. Sulfasalazine loaded liposomes were prepared with good stability and the highest entrapment efficiency.
本研究的目的是制备并表征载柳氮磺胺脂质体,以提高药物的生物利用度,减轻药物的不良反应。像炎症性肠病这样的疾病可以用抗炎剂治疗,比如“磺胺硫氮嗪”,它也可以用来治疗溃疡性结肠炎和克罗恩病。磺胺吡啶的生物半衰期为5-10hr;与传统疗法一样,有可能错过剂量。因此,频繁给药对于维持理想的稳态水平是必要的。副作用包括血小板减少、巨幼细胞性贫血、骨髓抑制、叶酸缺乏、男性生育能力受损(少精子症)、5-ASA引起的肠道肾炎、腹泻、头痛和皮疹。磺胺吡啶的生物利用度为15%。这项工作是为了提高生物利用度和减少副作用。本研究的主要目的是通过制定一种脂质体给药系统来提高磺胺嘧啶的溶解度。主要目的是开发一种具有良好稳定性和最高包封效率的脂质体制剂。采用薄膜水化法制备脂质体。通过改变大豆卵磷脂和胆固醇的浓度和药物配比,制备了9种脂质体配方。对所得脂质体进行了表面形貌、FTIR、粒径、zeta电位、药物含量、包封效率和体外扩散研究。在9个脂质体配方中,F3为最佳配方,包封效率为97.8%,zeta电位值为-37.2mV。脂质体遵循一级动力学,具有非粘性扩散途径。该脂质体稳定性好,包封效率高。
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Q3 Medicine Pub Date : 2021-12-01 DOI: 10.2174/246818731104211228095125
S. Alshahateet
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引用次数: 0
Folate conjugated solid lipid nanoparticle: formulation development, optimization and characterization 叶酸共轭固体脂质纳米颗粒:配方开发,优化和表征
Q3 Medicine Pub Date : 2021-12-01 DOI: 10.2174/2468187311666211201111858
Vaibhav Rajoriya, Varsha Kashaw, S. Kashaw
The current paper represents the development, optimization, and characterization of paclitaxel-loaded folate conjugated solid lipid nanoparticles (FA-SLNs). The ligand (FA-SLNs) conjugated and non-conjugated SLNs (PTX-SLNs) were prepared by hot homogenization method. Both of the formulations (FA-SLNs and PTX-SLNs) were optimized with various parameters i.e. drug loading, stirring time, stirring speed, particle size, and polydispersity index, and characterized. The in-vitro drug release study was performed in different pH environments by using the dialysis bag method. The surface morphology and particle size were determined through scanning electron micorscopy and Transmission Electron Microscopy respectively, The SLNs formulations were also evaluated for the stability study. The particle size of PTX-SLNs and FA-SLNs was determined and found to be 190.1±1.9 and 231.3±2.3 nm respectively. The surface morphology of the SLNs indicates that the prepared formulations are round-shaped and show smooth surfaces. The TEM study indicated that particles were in the range of 100-300 nm. The entrapment efficiency and drug loading capacity of FA-SLNs were found to be 79.42±1.6% and 17.3±1.9%, respectively. In-vitro drug release study data, stated that the optimum drug release was found in an acidic environment at pH 4.0, that showed 94.21% drug release after 16 hours and it proves that optimized formulation FA-SLNs will gave the sustained and better release in tumor tissue that owing acidic environment because of the angiogenesis process. In this research paper, different formulation parameters, found to influence fabrication of drug into Solid lipid nanoparticles, were optimized for high entrapment efficiency and drug loading. The most important parameters were drug:lipid ratio, drug:polymer ratio and lipid: surfactant ratio. Higher in-vitro drug release was observed in pH 4 as compared to the pH 7.4. These result data concludes that FA-SLNs formulation was successfully prepared, optimized and characterized.
本文介绍了紫杉醇负载叶酸偶联固体脂质纳米颗粒(FA-SLN)的开发、优化和表征。采用热均化法制备了配体(FA SLNs)共轭和非共轭SLNs(PTX-SLNs。两种制剂(FA SLNs和PTX SLNs)都用各种参数进行了优化,即药物负载量、搅拌时间、搅拌速度、粒度和多分散指数,并进行了表征。采用透析袋法在不同pH环境下进行体外药物释放研究。通过扫描电子显微镜和透射电子显微镜分别测定了SLNs的表面形态和粒径,并对SLNs制剂的稳定性进行了评价。PTX SLNs和FA SLNs的粒径分别为190.1±1.9和231.3±2.3nm。SLNs的表面形态表明所制备的制剂是圆形的,并显示出光滑的表面。TEM研究表明,颗粒在100-300nm的范围内。FA SLNs的包封率和载药量分别为79.42±1.6%和17.3±1.9%。体外药物释放研究数据表明,最佳药物释放是在pH 4.0的酸性环境中发现的,16小时后药物释放率为94.21%,这证明了优化配方的FA SLNs将在肿瘤组织中获得持续和更好的释放,这是由于血管生成过程导致的酸性环境。在这篇研究论文中,发现不同的配方参数会影响药物制备成固体脂质纳米颗粒,并对其进行了优化,以获得较高的包封效率和载药量。最重要的参数是药物与脂质的比例、药物与聚合物的比例和脂质与表面活性剂的比例。与pH 7.4相比,在pH 4中观察到更高的体外药物释放。这些结果数据表明,FA SLNs制剂是成功制备、优化和表征的。
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引用次数: 0
Corrigendum to: Double PEGylation Significantly Improves Pharmacokinetic Properties of Irinotecan Containing Nanoparticles in a Zebrafish Model 更正:双PEG显著改善斑马鱼模型中含伊立替康纳米颗粒的药代动力学特性
Q3 Medicine Pub Date : 2021-09-21 DOI: 10.2174/246818731102210809145450
U. Saxena, M. Rajadurai, S. Basaveni, Swapna Yellanki, Raghavender Medishetti, Aarti Sevilimedu, P. Kulkarni
Due to an editorial oversight, we would like to apologize for an error that occurred in the print version of an article entitled“Double PEGylation Significantly Improves Pharmacokinetic Properties of Irinotecan Containing Nanoparticles in aZebrafish Model, 2019, 9(2), 173-181 [1]. It was published as a case report; the article type has been changed to research articlenow.The original article can be found online at https://doi.org/10.2174/2468187308666180925143701
由于编辑疏忽,我们对一篇题为“双PEG显著改善斑马鱼模型中含伊立替康纳米颗粒的药代动力学特性,2019,9(2),173-181[1]”的文章的印刷版中出现的错误表示歉意。该文章作为病例报告发表;文章类型已改为研究性文章。原始文章可在https://doi.org/10.2174/2468187308666180925143701
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
Q3 Medicine Pub Date : 2021-09-01 DOI: 10.2174/246818731103211223165610
Yo-il Jeong
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引用次数: 0
Meet Our Editorial Board Member 见见我们的编辑委员会成员
Q3 Medicine Pub Date : 2020-12-28 DOI: 10.2174/246818731004201209111708
Tae-Il Kim
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引用次数: 0
Meet Our Editorial Board Member 见见我们的编辑委员会成员
Q3 Medicine Pub Date : 2020-11-05 DOI: 10.2174/246818731003201001093737
C. Celia
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引用次数: 0
Catalytic Nanomedicine. Cu/TiO2–SiO2 Nanoparticles as Treatment of Diabetic Foot Ulcer: A Case Report 催化纳米医学。Cu/TiO2–SiO2纳米粒子治疗糖尿病足溃疡1例
Q3 Medicine Pub Date : 2020-08-31 DOI: 10.2174/2468187309666190906121924
López-Goerne Tessy, Ramírez-Olivares Paola, Armando Pérez-Dávalos Luis, A. Javier, Reyes-González Jesús, Zatta Simone Meneghetti, Murad Neif, Alves Beatriz da Costa Aguiar, Azzalis Ligia Ajaime, Junqueira Virginia Berlanga Campos, Rocha Roberto Odebrecht, Bacci, Marcelo Rodrigues, Feder David, Chagas Antonio Carlos Palandri, Adami Fernando, Fonseca Fernando Luiz Affonso, Chauhan Ritika, Chauhan Vinita, Sonkar Priyanka, Kumar Dhaked Ram, Avenoso Angela, Bruschetta Giuseppe, DAscola Angela, Scuruchi Michele, Mandraffino Giuseppe, Saitta Antonino, Campo Salvatore, M. Giuseppe, Li Tianzhong, Yang Mengsu, M. Madhumalini, Devi T. Meera, Azizi Mahsa, Rahimifard Nahid, Bahari Gholamreza, Mehdi Hashemi Seyed, Hashemi Mohammad, Li Zheng, Zhang Li-ping, Du Lei, Dong Weichao, S. Hexu, Shi Jijun, Zhang Chunyuan, Cao Yongjun, Qu Xinyuan, Liu Hui-Hui, You Shoujiang, Jin Xu, Yilin Guo
Diabetes mellitus is one of the most important health issuesworldwide. The rising incidence of the disease has resulted in a parallel increase of complicationssuch as diabetic foot ulcers (DFU). It is estimated that 25% of patients with diabeteswill develop foot ulcers over a lifetime. In Mexico, this lifetime incidence is about40% to 50%, and 20% of the cases will require amputations. DFU can result in staggeringfinancial burdens for the healthcare system and the patient. Therapies that promote rapidand complete healing and reduce the need for expensive surgical procedures would impactthese costs substantially.Cu/TiO2–SiO2 nanoparticles were synthesized by T. López et al. sol-gel patentedmethod. After synthesis, they were characterized using transmission electron microscopy(TEM) and X-ray diffraction. Then, they were embedded in a polymeric gel matrix.The Cu/TiO2–SiO2 nanogel was used as conservative therapy for a chronic non-healingDFU on a 62-year old female with several comorbidities and chronic complications of diabetes.Wound debridement was performed prior to nanogel administration. The nanogelwas applied over the ulcer on alternate days for an initial period of 2 weeks and then continuedfor 10 months.Significant improvement was observed in the wound healing process since thefirst applications. The infection was limited and tissue regeneration was enhanced untilcomplete healing of the ulcer.Cu/TiO2–SiO2 nanogel therapy enhanced reepithelialization and healing ofthe DFU. The successful outcome allowed to avoid the amputation that was proposed forthe patient.
糖尿病是世界上最重要的健康问题之一。该疾病发病率的上升导致糖尿病足溃疡(DFU)等并发症的同时增加。据估计,25%的糖尿病患者一生都会出现足部溃疡。在墨西哥,这种终生发病率约为40%至50%,20%的病例需要截肢。DFU可能会给医疗系统和患者带来巨大的财务负担。促进快速完全愈合并减少昂贵手术需求的疗法将对这些成本产生重大影响。通过T.López等人的溶胶凝胶专利方法合成了Cu/TiO2–SiO2纳米颗粒。合成后,使用透射电子显微镜(TEM)和X射线衍射对它们进行了表征。然后,将它们嵌入聚合物凝胶基质中。Cu/TiO2–SiO2纳米凝胶被用作一名患有多种糖尿病合并症和慢性并发症的62岁女性的慢性非治疗性DFU的保守疗法。在给予纳米凝胶之前进行伤口清创术。每隔几天将纳米凝胶涂抹在溃疡上,最初持续2周,然后持续10个月。自首次应用以来,观察到伤口愈合过程有显著改善。感染受到限制,组织再生得到增强,直至溃疡完全愈合。Cu/TiO2–SiO2纳米凝胶治疗增强了DFU的再上皮化和愈合。成功的结果避免了为患者提出的截肢手术。
{"title":"Catalytic Nanomedicine. Cu/TiO2–SiO2 Nanoparticles as Treatment of Diabetic Foot Ulcer: A Case Report","authors":"López-Goerne Tessy, Ramírez-Olivares Paola, Armando Pérez-Dávalos Luis, A. Javier, Reyes-González Jesús, Zatta Simone Meneghetti, Murad Neif, Alves Beatriz da Costa Aguiar, Azzalis Ligia Ajaime, Junqueira Virginia Berlanga Campos, Rocha Roberto Odebrecht, Bacci, Marcelo Rodrigues, Feder David, Chagas Antonio Carlos Palandri, Adami Fernando, Fonseca Fernando Luiz Affonso, Chauhan Ritika, Chauhan Vinita, Sonkar Priyanka, Kumar Dhaked Ram, Avenoso Angela, Bruschetta Giuseppe, DAscola Angela, Scuruchi Michele, Mandraffino Giuseppe, Saitta Antonino, Campo Salvatore, M. Giuseppe, Li Tianzhong, Yang Mengsu, M. Madhumalini, Devi T. Meera, Azizi Mahsa, Rahimifard Nahid, Bahari Gholamreza, Mehdi Hashemi Seyed, Hashemi Mohammad, Li Zheng, Zhang Li-ping, Du Lei, Dong Weichao, S. Hexu, Shi Jijun, Zhang Chunyuan, Cao Yongjun, Qu Xinyuan, Liu Hui-Hui, You Shoujiang, Jin Xu, Yilin Guo","doi":"10.2174/2468187309666190906121924","DOIUrl":"https://doi.org/10.2174/2468187309666190906121924","url":null,"abstract":"\u0000\u0000Diabetes mellitus is one of the most important health issues\u0000worldwide. The rising incidence of the disease has resulted in a parallel increase of complications\u0000such as diabetic foot ulcers (DFU). It is estimated that 25% of patients with diabetes\u0000will develop foot ulcers over a lifetime. In Mexico, this lifetime incidence is about\u000040% to 50%, and 20% of the cases will require amputations. DFU can result in staggering\u0000financial burdens for the healthcare system and the patient. Therapies that promote rapid\u0000and complete healing and reduce the need for expensive surgical procedures would impact\u0000these costs substantially.\u0000\u0000\u0000\u0000Cu/TiO2–SiO2 nanoparticles were synthesized by T. López et al. sol-gel patented\u0000method. After synthesis, they were characterized using transmission electron microscopy\u0000(TEM) and X-ray diffraction. Then, they were embedded in a polymeric gel matrix.\u0000The Cu/TiO2–SiO2 nanogel was used as conservative therapy for a chronic non-healing\u0000DFU on a 62-year old female with several comorbidities and chronic complications of diabetes.\u0000Wound debridement was performed prior to nanogel administration. The nanogel\u0000was applied over the ulcer on alternate days for an initial period of 2 weeks and then continued\u0000for 10 months.\u0000\u0000\u0000\u0000Significant improvement was observed in the wound healing process since the\u0000first applications. The infection was limited and tissue regeneration was enhanced until\u0000complete healing of the ulcer.\u0000\u0000\u0000\u0000Cu/TiO2–SiO2 nanogel therapy enhanced reepithelialization and healing of\u0000the DFU. The successful outcome allowed to avoid the amputation that was proposed for\u0000the patient.\u0000","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/2468187309666190906121924","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43647373","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 5
Development of Pramipexole Hydrochloride Nanocrystals and their Characterization based on In vitro Dissolution Studies 盐酸普拉克索纳米晶的制备及其体外溶出度表征
Q3 Medicine Pub Date : 2020-08-31 DOI: 10.2174/2468187310999201023151231
Harshita Gupta, Rutu Panchal, P. Mehta, R. Momin
There are numerous unavoidable hurdles encountered by scientists toachieve an ideal drug delivery. Among them, the high-water solubility of a therapeutic molecule hasbeen observed as a chief pausing factor that diminishes the biological stay and shortens the half-lifeof a drug. The ramification of this occurs that patients have to take medications multiple times in asingle day to maintain the drug-plasma concentration. These consequences lead to poor pharmacologicalresponses and ultimately do not add any significant outcomes in the betterment of patient’shealth. A similar phenomenon has been observed with the delivery of some potent Anti-Parkinson’smedications, for instance, Pramipexole. The current research is aimed at developing the biologicalresidue of Pramipexole Hydrochloride (PRP) based on the counter ion technology that has provided asojourn release of PRP by retarding the aqueous solubility, which is further characterized using thedissolution study. Initially, the molar ratio of PRP and the selected counter ion, i.e., DisodiumPamoate (NaPAM), was quantified to produce the stable salt. Thereafter, the salt formation was precededby the precipitation method and this primarily obtained salt is called microcrystals. In the nextstage, the microcrystals were characterized by numerous analytical tools such as Differential ScanningCalorimetry (DSC), melting point, and Mass Spectrometry (MS). On the other hand, UltravioletSpectroscopy (UV) was used for the simultaneous determination of PRP and NaPAM in theformed salt. After this, the development of nanocrystals from microcrystals was carried out usinghigh-shear homogenization (HSH) with the aid of α-Tocopherol Polyethylene Glycol 1000 Succinate(TPGS), employed as a stabilizer. The preceding step was performed by analyzing the particle size.Following this, an in vitro dissolution study was planned using a dialysis bag system (at 6.8 pH buffer)along with vehicle development and characterization being taken into consideration.An equimolar ratio (1:1) of PRP and counter ion stipulated the complete reaction occurredamong them and then considering this ratio (based on the percent loading efficiency (%LE) andcomplexation efficiency) (%CE), salt preparation was done. Upon analysis of the developed salt (microcrystal),satisfactory outcomes have assured the complete and compatible salt formation. Besidesit, simultaneous estimation certified that the presence of PRP and NaPAM in the formulation does notaffect each other, qualitatively and quantitatively. Apart from that, the particle size of these nanocrystalswas also found in the acceptable range. Furthermore, Pramipexole Pamoate Nanocrystals Salt(PPNS) was formulated, and in vitro dissolution study showed that PPNS was significantly able toextend the release (93.87 % release, i.e., sustainable) up to 48 hours as compared to the standard PRP.Additionally, the developed vehicle was found suitable and stable, both at room
要实现理想的药物递送,科学家们遇到了许多不可避免的障碍。其中,治疗分子的高水溶性已被观察为减少生物停留时间和缩短药物半衰期的主要暂停因素。其后果是患者必须在一天内多次服药以维持药物的血浆浓度。这些后果导致不良的药物反应,最终不会增加任何改善患者健康的显著结果。在一些强效抗帕金森病药物的治疗中也观察到了类似的现象,例如普拉克索。本研究旨在开发基于反离子技术的盐酸普拉克索(PRP)的生物制剂,该技术通过延缓水溶性来提供PRP的快速释放,并通过溶解研究对其进行进一步表征。最初,定量PRP和所选反离子,即帕酸二钠(NaPAM)的摩尔比,以产生稳定的盐。此后,通过沉淀法进行盐的形成,这种主要获得的盐被称为微晶。在下一阶段,通过差示扫描量热法(DSC)、熔点和质谱法(MS)等多种分析工具对微晶进行了表征。另一方面,采用紫外光谱法同时测定了成型盐中PRP和NaPAM的含量。之后,在α-生育酚聚乙二醇1000琥珀酸酯(TPGS)作为稳定剂的帮助下,使用高剪切均化(HSH)从微晶中开发纳米晶体。前面的步骤是通过分析颗粒尺寸来进行的。随后,计划使用透析袋系统(在6.8 pH缓冲液下)进行体外溶出研究,同时考虑载体的开发和表征。PRP和反离子的等摩尔比(1:1)规定了它们之间发生的完全反应,然后考虑到这个比率(基于百分比负载效率(%LE)和络合效率)(%CE),进行了盐制备。通过对所形成的盐(微晶)的分析,令人满意的结果确保了盐的完全和相容的形成。除此之外,同时估计证明配方中PRP和NaPAM的存在在定性和定量上不会相互影响。除此之外,这些纳米晶体的粒度也在可接受的范围内。此外,配制了普拉克索帕姆酸盐纳米晶体(PPNS),体外溶出度研究表明,与标准PRP相比,PPNS能够显著延长释放时间(93.87%的释放,即可持续)长达48小时。此外,所开发的载体在室温和应力条件下都是合适和稳定的。总之,这里收集的数据表达了有希望的结果,并表明PPNS可能是一个很好的选择(如果临床证明是安全有效的),在最近的将来通过最大限度地减少帕金森病患者对PRP的日常需求来提高患者的依从性。据我们所知,我们是第一个报道使用纳米概念治疗帕金森氏症的仓库配方的人。然而,必须设计体内动物模型研究以及药物动力学数据,以确定PPNS的安全性和有效性。
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引用次数: 1
Fundamentals of Nanocarriers and Probiotics in the Treatment of Cervical Cancer 纳米载体和益生菌治疗宫颈癌的基础
Q3 Medicine Pub Date : 2020-08-31 DOI: 10.2174/2468187310999201105143429
Amandeep Singh, Deepak Negi, Simranjeet Kaur, S. Bhattachary, Gurmeet Singh
Cancer is a pivotal disease, which is a serious concern towards scientific research.In the recent era of scientific discovery and innovation, probiotics have been proposedas a new preventive and therapeutic option in therapy and to control cancer growth.Probiotics may thus offer a new way in research to investigate active compounds in differentprobiotic strains having anticancer features. Studies in laboratory animals and cell lineswith respect to cancer treatments are encouraging. With rare conventional treatments, theneed for new alternatives as the transportation of chemotherapeutic agents by nanocarriersusing nanotechnology is one such approach. This review considers various drug deliverysystems used in the therapy of cervical cancer, such as dendrimers, liposomes and nanoparticles.These drug delivery systems assist in the improvement of pharmacological activity,solubility, bioavailability and, thus, facilitating new innovative therapeutic technologies.This review summarizes the application of nanotechnology and probiotics in the treatmentof cervical cancer.
癌症是一种关键性疾病,是科学研究的一个热点。在最近的科学发现和创新时代,益生菌被认为是治疗和控制癌症生长的一种新的预防和治疗选择。因此,益生菌可能为研究具有抗癌特征的不同益生菌菌株中的活性化合物提供一种新的方法。在癌症治疗方面对实验动物和细胞系的研究是令人鼓舞的。在罕见的传统治疗中,寻找新的替代品,如使用纳米技术通过纳米载体运输化疗药物就是这样一种方法。这篇综述考虑了用于治疗癌症的各种药物递送系统,如树枝状聚合物、脂质体和纳米颗粒。这些药物递送系统有助于提高药理活性、溶解度和生物利用度,从而促进新的创新治疗技术。本文综述了纳米技术和益生菌在癌症治疗中的应用。
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引用次数: 1
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Current Nanomedicine
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