Background:: The tumour microenvironment (TME) affects tumour development in a crucial way. Infinite stromal cells and extracellular matrices located in the tumour form complex tissues. The mature TME of epithelial-derived tumours exhibits common features irrespective of the tumour's anatomical locale. TME cells are subjected to hypoxia, oxidative stress, and acidosis, eliciting an extrinsic extracellular matrix (ECM) adjustment initiating responses by neighbouring stromal and immune cells (triggering angiogenesis and metastasis). Objective:: This report delivers challenges associated with targeting the TME for therapeutic pur-poses, technological advancement attempts to enhance understanding of the TME, and debate on strategies for intervening in the pro-tumour microenvironment to boost curative benefits. Conclusion:: Therapeutic targeting of TME has begun as an encouraging approach for cancer treatment owing to its imperative role in regulating tumour progression and modulating treatment response.
{"title":"Cancer-Specific Nanomedicine Delivery Systems and the Role of the Tumor Microenvironment: A Critical Linkage","authors":"Debarupa Dutta Chakraborty, Prithviraj Chakraborty","doi":"10.2174/0124681873270736231024060618","DOIUrl":"https://doi.org/10.2174/0124681873270736231024060618","url":null,"abstract":"Background:: The tumour microenvironment (TME) affects tumour development in a crucial way. Infinite stromal cells and extracellular matrices located in the tumour form complex tissues. The mature TME of epithelial-derived tumours exhibits common features irrespective of the tumour's anatomical locale. TME cells are subjected to hypoxia, oxidative stress, and acidosis, eliciting an extrinsic extracellular matrix (ECM) adjustment initiating responses by neighbouring stromal and immune cells (triggering angiogenesis and metastasis). Objective:: This report delivers challenges associated with targeting the TME for therapeutic pur-poses, technological advancement attempts to enhance understanding of the TME, and debate on strategies for intervening in the pro-tumour microenvironment to boost curative benefits. Conclusion:: Therapeutic targeting of TME has begun as an encouraging approach for cancer treatment owing to its imperative role in regulating tumour progression and modulating treatment response.","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135516252","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}
Pub Date : 2023-10-24DOI: 10.2174/0124681873259506231015050850
Sanjana Datta, Asmita Gajbhiye, Shailendra Patil
Background:: Alzheimer's disease (AD) is a progressive neurodegenerative condition characterized by the gradual decline of cognitive abilities, primarily caused by impairments in the cholinergic system. AD is diagnosed based on the presence of specific pathological features, in-cluding senile plaques, neurofibrillary tangles, and the loss of neurons and synapses. Despite on-going efforts, the etiology of AD remains unclear, and there is a significant lack of effective treatments to meet the medical needs of affected individuals. The complex nature of AD, involv-ing multiple factors, presents challenges in the development of potential therapies. Numerous ob-stacles hinder the achievement of optimal pharmacological concentration of promising molecules for AD treatment. These obstacles include the presence of the blood-brain barrier (BBB), which restricts the entry of therapeutic agents into the brain, as well as issues related to poor bioavaila-bility and unfavorable pharmacokinetic profiles. Unfortunately, many therapeutically promising compounds have failed to overcome these hurdles and demonstrate efficacy in treating AD. background: Alzheimer’s disease (AD) is a progressive neurodegenerative disease that is manifested by depleted cognitive abilities resulted due to cholinergic impairments. AD is further diagnosed with pathological hallmarks including senile plaques, neurofibrillary tangles and neuronal and synaptic death. With constant efforts, few therapeutic targets and interventions have been identified but AD is still a disease with unclear etiopathology and unmet medical needs. The multifactorial nature of AD poses difficulties to develop a potential treatment. Unfortunately, large numbers of therapeutically efficient molecules for the treatment of AD failed to attain optimal pharmacological concentration due to numerous hurdles such as the presence of blood-brain barrier (BBB), poor bioavailability, or pharmacokinetic profile. Methods:: The PEGylated chitosan nanoconjugate was developed and evaluated for delivery of anti-Alzheimer natural extract of Salvia officinalis and Melissa officinalis to the brain. The nano-conjugates (S-PCN and M-PCN) were developed by ionic gelation technique. Result:: The nanoconjugates (S-PCN and M-PCN) were evaluated for various optical and in-vitro parameters. MTT assay on UCSD229i-SAD1-1 human astrocytoma cells indicated IC50 values of 0.42, 0.49, 0.67, and 0.75 μM for S-PCN, M-PCN formulations, and free Salvia officinalis and Melissa officinalis extracts, respectively. The In vitro assessments using cell lines have confirmed the improved uptake and distribution of nanoconjugates compared to free extracts. These findings were validated through confocal microscopy and apoptosis assays, revealing a substantial in-crease in the accumulation of nanoconjugates within the brain. The targeting potential OF M- PCN over S-PCN was found to be 2-fold significant. method: 1. Sample Preparation - Crude drug Salvia offici
背景:阿尔茨海默病(AD)是一种以认知能力逐渐下降为特征的进行性神经退行性疾病，主要由胆碱能系统损伤引起。AD的诊断是基于特定病理特征的存在，包括老年斑、神经原纤维缠结、神经元和突触的丧失。尽管正在进行努力，但阿尔茨海默病的病因仍不清楚，而且明显缺乏有效的治疗方法来满足受影响个体的医疗需求。阿尔茨海默病的复杂性涉及多种因素，对潜在治疗方法的开发提出了挑战。许多障碍阻碍了有希望的AD治疗分子的最佳药理学浓度的实现。这些障碍包括血脑屏障(BBB)的存在，这限制了治疗剂进入大脑，以及与生物利用度差和不利的药代动力学特征相关的问题。不幸的是，许多具有治疗前景的化合物未能克服这些障碍并证明治疗AD的有效性。背景:阿尔茨海默病(AD)是一种进行性神经退行性疾病，表现为胆碱能损伤导致认知能力下降。阿尔茨海默病进一步诊断为病理特征，包括老年斑，神经原纤维缠结和神经元和突触死亡。经过不断的努力，目前已经确定的治疗靶点和干预措施很少，但阿尔茨海默病仍然是一种病因不明、医疗需求未得到满足的疾病。阿尔茨海默病的多因素性质给开发潜在的治疗方法带来了困难。不幸的是，由于血脑屏障(BBB)的存在、生物利用度差或药代动力学特征等诸多障碍，大量治疗AD的有效分子未能达到最佳药理学浓度。方法:制备聚乙二醇化壳聚糖纳米缀合物，并对其抗阿尔茨海默病的脑内给药效果进行评价。采用离子凝胶技术制备了S-PCN和M-PCN纳米缀合物。结果:对纳米偶联物(S-PCN和M-PCN)进行了各种光学参数和体外参数的评价。MTT检测UCSD229i-SAD1-1人星形细胞瘤细胞的IC50值分别为0.42、0.49、0.67和0.75 μM，其中S-PCN、M-PCN组方和游离鼠尾草提取物和菝葜提取物的IC50值分别为0.42、0.49、0.67和0.75 μM。利用细胞系进行的体外评估证实，与游离提取物相比，纳米缀合物的吸收和分布得到了改善。这些发现通过共聚焦显微镜和细胞凋亡实验得到了证实，揭示了脑内纳米偶联物积累的实质性增加。M- PCN的靶向潜力是S-PCN的2倍。方法:1。样品制备-原料药丹参和药用草，植物采自瓦朗加尔和蒂鲁帕蒂植物园并鉴定。这两种植物，各1克，粉碎(使用实验室磨)1分钟，得到相应的粉末。提取粉末按先前报道的方法进行，将100 mL沸水加入1 g植物粉末中，5 min后，用0.45 mm过滤器过滤。优化了该工艺以获得这些植物的最高潜在活性。植物粗沉淀后，将样品过滤并保持在80ºC，进行冷冻干燥程序(Heto Holten A/S Drywinner, Allerød，丹麦)。然后，1% (w/v)的冻干粉溶液溶解在甲醇中进行分析评价和其他活性试验。注射前，样品再次通过0.45 mm过滤器过滤。2. 聚乙二醇化壳聚糖纳米颗粒的制备-采用离子化凝胶法制备壳聚糖，分别包封整个鼠尾草和药用草提取物。将100 mg鼠尾草、药用草提取物和0.4% w/v的壳聚糖，精确称重，溶于1% v/v的冰乙酸水溶液中。在药物聚合物溶液中滴加0.4%三聚磷酸钠溶液(TPP)，速度为2ml/min (12 ml TPP加入20ml药物聚合物溶液)。得到的粒子分散用探测声呐(S-4000;Misonix, Farmingdale, NY)在中等振幅(50%)下加热5分钟，以获得纳米大小的颗粒。然后通过0.2 um亲水过滤器(Minsart, Sartorius)过滤分散体，以分离较小的纳米颗粒，以便在目标位点实现最大的运输。在最佳温度下，用Amicon 8200(微孔PBMK膜，MWCO 300000)对双重蒸馏水进行超滤纯化，得到纳米级颗粒。 超滤有利于消除未反应溶剂和未结合药物的残留。在聚乙二醇化过程中，将准确的50 mL 0.3%壳聚糖纳米颗粒以3:1的比例加入聚乙二醇(PEG)溶液中，并在500 rpm下搅拌1 h。进一步，将分散液应用于混合物中60秒，以获得均匀的PEG-壳聚糖纳米颗粒。结果将小阴离子TPP冲激结合到一致的壳聚糖聚合物溶液中，形成了包裹丹参和菝葜天然提取物的聚乙二醇化壳聚糖纳米颗粒。纳米粒子的形成是由负电荷离子TPP与壳聚糖的正电荷氨基之间的离子相互作用引起的。优化了CS/TPP的配比，以获得稳定的分散和纳米级颗粒的形成。为了确定CS和TPP形成NP的最佳浓度，进行了初步实验。对制备工艺参数和配方参数进行了优化，以获得物理化学和热稳定的纳米颗粒。所获得的纳米级颗粒被广泛地表征为透明溶液、显示tyndall效应(NPs)的乳白色悬浮液或聚集体。Zeta尺寸仪测量的结果显示，制备的S-PCN和M-PCN配方的尺寸在150-250 nm之间差别很大(图1- a &b).通过配方和工艺优化，S-PCN、M-PCN纳米级配方的提取物在聚合物基体中表现出良好的包封性。S-PCN和M-PCN的表面电荷分别为-10.89 mV和-16.21 mV(图1- e &F)证明了两种配方的负电荷性质。该配方的负电荷具有较好的稳定性和增强脑靶向的最佳候选性。S-PCN、M-PCN制剂的pH值为6.9±0.01，在接近中性的微环境中起着至关重要的作用。pH促靶机制是聚合物基体现场降解的关键因素。这种聚合物降解激活机制以可控的速率增强了药物释放，从而产生所需的治疗潜力。2 DLS分析制备的S-PCN和M-PCN纳米制剂的DLS结果再次在纳米尺度范围内分散。两种纳米配方的尺寸分布模式有些相同，S-PCN的尺寸范围为160-240 nm, M-PCN的尺寸范围为150-230 nm。两种纳米制剂的最佳纳米尺寸范围均表现出增强的脑传递和现场靶向性，有效地符合细胞及其微环境的大小。DLS调查显示出不同的大小分布和分散模式。S-PCN和M-PCN显示的PDI分别为0.271±0.08和0.259±0.11。DLS结果表明，制备的纳米颗粒在100-500 nm之间均匀分布，稳定性增强(图1-c &d).这种纳米尺寸的稳定模式有助于增强制备的纳米颗粒在血脑屏障上的扩散，从而在脑靶向过程中产生最佳的药理潜力。因此，可以坚定地指出，这两种纳米制剂在临床平台上对手术脑靶向治疗阿尔茨海默病表现出最佳和稳定的纳米分散特性。透射电子显微镜(TEM)透射电子显微镜分析显示，两种纳米配方的颗粒尺寸非常分散，呈椭圆形。TEM分析显示S-PCN和M-PCN的尺寸范围为100-250 nm，验证了DLS测量zeta尺寸分析(图2- a &b).包埋天然萃取物形成的纳米颗粒在聚合物和交联剂之间表现出更好的交联，避免了不必要的泄漏。此外，纳米颗粒的聚集可以忽略不计，表明壳聚糖边界的聚乙二醇化过程更好。透射电镜结果显示，纳米载体系统适合有效的脑递送，显示出良好的血脑屏障浸润外观。扫描电子显微镜(SEM)扫描电子显微镜(SEM)分析结果与zeta浆料机和TEM分析结果明显一致，显示细颗粒形成呈球形，形貌光滑。值得注意的是，扫描电镜图像验证了两种纳米配方的尖锐椭圆形边界，显示出更好的聚乙二醇化过程。扫描电镜图像也澄清没有团簇形成的迹象，颗粒团聚显示明显的聚乙二醇外层。SEM分析显示尺寸范围为150-250 nm，再次定性验证了TEM和zeta尺寸分析，并确认了S-PCN
Pub Date : 2023-10-18DOI: 10.2174/0124681873264353231013054240
Surbhi Joshi, Ibrahim Mithawala, Yash Savaliya, Rohit Patil
Background: Synthesis of copper nanoparticles needs to be carried out with the use of environmentally safer alternatives. Plant-mediated nano-fabrication is a new area of nanotechnology that is favoured over traditional methods due to its effectiveness with respect to safety, affordability, environmental friendliness, and biocompatibility. Synthesis of copper nanoparticles using natural sources is the demand of this era. Methods: In the present study, the synthesis of copper nanoparticles (CuNPs) was carried out using three different plant extracts, i.e., Mentha piperita, Anethum graveolens L., and Calotropis procera. This synthesis was carried out in different conditions and the visual colour change in the solution confirmed the presence of copper nanoparticles. The nanoparticles were also characterized with UV-vis absorption spectroscopy and scanning electron microscope (SEM). Conclusion: In comparison to the synthetic route, the current work represents a cost-effective and sustainable way for the synthesis of nanoparticles.
{"title":"Synthesis and Characterization of Copper Nanoparticles Using Plant Extract of Mentha piperita Leaves, Anethum graveolens L., and Calotropis procera","authors":"Surbhi Joshi, Ibrahim Mithawala, Yash Savaliya, Rohit Patil","doi":"10.2174/0124681873264353231013054240","DOIUrl":"https://doi.org/10.2174/0124681873264353231013054240","url":null,"abstract":"Background: Synthesis of copper nanoparticles needs to be carried out with the use of environmentally safer alternatives. Plant-mediated nano-fabrication is a new area of nanotechnology that is favoured over traditional methods due to its effectiveness with respect to safety, affordability, environmental friendliness, and biocompatibility. Synthesis of copper nanoparticles using natural sources is the demand of this era. Methods: In the present study, the synthesis of copper nanoparticles (CuNPs) was carried out using three different plant extracts, i.e., Mentha piperita, Anethum graveolens L., and Calotropis procera. This synthesis was carried out in different conditions and the visual colour change in the solution confirmed the presence of copper nanoparticles. The nanoparticles were also characterized with UV-vis absorption spectroscopy and scanning electron microscope (SEM). Conclusion: In comparison to the synthetic route, the current work represents a cost-effective and sustainable way for the synthesis of nanoparticles.","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135942888","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}
Pub Date : 2023-10-10DOI: 10.2174/0124681873255919231002044416
Sarvesh S. Pawar, Punam S. Gadekar, Bhushan R. Rane, Ashish S. Jain
Background: Sertaconazole nitrate is a topical antifungal drug used to treat interdigital tinea pedis in patients with immunocompetent conditions. The class of imidazole includes the antifungal medication sertaconazole nitrate. It is available in topical formulations for treating skin infections, including athlete's foot. Solid lipid nanoparticles (SLN) are at the cutting edge of nanotechnology, with several potential uses in drug delivery and research. Because of their unique size-dependent features, lipid nanoparticles hold the promise of novel therapies. Objective: Drug incorporation into nanocarriers creates a new drug delivery prototype that could be employed for drug targeting. The research aims to study the formulation and evaluation of Sertaconazole nitrate solid lipid nanoparticles. The goal behind formulating SLN gel is to provide and maintain therapeutic concentrations of the drug at the target biological site to maximise therapeutic efficacy and minimise side effects. Methods: Sertaconazole Nitrate Solid Lipid Nanoparticles are prepared by using High Pressure Homogenizer to get nanogel formulation as the final formulation and In-vitro drug release using a diffusion apparatus. The prepared SLNs were evaluated in their FTIR studies to determine compatibility between the drug and the excipients; zeta potential indicates the solid lipid nanoparticle was stable, and polydispersity index was used to determine particle size. Result: The results demonstrate that optimised SLN-based Sertaconazole nitrate gel exhibited the best physicochemical properties, including FTIR studies of the drug, excipients, and optimised formulation demonstrate that all are compatible with each other, particle size is less than 200 nm, zeta potential ranging from 12 to -20 mV, and highest entrapment efficiency is 71.48%. Optimised solid lipid nanoparticles showed good in vitro release and antimicrobial results. The main application of SLN large scale-up is possible, and the drug can be effective with less dose incorporation. Conclusion: In this research work, the proposed plan of work SLN of Sertaconazole Nitrate was formulated successfully. The preliminary identification tests were performed, such as melting point determination, estimation of λmax by UV-visible spectrophotometry and plot of its calibration curve in solvent and buffer system, and FT-IR investigation to confirm the purity and confirmation of medication. High physical stability and drug loading are advantageous to SLN.
{"title":"Formulation of Lipid Nanoparticles based Nanogel of Sertaconazole Nitrate and its Evaluation","authors":"Sarvesh S. Pawar, Punam S. Gadekar, Bhushan R. Rane, Ashish S. Jain","doi":"10.2174/0124681873255919231002044416","DOIUrl":"https://doi.org/10.2174/0124681873255919231002044416","url":null,"abstract":"Background: Sertaconazole nitrate is a topical antifungal drug used to treat interdigital tinea pedis in patients with immunocompetent conditions. The class of imidazole includes the antifungal medication sertaconazole nitrate. It is available in topical formulations for treating skin infections, including athlete's foot. Solid lipid nanoparticles (SLN) are at the cutting edge of nanotechnology, with several potential uses in drug delivery and research. Because of their unique size-dependent features, lipid nanoparticles hold the promise of novel therapies. Objective: Drug incorporation into nanocarriers creates a new drug delivery prototype that could be employed for drug targeting. The research aims to study the formulation and evaluation of Sertaconazole nitrate solid lipid nanoparticles. The goal behind formulating SLN gel is to provide and maintain therapeutic concentrations of the drug at the target biological site to maximise therapeutic efficacy and minimise side effects. Methods: Sertaconazole Nitrate Solid Lipid Nanoparticles are prepared by using High Pressure Homogenizer to get nanogel formulation as the final formulation and In-vitro drug release using a diffusion apparatus. The prepared SLNs were evaluated in their FTIR studies to determine compatibility between the drug and the excipients; zeta potential indicates the solid lipid nanoparticle was stable, and polydispersity index was used to determine particle size. Result: The results demonstrate that optimised SLN-based Sertaconazole nitrate gel exhibited the best physicochemical properties, including FTIR studies of the drug, excipients, and optimised formulation demonstrate that all are compatible with each other, particle size is less than 200 nm, zeta potential ranging from 12 to -20 mV, and highest entrapment efficiency is 71.48%. Optimised solid lipid nanoparticles showed good in vitro release and antimicrobial results. The main application of SLN large scale-up is possible, and the drug can be effective with less dose incorporation. Conclusion: In this research work, the proposed plan of work SLN of Sertaconazole Nitrate was formulated successfully. The preliminary identification tests were performed, such as melting point determination, estimation of λmax by UV-visible spectrophotometry and plot of its calibration curve in solvent and buffer system, and FT-IR investigation to confirm the purity and confirmation of medication. High physical stability and drug loading are advantageous to SLN.","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":"89 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136358871","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}
Pub Date : 2023-10-04DOI: 10.2174/0124681873274871230927105142
Bhawana Singh, Manish Kumar, Prabhat Kumar Upadhyay, AMIT KUMAR SINGH
Abstract:: Dermatological disease states have psychological impacts that affect a patient’s life. In the management of such disorders, topical delivery has an important role. However, the conven-tional topical delivery systems suffer from various limitations, like skin irritation, a minute quan-tity of drugs reaching disease sites, and over and under medication, which leads to an adverse re-action and therapeutic failure, respectively. Therefore, researchers continuously search for an al-ternate delivery system for treating skin disease. In recent years, nanostructured lipid carriers (NLC) have emanated as promising carrier systems for topical delivery. The current review pro-vides an in-depth insight into topical administration for treating a variety of dermatological issues using NLCs as a carrier. This review highlights the suitability of NLCs as carriers for topical de-livery, their method of preparation, and their characterization. In the present review, the main emphasis has been given to the management of various dermatological problems by using NLCs as a carrier; a plethora of literature investigating NLC as the carrier for topical delivery has been included in this review. In this paper, an attempt has been made to provide a summary of the re-search carried out in this field that will encourage further research in this arena.
{"title":"Nanostructured Lipid Carrier for Dermatological Application: A Comprehensive Review and Future Perspective","authors":"Bhawana Singh, Manish Kumar, Prabhat Kumar Upadhyay, AMIT KUMAR SINGH","doi":"10.2174/0124681873274871230927105142","DOIUrl":"https://doi.org/10.2174/0124681873274871230927105142","url":null,"abstract":"Abstract:: Dermatological disease states have psychological impacts that affect a patient’s life. In the management of such disorders, topical delivery has an important role. However, the conven-tional topical delivery systems suffer from various limitations, like skin irritation, a minute quan-tity of drugs reaching disease sites, and over and under medication, which leads to an adverse re-action and therapeutic failure, respectively. Therefore, researchers continuously search for an al-ternate delivery system for treating skin disease. In recent years, nanostructured lipid carriers (NLC) have emanated as promising carrier systems for topical delivery. The current review pro-vides an in-depth insight into topical administration for treating a variety of dermatological issues using NLCs as a carrier. This review highlights the suitability of NLCs as carriers for topical de-livery, their method of preparation, and their characterization. In the present review, the main emphasis has been given to the management of various dermatological problems by using NLCs as a carrier; a plethora of literature investigating NLC as the carrier for topical delivery has been included in this review. In this paper, an attempt has been made to provide a summary of the re-search carried out in this field that will encourage further research in this arena.","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":"50 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135647544","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}
Pub Date : 2023-09-14DOI: 10.2174/2468187313666230914121457
Raghav Sharma, Bijal Prajapati
Introduction: Tobacco use is the leading preventable cause of various diseases, disabilities, and death. It is estimated that 480000 deaths annually are attributed to cigarette smoking, including secondhand smoke exposure. The treatment of brain disorders is particularly challenging due to the presence of a variety of formidable obstacles to delivering drugs selectively and effectively to the brain. The blood-brain barrier (BBB) and first-pass metabolism constitute the major obstacle to the uptake of drugs into the brain following systemic administration. Intranasal delivery offers a non-invasive and convenient method to bypass the BBB and avoid first-pass metabolism, which leads to the delivery of therapeutics directly to the brain. Objective: The objective of this study was to develop an In-situ gel of Bupropion Hydrochloride-loaded chitosan nanoparticles using the inotropic gelation method for Smoking Cessation via the nose to the brain to improve the bioavailability of Bupropion Hydrochloride, avoiding first-pass metabolism and bypassing Blood Brain Barrier. Method: Fourier transform infrared spectroscopy (FTIR) was used to determine the identity and purity of the drug. A UV Spectrophotometer was employed in the analytical procedure. Chitosan nanoparticles loaded with bupropion HCl were made using the ionic gelation method, and then the optimized batch was made using simulated in-situ gelation. Utilizing Central composite design, optimization was done by Design Expert-13. Evaluation of polymeric nanoparticles was performed by measuring their particle size, PDI, and entrapment efficiency. Additionally, they were tested for drug release in vitro. The final nanoparticles were subsequently tested for gelation using nasal simulation fluid, and an ex vivo investigation was also conducted. An ion-sensitive polymer gellan gum was used as a gelling agent, which formed an immediate gel and remained for an extended period. The finished formulation was also subjected to several characterizations, including TEM and FTIR. Results: The developed formulation was stable and showed enhanced contact time in the nasal mucosa, minimizing the frequency of administration. In-vitro studies through Franz diffusion cell and Ex-vivo studies on sheep nasal mucosa showed good results. In the Histopathological study, the optimized batch was found to be safe and stable in an accelerated stability study for one month. Conclusion: Bupropion HCl-loaded chitosan nanoparticles In-situ gel proved to be suitable for the administration of Bupropion HCl through the nasal route. The ease of administration coupled with less frequent administration enhanced patient compliance. The formulation was found to be liquid at the formulated condition and formed gel in the presence of ions present in the nasal mucosa. The gel formed in situ showed sustained drug release. The formulations were less viscous before instillation and formed a strong gel after instilling in the nasal cavity.
{"title":"Development of In-situ Gel of Bupropion Hydrochloride-loaded Chitosan Nanoparticles using an Inotropic Gelation Method for Smoking Cessation via Nose to Brain: In-vitro and Ex-vivo Characterization and Evaluation","authors":"Raghav Sharma, Bijal Prajapati","doi":"10.2174/2468187313666230914121457","DOIUrl":"https://doi.org/10.2174/2468187313666230914121457","url":null,"abstract":"Introduction: Tobacco use is the leading preventable cause of various diseases, disabilities, and death. It is estimated that 480000 deaths annually are attributed to cigarette smoking, including secondhand smoke exposure. The treatment of brain disorders is particularly challenging due to the presence of a variety of formidable obstacles to delivering drugs selectively and effectively to the brain. The blood-brain barrier (BBB) and first-pass metabolism constitute the major obstacle to the uptake of drugs into the brain following systemic administration. Intranasal delivery offers a non-invasive and convenient method to bypass the BBB and avoid first-pass metabolism, which leads to the delivery of therapeutics directly to the brain. Objective: The objective of this study was to develop an In-situ gel of Bupropion Hydrochloride-loaded chitosan nanoparticles using the inotropic gelation method for Smoking Cessation via the nose to the brain to improve the bioavailability of Bupropion Hydrochloride, avoiding first-pass metabolism and bypassing Blood Brain Barrier. Method: Fourier transform infrared spectroscopy (FTIR) was used to determine the identity and purity of the drug. A UV Spectrophotometer was employed in the analytical procedure. Chitosan nanoparticles loaded with bupropion HCl were made using the ionic gelation method, and then the optimized batch was made using simulated in-situ gelation. Utilizing Central composite design, optimization was done by Design Expert-13. Evaluation of polymeric nanoparticles was performed by measuring their particle size, PDI, and entrapment efficiency. Additionally, they were tested for drug release in vitro. The final nanoparticles were subsequently tested for gelation using nasal simulation fluid, and an ex vivo investigation was also conducted. An ion-sensitive polymer gellan gum was used as a gelling agent, which formed an immediate gel and remained for an extended period. The finished formulation was also subjected to several characterizations, including TEM and FTIR. Results: The developed formulation was stable and showed enhanced contact time in the nasal mucosa, minimizing the frequency of administration. In-vitro studies through Franz diffusion cell and Ex-vivo studies on sheep nasal mucosa showed good results. In the Histopathological study, the optimized batch was found to be safe and stable in an accelerated stability study for one month. Conclusion: Bupropion HCl-loaded chitosan nanoparticles In-situ gel proved to be suitable for the administration of Bupropion HCl through the nasal route. The ease of administration coupled with less frequent administration enhanced patient compliance. The formulation was found to be liquid at the formulated condition and formed gel in the presence of ions present in the nasal mucosa. The gel formed in situ showed sustained drug release. The formulations were less viscous before instillation and formed a strong gel after instilling in the nasal cavity.","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":"39 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134969915","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}
Pub Date : 2023-09-04DOI: 10.2174/2468187313666230904150849
Utsav Gupta, Shaheen Sultana
As the blood-brain barrier (BBB) stops hazardous substances from entering the brain, creating treatment strategies to treat central nervous system (CNS) conditions is difficult. By circumventing the BBB, nanotechnology has emerged as a viable method for targeted medicine delivery to the brain. PEGylated nanoparticles (PEGNPs) have shown the ability to encapsulate a range of drugs and deliver them to the deepest regions of the brain. PEGNPs are a helpful tool in preclinical research for CNS diseases because of their extreme flexibility. Before PEGNPs can be employed in clinical practise, however, issues with their design and optimization for efficient brain targeting, as well as their long-term safety, must be resolved. Moreover, it is crucial to comprehend the basic principles of PEGNP trafficking through the BBB and how they affect CNS cells. Despite these difficulties, PEGNPs have the potential to completely alter the way CNS diseases are treated by allowing for precise medication delivery to the brain. This review emphasizes the potential and difficulties in using PEGNPs for brain targeting and describes current breakthroughs in PEGNP research for CNS diseases.
{"title":"Pegylated Nanoparticles for Brain Targeting- Opportunities and Challenges","authors":"Utsav Gupta, Shaheen Sultana","doi":"10.2174/2468187313666230904150849","DOIUrl":"https://doi.org/10.2174/2468187313666230904150849","url":null,"abstract":"\u0000\u0000As the blood-brain barrier (BBB) stops hazardous substances from entering the brain,\u0000creating treatment strategies to treat central nervous system (CNS) conditions is difficult. By circumventing the BBB, nanotechnology has emerged as a viable method for targeted medicine delivery to the brain. PEGylated nanoparticles (PEGNPs) have shown the ability to encapsulate a range\u0000of drugs and deliver them to the deepest regions of the brain. PEGNPs are a helpful tool in preclinical research for CNS diseases because of their extreme flexibility. Before PEGNPs can be employed\u0000in clinical practise, however, issues with their design and optimization for efficient brain targeting,\u0000as well as their long-term safety, must be resolved. Moreover, it is crucial to comprehend the basic\u0000principles of PEGNP trafficking through the BBB and how they affect CNS cells. Despite these difficulties, PEGNPs have the potential to completely alter the way CNS diseases are treated by allowing for precise medication delivery to the brain. This review emphasizes the potential and difficulties in using PEGNPs for brain targeting and describes current breakthroughs in PEGNP research\u0000for CNS diseases.\u0000","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49332007","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}
Pub Date : 2023-08-25DOI: 10.2174/2468187313666230825105753
Abdul Hafeez, Rabia Aqeel, S. Usmani
Cancer of the skin is one of the most frequent kinds of cancer around the globe and has substantial consequences for both public health and the economy. Co-delivery of drugs using nanotechnology are attractive for the reason that they make it possible for the effective targeting of medications with minimal side effects. The aim of the review is to provide an overview on the management of skin cancer with co-delivery via nanocarriers. Using a number of different search engines, search of the published literature was conducted using specific key terms such as co-delivery, skin cancer, nanoparticles, liposomes, and ethosomes. The articles were screened on the basis of target purpose and author’s expertise. Nanocarriers based co-delivery systems have been found to improve the pharmacokinetic profile of medications, which resulted in enhanced therapeutic effectiveness with reduction in dose and side effects. Lipid based systems and polymeric nanoparticles have been utilized to incorporate different drugs with different physicochemical characteristics for the management of skin cancer. The management of skin cancer may be significantly manageable with co-drug delivery approach by integration of nanotechnology. Polymeric nanoparticles, liposomes, ethosomes, nanostructured lipid carriers and polymeric micelles have shown the potential for skin cancer treatment.
{"title":"Nanocarrier-based Systems for Co-delivery of Drugs in the Management of Skin Cancer: A Review","authors":"Abdul Hafeez, Rabia Aqeel, S. Usmani","doi":"10.2174/2468187313666230825105753","DOIUrl":"https://doi.org/10.2174/2468187313666230825105753","url":null,"abstract":"\u0000\u0000Cancer of the skin is one of the most frequent kinds of cancer around the globe and has substantial consequences for both public health and the economy. Co-delivery of drugs using nanotechnology are attractive for the reason that they make it possible for the effective targeting of medications with minimal side effects. The aim of the review is to provide an overview on the management of skin cancer with co-delivery via nanocarriers.\u0000\u0000\u0000\u0000Using a number of different search engines, search of the published literature was conducted using specific key terms such as co-delivery, skin cancer, nanoparticles, liposomes, and ethosomes. The articles were screened on the basis of target purpose and author’s expertise.\u0000\u0000\u0000\u0000Nanocarriers based co-delivery systems have been found to improve the pharmacokinetic profile of medications, which resulted in enhanced therapeutic effectiveness with reduction in dose and side effects. Lipid based systems and polymeric nanoparticles have been utilized to incorporate different drugs with different physicochemical characteristics for the management of skin cancer.\u0000\u0000\u0000\u0000The management of skin cancer may be significantly manageable with co-drug delivery approach by integration of nanotechnology. Polymeric nanoparticles, liposomes, ethosomes, nanostructured lipid carriers and polymeric micelles have shown the potential for skin cancer treatment.\u0000","PeriodicalId":10818,"journal":{"name":"Current Nanomedicine","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42249873","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}
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