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Nanoemulsion Carriers for Ocular Fungal Infection: Main Emphasis on Keratomycosis. 眼部真菌感染的纳米乳液载体:重点关注角霉菌病。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385294591240427051402
Anjali Mishra, Manisha Bhatia, Manish Kumar, Abhishek Tiwari, Varsha Tiwari

Keratomycosis, also termed fungal keratitis (FK), is an invasive eye condition for which there is a lack of available effective treatment due to pharmacological shortages and vital ocular obstacles. This severe corneal infection typically suppurates and eventually ulcerates, ultimately causing blindness or decreased vision. According to epidemiological studies, FK is more common in warm, humid places with an agricultural economy. The use of nanoemulsion carriers for ocular fungal infection has been promoting better treatment and patient compliance. The persistent fungal infection like FK, affecting particularly the stroma heralds complications thereby posing difficulty in diagnosis and treatment. To help treat refractory cases and improve outcomes, recently targeted drug delivery techniques and novel antifungal drugs shall be explored. A delay in diagnosis may cause corneal fungal infections to have irreversible consequences, which cannot be avoided. However, infections can develop into ocular perforation even after receiving intense care. The commonly used chemotherapy for FK is based on topical (natamycin 5% is typically first-line therapy) and systemic administration of azole drugs. To address the problems related to better treatment, various nanoemulsion carriers were discussed. Novel drug delivery systems based on nanoemulsions are a viable therapeutic option for treating keratomycosis and may be a candidate method for overcoming obstacles in the treatment of many other ocular illnesses when combined with different hydrophobic medicines. With a brief explanation of the pathogenesis, this article seeks to give readers a thorough analysis of current trends, various treatment choices, and care strategies for fungal keratitis.

角膜炎又称真菌性角膜炎(FK),是一种侵袭性眼病,由于药物短缺和重要的眼部障碍,目前缺乏有效的治疗方法。这种严重的角膜感染通常会化脓并最终溃疡,最终导致失明或视力下降。根据流行病学研究,FK 在农业经济发达的温暖潮湿地区更为常见。纳米乳剂载体在眼部真菌感染中的使用促进了更好的治疗和患者依从性。像 FK 这样的顽固性真菌感染尤其影响基质,预示着并发症的出现,从而给诊断和治疗带来困难。为帮助治疗难治性病例并提高疗效,应探索最新的靶向给药技术和新型抗真菌药物。延误诊断可能导致角膜真菌感染造成不可逆转的后果,这是无法避免的。然而,即使接受了精心护理,感染也可能发展成眼球穿孔。FK 常用的化疗方法是局部用药(5% 纳他霉素通常是一线疗法)和全身使用唑类药物。为了解决与更好的治疗相关的问题,对各种纳米乳液载体进行了讨论。以纳米乳液为基础的新型给药系统是治疗角霉菌病的一种可行的治疗方法,与不同的疏水性药物结合使用,也可能成为克服许多其他眼部疾病治疗障碍的一种候选方法。通过对发病机理的简要说明,本文旨在为读者全面分析真菌性角膜炎的当前趋势、各种治疗选择和护理策略。
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引用次数: 0
Lipid-based Nanomedicine for Alzheimer's Disease: A Comprehensive Review of Recent Advances. 基于脂质的纳米药物治疗阿尔茨海默病:最新进展综述》。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385300234240522100826
Sanchit Dhankhar, Nitika Garg, Himanshu Sharma, Samrat Chauhan, Monika Saini

Background: Alzheimer's disease (AD) is the most common form of dementia and is expected to greatly rise in future, making it a major worldwide health concern with severe impacts on individuals and society. Despite advancements in understanding the cellular and molecular aspects of Alzheimer's disease (AD) in recent decades, it still poses a significant problem. A major problem is accurately delivering drugs to diseased neurons while minimising effects on healthy neurons. This difficulty is worsened by the low water solubility of anti-Alzheimer's disease medicines and the blood-brain barrier (BBB) that hinders the entry of central nervous system pharmaceuticals that are highly lipophilic.

Objective: The focus of this article is on nanocarriers that are lipid-based. This is one of the more widely accepted methods of treating Alzheimer's disease, as it increases therapeutic efficacy while decreasing side effects related to cooperated neurological disorder payload.

Method: Searched many databases for papers published under the title (including PubMed, Elsevier, and Google Scholar).

Results/conclusion: Nano Lipid Carriers (NLCs) are recognized for their ability to target the brain effectively due to their lipid-loving properties and compatibility with living tissues. They improve the absorption of drugs in the brain while decreasing the accumulation of drugs in unintended organs. This work emphasises the importance of nano lipid carriers, which are lipophilic and biocompatible and have demonstrated exceptional targeting efficiency, making them an ideal carrier system for delivering medications to the brain.

背景:阿尔茨海默病(AD)是最常见的痴呆症,预计今后将大幅增加,成为全球关注的主要健康问题,对个人和社会造成严重影响。尽管近几十年来人们对阿尔茨海默病(AD)的细胞和分子方面的认识取得了进步,但它仍然是一个重大问题。一个主要问题是如何准确地将药物输送到患病神经元,同时尽量减少对健康神经元的影响。由于抗阿尔茨海默病药物的水溶性较低,而血脑屏障(BBB)又阻碍了亲脂性较强的中枢神经系统药物的进入,因此这一难题更加严峻:本文的重点是基于脂质的纳米载体。这是目前较为广泛接受的治疗阿尔茨海默病的方法之一,因为它在提高疗效的同时减少了与配合神经紊乱有效载荷有关的副作用:搜索了许多数据库中以该标题发表的论文(包括 PubMed、Elsevier 和 Google Scholar):纳米脂质载体(NLCs)因其亲脂特性和与活体组织的相容性而被公认为能够有效靶向大脑。纳米脂质载体可促进药物在大脑中的吸收,同时减少药物在非预期器官中的蓄积。这项工作强调了纳米脂质载体的重要性,因为纳米脂质载体具有亲脂性和生物相容性,并已证明具有卓越的靶向效率,使其成为向大脑输送药物的理想载体系统。
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引用次数: 0
The Future of Healthcare: Pharmaceutical Nanotechnology. 医疗保健的未来:医药纳米技术。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/221173851301240923101614
Zongjin Li
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引用次数: 0
Potential of Plant-derived Exosome-like Nanoparticles from Physalis peruviana Fruit for Human Dermal Fibroblast Regeneration and Remodeling. 从秘鲁苦蘵果实中提取的植物外泌体纳米颗粒对人类真皮成纤维细胞再生和重塑的潜力
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385281838240105110106
Filia Natania, Iriawati Iriawati, Fitria Dwi Ayuningtyas, Anggraini Barlian

Aims: This research aimed to study the potential of PDEN from P. peruviana fruits (PENC) for regenerating and remodeling HDF.

Background: Large wounds are dangerous and require prompt and effective healing. Various efforts have been undertaken, but have been somewhat ineffective. Plant-derived exosome-like nanoparticles (PDEN) are easily sampled, relatively cost-effective, exhibit high yields, and are nonimmunogenic.

Objectives: The objective of the study was to isolate and characterize PDEN from Physalis peruviana (PENC), and determine PENC's internalization and toxicity on HDF cells, PENC's ability to regenerate HDF (proliferation and migration), and PENC ability's to remodel HDF (collagen I and MMP-1 production).

Methods: PENC was isolated using gradual filtration and centrifugation, followed by sedimentation using PEG6000. Characterization was done using a particle size analyzer, zeta potential analyzer, TEM, and BCA assay. Internalization was done using PKH67 staining. Toxicity and proliferation assays were conducted using MTT assay; meanwhile, migration assay was carried out by employing the scratch assay. Collagen I production was performed using immunocytochemistry and MMP-1 production was conducted using ELISA.

Results: MTT assay showed a PENC concentration of 2.5 until 500 μg/mL and being non-toxic to cells. PENC has been found to induce cell proliferation in 1, 3, 5, and 7 days. PENC at a concentration of 2.5, 5, and 7.5 μg/mL, also accelerated HDF migration using the scratch assay in two days. In remodeling, PENC upregulated collagen-1 expression from day 7 to 14 compared to control. MMP-1 declined from day 2 to 7 in every PENC concentration and increased on day 14. Overall, PENC at concentrations of 2.5, 5, and 7.5 μg/mL induced HDF proliferation and migration, upregulated collagen I production, and decreased MMP-1 levels.

Conclusion: Isolated PENC was 190-220 nm in size, circular, covered with membrane, and its zeta potential was -6.7 mV; it could also be stored at 4°C for up to 2 weeks in aqua bidest. Protein concentration ranged between 170-1,395 μg/mL. Using PKH67, PENC could enter HDF within 6 hours. PENC was non-toxic up to a concentration of 500 μg/mL. Using MTT and scratch assay, PENC was found to elevate HDF proliferation and migration, and reorganize actin. Using immunocytochemistry, collagen I was upregulated by PENC, whereas MMP-1 concentration was reduced.

目的:本研究旨在研究来自秘鲁果实(PENC)的 PDEN 在再生和重塑 HDF 方面的潜力:背景:大面积伤口非常危险,需要及时有效的愈合。背景:大面积伤口非常危险,需要及时、有效地愈合。人们已经做出了各种努力,但效果不佳。植物外泌体纳米颗粒(PDEN)易于取样、成本效益相对较高、产量高且无免疫原性:本研究的目的是从秘鲁苦蘵(Physalis peruviana,PENC)中分离和鉴定 PDEN,并确定 PENC 对 HDF 细胞的内化和毒性、PENC 再生 HDF 的能力(增殖和迁移)以及 PENC 重塑 HDF 的能力(胶原蛋白 I 和 MMP- 1 的产生):方法:使用渐进过滤和离心法分离 PENC,然后使用 PEG6000 进行沉淀。使用粒度分析仪、ZETA 电位分析仪、TEM 和 BCA 分析法进行表征。内化是通过 PKH67 染色法完成的。毒性和增殖试验采用 MTT 法进行;迁移试验采用划痕法进行。胶原蛋白 I 的产生采用免疫细胞化学法,MMP-1 的产生采用酶联免疫吸附法:MTT 检测显示,PENC 的浓度为 2.5 至 500 μg/mL,对细胞无毒性。研究发现,PENC 可在 1、3、5 和 7 天内诱导细胞增殖。浓度为 2.5、5 和 7.5 μg/mL 的 PENC 还能在两天内通过划痕试验加速 HDF 的迁移。在重塑过程中,与对照组相比,PENC 可在第 7 到 14 天内上调胶原蛋白-1 的表达。从第 2 天到第 7 天,MMP-1 在每个 PENC 浓度下都会下降,并在第 14 天上升。同时,与对照组相比,ROS 在第 2 天至第 7 天和第 14 天均有所下降,而 PENC 则会诱导 ROS 水平上升。总之,浓度为 2.5、5 和 7.5 μg/mL 的 PENC 可诱导 HDF 增殖和迁移,上调胶原蛋白 I 的生成,并降低 MMP-1 的水平:分离出的PENC大小为190-220 nm,呈圆形,被膜覆盖,其zeta电位为-6.7 mV;在4°C水溶液中可保存2周。蛋白质浓度在 170-1,395 μg/mL 之间。使用 PKH67,PENC 可在 6 小时内进入 HDF。五氯苯甲醚在浓度为 500 μg/mL 时无毒。通过 MTT 和划痕试验发现,五氯苯甲醚能促进 HDF 的增殖和迁移,并使肌动蛋白重组。通过免疫细胞化学,PENC 上调了胶原蛋白 I 的浓度,而 MMP-1 的浓度则有所降低。
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引用次数: 0
Preparation, In-vitro, Ex-vivo, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based In Situ Gel. 以纳米乳液为基础的鼻内原位凝胶 Lasmiditan 的制备、体外、体内和药代动力学研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385285009231222072303
Saba Abdulhadi Jabir, Nawal A Rajab
<p><strong>Background: </strong>Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.</p><p><strong>Objectives: </strong>This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased <i>in situ</i> gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) <i>via</i> using rabbits.</p><p><strong>Methods: </strong>Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive <i>in situ</i> gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (<i>in vitro</i>) and the nasal permeation (<i>ex vivo</i>) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics <i>in vivo</i> studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by Kumar et al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt<sub>0-∞</sub>) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5.</p><p><strong>Results: </strong>The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589 ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p < 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5
背景:Lasmiditan(LAS)是最近开发的一种抗偏头痛药物,于2019年10月获批用于治疗急性偏头痛,但其口服生物利用度较低,约为40%:本研究旨在通过原位凝胶纳米乳液制剂(NEIG)提高 LAS 的生物利用度,然后将传统的 LAS 水悬浮剂(AQS)与两种成功的鼻内制剂(NEIG 2 和 NEIG 5)进行比较,从而通过兔子确定其相对生物利用度(F-relative):方法:选择两种成功制备的纳米乳液(NE)配方(a和b),加入不同比例的pH敏感原位胶凝聚合物(Carbopol 934),制备NEIG 1、2、3、4、5和6。对所制备的 NEIG 的 pH 值、凝胶能力、凝胶强度和粘度进行了预测。测定了 NEIG 2 和 5 的释放(体外)和鼻腔渗透(体外),然后对两者进行了体内药代动力学研究。研究采用了 18 只体重为 2.0 至 2.5 千克的雄性兔子进行平行设计研究。在计算 LAS 剂量时,采用了体表面积(BSA)归一化方法。采用 Santosh Kumar 之前开发和验证的高效液相色谱法提取连续血样并进行药物分析。计算了主要的药代动力学参数,包括血浆中的最大药物浓度(Cmax)、达到 Cmax 的时间(T-max)和从零时到亲和力的浓度-时间曲线下面积(AUCt0-∞)。对 NE(a 和 b)以及 NEIG(2 和 5)配方进行了稳定性研究。最后,进行了鼻腔纤毛虫毒性研究,以评估所开发的 NEIG 2 和 5 的鼻腔毒性:结果表明,NEIGs 2 和 5 可被选为优化的 NEIGs,因为这两种药物在 20 分钟内达到 100% 的渗透率,然后分别在 25 分钟和 35 分钟内释放,因此与 AQS 相比,渗透率提高了 3.3 倍。NEIG 2 和 5 的释放值和渗透值与相应的 NE a 和 b 相当,但停留时间更长,以克服正常的鼻腔生理清除率。NEIG 2 和 NEIG 5 的 C-max、Tmax 和 AUC0-∞ 值分别为 8066±242 ng/ml、0.75±0.05 h、19616.86±589 ng. h/ml 和 7975.67±239 ng/ml、1.0±0.05 h、17912.36±537 ng. h/ml,而传统的 AQS 分别为 4181.09±125 ng/ml、2±0.2 h、8852.27±266 ng. h/ml。研究发现,NEIG 2 和 NEIG 5 具有更好的 LAS 鼻内给药效果,并能显著(p 结论:NEIG 2 和 NEIG 5 具有更好的 LAS 鼻内给药效果:与口服剂型(AQS)相比,NEIG 2 和 NEIG 5 具有更快的起效时间和更高的生物利用度,是很有前途的新型鼻内给药配方。最后,选定的最佳黄金配方是 NEIG 2,可用于进一步的临床研究。
{"title":"Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel.","authors":"Saba Abdulhadi Jabir, Nawal A Rajab","doi":"10.2174/0122117385285009231222072303","DOIUrl":"10.2174/0122117385285009231222072303","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Objectives: &lt;/strong&gt;This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased &lt;i&gt;in situ&lt;/i&gt; gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) &lt;i&gt;via&lt;/i&gt; using rabbits.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive &lt;i&gt;in situ&lt;/i&gt; gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (&lt;i&gt;in vitro&lt;/i&gt;) and the nasal permeation (&lt;i&gt;ex vivo&lt;/i&gt;) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics &lt;i&gt;in vivo&lt;/i&gt; studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by Kumar et al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt&lt;sub&gt;0-∞&lt;/sub&gt;) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589 ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p &lt; 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"239-253"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139087984","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: 0
A Review on Ocular Nanoformulation Based Formulations with Highlights on Pediatric Ocular Pharmacokinetics. 眼部纳米制剂综述,重点介绍小儿眼部药代动力学。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385307184240826041920
Ravinder Verma, Manisha Bhatia, Mithun Mojumder, Suraj Patel, Vivek Kumar Mishra, Pooja Mathur, Shailendra Bhatt, Jai Bharti Sharma

The potential use of nanoparticle-based formulations is being explored rapidly for drug delivery in ocular treatment. Despite having several advancements in the area of ocular therapy, the pharmacokinetics-based formulation development for pediatric ocular treatment is still not in proper focus. There are an inadequate number of degenerative ocular ailments with childhood onset. The purpose of this review is to focus on the pharmacokinetics studies of nanoparticle- based formulations for treating ocular diseases and problems associated with the ocular treatment of the pediatric population. Recent studies on pharmaceutical modeling of ocular formulations have also been discussed. Nanoparticle-based formulations were collected by conducting a literature survey on PubMed, Science Direct, and other portals. In this review, we have explored in detail the explanation behind the inequality among available ocular treatment regimens for youngsters as well as adults by specifically focusing on those diseases that can be distressing for children. Latest innovative developments and advancements in drug delivery systems and challenges in their usage particularly for young infant patients were also discussed. It can be concluded that the bioavailability of ocular formulations and their effect on ocular cells can be further enhanced manifolds by the development of nanoparticles-based formulations.

纳米颗粒制剂在眼科治疗中的给药潜力正在被迅速发掘。尽管在眼科治疗领域取得了一些进展,但基于药代动力学的儿科眼科治疗制剂开发仍未得到应有的重视。儿童发病的退行性眼部疾病数量不足。本综述的目的是重点介绍治疗眼部疾病的纳米颗粒制剂的药代动力学研究以及与儿童眼部治疗相关的问题。此外,还讨论了眼科制剂药物模型的最新研究。我们通过在 PubMed、Science Direct 和其他门户网站上进行文献调查,收集了基于纳米粒子的制剂。在这篇综述中,我们详细探讨了青少年和成人现有眼科治疗方案不平等背后的原因,并特别关注了那些可能给儿童带来痛苦的疾病。此外,我们还讨论了给药系统的最新创新发展和进步,以及在使用这些系统(尤其是针对婴幼儿患者)过程中遇到的挑战。可以得出的结论是,通过开发基于纳米颗粒的制剂,眼部制剂的生物利用度及其对眼部细胞的作用可进一步成倍提高。
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引用次数: 0
Phytosomes Nanocarrier with Insight Towards the Future in Cancer Therapy: A Mini-Review. 洞察癌症治疗未来的植物载体纳米载体:微型综述。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385304559240626101716
Innocent Sutnga, Akash Sharma, Raja Chakraborty

Cancer is classified as having one of the highest mortality rates on a global scale, presenting a significant challenge in its treatment, especially when conventional chemotherapy methodologies are used. Conversely, there is a growing interest in utilizing herbal medicine as an alternative to the treatment of cancer because of its lack of adverse effects compared to contemporary medical strategies. The incorporation of nanotechnology into therapy has attracted attention owing to its efficacy in the treatment of various illnesses. Phytosomes play a crucial role in the treatment of cancer by enhancing the characteristics of drugs and nanostructures within carriers to enable targeted drug delivery. The establishment of chemical bonds between phospholipid molecules and bioactive compounds from plants ensures the stability of phytosomes, thus establishing them as an innovative mechanism for drug delivery systems that transport plant-derived constituents to specific areas. This mini-overview discusses the potential phytosome complexes, uses, drawbacks, patents, challenges, and prospects of phytosomes in cancer treatment. Thus, numerous phytosomal formulations incorporating plant-derived components have exhibited promising anticancer properties, with several formulations currently undergoing clinical trials.

癌症被列为全球死亡率最高的疾病之一,给治疗带来了巨大挑战,尤其是在使用传统化疗方法的情况下。相反,由于中草药与现代医学策略相比没有不良反应,因此人们对利用中草药作为治疗癌症的替代方法越来越感兴趣。由于纳米技术在治疗各种疾病方面的疗效,将其纳入疗法已引起人们的关注。植物载体通过增强载体内药物和纳米结构的特性来实现靶向给药,在癌症治疗中发挥着至关重要的作用。磷脂分子与植物中的生物活性化合物之间建立的化学键确保了植物载体的稳定性,从而使植物载体成为一种创新的药物输送系统机制,可将植物提取的成分输送到特定区域。本小结将讨论潜在的植物体复合物、植物体在癌症治疗中的用途、缺点、专利、挑战和前景。目前,许多含有植物提取成分的植物载体制剂已显示出良好的抗癌特性,有几种制剂目前正在进行临床试验。
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引用次数: 0
Emulgel-Based Formulations of Clobetasol Propionate: Formulation Development, Characterization, and Pharmacological Evaluation. 丙酸氯倍他索乳状制剂:制剂开发、表征和药理学评价。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385327270241224080729
Kuldeep Singh, Jeetendra Kumar Gupta, Divya Jain, Mukesh Chandra Sharma, Shivendra Kumar, Ramkumar Chaudhary, Sakshi Mishra

Topical formulations of corticosteroids, particularly clobetasol propionate (CP), are commonly used to treat a range of dermatological conditions. CP is a potent corticosteroid known for its efficacy in managing inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Emulgel-based formulations of CP have emerged as an innovative approach, offering advantages like improved drug solubility, enhanced skin penetration, and extended drug release. This review aims to provide an updated overview of the latest advancements in the development and evaluation of CP emulgel formulations. Key aspects discussed include the selection and optimization of emulgel components, formulation characterization, in vitro drug release, and pharmacological activities such as anti-inflammatory and anti-pruritic effects. Emphasis is placed on recent studies and innovations that underscore the potential of CP emulgels in dermatological therapy, highlighting their promising applications in enhancing therapeutic efficacy and patient outcomes.

皮质类固醇的外用制剂,尤其是丙酸氯倍他索(CP),常用于治疗一系列皮肤病。氯倍他索丙酸酯是一种强效皮质类固醇,在治疗皮质类固醇反应性皮肤病的炎症和瘙痒表现方面疗效显著。基于 Emulgel 的氯化石蜡制剂已成为一种创新方法,具有改善药物溶解度、增强皮肤渗透性和延长药物释放时间等优点。本综述旨在概述在开发和评估氯化石蜡凝胶制剂方面取得的最新进展。讨论的主要方面包括乳凝胶成分的选择和优化、配方表征、体外药物释放以及药理活性(如抗炎和止痒作用)。重点放在最近的研究和创新上,这些研究和创新强调了氯化石蜡凝胶在皮肤病治疗中的潜力,突出了其在提高疗效和患者预后方面的应用前景。
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引用次数: 0
Nanostructured Lipid Carrier-loaded In Situ Gel for Ophthalmic Drug Delivery: Preparation and In Vitro Characterization Studies. 用于眼科给药的纳米结构脂质载体原位凝胶:制备和体外表征研究。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385266639231029192409
Vidya Sabale, Vaishnavi Belokar, Manasi Jiwankar, Prafulla Sabale

Background: Nanostructured lipid carriers (NLCs) are explored as vehicles for ophthalmic drug delivery owing to their better drug loading, good permeation, and satisfactory safety profile.

Objectives: The purpose of the study was to fabricate and characterize an in situ ocular gel of loratadine as a model drug based on NLCs to enhance the drug residence time.

Methods: NLCs were fabricated using the microemulsion method in which solid lipid as Compritol 888 ATO, lipid as oleic acid, surfactant as Tween 80, and isopropyl alcohol as co-surfactant as alcohol were used. Based on the evaluation of formulation batches of NLCs, the optimized batch was selected and further utilized for the formulation of in situ gel containing Carbopol 934 and HPMC K15M as gelling agents, and characterized Results: The optimized NLCs of loratadine exhibited entrapment efficiency of 83.13 ± 0.13% and an average particle size of 18.98 ± 1.22 nm. Drug content and drug release were found to be 98.67 and 92.48%, respectively. Excellent rheology and mucoadhesion were demonstrated by the loratadine NLC-loaded in situ gel to enhance its attachment to the mucosa. NLC-based in situ ocular gel showed the desired results for topical administration. The prepared gel was observed to be non-irritating to the eye.

Conclusion: The optimized NLC-based in situ gel formulation presented better corneal retention and it was found to be stable, offering sustained release of the drug. Thus, the joined system of sol-gel was found promising for ophthalmic drug delivery.

背景:纳米结构脂质载体(NLCs)具有更好的载药量、良好的渗透性和令人满意的安全性,因此被探索用作眼科给药的载体:本研究的目的是以 NLCs 为基础,以氯雷他定(Loratadine)为模型药物,制作眼部原位凝胶并对其进行表征,以延长药物的停留时间:方法:采用微乳液法制备 NLCs,其中固体脂质为康普瑞托 888 ATO,脂质为油酸,表面活性剂为吐温 80,助表面活性剂为异丙醇。根据对 NLCs 配方批次的评估,选出优化批次,进一步用于配制含有 Carbopol 934 和 HPMC K15M 胶凝剂的原位凝胶,并对其进行表征:结果:优化后的氯雷他定 NLC 的包埋效率为 83.13 ± 0.13 %,平均粒径为 18.98 ± 1.22 nm。药物含量和药物释放率分别为 98.67% 和 92.48%。装载了氯雷他定的 NLC 原位凝胶具有出色的流变性和粘附性,可增强其对粘膜的附着力。基于 NLC 的原位眼用凝胶在局部用药方面表现出了理想的效果。制备的凝胶对眼睛无刺激:结论:优化后的 NLC 原位凝胶配方具有更好的角膜保持力,而且性质稳定,能持续释放药物。因此,溶胶-凝胶联合体系有望用于眼科给药。
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引用次数: 0
Nano-formulation Approaches to Enhance Transdermal Drug Delivery- an Updated Review of Nanovesicular Carrier "Transethosomes". 增强透皮给药的纳米制剂方法--纳米囊状载体 "Transethosomes "的最新回顾。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385306281240427073651
Jitendra Pratap Singh, Geetanjali Saini, Bhupendra Singh, Gaurav Tiwari

Transdermal drug delivery is an attractive and patient-friendly route for administering therapeutic agents. However, the skin's natural barrier, the stratum corneum, restricts the passage of many drugs, limiting their effectiveness. To overcome this challenge, researchers have developed various nanocarriers to enhance drug penetration through the skin. Transethosomes, a novel and promising drug delivery system, have emerged as an innovative solution for improving transdermal drug delivery. Transethosomes are a hybrid of two established nanocarriers: ethosomes and transfersomes. Ethosomes are lipid-based vesicles that can accommodate lipophilic and hydrophilic drugs, while transfersomes are deformable lipid vesicles designed to enhance skin penetration. Transethosomes combine the advantages of both systems, making them ideal candidates for efficient transdermal drug delivery. They are composed of phospholipids, ethanol, and water and exhibit high flexibility, enabling them to squeeze through the tight junctions of the stratum corneum. This abstract reviews the key characteristics of transethosomes, including their composition, preparation methods, mechanisms of action, characterization parameters, and prospects. Moreover, the recent advancements and applications of transethosomes in delivering various therapeutic agents, such as analgesics, anti-inflammatories, hormones, and skincare products, are explored. The enhanced skin penetration capabilities of transethosomes can potentially reduce systemic side effects and improve patient compliance, making them a valuable tool in the field of transdermal drug delivery. In conclusion, transethosomes represent a promising platform for overcoming the challenges of transdermal drug delivery. Their unique properties enable efficient drug permeation through the skin, offering a more controlled and effective means of administering a wide range of pharmaceutical and cosmetic products. This abstract highlights the potential of transethosomes as a valuable addition to the field of transdermal drug delivery and paves the way for further research and development in this area.

透皮给药是一种极具吸引力且对患者友好的给药途径。然而,皮肤的天然屏障--角质层限制了许多药物的通过,从而限制了药物的有效性。为了克服这一难题,研究人员开发了各种纳米载体,以增强药物在皮肤中的渗透。透硫体是一种新型的、前景广阔的给药系统,已成为改善透皮给药的创新解决方案。Transethosomes 是两种成熟纳米载体的混合体:ethosomes 和 transfersomes。乙硫体是一种基于脂质的囊泡,可容纳亲脂性和亲水性药物,而转移体是一种可变形的脂质囊泡,旨在增强皮肤渗透性。转运体结合了这两种系统的优点,是高效透皮给药的理想候选物质。它们由磷脂、乙醇和水组成,具有很高的柔韧性,能够挤压穿过角质层的紧密连接处。本摘要回顾了透硫体的主要特点,包括其组成、制备方法、作用机制、表征参数和前景。此外,摘要还探讨了最近在递送各种治疗剂(如镇痛剂、消炎药、激素和护肤品)方面跨硫体的进展和应用。透硫体具有更强的皮肤渗透能力,有可能减少全身副作用,提高患者的依从性,使其成为透皮给药领域的重要工具。总之,透硫体是克服透皮给药挑战的一个前景广阔的平台。它们的独特特性使药物能够高效地透过皮肤,为多种药物和化妆品的给药提供了一种更可控、更有效的方法。本摘要强调了透硫体作为透皮给药领域宝贵补充的潜力,并为该领域的进一步研究和开发铺平了道路。
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引用次数: 0
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Pharmaceutical nanotechnology
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