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Pharmacists’s knowledge, attitude, and practices towards pharmaceutical and patient-centred care in asthma management: A national study 药剂师在哮喘治疗中对药物和以患者为中心的护理的认识、态度和实践:一项全国性研究
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-08 DOI: 10.1016/j.jsps.2024.102140
Dilan Çakmak , Muhammed Yunus Bektay , Anmar Al‑Taie , Saad Ahmed Ali Jadoo , Fikret Vehbi Izzettin

Background

Asthma, a chronic respiratory disease, is effectively managed with medications, yet many patients struggle due to irregular treatment and poor adherence. Pharmacists play a crucial role in improving asthma care through pharmaceutical care (PC) services. This study aims to assess pharmacists’ knowledge, attitudes, and behaviors regarding asthma PC in Türkiye.

Methods

This cross-sectional study in Türkiye evaluated community (CP) and hospital pharmacists’ (HP) knowledge level, attitudes, and behaviors regarding asthma care. A validated Asthma Pharmaceutical Care Knowledge (APCL) and Asthma Attitudes and Behaviors (AAB) questionnaires were used to assess their knowledge levels and attitudes toward asthma pharmaceutical care.

Results

Out of 400 pharmacists participated the questionnaire, the majority were CP (297, 74.25 %). Both CP and HP demonstrated adequate knowledge scores, 79.39 ± 12.32 and 80.66 ± 12.25, respectively. APCL mean scores of CP and HP were 4.22 ± 0.523 and 4.29 ± 0.383. No statistically significant difference in asthma knowledge levels was observed between CP and HP. Both groups reported positive attitudes and behaviors toward asthma care, with CP scoring 4.71 ± 0.446 and HP scoring 4.74 ± 0.330 on the AAB questionnaire.

Conclusions

This study revealed that both CP and HP have sufficient knowledge about asthma and they have positive attitudes towards providing asthma PC. Pharmacists have crucial role in asthma care with leveraging their expertise, patient interactions, and ability to referral capabilities.

背景哮喘是一种慢性呼吸道疾病,可通过药物有效控制,但许多患者由于治疗不规范和依从性差而陷入困境。药剂师在通过药物护理(PC)服务改善哮喘护理方面发挥着至关重要的作用。本研究旨在评估土耳其药剂师在哮喘药物护理方面的知识、态度和行为。方法这项在土耳其进行的横断面研究评估了社区药剂师(CP)和医院药剂师(HP)在哮喘药物护理方面的知识水平、态度和行为。采用经过验证的哮喘药物护理知识(APCL)和哮喘态度与行为(AAB)问卷来评估他们对哮喘药物护理的知识水平和态度。结果 在参与问卷调查的 400 名药剂师中,大多数是社区药剂师(297 人,占 74.25%)。CP 和 HP 的知识得分都很高,分别为 79.39 ± 12.32 和 80.66 ± 12.25。CP 和 HP 的 APCL 平均得分分别为 4.22 ± 0.523 和 4.29 ± 0.383。CP和HP在哮喘知识水平上没有明显的统计学差异。CP 和 HP 在 AAB 问卷上的得分分别为 4.71 ± 0.446 和 4.74 ± 0.330。药剂师在哮喘护理中发挥着至关重要的作用,他们可以充分利用自己的专业知识、与患者的互动以及转诊能力。
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引用次数: 0
High throughput virtual screening and validation of Plant-Based EGFR L858R kinase inhibitors against Non-Small cell lung Cancer: An integrated approach Utilizing GC–MS, network Pharmacology, Docking, and molecular dynamics 高通量虚拟筛选和验证针对非小细胞肺癌的植物表皮生长因子受体 L858R 激酶抑制剂:利用 GC-MS、网络药理学、对接和分子动力学的综合方法
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-06 DOI: 10.1016/j.jsps.2024.102139
Kun Gao , Zujian Chen , Na Zhang , Pu Jiang

Lung cancer ranks as the 2nd most common cancer globally. It’s the most prevalent cancer in men and the 2nd most common in women. The prominent events in EGFR-mutated non-small-cell lung cancer (NSCLC) include the emergence of the L858R mutation within EGFR exon 21. Despite the promising efficacy of EGFR inhibitors in managing lung cancer, the development of acquired resistance poses a significant hurdle. In the current investigation, we focused on the screening of two phytochemicals, namely Dehydrocostus lactone and Mokkolactone, derived from the Saussurea lappa plant, as potential inhibitors targeting EGFR L858R mutant lung cancer. The chloroform and ethanol extract of the plant demonstrated anti-proliferative activity through the Resazurin chemosensitivity assay, exhibiting an IC50 value of 37.90 ± 0.29 µg/ml with selectivity index 2.4. Through a GC–MS study, we identified 11 phytochemicals for further insilico analysis. These compounds underwent ADMET assessment followed by drug likeliness analysis before being subjected to molecular docking against EGFR L858R, identified through protein–protein interaction network analysis. All phytochemicals exhibited binding energy scores ranging from −6.9 to −8.1 kcal/mol. Dehydrocostus lactone and Mokkolactone were specifically identified for their binding profile. Findings from 100 ns molecular dynamics simulations demonstrated their enhanced stability compared to the reference ligand DJK. This was evident in the root mean square deviation (RMSD) values, ranging from 0.23 ± 0.01 nm to 0.30 ± 0.05 nm, the radius of gyration values, from 1.71 ± 0.01 nm to 1.72 ± 0.01 nm, and the solvent accessible surface area values, from 155.39 ± 2.40 nm2 to 159.32 ± 2.14 nm2. Additionally, favourable characteristics were observed in terms of hydrogen bonding, principal component analysis, and free energy landscape analysis. Examination of their electronic structure via density functional theory revealed efficient properties, with the highest occupied molecular orbital-least unoccupied molecular orbital energy gap values ranging from −3.984 eV to −6.547 eV. Further, in vivo analysis is required to gain a more comprehensive understanding and efficacy of these identified phytochemicals against lung cancer.

肺癌是全球第二大常见癌症。它是男性发病率最高的癌症,也是女性发病率第二高的癌症。表皮生长因子受体(EGFR)突变的非小细胞肺癌(NSCLC)的突出事件包括表皮生长因子受体(EGFR)外显子 21 中 L858R 突变的出现。尽管表皮生长因子受体(EGFR)抑制剂在治疗肺癌方面疗效显著,但获得性耐药性的产生仍是一个重大障碍。在目前的研究中,我们重点筛选了两种植物化学物质,即从红豆杉植物中提取的去氢木香内酯和木香内酯,作为针对表皮生长因子受体(EGFR)L858R突变肺癌的潜在抑制剂。该植物的氯仿和乙醇提取物通过利血平化学敏感性试验显示了抗增殖活性,其 IC50 值为 37.90 ± 0.29 µg/ml,选择性指数为 2.4。通过气相色谱-质谱(GC-MS)研究,我们确定了 11 种植物化学物质,并对其进行了进一步的内部分析。这些化合物在与表皮生长因子受体 L858R 进行分子对接之前进行了 ADMET 评估和药物相似性分析,后者是通过蛋白质-蛋白质相互作用网络分析确定的。所有植物化学物质的结合能得分范围为 -6.9 至 -8.1 kcal/mol。去氢木香内酯和木香内酯因其结合特征而被特别识别。100 ns 分子动力学模拟结果表明,与参考配体 DJK 相比,它们的稳定性更强。这表现在均方根偏差(RMSD)值从 0.23 ± 0.01 nm 到 0.30 ± 0.05 nm,回转半径值从 1.71 ± 0.01 nm 到 1.72 ± 0.01 nm,溶剂可接触表面积值从 155.39 ± 2.40 nm2 到 159.32 ± 2.14 nm2。此外,在氢键、主成分分析和自由能景观分析方面也观察到了有利的特征。通过密度泛函理论对其电子结构进行的研究显示了其高效特性,最高占用分子轨道-最低未占用分子轨道能隙值范围为 -3.984 eV 至 -6.547 eV。为了更全面地了解这些已发现的植物化学物质对肺癌的疗效,还需要进一步进行体内分析。
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引用次数: 0
The potential effect of α7 nicotinic receptors modulation on palatable food-induced dependence-like behaviors 调节α7烟碱受体对美味食物诱发的类似依赖行为的潜在影响
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-04 DOI: 10.1016/j.jsps.2024.102138
Alaa A. Alameen , Shakir D. AlSharari , Musaad A. Alshammari , M.I. Damaj , Y. Sari

Background

The recent global increase in obesity rates, coupled with excessive palatable food (PF) consumption, has become a serious societal concern. Literature indicates that rewarding PF, especially upon cessation, can lead to overeating, binge eating, and compulsive eating, potentially resulting in obesity. Challenges in dietary paradigms, alongside limitations in approved treatments for eating disorders and anti-obesity medications, underscore the need to explore novel targets. In this context, α7nAChR (alpha-7 nicotinic acetylcholine receptor) may serve as a promising therapeutic target in combating food dependence and obesity. The present study aims to assess the role of α7nAChR in palatable food-induced dependence-like behaviors.

Method

The study involved male C57BL/6J mice exposed to three different feeding paradigms over 6 weeks to induce obesity and food addiction. On day 43, palatable food was replaced with standard chow, and the mice received treatments (vehicle, PNU-282987 [α7nAChR agonist], or methyllycaconitine citrate [MLA; α7nAChR antagonist]). Addiction-like behaviors, including craving for palatable food, motivation-effort interaction tests, and compulsive eating-like behavior, were measured during abstinence with and without treatment.

Results

The present study shows that chronic intermittent and continuous exposure to palatable food induces craving, motivation, and effort interaction behaviors as well as compulsive eating-like behaviors in palatable food-abstinent mice. Administration of the α7nAChR agonist, PNU-282987, significantly attenuated the craving behavior only in mice continuously fed palatable food (reduced calorie intake from 63.19 % to 48.21 %; p = 0.0053). Also, PNU-282987 suppressed the effort behaviors in either intermittently or continuously fed mice (significant reduction in the Δ number of active events per minute; p-values = 0.038 and 0.0098, respectively). However, it attenuated the compulsive-like eating behavior exclusively in the continuously fed group (p = 0.0433). Active and total interaction efforts were reversed by the MLA. These findings indicate the involvement of α7nAChR in dependence-like behaviors toward palatable food in mice.

Conclusion

Our findings demonstrate that dependence-like behaviors toward palatable food can emerge after prolonged exposure. Mice fed on palatable food continuously exhibited more dependence-like behaviors toward palatable food, and activation of α7nAChR signaling attenuated the vulnerability to develop such behaviors.

背景近年来,全球肥胖率上升,再加上适口食物(PF)消费过多,已成为一个严重的社会问题。文献表明,奖励性适口食物(尤其是在停止食用时)会导致暴饮暴食、暴饮暴食和强迫性进食,从而可能导致肥胖。饮食范式面临的挑战,以及已获批准的饮食失调症治疗方法和抗肥胖药物的局限性,凸显了探索新靶点的必要性。在这种情况下,α7nAChR(α-7 尼古丁乙酰胆碱受体)可能成为对抗食物依赖和肥胖症的一个有希望的治疗靶点。本研究旨在评估α7nAChR在适口食物诱导的类似依赖行为中的作用。第43天,用标准饲料取代适口食物,小鼠接受治疗(载体、PNU-282987[α7nAChR激动剂]或柠檬酸甲酯[MLA;α7nAChR拮抗剂])。结果本研究表明,长期间歇性和持续暴露于适口食物会诱发成瘾小鼠的渴求、动机和努力相互作用行为以及强迫性进食行为。服用α7nAChR激动剂PNU-282987仅能显著减轻连续喂食适口食物的小鼠的渴求行为(卡路里摄入量从63.19%降至48.21%;p = 0.0053)。此外,PNU-282987 还能抑制间歇或连续喂食小鼠的努力行为(显著减少每分钟活动事件的 Δ 数量;p 值分别为 0.038 和 0.0098)。然而,它只减轻了连续喂食组的强迫性进食行为(p = 0.0433)。主动和全面的交互作用被 MLA 逆转。这些研究结果表明,α7nAChR 参与了小鼠对适口食物的依赖行为。连续喂食适口食物的小鼠对适口食物表现出更多类似依赖的行为,而激活α7nAChR信号转导可减轻出现此类行为的脆弱性。
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引用次数: 0
Evaluation of the vitamin D response index in a Saudi cohort 评估沙特队列中的维生素 D 反应指数
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-06-22 DOI: 10.1016/j.jsps.2024.102137
Shareefa A. AlGhamdi , Ranjini Ghosh Dastidar , Maciej Rybiński , Hadeil M. Alsufiani , Sawsan O. Khoja , Nusaibah N. Enaibsi , Safa F. Saif , Carsten Carlberg

The concept of the vitamin D response index was developed based on vitamin D intervention studies conducted with Finnish cohorts. In this study, we challenged the concept by performing a single vitamin D3 bolus (80,000 IU) intervention with a cohort of 100 native Saudis. The change of serum levels of the proinflammatory cytokines interleukin 6, interleukin 8 and tumor necrosis factor measured directly before intervention in comparison to samples taken one and thirty days after vitamin D3 supplementation were used as biomarkers for distinguishing low, mid and high responders. Interestingly, we identified 39 % of the study participants as low responders. In contrast, when we used in a subset of 37 study participants whole blood expression changes of seven well-known vitamin D target genes one and thirty days after supplementation as alternative biomarkers, only 9 persons (24 %) were identified as low responders. In conclusion, in Saudi Arabia the rate of low vitamin D responders is equal or even higher than that in Finland. Therefore, similar to Nordic countries also in Saudi Arabia appropriate vitamin D3 supplementation is essential, in order to fulfill the needs of low responders.

维生素 D 反应指数的概念是在芬兰队列维生素 D 干预研究的基础上提出的。在本研究中,我们对这一概念提出了质疑,对 100 名沙特本地人进行了一次维生素 D3 栓剂(80,000 IU)干预。干预前直接测量的血清促炎细胞因子白细胞介素 6、白细胞介素 8 和肿瘤坏死因子的水平变化,与补充维生素 D3 一、三十天后采集的样本进行比较,以此作为区分低、中、高应答者的生物标志物。有趣的是,我们发现 39% 的研究参与者属于低反应者。与此相反,当我们使用补充维生素 D 一、三十天后七个著名维生素 D 目标基因的全血表达变化作为替代生物标志物时,37 名研究参与者中只有 9 人(24%)被确定为低反应者。总之,在沙特阿拉伯,维生素 D 低反应者的比例与芬兰相当,甚至更高。因此,与北欧国家类似,沙特阿拉伯也必须适当补充维生素 D3,以满足低反应者的需求。
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引用次数: 0
Impacts of storage conditions on the dissolution performance of commercial metronidazole tablets available in Saudi Arabia 储存条件对沙特阿拉伯市售甲硝唑商用片剂溶解性能的影响
IF 4.1 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-06-12 DOI: 10.1016/j.jsps.2024.102134
Basmah N. Aldosari, Areej M. Al-Mutairi, Alanood S. Almurshedi, Iman M. Alfagih, Bushra T. Al Quadeib, Eram Eltahir, Salma S. Almarshidy, Mohamed A. Ibrahim, Amal El Sayeh F. Abou El Ela

This study aimed to investigate the impact of storage conditions on the dissolution performance of commercial metronidazole (MTZ) tablets available in Saudi Arabia; these were coded as the reference and Test A, Test B, and Test C products. Moreover, the hardness and the disintegration time were measured. The UV spectrophotometrically analytical technique was utilized to quantify MTZ. All the control tablets, which were tested upon receipt, met the USP requirement as not less than 85 % of the labeled amount of MTZ was dissolved in 60 min. The MTZ reference released 91.79 % ± 1.23 after 60 min, while the products A, B, and C released 87.96 % ± 2.60, 93.26 % ± 2.01, and 88.61 % ± 2.04, respectively. The different dissolution parameters calculated for all the control tablets showed that the MTZ products A and B had optimal dissolution performances and were considered similar to the reference product. The product C showed a significantly reduced dissolution performance and was considered different from the reference. The in vitro dissolution of the MTZ tablets stored at 40oC ± 2 oC/75 % RH ± 5 % for 6 months indicated that the tablets maintained compliance with the USP requirement. The MTZ reference released 89.36 % ± 3.64 after 60 min, while the products A, B, and C released 95.79 % ± 3.91, 88.52 % ± 2.52, and 87.79 % ± 5.04, respectively. However, a slight reduction in the percentage released after 30 min (% DE30) and a slight increase in the mean dissolution time (MDT) were observed during the first 3 months of storage under stressed conditions. These changes were more obvious after 6 months of storage under the same conditions. Furthermore, in vitro dissolution of the product C stored at 40oC ± 2 oC/75 % RH ± 5 % for 3 months with further protection against high humidity revealed an improvement in the dissolution parameters due to the similar protective effects exerted by the two packaging forms. Furthermore, the study shows that storage conditions such as humidity and temperature affect in vitro dissolution of MTZ marketed tablets which may have an impact on efficiency and patient safety.

本研究旨在调查贮藏条件对沙特阿拉伯市售甲硝唑(MTZ)商用片剂溶出性能的影响;这些片剂被编码为参考产品、试验 A、试验 B 和试验 C 产品。此外,还测量了硬度和崩解时间。采用紫外分光光度分析技术对 MTZ 进行定量。所有对照药片在收到后都进行了测试,符合美国药典的要求,即在 60 分钟内溶解的 MTZ 含量不少于标签量的 85%。60 分钟后,MTZ 参考品释放了 91.79 % ± 1.23%,而产品 A、B 和 C 分别释放了 87.96 % ± 2.60%、93.26 % ± 2.01% 和 88.61 % ± 2.04%。对所有对照药片计算的不同溶出度参数表明,MTZ 产品 A 和 B 具有最佳的溶出性能,与参比产品相似。产品 C 的溶出性能明显降低,被认为与参比产品不同。MTZ 片剂在 40oC ± 2 oC/75 % RH ± 5 % 的条件下储存 6 个月的体外溶出度表明,这些片剂始终符合美国药典的要求。60 分钟后,MTZ 参考品释放出 89.36 % ± 3.64%,而产品 A、B 和 C 分别释放出 95.79 % ± 3.91%、88.52 % ± 2.52% 和 87.79 % ± 5.04%。不过,在受压条件下储存的前 3 个月,观察到 30 分钟后释放的百分比(DE30%)略有下降,平均溶解时间(MDT)略有增加。在相同条件下储存 6 个月后,这些变化更加明显。此外,将产品 C 在 40oC ± 2 oC/75 % RH ± 5 % 的条件下存放 3 个月,并进一步防止高湿度,体外溶出度显示,由于两种包装形式具有类似的保护作用,溶出度参数有所改善。此外,该研究还表明,湿度和温度等储存条件会影响 MTZ 上市片剂的体外溶出度,这可能会影响效率和患者安全。
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引用次数: 0
Epidemiologic and clinical updates on viral infections in Saudi Arabia 沙特阿拉伯病毒感染的流行病学和临床最新情况
IF 4.1 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-06-08 DOI: 10.1016/j.jsps.2024.102126
Noura M. Alshiban , Munirah S. Aleyiydi , Majed S. Nassar , Nada K. Alhumaid , Thamer A. Almangour , Yahya M.K. Tawfik , Laila A. Damiati , Abdulaziz S. Almutairi , Essam A. Tawfik

In the past two decades, the world has witnessed devastating pandemics affecting the global healthcare infrastructure and disrupting society and the economy worldwide. Among all pathogens, viruses play a critical role that is associated with outbreaks due to their wide range of species, involvement of animal hosts, easily transmitted to humans, and increased rates of infectivity. Viral disease outbreaks threaten public health globally due to the challenges associated with controlling and eradicating them. Implementing effective viral disease control programs starts with ongoing surveillance data collection and analyses to detect infectious disease trends and patterns, which is critical for maintaining public health. Viral disease control strategies include improved hygiene and sanitation facilities, eliminating arthropod vectors, vaccinations, and quarantine. The Saudi Ministry of Health (MOH) and the Public Health Authority (also known as Weqayah) in Saudi Arabia are responsible for public health surveillance to control and prevent infectious diseases. The notifiable viral diseases based on the Saudi MOH include hepatitis diseases, viral hemorrhagic fevers, respiratory viral diseases, exanthematous viral diseases, neurological viral diseases, and conjunctivitis. Monitoring trends and detecting changes in these viral diseases is essential to provide proper interventions, evaluate the established prevention programs, and develop better prevention strategies. Therefore, this review aims to highlight the epidemiological updates of the recently reported viral infections in Saudi Arabia and to provide insights into the recent clinical treatment and prevention strategies.

在过去二十年里,世界上发生了毁灭性的大流行病,影响了全球医疗保健基础设施,扰乱了全球社会和经济。在所有病原体中,病毒因其种类繁多、涉及动物宿主、易传播给人类以及感染率高而在疾病爆发中扮演着重要角色。病毒性疾病的爆发威胁着全球公共卫生,因为控制和根除病毒性疾病是一项艰巨的任务。实施有效的病毒性疾病控制计划首先要不断收集和分析监测数据,以发现传染病的趋势和模式,这对维护公共卫生至关重要。病毒性疾病控制策略包括改善个人卫生和环境卫生设施、消灭节肢动物病媒、接种疫苗和隔离。沙特阿拉伯卫生部和公共卫生局(又称 Weqayah)负责公共卫生监测,以控制和预防传染病。根据沙特卫生部的规定,应通报的病毒性疾病包括肝炎、病毒性出血热、呼吸道病毒性疾病、出血性病毒性疾病、神经系统病毒性疾病和结膜炎。监测这些病毒性疾病的趋势和检测其变化对于提供适当的干预措施、评估既定的预防计划和制定更好的预防策略至关重要。因此,本综述旨在重点介绍沙特阿拉伯最近报告的病毒感染的最新流行病学情况,并深入探讨近期的临床治疗和预防策略。
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引用次数: 0
Recognition on pharmacodynamic ingredients of natural products 认识天然产品的药效学成分
IF 4.1 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-06-02 DOI: 10.1016/j.jsps.2024.102124
Tao Wang , Zhong-Yu Fu , Yan-Juan Li , Lei Zi , Cheng-Zhu Song , Yu-Xuan Tao , Mei Zhang , Wen Gu , Jie Yu , Xing-Xin Yang

Natural products (NPs) play an irreplaceable role in the intervention of various diseases and have been considered a critical source of drug development. Many new pharmacodynamic compounds with potential clinical applications have recently been derived from NPs. These compounds range from small molecules to polysaccharides, polypeptides, proteins, self-assembled nanoparticles, and extracellular vesicles. This review summarizes various active substances found in NPs. The investigation of active substances in NPs can potentiate new drug development and promote the in-depth comprehension of the mechanism of action of NPs that can be beneficial in the prevention and treatment of human diseases.

天然产物(NPs)在干预各种疾病方面发挥着不可替代的作用,一直被认为是药物开发的重要来源。最近,许多具有潜在临床应用价值的新药效化合物都是从天然产物中提取出来的。这些化合物包括小分子、多糖、多肽、蛋白质、自组装纳米颗粒和细胞外囊泡。本综述总结了在纳米粒子中发现的各种活性物质。对 NPs 中活性物质的研究可促进新药开发,并有助于深入了解 NPs 的作用机制,从而有利于预防和治疗人类疾病。
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引用次数: 0
Development of topical silver nano gel formulation of Bixin: Characterization, and evaluation of anticancer activity 开发局部银纳米凝胶制剂 "碧欣":表征和抗癌活性评估
IF 4.1 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-06-02 DOI: 10.1016/j.jsps.2024.102125
Swapnil S. Patil , Preeti khulbe , Manojkumar M. Nitalikar , Kuntal Das , Mallikarjuna B.P. , Sultan Alshehri , Amro Mohammed Sawadi Khormi , Mutlaq Eidhah M. Almalki , Syed Arif Hussain , Syed Imam Rabbani , Syed Mohammed Basheeruddin Asdaq

Objective

Skin cancer refers to the pathological condition characterized by the proliferation of atypical skin cells in an uncontrolled manner. Plant-based products such as bixin although show promising anticancer properties, but maintaining their stability in a formulation is a difficult task. The objective of the research is to formulate a silver nanoparticle gel preparation of bixin and evaluate its anticancer properties.

Methods

The extract from Bixa orellana seed was prepared by hot extraction technique to isolate the active ingredient, bixin. A green synthesis approach was utilized for preparing the silver nanoparticle gel of bixin (BOAgNPs). Characterization of silver nanoparticles was done using FTIR, scanning electron microscopy, compatibility study, homogeneity testing, pH evaluation, and drug content determination. The in-vitro anticancer activity was performed using cell lines (B16F10) and in-vivo by chemical carcinogen (7,12-dimethylbenz (a) anthracene) in mice.

Results

The BOAgNPs-loaded topical gel was found to be homogeneous (clear orange color) and pH-compatible (pH ≈ 6.66) with the skin. The characterization studies indicated the presence of all functional groups in the formulation. An optimized batch of bixin-nano gel showed about 60% inhibitory effects on B16F10 cell lines (in-vitro activity) when equated with a reference drug, 5-fluorouracil. The in-vivo anticancer study suggested suppression of tumorigenesis and promotion of the healing process with bixin-nano gel application on the skin.

Conclusion

The results suggested the promising anticancer property of bixin when formulated in silver nanoparticle gel. The preparation of silver particles nano gel with bixin might provide an effective alternative option for treating skin cancers, provided more research complements the findings of the present study.

目的皮肤癌是指非典型皮肤细胞不受控制地增殖的病理状态。以植物为原料的产品(如碧欣)虽然显示出良好的抗癌特性,但在配方中保持其稳定性是一项艰巨的任务。研究目的是配制一种银纳米颗粒的碧蟾素凝胶制剂,并评估其抗癌特性。方法采用热萃取技术从碧蟾素种子中提取精华,分离出有效成分碧蟾素。采用绿色合成方法制备了银纳米颗粒凝胶(BOAgNPs)。利用傅立叶变换红外光谱、扫描电子显微镜、相容性研究、均匀性测试、pH 值评估和药物含量测定对银纳米粒子进行了表征。使用细胞系(B16F10)进行了体外抗癌活性测试,并使用化学致癌物(7,12-二甲基苯(a)蒽)对小鼠进行了体内抗癌活性测试。表征研究表明制剂中存在所有官能团。与参考药物 5-氟尿嘧啶相比,优化批次的 bixin 纳米凝胶对 B16F10 细胞株的抑制效果约为 60%(体外活性)。体内抗癌研究表明,将比克辛纳米凝胶涂抹在皮肤上可抑制肿瘤发生并促进愈合过程。如果有更多的研究能够补充本研究的结果,那么用比克信制备银颗粒纳米凝胶可能会为治疗皮肤癌提供一种有效的替代选择。
{"title":"Development of topical silver nano gel formulation of Bixin: Characterization, and evaluation of anticancer activity","authors":"Swapnil S. Patil ,&nbsp;Preeti khulbe ,&nbsp;Manojkumar M. Nitalikar ,&nbsp;Kuntal Das ,&nbsp;Mallikarjuna B.P. ,&nbsp;Sultan Alshehri ,&nbsp;Amro Mohammed Sawadi Khormi ,&nbsp;Mutlaq Eidhah M. Almalki ,&nbsp;Syed Arif Hussain ,&nbsp;Syed Imam Rabbani ,&nbsp;Syed Mohammed Basheeruddin Asdaq","doi":"10.1016/j.jsps.2024.102125","DOIUrl":"10.1016/j.jsps.2024.102125","url":null,"abstract":"<div><h3>Objective</h3><p>Skin cancer refers to the pathological condition characterized by the proliferation of atypical skin cells in an uncontrolled manner. Plant-based products such as bixin although show promising anticancer properties, but maintaining their stability in a formulation is a difficult task. The objective of the research is to formulate a silver nanoparticle gel preparation of bixin and evaluate its anticancer properties.</p></div><div><h3>Methods</h3><p>The extract from <em>Bixa orellana</em> seed was prepared by hot extraction technique to isolate the active ingredient, bixin. A green synthesis approach was utilized for preparing the silver nanoparticle gel of bixin (BOAgNPs). Characterization of silver nanoparticles was done using FTIR, scanning electron microscopy, compatibility study, homogeneity testing, pH evaluation, and drug content determination. The <em>in-vitro</em> anticancer activity was performed using cell lines (B16F10) and <em>in-vivo</em> by chemical carcinogen (7,12-dimethylbenz (a) anthracene) in mice.</p></div><div><h3>Results</h3><p>The BOAgNPs-loaded topical gel was found to be homogeneous (clear orange color) and pH-compatible (pH ≈ 6.66) with the skin. The characterization studies indicated the presence of all functional groups in the formulation. An optimized batch of bixin-nano gel showed about 60% inhibitory effects on B16F10 cell lines (<em>in-vitro</em> activity) when equated with a reference drug, 5-fluorouracil. The <em>in-vivo</em> anticancer study suggested suppression of tumorigenesis and promotion of the healing process with bixin-nano gel application on the skin.</p></div><div><h3>Conclusion</h3><p>The results suggested the promising anticancer property of bixin when formulated in silver nanoparticle gel. The preparation of silver particles nano gel with bixin might provide an effective alternative option for treating skin cancers, provided more research complements the findings of the present study.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 7","pages":"Article 102125"},"PeriodicalIF":4.1,"publicationDate":"2024-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001750/pdfft?md5=9b1badc86ff0ecec6f2ca42fdc1401d2&pid=1-s2.0-S1319016424001750-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141278111","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Recent advances in the development of poly(ester amide)s-based carriers for drug delivery 开发基于聚酯酰胺的药物传输载体的最新进展
IF 4.1 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-06-01 DOI: 10.1016/j.jsps.2024.102123
Rui Xie, Jiang Li, Min Zhao, Fan Wu

Biodegradable and biocompatible biomaterials have several important applications in drug delivery. The biomaterial family known as poly(ester amide)s (PEAs) has garnered considerable interest because it exhibits the benefits of both polyester and polyamide, as well as production from readily available raw ingredients and sophisticated synthesis techniques. Specifically, α-amino acid-based PEAs (AA-PEAs) are promising carriers because of their structural flexibility, biocompatibility, and biodegradability. Herein, we summarize the latest applications of PEAs in drug delivery systems, including antitumor, gene therapy, and protein drugs, and discuss the prospects of drug delivery based on PEAs, which provides a reference for designing safe and efficient drug delivery carriers.

可生物降解且具有生物相容性的生物材料在给药领域有多种重要应用。被称为聚酯酰胺(PEAs)的生物材料家族引起了人们的极大兴趣,因为它同时具有聚酯和聚酰胺的优点,而且可以用现成的原料和复杂的合成技术生产。具体来说,α-氨基酸基 PEAs(AA-PEAs)因其结构灵活、生物相容性和生物降解性而成为前景广阔的载体。在此,我们总结了 PEAs 在药物递送系统中的最新应用,包括抗肿瘤、基因治疗和蛋白质药物,并探讨了基于 PEAs 的药物递送前景,为设计安全高效的药物递送载体提供参考。
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引用次数: 0
Skin anti-aging potential of Launaea procumbens extract: Antioxidant and enzyme inhibition activities supported by ADMET and molecular docking studies Launaea procumbens 提取物的皮肤抗衰老潜力:ADMET 和分子对接研究支持的抗氧化和酶抑制活性
IF 4.1 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-25 DOI: 10.1016/j.jsps.2024.102107
Hanan Khojah , Shaima R. Ahmed , Shahad Y. Alharbi , Kholood K. AlSabeelah , Hatham Y. Alrayyes , Kadi B. Almusayyab , Shahad R. Alrawiliy , Raghad M. Alshammari , Sumera Qasim

Aging is a natural process that occurs in all living organisms. Particularly, the skin embodies aging since it serves as a barrier between the body and its surroundings. Previously, we reported the wound healing effect of Launaea procumbens and identified compounds therein. The study aims to explore the skin anti-aging properties of the plant extract. To that effect, the antioxidant potential of L. procumbens methanolic extract (LPM) was assessed using two complementary DPPH and FRAP assays. The enzyme inhibitory effect of the extract on collagenase, elastase, hyaluronidase, and tyrosinase was evaluated to assess the direct skin anti-aging effects. Similarly, the anti-inflammatory activity was evaluated to explore the indirect anti-aging effects via the assessment of extract inhibitory effects on cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). In addition, ADMET and molecular docking studies were performed to explore the interaction mechanisms of identified compounds in LPM with target enzymes. LPM demonstrated significant antioxidant activity in DPPH (IC50 = 29.08 µg/mL) and FRAP (1214.67 µM FeSO4/g extract) assays. Plant extract showed significant inhibition of collagenase, elastase, hyaluronidase, and tyrosinase (IC50 = 52.68, 43.76, 31.031, and 37.13 µg/mL, respectively). The extract demonstrated significant COX-2 and 5-LOX inhibition capacity with IC50 values of 8.635 and 10.851 µg/mL, respectively. The molecular docking study revealed the high potential of the identified compounds to bind to the active sites of enzymes crucially involved in the skin aging process. ADMET analysis of the compounds revealed their good absorption, distribution, and metabolism profiles, and they were found to be safe as well. Study findings suggest L. procumbens as a promising source for the development of natural skin anti-aging and antioxidant compounds. This, in turn, may facilitate its incorporation into cosmetic formulations after further investigation.

衰老是所有生物都会经历的一个自然过程。尤其是皮肤,因为它是人体与周围环境之间的屏障,所以也体现了衰老。此前,我们曾报道过这种植物的伤口愈合效果,并确定了其中的化合物。本研究旨在探索该植物提取物的皮肤抗衰老特性。为此,我们使用两种互补的 DPPH 和 FRAP 试验评估了甲醇提取物(LPM)的抗氧化潜力。还评估了萃取物对胶原酶、弹性蛋白酶、透明质酸酶和酪氨酸酶的酶抑制作用,以评估其直接的皮肤抗衰老效果。同样,通过评估萃取物对环氧合酶-2(COX-2)和 5-脂氧合酶(5-LOX)的抑制作用,评估了抗炎活性,以探索间接抗衰老效果。此外,还进行了 ADMET 和分子对接研究,以探索 LPM 中已鉴定化合物与目标酶的相互作用机制。在 DPPH(IC = 29.08 µg/mL)和 FRAP(1214.67 µM FeSO4/g提取物)试验中,LPM表现出明显的抗氧化活性。植物提取物对胶原酶、弹性蛋白酶、透明质酸酶和酪氨酸酶有明显的抑制作用(IC 分别为 52.68、43.76、31.031 和 37.13 µg/mL)。该提取物具有明显的 COX-2 和 5-LOX 抑制能力,IC 值分别为 8.635 和 10.851 µg/mL。分子对接研究表明,所鉴定的化合物极有可能与皮肤老化过程中关键酶的活性位点结合。化合物的 ADMET 分析表明,它们具有良好的吸收、分布和代谢特征,而且是安全的。研究结果表明,这是开发天然皮肤抗衰老和抗氧化化合物的一个很有前景的来源。这反过来又有助于在进一步研究后将其纳入化妆品配方中。
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引用次数: 0
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Saudi Pharmaceutical Journal
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