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Propranolol HCL-loaded liposomes for intranasal delivery: in vitro and ex vivo evaluation of optimized formulation using design of experiments. 经鼻给药的盐酸普萘洛尔脂质体:利用实验设计对优化配方进行体外和离体评价。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-11-01 Epub Date: 2023-11-28 DOI: 10.4155/tde-2023-0044
Vishal Kumar, Nethish Kumaar R, D Aswin, Sreeja C Nair

Aim: To develop a propranolol HCL-loaded liposomal nasal formulation for migraine prophylaxis. Materials & methods: Formulated the liposomes through thin layer hydration method and optimized via design of experiments (DOE). The prepared liposomes were characterized for particle size, zeta potential, PDI, drug entrapment and drug loading. Assessed for in vitro release kinetics, ex vivo permeability, histopathology and stability. Results: Optimized liposomes: 135.52 ± 5.87 nm, -19.9 ± 0.075 mV, 95.41 ± 0.05% entrapment, 43.37 ± 0.02% loading. Showed immediate (30.07 ± 2.09%) and sustained release (95.69 ± 4.58%) over 10 h. Enhanced permeation compared with controls; well-tolerated histopathologically. Conclusion: Liposomal formulation offers promise for intranasal propranolol HCL delivery in migraine prophylaxis, with stability under refrigeration.

目的:研制一种盐酸普萘洛尔鼻用脂质体预防偏头痛的制剂。材料与方法:采用薄层水合法制备脂质体,并通过实验设计(DOE)进行优化。对所制备的脂质体进行了粒径、zeta电位、PDI、药物包载和载药量的表征。评估体外释放动力学,体外渗透性,组织病理学和稳定性。结果:优化脂质体:135.52±5.87 nm, -19.9±0.075 mV,包封95.41±0.05%,载药量43.37±0.02%。10 h内即刻释放(30.07±2.09%),缓释(95.69±4.58%);良好的组织病理学。结论:脂质体制剂为盐酸心得安鼻内给药预防偏头痛提供了希望,在冷藏条件下具有稳定性。
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引用次数: 0
In situ gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation. 用于持续释放的硫酸阿扎那韦原位胃漂浮凝胶:配方、优化和评估。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-01 Epub Date: 2023-12-06 DOI: 10.4155/tde-2023-0037
Rajashree Masareddy, Pradnya Sandure, Archana Patil, Yadishma Gaude, Arpana Patil

Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The in situ floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion: In situ floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.

目的:硫酸阿扎那韦属 BCS II 类药物,由于其快速的首过代谢和 P-gp 外流,其口服生物利用度有限。材料与方法:采用离子凝胶法制备了使用复方药物的原位浮动凝胶,并按照 32 全因子设计优化了配方。结果:胶凝聚合物的浓度会影响药物释放和浮滞时间,反之亦然。结论硫酸阿扎那韦原位浮动凝胶由于增加了胃停留时间而有望持续释放药物,从而提高了潜在治疗效果。
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引用次数: 0
Formulation, optimization and evaluation of amisulpride-loaded niosomal intranasal gel for brain targeting. 用于脑部靶向治疗的氨磺必利鼻腔内凝胶的配制、优化和评估。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-01 Epub Date: 2023-12-05 DOI: 10.4155/tde-2023-0059
Vinayak S Patil, Kishori P Sutar, Rachana D Pockle, Siddarth Usulkar, Vishwanath A Jadhav

Aim: To develop stable non-ionic surfactant vesicles containing amisulpride (AMS) to improve brain uptake via nose to brain mechanism. Methods: Niosomes were developed using a modified ethanol injection technique, optimized using 32 factorial design and evaluated for the vesicle size (VS), percent encapsulation efficiency (EE), zeta potential (ZP) and % cumulative drug release (%CDR). Results: Optimized niosomes (Span-60: cholesterol ratio 0:1) showed 191.4 nm VS, 84.25% EE, -38.2 ZP and 81.31% CDR. In situ gel with these niosomes displayed 78% CDR. TEM analysis revealed spherical niosomes. Pharmacokinetic and brain tissue distribution studies in rats showed enhanced plasma and brain concentrations, indicating successful brain targeting. Conclusion: This strategy demonstrates improved AMS permeation via the nasal cavity, enhancing bioavailability for treating schizophrenia.

目的:开发含有阿米舒必利(AMS)的稳定非离子表面活性剂囊泡,以改善通过鼻脑机制的脑摄取。方法采用改良的乙醇注射技术开发了 Niosomes,使用 32 因子设计进行了优化,并对囊泡大小 (VS)、封装效率 (EE)、Zeta 电位 (ZP) 和累积药物释放率 (%CDR) 进行了评估。结果优化后的 niosomes(Span-60:胆固醇比率为 0:1)显示出 191.4 nm 的 VS、84.25% 的 EE、-38.2 ZP 和 81.31% 的 CDR。使用这些 niosomes 的原位凝胶显示出 78% 的 CDR。TEM 分析表明,该药物呈球形。对大鼠进行的药代动力学和脑组织分布研究显示,血浆和脑浓度均有所提高,表明成功实现了脑靶向。结论:这种策略改善了 AMS 经鼻腔的渗透,提高了治疗精神分裂症的生物利用度。
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引用次数: 0
Role of inorganic ions in wound healing: an insight into the various approaches for localized delivery. 无机离子在伤口愈合中的作用:对局部递送的各种方法的洞察。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-01 Epub Date: 2023-11-28 DOI: 10.4155/tde-2023-0036
M C Linju, M R Rekha

Recently, the role of inorganic ions has been explored for its wound-healing applications. Ions do play key role in the normal functioning of the skin, including the epidermal barrier property, maintaining redox balance, enzymatic activities, tissue remodeling, etc. The care of chronic wounds is a concern and new cost-effective therapeutic strategies that modulate the wound microenvironment and cell behaviour are needed. First, this review illustrates the ions that play a role in wound healing and their molecular mechanisms that are accountable for modifying the wound. Further, the emerging strategies using metal ions to modulate the healing will be discussed. In this direction, localized delivery of inorganic ions of importance using advanced wound care biomaterials for wound healing applications is discussed.

近年来,无机离子在伤口愈合中的应用得到了广泛的研究。离子确实在皮肤的正常功能中起着关键作用,包括表皮屏障特性、维持氧化还原平衡、酶活性、组织重塑等。慢性伤口的护理是一个值得关注的问题,需要新的具有成本效益的治疗策略来调节伤口微环境和细胞行为。首先,本文综述了在伤口愈合中起作用的离子及其修饰伤口的分子机制。此外,还将讨论利用金属离子调节愈合的新策略。在这个方向上,无机离子的重要局部递送使用先进的伤口护理生物材料的伤口愈合应用进行了讨论。
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引用次数: 0
The potential of DNA nanotechnology to advance multiple therapeutic systems. DNA纳米技术推进多种治疗系统的潜力。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-01 Epub Date: 2023-11-28 DOI: 10.4155/tde-2023-0060
Igor L Medintz, Divita Mathur
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引用次数: 0
Influence of poly-L-ornithine-bile acid nano hydrogels on cellular bioactivity and potential pharmacological applications. 聚l -鸟氨酸胆汁酸纳米水凝胶对细胞生物活性的影响及其潜在的药理应用。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-05 DOI: 10.4155/tde-2023-0034
Bozica Kovacevic, Melissa Jones, Susbin Raj Wagle, Corina Mihaela Ionescu, Thomas Foster, Maja Đanić, Momir Mikov, Armin Mooranian, Hani Al-Salami

Aim: Cellular bioactivity and pathophysiological changes associated with chronic disorders are considered pivotal detrimental factors when developing novel formulations for biomedical applications. Methods: This paper investigates the use of bile acids and synthetic polypeptide poly-L-ornithine (PLO) in formulations and their impacts on a variety of cell lines, with a particular focus on their cellular bioactivity. Results: The hepatic cell line was the most negatively affected by the presence of PLO, while the muscle and beta-pancreatic cell lines did not show as profound of a negative impact of PLO on cellular viability. PLO was the least disruptive regarding mitochondrial function for muscle and beta cells. Conclusion: The addition of bile acids generally decreased mitochondrial respiration and altered bioenergetic parameters in all cell lines.

目的:细胞生物活性和与慢性疾病相关的病理生理变化被认为是开发用于生物医学应用的新配方时关键的有害因素。方法:本文研究了胆汁酸和合成多肽聚l -鸟氨酸(PLO)在制剂中的使用及其对多种细胞系的影响,特别关注了它们的细胞生物活性。结果:肝细胞系受PLO的负面影响最大,而肌肉和β -胰腺细胞系对PLO的细胞活力没有明显的负面影响。PLO对肌肉细胞和β细胞的线粒体功能破坏最小。结论:胆汁酸的添加普遍降低了线粒体呼吸,改变了所有细胞系的生物能量参数。
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引用次数: 0
Emerging nanotechnology backed formulations for the management of atopic dermatitis. 新兴的纳米技术支持治疗特应性皮炎的配方。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-09-06 DOI: 10.4155/tde-2023-0033
Ranjit Kumar Mahato, Mohini Singh, Hemanta Pathak, Niva Rani Gogoi, Rikynjai Kharbithai, Pinky Chowrasia, Pankaj Lochan Bora, Tumpa Sarkar, Bani Kumar Jana, Bhaskar Mazumder

Atopic dermatitis is a prevalent chronic skin inflammation affecting 2.1 to 4.1% of adults globally. The complexity of its pathogenesis and the relapsing nature make it challenging to treat. Current treatments follow European Academy of Dermatology and Venerology guidelines, but advanced cases with recurring lesions lack effective therapies. To address this gap, researchers are exploring nanotechnology for targeted drug delivery. Nanoparticles offer benefits such as improved drug retention, stability, controlled release and targeted delivery through the disrupted epidermal barrier. This integrated review evaluates the current state of AD treatment and highlights the potential of novel nano-formulations as a promising approach to address the disease.

特应性皮炎是一种常见的慢性皮肤炎症,影响全球2.1%至4.1%的成年人。其发病机制的复杂性和复发性使其治疗具有挑战性。目前的治疗方法遵循欧洲皮肤病学会和性病学指南,但复发性病变的晚期病例缺乏有效的治疗方法。为了解决这一差距,研究人员正在探索用于靶向药物递送的纳米技术。纳米颗粒具有改善药物保留、稳定性、控制释放和通过破坏的表皮屏障靶向递送等优点。这篇综合综述评估了AD治疗的现状,并强调了新型纳米制剂作为治疗该疾病的一种有前途的方法的潜力。
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引用次数: 0
Internal stimuli-responsive nanocarriers for controlled anti-cancer drug release: a review. 内刺激反应型纳米载体抗癌药物控释研究进展。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-10-25 DOI: 10.4155/tde-2023-0041
Baji Baba Shaik, Naresh Kumar Katari, Sreekanth B Jonnalagadda

Cancer disease is one of the most frequent life-threatening, with a high fatality rate worldwide. However, recent immunotherapy studies in various tumours have yielded unsatisfactory outcomes, with just a few individuals experiencing long-term responses. To overcome these issues, nowadays internal stimuli-responsive nanocarriers have been widely exploited to transport a wide range of active substances, including peptides, genes and medicines. These nanosystems could be chemically adjusted to produce target-based drug release at the target location, minimizing pathological and physiological difficulties while increasing therapeutic efficiency. This review highlights the various types of internal stimuli-responsive nanocarriers and applications in cancer diagnosis. This study can provide inspiration and impetus for exploiting more promising internal stimuli-responsive nanosystems for drug delivery.

癌症是最常见的危及生命的疾病之一,在全球范围内死亡率很高。然而,最近对各种肿瘤的免疫疗法研究结果并不令人满意,只有少数人出现了长期反应。为了克服这些问题,如今,内部刺激响应性纳米载体已被广泛用于运输广泛的活性物质,包括肽、基因和药物。这些纳米系统可以进行化学调整,在目标位置产生基于靶点的药物释放,最大限度地减少病理和生理困难,同时提高治疗效率。本文着重介绍了各种类型的内刺激响应纳米载体及其在癌症诊断中的应用。这项研究可以为开发更有前景的内部刺激响应纳米系统用于药物递送提供灵感和动力。
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引用次数: 0
Intranasal nanoparticulate delivery systems for neurodegenerative disorders: a review. 神经退行性疾病的鼻内纳米颗粒递送系统:综述。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-09-11 DOI: 10.4155/tde-2023-0019
Someshbabu Ramesh Babu, Harshith Hosahalli Shekara, Ashish Kumar Sahoo, Pyda Venkata Harsha Vardhan, Nitheesh Thiruppathi, Madhugiri Prakash Venkatesh

Neurodegenerative diseases are a significant cause of mortality worldwide, and the blood-brain barrier (BBB) poses a significant challenge for drug delivery. An intranasal route is a prominent approach among the various methods to bypass the BBB. There are different pathways involved in intranasal drug delivery. The drawbacks of this method include mucociliary clearance, enzymatic degradation and poor drug permeation. Novel nanoformulations and intranasal drug-delivery devices offer promising solutions to overcome these challenges. Nanoformulations include polymeric nanoparticles, lipid-based nanoparticles, microspheres, liposomes and noisomes. Additionally, intranasal devices could be utilized to enhance drug-delivery efficacy. Therefore, intranasal drug-delivery systems show potential for treating neurodegenerative diseases through trigeminal or olfactory pathways, which can significantly improve patient outcomes.

神经退行性疾病是全球死亡的重要原因,血脑屏障(BBB)对药物递送构成了重大挑战。在各种绕过血脑屏障的方法中,鼻内途径是一种突出的方法。鼻内给药有不同的途径。这种方法的缺点包括粘膜纤毛清除、酶降解和药物渗透性差。新型纳米制剂和鼻内给药装置为克服这些挑战提供了有前景的解决方案。纳米制剂包括聚合物纳米颗粒、脂质基纳米颗粒、微球、脂质体和黑色体。此外,鼻内装置可用于增强药物递送功效。因此,鼻内给药系统显示出通过三叉神经或嗅觉通路治疗神经退行性疾病的潜力,这可以显著改善患者的预后。
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引用次数: 0
Industry update: the latest developments in the field of therapeutic delivery, July 2023. 行业更新:治疗递送领域的最新进展,2023年7月。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-10-03 DOI: 10.4155/tde-2023-0085
Peter Timmins
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引用次数: 0
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Therapeutic delivery
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