兔内耳模型腹腔内注射乳剂样分散体共递送肉桂碱和莫里苷水合物-脂质E80复合物。

IF 2.2 Q2 PHARMACOLOGY & PHARMACY

Therapeutic delivery Pub Date : 2025-06-11 DOI:10.1080/20415990.2025.2516411

Abhinab Goswami, Srikanth Ponneganti, Vijayakumar Gangipangi, Hariprasad Vavilala, Pullapanthula Radhakrishnanand, Sudhagar Selvaraju, Srinivasa Rao Mutheneni, Shreekant Bharti, Tamilvanan Shunmugaperumal

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引用次数: 0

摘要

背景：药物经圆窗膜进入淋巴管周围是内耳疾病治疗的重要手段。在健康家兔内耳模型中，鼓腔内注射乳状分散体可增加肉桂碱（CNZ）和水合莫里素(MH)-脂质E80复合物在淋巴周围的渗透。方法：采用Box-Behnken设计（BBD）和人工神经网络（ANN）连接Levenberg - Marquardt （LM）算法对注射配方进行优化。注射后30-120分钟，立即监测淋巴周围和血浆中CNZ和MH的浓度水平。结果：与BBD相比，ANN-linked LM算法对所有响应的预测误差和均方误差更小，相关系数值更高。其平均粒径为156.8±8.5 nm， zeta电位为42.70±4.20 mV，在pH为7.4的人工淋巴周围溶液中，10-20分钟内CNZ和MH释放量为>98%，MTT检测细胞存活率为>97.26%，组织病理学接近正常。注射后60分钟，淋巴周围的CNZ为63.07±23.62µg/ml， MH为82.51±8.33µg/ml。结论：该制剂可用于治疗内耳疾病，可用于两种药物的淋巴旁联合给药。

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Intratympanic injection of emulsion-like dispersions to co-deliver cinnarizine and morin hydrate-lipoid E80 complex in a rabbit inner ear model.

Background: Drug delivery to perilymph after crossing the round window membrane is paramount important for inner ear disease management. Intratympanic (IT) injection of emulsion-like dispersions augments cinnarizine (CNZ) and morin hydrate (MH)-Lipoid E80 complex permeation into perilymph in a healthy rabbit inner ear model.

Methods: A Box-Behnken design (BBD) followed by artificial neural network (ANN)-linked Levenberg - Marquardt (LM) algorithm was used for optimizing the injection formula. Immediately after 30-120 minutes post-IT injections, the concentration levels of CNZ and MH in both perilymph and plasma were monitored.

Results: The ANN-linked LM algorithm displayed lower prediction and mean squared errors as well as higher correlation coefficient values for all responses when compared to the corresponding values shown by BBD. The IT injections possessed 156.8 ± 8.5 nm mean particle size, 42.70 ± 4.20 mV zeta potential, >98% CNZ and MH release within 10-20 minutes dissolution in pH 7.4 artificial perilymph solution, >97.26% cell viability in MTT assay and near normal histopathology. The 63.07 ± 23.62 µg/ml CNZ and 82.51 ± 8.33 µg/ml MH were attained in perilymph at 60 minutes post-IT injections.

Conclusion: The IT-injected formulation can be used to co-deliver two drugs in perilymph for managing inner ear diseases.

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.