Belenichev Igor, Aliyeva Olena, Burlaka Bogdan, Burlaka Kristina, Kuchkovskyi Oleh, Savchenko Dmytro, Oksenych Valentyn, Kamyshnyi Oleksandr
Department of Pharmacology and Medical Formulation with Course of Normal Physiology, Zaporizhzhia State Medical and Pharmaceutical University, 69000 Zaporizhzhia, Ukraine.
Department of Histology, Cytology and Embryology, Zaporizhzhia State Medical and Pharmaceutical University, 69000 Zaporizhzhia, Ukraine.
Pharmaceuticals (Basel). 2024 Jul 26;17(8):990. doi: 10.3390/ph17080990.
The intranasal route of drug administration is characterized by high bioavailability and is considered promising for rapid delivery of drugs with systemic action to the central nervous system (CNS), bypassing the blood-brain barrier. This is particularly important for the use of neuroprotective drugs in the treatment of brain tissue damage in infants caused by the effects of intrauterine hypoxia. The creation of new dosage forms for neonatology using mathematical technologies and special software in pharmaceutical development allows for the creation of cerebroprotective drugs with controlled pharmaco-technological properties, thus reducing time and resources for necessary research. We developed a new nasal gel formulation with Angiolin using a Box-Behnken experiment design for the therapy of prenatal CNS damage. It was found that the consistency characteristics of the nasal gel were significantly influenced by the gelling agent and mucoadhesive component-sodium salt of carboxymethylcellulose. We optimized the composition of nasal gel formulation with Angiolin using the formed models and relationships between the factors. The optimized nasal gel composition demonstrated satisfactory thixotropic properties. The 1% gel for neuroprotection with Angiolin, developed for intranasal administration, meets all safety requirements for this group of drug forms, showing low toxicity and no local irritant or allergic effects.
鼻腔给药途径具有生物利用度高的特点,被认为有望将具有全身作用的药物快速递送至中枢神经系统(CNS),绕过血脑屏障。这对于使用神经保护药物治疗因宫内缺氧影响导致的婴儿脑组织损伤尤为重要。在药物研发中利用数学技术和特殊软件为新生儿学创建新剂型,能够制备出具有可控药物技术特性的脑保护药物,从而减少必要研究的时间和资源。我们采用Box-Behnken实验设计开发了一种含血管生成素的新型鼻腔凝胶制剂,用于治疗产前中枢神经系统损伤。研究发现,凝胶剂和黏膜黏附成分羧甲基纤维素钠盐对鼻腔凝胶的稠度特性有显著影响。我们利用所建立的模型以及各因素之间的关系,对含血管生成素的鼻腔凝胶制剂组成进行了优化。优化后的鼻腔凝胶组合物表现出令人满意的触变性。为鼻腔给药开发的含1%血管生成素的神经保护凝胶,符合该类药物剂型的所有安全要求,毒性低,无局部刺激或过敏作用。