Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis.
Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis.
复制标题
DOI：
10.3390/pharmaceutics14071374
复制
发表时间：
2022-06-29
期刊：
影响因子：
5.4
通讯作者：
Hassan, Amira H.
中科院分区：
文献类型：
--
作者：
Eissa, Essam M.;Elkomy, Mohammed H.;Eid, Hussein M.;Ali, Adel A.;Abourehab, Mohammed A. S.;Alsubaiyel, Amal M.;Naguib, Ibrahim A.;Alsalahat, Izzeddin;Hassan, Amira H.
本研究旨在通过鼻内途径促进格拉司琼（GS）向大脑的递送，以更好地管理化疗诱导的呕吐。以单油酸甘油酯（GMO）、泊洛沙姆407（P 407）和吐温80（T 80）为原料，采用熔融分散-乳化技术制备了载GS的立方体（GS-CBS）。通过粒径、表面电荷和包封率的测定对GS-CBS进行了表征。采用Box-Behnken统计设计对处方进行优化，并对最佳处方（包括浓度为4.9%的GMO、浓度为10%的P 407和浓度为1%的T 80）的形态、释放行为、离体渗透性进行了考察。通过鼻粘膜和物理稳定性。此外，最佳配方被纳入一个热敏凝胶，并进行组织病理学和体内生物分布实验。它表现出持续释放特性、增加的离体渗透性和改善的物理稳定性。此外，立方体原位凝胶用于鼻粘膜时是安全的和生物相容性的。此外，与药物溶液相比，鼻-脑途径提高了生物利用度和脑分布。最后，立方体原位凝胶可能是一个潜在的纳米载体GS通过鼻-脑途径传递到大脑。
This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol monooleate (GMO), Poloxamer 407 (P 407) and Tween 80 (T 80) were used to formulate GS-loaded cubosomes (GS-CBS) utilizing a melt dispersion-emulsification technique. GS-CBS were characterized by testing particle diameter, surface charge and entrapment efficiency. The formulations were optimized using a Box–Behnken statistical design, and the optimum formula (including GMO with a concentration of 4.9%, P 407 with a concentration of 10%, and T 80 with a concentration of 1%) was investigated for morphology, release behavior, ex vivo permeation through the nasal mucosa, and physical stability. Moreover, the optimal formula was incorporated into a thermosensitive gel and subjected to histopathological and in vivo biodistribution experiments. It demonstrated sustained release characteristics, increased ex vivo permeability and improved physical stability. Moreover, the cubosomal in situ gel was safe and biocompatible when applied to the nasal mucosa. Furthermore, compared to a drug solution, the nose-to-brain pathway enhanced bioavailability and brain distribution. Finally, the cubosomal in situ gel may be a potential nanocarrier for GS delivery to the brain through nose-to-brain pathway.
登录
查看更多内容
影响因子：
6
作者：
Abdelmonem, Rehab;el Nabarawi, Mohamed;Attia, Alshaimaa
通讯作者：
Attia, Alshaimaa
DOI：
10.3390/ph15030281
发表时间：
2022-02-24
期刊：
Pharmaceuticals (Basel, Switzerland)
影响因子：
--
作者：
Abo El-Enin HA;Elkomy MH;Naguib IA;Ahmed MF;Alsaidan OA;Alsalahat I;Ghoneim MM;Eid HM
通讯作者：
Eid HM
影响因子：
5.4
作者：
Elkomy MH;Alruwaili NK;Elmowafy M;Shalaby K;Zafar A;Ahmad N;Alsalahat I;Ghoneim MM;Eissa EM;Eid HM
通讯作者：
Eid HM
影响因子：
8
作者：
Elsenosy FM;Abdelbary GA;Elshafeey AH;Elsayed I;Fares AR
通讯作者：
Fares AR
影响因子：
3.4
作者：
Elkomy, Mohammed H.;El Menshawe, Shahira F.;Ali, Ahmed M. A.
通讯作者：
Ali, Ahmed M. A.