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Investigating the Potential of Phosphatidylcholine-Based Nano-Sized Carriers in Boosting the Oto-Topical Delivery of Caroverine: in vitro Characterization, Stability Assessment and ex vivo Transport Studies
International Journal of Nanomedicine ( IF 8 ) Pub Date : 2020-11-13 , DOI: 10.2147/ijn.s259172 Amira Yousry Farrah 1 , Abdulaziz M Al-Mahallawi 2, 3 , Emad B Basalious 2 , Demiana I Nesseem 1
International Journal of Nanomedicine ( IF 8 ) Pub Date : 2020-11-13 , DOI: 10.2147/ijn.s259172 Amira Yousry Farrah 1 , Abdulaziz M Al-Mahallawi 2, 3 , Emad B Basalious 2 , Demiana I Nesseem 1
Affiliation
Purpose: Drug delivery into the inner ear across the intact tympanic membrane (TM) has been a challenge in the treatment of inner ear disorders. In this study, nano-sized carriers were formulated for improving the non- invasive oto-topical delivery of caroverine for the treatment of tinnitus.
Methods: Caroverine was loaded into two types of phospholipid-containing systems, namely, nano elastic vesicles (EVs) and phosphatidylcholine-based liquid crystalline nano-particles (PC-LCNPs). The prepared formulations were characterized for their drug loading, particle size, polydispersity index, zeta potential, morphological features by transmission electron microscopy (TEM), and physicochemical stability. In addition, comparative ex vivo transport study was carried out using rabbits’ TM for both types of formulations.
Results: The findings show a significant superiority of PC-LCNPs over the EVs formulations in the drug payload (1% and 0.25%, respectively), physical stability and the efficiency of permeation across rabbits’ TM. The results showed a more than twofold increase in the cumulative drug flux values of PC-LCNPs (699.58 ± 100 μg/cm2) compared to the EVs (250 ± 45 μg/cm2) across the TM.
Conclusion: The current study revealed the smart physicochemical properties of PC-LCNPs demonstrating the potential of this carrier as a new attractive candidate for improving the non-invasive oto-topical delivery of caroverine.
Keywords: caroverine, nanovesicles, liquid crystals, permeation, tympanic membrane
中文翻译：
研究基于磷脂酰胆碱的纳米载体在促进 Caroverine 耳外给药方面的潜力：体外表征、稳定性评估和离体转运研究
目的：药物通过完整的鼓膜 (TM) 进入内耳一直是治疗内耳疾病的挑战。在这项研究中，配制了纳米尺寸的载体，用于改善卡洛维林治疗耳鸣的无创耳局部给药。
方法：Caroverine 被加载到两种类型的含磷脂系统中，即纳米弹性囊泡 (EVs) 和基于磷脂酰胆碱的液晶纳米颗粒 (PC-LCNPs)。对制备的制剂的载药量、粒径、多分散性指数、zeta 电位、透射电子显微镜 (TEM) 的形态特征和物理化学稳定性进行了表征。此外，使用 rabbits'TM 对两种类型的制剂进行了比较的离体转运研究。
结果：研究结果表明，PC-LCNPs 在药物有效载荷（分别为 1% 和 0.25%）、物理稳定性和通过兔 TM 的渗透效率方面优于 EVs 制剂。结果显示，与 TM 上的 EV（250 ± 45 μg/cm 2）相比，PC-LCNPs 的累积药物通量值（699.58 ± 100 μg/cm 2 ）增加了两倍多。结论：目前的研究揭示了 PC-LCNPs 的智能物理化学特性，证明了这种载体作为改善 caroverine 无创耳局部给药的新的有吸引力的候选者的潜力。关键词： caroverine，纳米囊泡，液晶，渗透，鼓膜
更新日期：2020-11-13
Methods: Caroverine was loaded into two types of phospholipid-containing systems, namely, nano elastic vesicles (EVs) and phosphatidylcholine-based liquid crystalline nano-particles (PC-LCNPs). The prepared formulations were characterized for their drug loading, particle size, polydispersity index, zeta potential, morphological features by transmission electron microscopy (TEM), and physicochemical stability. In addition, comparative ex vivo transport study was carried out using rabbits’ TM for both types of formulations.
Results: The findings show a significant superiority of PC-LCNPs over the EVs formulations in the drug payload (1% and 0.25%, respectively), physical stability and the efficiency of permeation across rabbits’ TM. The results showed a more than twofold increase in the cumulative drug flux values of PC-LCNPs (699.58 ± 100 μg/cm2) compared to the EVs (250 ± 45 μg/cm2) across the TM.
Conclusion: The current study revealed the smart physicochemical properties of PC-LCNPs demonstrating the potential of this carrier as a new attractive candidate for improving the non-invasive oto-topical delivery of caroverine.
Keywords: caroverine, nanovesicles, liquid crystals, permeation, tympanic membrane
中文翻译：
研究基于磷脂酰胆碱的纳米载体在促进 Caroverine 耳外给药方面的潜力：体外表征、稳定性评估和离体转运研究
目的：药物通过完整的鼓膜 (TM) 进入内耳一直是治疗内耳疾病的挑战。在这项研究中，配制了纳米尺寸的载体，用于改善卡洛维林治疗耳鸣的无创耳局部给药。
方法：Caroverine 被加载到两种类型的含磷脂系统中，即纳米弹性囊泡 (EVs) 和基于磷脂酰胆碱的液晶纳米颗粒 (PC-LCNPs)。对制备的制剂的载药量、粒径、多分散性指数、zeta 电位、透射电子显微镜 (TEM) 的形态特征和物理化学稳定性进行了表征。此外，使用 rabbits'TM 对两种类型的制剂进行了比较的离体转运研究。
结果：研究结果表明，PC-LCNPs 在药物有效载荷（分别为 1% 和 0.25%）、物理稳定性和通过兔 TM 的渗透效率方面优于 EVs 制剂。结果显示，与 TM 上的 EV（250 ± 45 μg/cm 2）相比，PC-LCNPs 的累积药物通量值（699.58 ± 100 μg/cm 2 ）增加了两倍多。结论：目前的研究揭示了 PC-LCNPs 的智能物理化学特性，证明了这种载体作为改善 caroverine 无创耳局部给药的新的有吸引力的候选者的潜力。关键词： caroverine，纳米囊泡，液晶，渗透，鼓膜
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