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

Amira Yousry Farrah,1 Abdulaziz M Al-mahallawi,2,3 Emad B Basalious,2 Demiana I Nesseem1 1Department of Pharmaceutics, National Organization for Drug Control and Research, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 3Depart...

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Autores principales: Farrah AY, Al-mahallawi AM, Basalious EB, Nesseem DI
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Publicado: Dove Medical Press 2020
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spelling oai:doaj.org-article:3bb888103a824e67aa17a8013c0169b12021-12-02T11:50:49ZInvestigating 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 Studies1178-2013https://doaj.org/article/3bb888103a824e67aa17a8013c0169b12020-11-01T00:00:00Zhttps://www.dovepress.com/investigating-the-potential-of-phosphatidylcholine-based-nano-sized-ca-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Amira Yousry Farrah,1 Abdulaziz M Al-mahallawi,2,3 Emad B Basalious,2 Demiana I Nesseem1 1Department of Pharmaceutics, National Organization for Drug Control and Research, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, EgyptCorrespondence: Emad B BasaliousDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptTel +2 01202000454Email emad.basalious@pharma.cu.edu.egPurpose: 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 membraneFarrah AYAl-mahallawi AMBasalious EBNesseem DIDove Medical Pressarticlecaroverinenanovesiclesliquid crystalspermeationtympanic membrane.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 8921-8931 (2020)
institution DOAJ
collection DOAJ
language EN
topic caroverine
nanovesicles
liquid crystals
permeation
tympanic membrane.
Medicine (General)
R5-920
spellingShingle caroverine
nanovesicles
liquid crystals
permeation
tympanic membrane.
Medicine (General)
R5-920
Farrah AY
Al-mahallawi AM
Basalious EB
Nesseem DI
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
description Amira Yousry Farrah,1 Abdulaziz M Al-mahallawi,2,3 Emad B Basalious,2 Demiana I Nesseem1 1Department of Pharmaceutics, National Organization for Drug Control and Research, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, EgyptCorrespondence: Emad B BasaliousDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptTel +2 01202000454Email emad.basalious@pharma.cu.edu.egPurpose: 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
format article
author Farrah AY
Al-mahallawi AM
Basalious EB
Nesseem DI
author_facet Farrah AY
Al-mahallawi AM
Basalious EB
Nesseem DI
author_sort Farrah AY
title 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
title_short 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
title_full 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
title_fullStr 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
title_full_unstemmed 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
title_sort 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
publisher Dove Medical Press
publishDate 2020
url https://doaj.org/article/3bb888103a824e67aa17a8013c0169b1
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