Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis

Menna M Abdellatif,1 Islam A Khalil,2 Yara E Elakkad,2 Hesham A Eliwa,3 Tamer M Samir,4 Asmaa K Al-Mokaddem5 1Department of Industrial Pharmacy, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics, College o...

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Main Authors: Abdellatif MM, Khalil IA, Elakkad YE, Eliwa HA, Samir TM, Al-Mokaddem AK
Format: Article
Language:English
Published: Dove Medical Press 2020-06-01
Series:International Journal of Nanomedicine
Subjects:
Online Access:https://www.dovepress.com/formulation-and-characterization-of-sertaconazole-nitrate-mucoadhesive-peer-reviewed-article-IJN
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author Abdellatif MM
Khalil IA
Elakkad YE
Eliwa HA
Samir TM
Al-Mokaddem AK
author_facet Abdellatif MM
Khalil IA
Elakkad YE
Eliwa HA
Samir TM
Al-Mokaddem AK
author_sort Abdellatif MM
collection DOAJ
description Menna M Abdellatif,1 Islam A Khalil,2 Yara E Elakkad,2 Hesham A Eliwa,3 Tamer M Samir,4 Asmaa K Al-Mokaddem5 1Department of Industrial Pharmacy, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 3Department of Pharmacology and Toxicology, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 4Department of Microbiology and Immunology, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 5Department of Pathology, Faculty of Veterinary Medicine, Cairo University, Giza, EgyptCorrespondence: Menna M Abdellatif Tel +201005647945Email dr.menna52@gmail.comPurpose: The aim of this study is to develop efficient localized therapy of sertaconazole nitrate for the treatment of vaginal candidiasis.Methods: Sertaconazole nitrate-loaded cationic liposomes were prepared by thin-film hydration method and coated with different concentrations of pectin (0.05%, 0.1% and 0.2%) to develop mucoadhesive liposomes. The formulated mucoadhesive vesicles were characterized in terms of morphology, entrapment efficiency, particle size, zeta value, mucoadhesive properties and drug release. The selected formula was incorporated into a gel base and further characterized by an ex vivo permeation study in comparison with conventional sertaconazole gel. Also, the in vivo study was performed to assess the efficacy of sertaconazole mucoadhesive liposomal gel in treating rats with vaginal candidiasis.Results: The mucoadhesive liposomes were spherical. Coating liposomes with pectin results in increased entrapment efficiency and particle size compared with uncoated vesicles. On the contrary, zeta values were reduced upon coating liposomes with pectin indicating efficient coating of liposomes with pectin. Mucoadhesive liposomes showed a more prolonged and sustained drug release compared with uncoated liposomes. Ex vivo study results showed that mucoadhesive liposomal gel increased sertaconazole tissue retention and reduced drug tissue penetration. In the invivo study, the mucoadhesive liposomal gel showed a significant reduction in the microbial count with a subsequent reduction in inflammatory responses with the lowest histopathological change compared with conventional gel.Conclusion: The study confirmed the potentiality of employing mucoadhesive liposomes as a successful carrier for the vaginal delivery of antifungal drugs.Keywords: sertaconazole nitrate, vaginal candidiasis, mucoadhesive liposomes
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spelling doaj.art-fa3770a744bf47b2b5491ac9de746e952022-12-21T23:11:10ZengDove Medical PressInternational Journal of Nanomedicine1178-20132020-06-01Volume 154079409054438Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal CandidiasisAbdellatif MMKhalil IAElakkad YEEliwa HASamir TMAl-Mokaddem AKMenna M Abdellatif,1 Islam A Khalil,2 Yara E Elakkad,2 Hesham A Eliwa,3 Tamer M Samir,4 Asmaa K Al-Mokaddem5 1Department of Industrial Pharmacy, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 3Department of Pharmacology and Toxicology, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 4Department of Microbiology and Immunology, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 5Department of Pathology, Faculty of Veterinary Medicine, Cairo University, Giza, EgyptCorrespondence: Menna M Abdellatif Tel +201005647945Email dr.menna52@gmail.comPurpose: The aim of this study is to develop efficient localized therapy of sertaconazole nitrate for the treatment of vaginal candidiasis.Methods: Sertaconazole nitrate-loaded cationic liposomes were prepared by thin-film hydration method and coated with different concentrations of pectin (0.05%, 0.1% and 0.2%) to develop mucoadhesive liposomes. The formulated mucoadhesive vesicles were characterized in terms of morphology, entrapment efficiency, particle size, zeta value, mucoadhesive properties and drug release. The selected formula was incorporated into a gel base and further characterized by an ex vivo permeation study in comparison with conventional sertaconazole gel. Also, the in vivo study was performed to assess the efficacy of sertaconazole mucoadhesive liposomal gel in treating rats with vaginal candidiasis.Results: The mucoadhesive liposomes were spherical. Coating liposomes with pectin results in increased entrapment efficiency and particle size compared with uncoated vesicles. On the contrary, zeta values were reduced upon coating liposomes with pectin indicating efficient coating of liposomes with pectin. Mucoadhesive liposomes showed a more prolonged and sustained drug release compared with uncoated liposomes. Ex vivo study results showed that mucoadhesive liposomal gel increased sertaconazole tissue retention and reduced drug tissue penetration. In the invivo study, the mucoadhesive liposomal gel showed a significant reduction in the microbial count with a subsequent reduction in inflammatory responses with the lowest histopathological change compared with conventional gel.Conclusion: The study confirmed the potentiality of employing mucoadhesive liposomes as a successful carrier for the vaginal delivery of antifungal drugs.Keywords: sertaconazole nitrate, vaginal candidiasis, mucoadhesive liposomeshttps://www.dovepress.com/formulation-and-characterization-of-sertaconazole-nitrate-mucoadhesive-peer-reviewed-article-IJNsertaconazole nitratevaginal candidiasismucoadhesive liposomes.
spellingShingle Abdellatif MM
Khalil IA
Elakkad YE
Eliwa HA
Samir TM
Al-Mokaddem AK
Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
International Journal of Nanomedicine
sertaconazole nitrate
vaginal candidiasis
mucoadhesive liposomes.
title Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
title_full Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
title_fullStr Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
title_full_unstemmed Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
title_short Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
title_sort formulation and characterization of sertaconazole nitrate mucoadhesive liposomes for vaginal candidiasis
topic sertaconazole nitrate
vaginal candidiasis
mucoadhesive liposomes.
url https://www.dovepress.com/formulation-and-characterization-of-sertaconazole-nitrate-mucoadhesive-peer-reviewed-article-IJN
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