Flexible nano-sized lipid vesicles for the transdermal delivery of colchicine; in vitro/in vivo investigation

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorEl-Feky G.S.
dc.contributor.authorEl-Naa M.M.
dc.contributor.authorMahmoud A.A.
dc.contributor.otherDepartment of Pharmaceutical Technology
dc.contributor.otherPharmaceutical and Drug Industries Research Division
dc.contributor.otherNational Research Center
dc.contributor.otherDokki
dc.contributor.otherCairo
dc.contributor.otherEgypt; October University for Modern Sciences and Arts
dc.contributor.otherEgypt; Department of Pharmacology and Toxicology
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherFayoum University
dc.contributor.otherEgypt; Department of Pharmaceutics and Pharmaceutical Technology
dc.contributor.otherFaculty of Pharmaceutical Sciences and Pharmaceutical Industries
dc.contributor.otherFuture University
dc.contributor.otherCairo
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:40:41Z
dc.date.available2020-01-09T20:40:41Z
dc.date.issued2019
dc.descriptionScopus
dc.description.abstractColchicine (CL) is the most effective treatment of acute gout, however, it is associated with side effects in 80% of the patients at therapeutic doses, in addition, it's a water-soluble strong base (pKa ?12.8) which ionizes at physiological gastrointestinal pH resulting in low oral bioavailability of 44%. This work employed enhancing the bioavailability and reducing the side effects of CL through combining the benefits of the transdermal route together with those of elastic lipid nano-vesicles. Transfersomes (TRs) have been studied as vehicles for transdermal drug delivery, however, poor encapsulation of drugs and drug leaking of the vesicles required complexation of CL with ?-cyclodextrin (?-CD) before formulation. The composition of the designed CL-?-CD-TR was studied to balance the flexibility of the vesicles to their entrapment ability. CL-?-CD-TR were characterized for their shape, size, entrapment efficiency, elasticity, release profile, ex vivo skin permeation, pharmacological efficacy, and histopathological effect. Encapsulation efficiency of CL-?-CD complex in the vesicular formulations ranged from 42.3% to 93.8%. Particle size ranged from 70.6 nm to 138.5 nm and zeta potential ranged from 16.1 mV to 23.4 mV. The in vitro release of CL from the selected CL-?-CD-TR formulation (F3) showed a controlled, biphasic profile. Ex vivo study reported the great potential of F3 (CL-?-CD-TR) for skin permeation. In vivo experiment demonstrated that F3 (CL-?-CD-TR) possessed high biological efficacy with reduced skin irritation. � 2018 Elsevier B.V.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=22204&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1016/j.jddst.2018.10.036
dc.identifier.doiPubMed ID :
dc.identifier.issn17732247
dc.identifier.otherhttps://doi.org/10.1016/j.jddst.2018.10.036
dc.identifier.otherPubMed ID :
dc.identifier.urihttps://t.ly/YZR0Y
dc.language.isoEnglishen_US
dc.publisherEditions de Santeen_US
dc.relation.ispartofseriesJournal of Drug Delivery Science and Technology
dc.relation.ispartofseries49
dc.subjectOctober University for Modern Sciences and Arts
dc.subjectUniversity for Modern Sciences and Arts
dc.subjectMSA University
dc.subjectجامعة أكتوبر للعلوم الحديثة والآداب
dc.subjectColchicineen_US
dc.subjectIn vivo studyen_US
dc.subjectLipid vesiclesen_US
dc.subjectTransdermalen_US
dc.subject?-cyclodextrinen_US
dc.subjectbeta cyclodextrinen_US
dc.subjectcolchicineen_US
dc.subjectdrug carrieren_US
dc.subjecttransfersomeen_US
dc.subjectunclassified drugen_US
dc.subjectanimal experimenten_US
dc.subjectanimal modelen_US
dc.subjectArticleen_US
dc.subjectcontrolled studyen_US
dc.subjectdrug bioavailabilityen_US
dc.subjectdrug delivery systemen_US
dc.subjectdrug efficacyen_US
dc.subjectdrug formulationen_US
dc.subjectdrug penetrationen_US
dc.subjectdrug releaseen_US
dc.subjectdrug solubilityen_US
dc.subjectelasticityen_US
dc.subjectex vivo studyen_US
dc.subjecthistopathologyen_US
dc.subjectin vitro studyen_US
dc.subjectlipid vesicleen_US
dc.subjectmaleen_US
dc.subjectnanoencapsulationen_US
dc.subjectnonhumanen_US
dc.subjectparticle sizeen_US
dc.subjectraten_US
dc.subjectskin permeabilityen_US
dc.subjectzeta potentialen_US
dc.titleFlexible nano-sized lipid vesicles for the transdermal delivery of colchicine; in vitro/in vivo investigationen_US
dc.typeArticleen_US
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