Nanoemulgel using a bicephalous heterolipid as a novel approach to enhance transdermal permeation of tenofovir.
Identifieur interne : 000503 ( Main/Exploration ); précédent : 000502; suivant : 000504Nanoemulgel using a bicephalous heterolipid as a novel approach to enhance transdermal permeation of tenofovir.
Auteurs : Sanjeev Rambharose [Afrique du Sud] ; Rahul S. Kalhapure [Afrique du Sud] ; Thirumala Govender [Afrique du Sud]Source :
- Colloids and surfaces. B, Biointerfaces [ 1873-4367 ] ; 2017.
Abstract
Improvements in permeation enhancement strategies, such as nanoemulsions (NEs) and nanoemulgels (NEGs), have led to a renewed interest in transdermal drug delivery (TDD). This study aimed to investigate the potential of LLA1E, a novel dendritic permeation enhancer, as an oily phase in the development of a NEG for the TDD of tenofovir (TNF). TNF loaded NEs (TNEs) were prepared and analysed for mean globule diameter (MGD), polydispersity index (PDI), zeta potential (ZP) and morphology. NEGs of the TNEs (TNEGs) were prepared and evaluated for ex vivo transdermal permeation efficacy. The skin integrity before and after the experiments was assessed using histology and transepithelial electrical resistance (TEER). TNEs had a MGD of 129.06±3.35nm, a PDI of 0.192±0.038 and a ZP of 20.9±2.02mV, with an incorporation efficiency of 91.94±0.84%. There was no significant change is these properties after incorporating the TNEs into the hydrogel, as MGD, PDI and ZP of TNEGs were found to be 136.13±5.21nm, 0.182±0.020 and -20.9±2.08mV respectively. Ex vivo permeation studies showed that the TNEG significantly enhanced the TNF permeation by 39.65-fold, with a cumulative amount of 1866.54±108.62μgcm(-2). Histological and TEER assessments showed no permanent effects on the skin by TNEG, indicating that this novel TNEG nanosystem has the potential to translate into clinical trials as treatment alternatives for HIV/AIDs patients.
DOI: 10.1016/j.colsurfb.2017.03.040
PubMed: 28343120
Affiliations:
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Kalhapure</name><affiliation wicri:level="1"><nlm:affiliation>Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa. Electronic address: kalhapure@ukzn.ac.za.</nlm:affiliation><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000</wicri:regionArea><wicri:noRegion>Durban 4000</wicri:noRegion></affiliation></author><author><name sortKey="Govender, Thirumala" sort="Govender, Thirumala" uniqKey="Govender T" first="Thirumala" last="Govender">Thirumala Govender</name><affiliation wicri:level="1"><nlm:affiliation>Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa. Electronic address: govenderth@ukzn.ac.za.</nlm:affiliation><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000</wicri:regionArea><wicri:noRegion>Durban 4000</wicri:noRegion></affiliation></author></analytic><series><title level="j">Colloids and surfaces. B, Biointerfaces</title><idno type="eISSN">1873-4367</idno><imprint><date when="2017" type="published">2017</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Improvements in permeation enhancement strategies, such as nanoemulsions (NEs) and nanoemulgels (NEGs), have led to a renewed interest in transdermal drug delivery (TDD). This study aimed to investigate the potential of LLA1E, a novel dendritic permeation enhancer, as an oily phase in the development of a NEG for the TDD of tenofovir (TNF). TNF loaded NEs (TNEs) were prepared and analysed for mean globule diameter (MGD), polydispersity index (PDI), zeta potential (ZP) and morphology. NEGs of the TNEs (TNEGs) were prepared and evaluated for ex vivo transdermal permeation efficacy. The skin integrity before and after the experiments was assessed using histology and transepithelial electrical resistance (TEER). TNEs had a MGD of 129.06±3.35nm, a PDI of 0.192±0.038 and a ZP of 20.9±2.02mV, with an incorporation efficiency of 91.94±0.84%. There was no significant change is these properties after incorporating the TNEs into the hydrogel, as MGD, PDI and ZP of TNEGs were found to be 136.13±5.21nm, 0.182±0.020 and -20.9±2.08mV respectively. Ex vivo permeation studies showed that the TNEG significantly enhanced the TNF permeation by 39.65-fold, with a cumulative amount of 1866.54±108.62μgcm(-2). Histological and TEER assessments showed no permanent effects on the skin by TNEG, indicating that this novel TNEG nanosystem has the potential to translate into clinical trials as treatment alternatives for HIV/AIDs patients.</div></front></TEI><affiliations><list><country><li>Afrique du Sud</li></country></list><tree><country name="Afrique du Sud"><noRegion><name sortKey="Rambharose, Sanjeev" sort="Rambharose, Sanjeev" uniqKey="Rambharose S" first="Sanjeev" last="Rambharose">Sanjeev Rambharose</name></noRegion><name sortKey="Govender, Thirumala" sort="Govender, Thirumala" uniqKey="Govender T" first="Thirumala" last="Govender">Thirumala Govender</name><name sortKey="Kalhapure, Rahul S" sort="Kalhapure, Rahul S" uniqKey="Kalhapure R" first="Rahul S" last="Kalhapure">Rahul S. Kalhapure</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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