Nanoemulgel using a bicephalous heterolipid as a novel approach to enhance transdermal permeation of tenofovir.
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.
Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa.
Sanjeev
S
Rambharose
Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa. Electronic address: kalhapure@ukzn.ac.za.
Rahul S
RS
Kalhapure
Department of Pharmaceutical Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa. Electronic address: govenderth@ukzn.ac.za.
Thirumala
T
Govender
D000818:Animals; D019380:Anti-HIV Agents / Q000378:metabolism*; D015194:Diffusion Chambers, Culture; D004337:Drug Carriers; D017097:Electric Impedance; D004655:Emulsions; D005782:Gels; D006651:Histocytochemistry; D007700:Kinetics; D008297:Male; D049329:Nanostructures / Q000737:chemistry*; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism*; D012869:Skin Absorption / Q000502:physiology; D013229:Stearic Acids / Q000737:chemistry*; D000068698:Tenofovir / Q000378:metabolism*
D019380:Anti-HIV Agents; D004337:Drug Carriers; D004655:Emulsions; D005782:Gels; D013229:Stearic Acids; D011092:Polyethylene Glycols; C067028:Solutol HS 15; D000068698:Tenofovir; C000595213:polyethylene glycol 400
Heterolipid; Linolenic acid; Nanoemulgel; Nanoemulsion; Tenofovir; Transdermal permeation enhancer