Abstract
Introduction: The nasal route of drug administration offers an alternative way for oral drug delivery and has the benefit of avoiding first-pass metabolism through drug delivery directly into the systemic circulation. The drug absorption enhancing effects of selected aloe leaf materials have been shown across various delivery routes, but their efficacies in this regard across nasal epithelia have not yet been investigated. The aim of this study was to determine the effects of gel and whole leaf extract materials from three selected aloe species (Aloe vera, Aloe ferox and Aloe muth-muth) on FITC-dextran 4400 permeation across two nasal epithelial models. Methods: Permeation of FITC-dextran 4400 and histological studies were conducted on both RPMI 2650 cell layers and excised sheep nasal mucosa, while toxicity studies were conducted using a neutral red assay on the RPMI 2650 cell model. Results: Significantly increased (P ≤ 0.05) apparent permeability coefficient (Papp) values of FITC-dextran 4400 in the presence of the aloe materials as compared to the control were found with all three aloe species at the highest concentrations (1.5% and 3% w/v) in the RPMI 2650 cell line, while only Aloe muth-muth at the highest concentration exhibited significantly (P ≤ 0.05) higher Papp values across the excised tissue model. Histological and neutral red analysis showed that Aloe vera materials exhibited detrimental effects, Aloe muth-muth only showed slight effects on cell viability and Aloe ferox exhibited no effect on the nasal epithelium. Conclusion: This in vitro study showed for the first time the potential of Aloe ferox and Aloe muth-muth leaf materials to enhance nasal drug delivery without causing damaging effects on the epithelium, while Aloe vera enhanced nasal drug delivery with detrimental effects as determined by means of cytotoxicity assays and histological analysis.
Highlights
The nasal route of drug administration offers an alternative way for oral drug delivery and has the benefit of avoiding first-pass metabolism through drug delivery directly into the systemic circulation
Discussion a slight decreased FD4 Papp value was found at the highest concentration of A. vera gel compared to that of the 1.5% w/v concentration during permeation across the RPMI 2650 cell layers, the permeation trends are generally in coherence with previous results where A. vera gel increased the transport of different molecules in a concentration dependent manner across other epithelial membranes including intestinal and buccal mucosal surfaces [2,4]
With regards to the aloe whole leaf extracts, the results found in the RPMI 2650 cell model are in line with previously published data on A. vera that increased paracellular permeation of insulin in a concentration dependent manner across human intestinal epithelial cell monolayers in vitro [2]
Summary
The nasal route of drug administration offers an alternative way for oral drug delivery and has the benefit of avoiding first-pass metabolism through drug delivery directly into the systemic circulation. The drug absorption enhancing effects of selected aloe leaf materials have been shown across various delivery routes, but their efficacies in this regard across nasal epithelia have not yet been investigated. The aim of this study was to determine the effects of gel and whole leaf extract materials from three selected aloe species (Aloe vera, Aloe ferox and Aloe muth-muth) on FITC-dextran 4400 permeation across two nasal epithelial models. Conclusion: This in vitro study showed for the first time the potential of Aloe ferox and Aloe muth-muth leaf materials to enhance nasal drug delivery without causing damaging effects on the epithelium, while Aloe vera enhanced nasal drug delivery with detrimental effects as determined by means of cytotoxicity assays and histological analysis. The current study deployed gel and whole leaf extract from this hybrid, A. muth-muth, in addition to gel and whole leaf materials from A. vera and A. ferox to investigate the possibility of drug delivery enhancement across the nasal epithelium
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