(M1130-12-78) Mechanistic Insights of Luteolin Loaded Elastic Liposomes for Transdermal Delivery: HSPiP Predictive Parameters and Instrumental Based Evidence

Purpose: The study aimed to gain a mechanistic understanding of luteolin loaded elastic liposomes (OLEL1) for transdermal delivery.

Methods: Various techniques, including HSPiP software based parameters, thermal analysis, infrared analysis, and morphological evaluations were employed to evaluate the permeation and drug deposition across rat skin as preclinical assessment.

Results: HSPiP provided HSP values of OLEL1, luteolin, excipients, and rat skin. Rat skin in different conditions were evaluated for vibrational and thermal changes using FTIR and DSC, respectively. Fluorescence microscopy and scanning electron microscopy (SEM) were used to compare the treated skin with control for vesicle permeation route across skin epidermis and composition mediated surficial perturbation. The HSP estimation of skin and PC showed close relation in terms of δd and δh. Similarly, OLEL1 and skin might be interacting with each other mainly through δd and δp forces as evidenced with predicted values. DSC showed changes in thermal behavior of skin after OLEL1 treatment as compared to untreated skin. Visualization of these changes were evident under fluorescence microscopy and confirmed enhanced drug permeation and deposition. SEM findings corroborated substantial reversible surface perturbation of skin protein layer for improved vesicle permeation and subsequent internalization with inner skin matrix.

Conclusion: The study demonstrated a mechanistic insight of luteolin loaded vesicle across rat skin for enhanced permeation and drug deposition.

References: Altamimi, Mohammad A., Afzal Hussain, Wael A. Mahdi, Syed Sarim Imam, Musaad A. Alshammari, Sultan Alshehri, and Mohammad Rashid Khan. "Mechanistic Insights into Luteolin-Loaded Elastic Liposomes for Transdermal Delivery: HSPiP Predictive Parameters and Instrument-Based Evidence." ACS omega (2022).

Acknowledgements: The authors extend their appreciation to the Deputyship for Research & Innovation, Ministry of Education in Saudi Arabia for funding this work

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