Journal
INTERNATIONAL JOURNAL OF NANOMEDICINE
Volume 14, Issue -, Pages 33-43Publisher
DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S187470
Keywords
bioavailability; box behnken design; citral; fluorescent laser microscope; nanostructured-based films; permeation
Funding
- Deanship of Scientific Research (DSR) at King Abdulaziz University, Jeddah [G-99-166-38]
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Background: Vinpocetine (VNP), a semisynthetic natural product, is used as a vasodilator for cerebrovascular and age-related memory disorders. VNP suffers from low oral bioavailability owing to its low water solubility and extensive first-pass metabolism. This work aimed at utilizing D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS) and alpha lipoic acid (ALA) to develop efficient micellar system for transdermal delivery of VNP. Materials and methods: VNP-TPGS-ALA micelles were prepared, characterized for particle size using particle size analyzer, and investigated for structure using transmission electron microscope. Optimization of VNP-TPGS-ALA micelles-loaded transdermal films was performed using Box-Behnken experimental design. The investigated factors were percentage of ALA in TPGS (X-1), citral concentration (X-2), and propylene glycol concentration (X-3). Elongation percent (Y-1), initial permeation after 2 hours (Y-2), and cumulative permeation after 24 hours (Y-3) were studied as responses. Results: Statistical analysis revealed optimum levels of 16.62%, 3%, and 2.18% for X-1, X-2, and X-3, respectively. Fluorescent laser microscopic visualization of skin penetration of the optimized transdermal film revealed marked widespread fluorescence intensity in skin tissue after 0.5, 2, and 4 hours compared with raw VNP transdermal film formulation, which indicated enhancement of VNP skin penetration. Conclusion: The obtained results highlighted the potentiality of VNP nanostructure-based films for controlling the transdermal permeation of the drug and improving its effectiveness.
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