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Optimized Vinpocetine-Loaded Vitamin E D-α-tocopherol Polyethylene Glycol 1000 Succinate-Alpha Lipoic Acid Micelles as a Potential Transdermal Drug Delivery System: In Vitro and Ex Vivo Studies

Osama Aa Ahmed, Khalid M El-Say, Bader M Aljaeid, Shaimaa M Badr-Eldin, Tarek A Ahmed

Int J Nanomedicine. 2018 Dec 18;14:33-43.

PMID: 30587983

Abstract:

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-α-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 (X1), citral concentration (X2), and propylene glycol concentration (X3). Elongation percent (Y1), initial permeation after 2 hours (Y2), and cumulative permeation after 24 hours (Y3) were studied as responses.
Results:
Statistical analysis revealed optimum levels of 16.62%, 3%, and 2.18% for X1, X2, and X3, 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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP25322683-A Polyethylene glycol 1000 Polyethylene glycol 1000 25322-68-3 Price
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