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

Abstract

BackgroundVinpocetine (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 methodsVNP-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.ResultsStatistical 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.ConclusionThe obtained results highlighted the potentiality of VNP nanostructure-based films for controlling the transdermal permeation of the drug and improving its effectiveness.

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

“…Figure 1 C and Figure 2 C representing the residual versus run plots depicted a random and uniform scatter of points, indicating no lurking variable affected any of the response. Furthermore, predicted versus actual values of both responses’ plots, Figure 1 D and Figure 2 D, were highly linear, revealing that the observed responses showed good analogy to the predicted ones [ 34 ].…”

<p>Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel</p>

“…Different optimized VPN-loaded lipid-based NCs, namely, SLNs, TFs, PEGylated liposomes (Peg-Lips) and TPGS-micelles were prepared as described in our previously published work 17,18,30–33Table 1 illustrates the composition of the prepared lipid-based NCs.…”

“…Ethanol was completely removed using Buchi Rotavapor R-200; BÜCHI Labortechnik AG (Flawil, Switzerland). The obtained micellar dispersion was kept in a refrigerator at 4°C until further characterization 33…”

Improved Transmucosal Delivery of Glimepiride via Unidirectional Release Buccal Film Loaded With Vitamin E TPGS-Based Nanocarrier

“…Our result is in good agreement with previous reports indicating the effectiveness of nanocarrier systems in skin permeation and delivery. 57,58 Accordingly, the optimized formulation showed a promise for improved absorption and bioavailability of GMD loaded into the nanocarrier-loaded film formula.…”