Abstract
The effect of transdermal vehicle (Pentravan®) on skin permeability was examined for unmodified ibuprofen (IBU) and ion pairs of ibuprofen with new L-valine alkyl esters [ValOR][IBU]. The percutaneous permeation across the human skin and transdermal diffusion test model (Strat-M® membranes) of ibuprofen and its structural modification were measured and compared using Franz diffusion cells. For comparison, the penetration of ibuprofen from a commercial product was also investigated. The cumulative amount of drug permeated through human skin at the end of the 24 h study was highest for ibuprofen derivatives containing propyl (C3), isopropyl (C3), ethyl (C2), and butyl (C4) esters. For Strat-M®, the best results were obtained with the alkyl chain length of the ester from C2 to C5. The permeation profiles and parameters were appointed, such as steady-state flux, lag time, and permeability coefficient. It has been shown that L-valine alkyl ester ibuprofenates, with the propyl, butyl, and amyl chain, exhibit a higher permeation rate than ibuprofen. The diffusion parameters of analyzed drugs through human skin and Strat-M® were similar and with good correlation. The resulting Pentravan-based creams with ibuprofen in the form of an ionic pair represent a potential alternative to other forms of the drug-containing analgesics administered transdermally. Furthermore, the Strat-M® membranes can be used to assess the permeation of transdermal preparations containing anti-inflammatory drugs.
Highlights
The numerous advantages of transdermal drug delivery, such as controlled or sustained drug release, constant levels of the drug in the plasma, minimizing first-pass metabolism, reduced dosing frequency, reduced drug toxicity, adverse events, and improved patient compliance, making it a convenient and frequently chosen route of drug administration [1]
The stratum corneum limits the penetration of the topically applied active compounds, consisting mainly of lipids and ceramides [3], which inhibit the penetration of exogenous cosmetic and therapeutic compounds
Due to the presence of ingredients that could increase the penetration of active substances, Pentravan® was used as a vehicle [5]
Summary
The numerous advantages of transdermal drug delivery, such as controlled or sustained drug release, constant levels of the drug in the plasma, minimizing first-pass metabolism, reduced dosing frequency, reduced drug toxicity, adverse events, and improved patient compliance, making it a convenient and frequently chosen route of drug administration [1]. Other permeation limiting factors include physicochemical properties of the drug (solubility, molecular weight, and lipophilicity) and the properties of the drugcontaining vehicle To overcome these challenges, various attempts are made to improve the transport of drugs across the skin, such as chemical or physical methods [1]. We presented the greater penetration compared to pure IBU of the ion pairs of ibuprofen with L-valine alkyl esters [ValOR][IBU], in which the alkyl chain R was extended from C1 to C8 For those studies alcohol such as methanol, ethanol, and isopropanol, was chosen as the vehicle. Pentravan® includes a complex called LIPOIL, butylhydroxytoluene, simethicone, urea, potassium sorbate, polyoxyethylene stearate, cetyl alcohol, stearic alcohol, stearic acid, glycerol monostearate, benzoic acid, carbomer, and hydrochloric acid These include substances that facilitate the transport of the drug through the skin, improve its hydration, preserve, stabilize, and improve the rheology of ointments and creams. The amount of ibuprofen and its derivatives in the supernatant were assayed by HPLC (section below) with pure methanol applied as a control
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