Evaluation of the in vitro permeation parameters of topical ketoprofen and lidocaine hydrochloride from transdermal Pentravan® products through human skin

Abstract

In the treatment of pain, especially chronic pain, the rule of multimodal therapy applies, based on various painkillers mechanisms of action. The aim of the conducted study was to evaluate the in vitro penetration of ketoprofen (KET) and lidocaine hydrochloride (LH) through the human skin from a vehicle with transdermal properties. The results obtained with the use of the Franz chamber showed statistically significantly higher penetration of KET from the transdermal vehicle as compared to commercial preparations. It was also shown that the addition of LH to the transdermal vehicle did not change the amount of KET permeated. The study also compared the penetration of KET and LH by adding various excipients to the transdermal vehicle. Comparing the cumulative mass of KET that penetrated after the 24-h study, it was observed that the significantly highest permeation was found for the vehicle containing additionally Tinctura capsici, then for that containing camphor and ethanol, and the vehicle containing menthol and ethanol as compared to that containing Pentravan® alone. A similar tendency was observed in the case of LH, where the addition of Tinctura capsici, menthol and camphor led to a statistically significant higher penetration. Adding certain drugs such as KET and LH to Pentravan®, and substances such as menthol, camphor or capsaicin, can be an interesting alternative to administered enteral drugs especially in the group of patients with multiple diseases and polypragmasy.

Use of Silybum marianum Extract and Bio-Ferment for Biodegradable Cosmetic Formulations to Enhance Antioxidant Potential and Effect of the Type of Vehicle on the Percutaneous Absorption and Skin Retention of Silybin and Taxifolin

“…The penetration degree of active substances may be different, depending on the compounds' physical and chemical properties as well as the vehicle used [54]. The primary impediment that restricts the permeation of active compounds into the skin is the stratum corneum (SC), which serves to prevent excessive transdermal water loss as well as the ingress of germs and chemical substances [33,55]. The SC is a thin membrane consisting primarily of cornified epidermal cells, while the main components are lipids, namely ceramides, cholesterol and its esters, and fatty acids [56].…”

Topical Delivery Systems Effectively Transport Analgesics to Areas of Localized Pain via Direct Diffusion

“…Absorption and subsequent penetration of a drug into deeper tissues (e.g., muscle) is a complex process limited by various factors [10]. The drug's molecular size, lipophilicity, and protein/tissue binding capacities affect the diffusion through the stratum corneum, epidermis, dermis, Pharmaceutics 2023, 15, 2563 2 of 11 and subcutaneous adipose tissue (SAT) into the muscle [11,12]. Capillaries within these tissues provide the route to systemic drug delivery [13], but it is not yet fully understood to what extent diffusion, systemic uptake and redistribution, or a combination of both affect a drug's efficacy in treating local pain [14].…”