Optimization and Evaluation of the In Vitro Permeation Parameters of Topical Products with Non-Steroidal Anti-Inflammatory Drugs through Strat-M® Membrane

Abstract

Pharmaceutical products containing non-steroidal anti-inflammatory drugs (NSAIDs) are among the most prescribed topical formulations used for analgesic and antirheumatic properties. These drugs must overcome the skin barrier to cause a therapeutic effect. Human skin has been widely used as a model to study in vitro drug diffusion and permeation, however, it suffers from many limitations. Therefore, to perform in vitro permeation test (IVPT), we used a Strat-M® membrane with diffusion characteristics well-correlated to human skin. This study’s objective was to optimize the IVPT conditions using Plackett–Burman experimental design for bio-predictive evaluation of the in vitro permeation rates of five non-steroidal anti-inflammatory drugs (diclofenac, etofenamate, ibuprofen, ketoprofen, naproxen) across Strat-M® membrane from commercial topical formulations. The Plackett–Burman factorial design was used to screen the effect of seven factors in eight runs with one additional center point. This tool allowed us to set the sensitive and discriminative IVPT final conditions that can appropriately characterize the NSAIDs formulations. The permeation rate of etofenamate (ETF) across the Strat-M® membrane was 1.7–14.8 times faster than other NSAIDs from selected semisolids but 1.6 times slower than the ETF spray formulation.

Comparison of Synthetic Membranes to Heat-Separated Human Epidermis in Skin Permeation Studies In Vitro

“…We already have some information about permeation across the Strat-M membrane correlating well with that through human skin [14,15,21] as well as animal skin [27]. In addition, the Strat-M membrane has low batch-to-batch variability, is easy to use, and does not need special storage conditions [28]. In our study, we demonstrated that the permeation profile across the Strat-M membrane was similar to HSE (Table 2), but the general permeation data (Q and J) were significantly higher (p < 0.05) (Figure 3) in the case of the Strat-M membrane.…”

Preparation and Characterization of Patch Loaded with Clarithromycin Nanovesicles for Transdermal Drug Delivery

“…For poorly water-soluble drugs, adding solubilizers such as Tween-80, ethanol, and isopropanol in the release medium is recommended [ 57 , 58 , 59 ]. PBS containing 20% isopropanol at pH 7.4 was chosen as the receptor media in both the drug-release and drug-permeation studies to achieve the required sink conditions.…”

“…PBS containing 20% isopropanol at pH 7.4 was chosen as the receptor media in both the drug-release and drug-permeation studies to achieve the required sink conditions. This was because sink conditions are attained when the equilibrium solubility of drugs in the dissolving medium is at least three times the volume required for drug saturation [ 59 ]. In addition, these tests were carried out using PBS solution containing 20% isopropanol (pH 7.4) at 37 ± 0.5 °C and 600 rpm to simulate physiological conditions, as has been previously described in [ 60 ].…”

Preparation, Characterization and Permeation Study of Topical Gel Loaded with Transfersomes Containing Asiatic Acid

“…According to the work presented by Tiwari et al (2020), the non-ionic EAs such as TW80 could contribute to deformation of the transfersomes, thereby played a main role in improving the drug permeation [ 44 ]. Moreover, the concentration of the drug and the physicochemical characteristics of the formulation can also significantly affect the drug permeation [ 45 , 46 ]. The significantly higher penetration efficiency exhibited by AATGs compared to hydroethanolic AA in gel could be due to the constituents of transfersomes and this proves the requirement of a carrier base delivery system for AA dermal delivery.…”