Effect of Penetration Enhancers on Transdermal Delivery of Oxcarbazepine, an Antiepileptic Drug Using Microemulsions

Virani, Amitkumar; Puri, Vinam; Mohd, Hana; Michniak‐Kohn, Bozena

doi:10.3390/pharmaceutics15010183

Cited by 26 publications

(15 citation statements)

References 50 publications

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“…In combination with Transcutol, the highest drug release was observed in our in vitro experiment, which can be explained by the synergistic penetration enhancer effect of the two excipients. Transcutol is often used in combination with other penetration enhancers; Amitkumar et al found that oleic acid and Transcutol in combination significantly improved the transdermal drug delivery of oxcarbazepine [ 49 ]. The dissolution from the patches without penetration enhancers was well described with the Weibull model.…”

Section: Discussionmentioning

confidence: 99%

Formulation and Evaluation of Transdermal Patches Containing BGP-15

Bácskay,

Hosszú,

Budai

et al. 2023

Pharmaceutics

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BGP-15 is an active ingredient with many advantages, e.g., beneficial cardiovascular and anti-inflammatory effects. The transdermal administration of BGP-15 has great potential, which has not been investigated yet, despite the fact that it is a non-invasive and safe form of treatment. The aim of our study was to formulate transdermal patches containing BGP-15 and optimize the production with the Box–Behnken design of experiment. The most optimal formulation was further combined with penetration enhancers to improve bioavailability of the active ingredient, and the in vitro drug release and in vitro permeation of BGP-15 from the patches were investigated. FTIR spectra of BGP-15, the formulations and the components were also studied. The most optimal formulation based on the tested parameters was dried for 24 h, with 67% polyvinyl alcohol (PVA) content and low ethanol content. The selected penetration enhancer excipients were not cytotoxic on HaCaT cells. The FTIR measurements and SEM photography proved the compatibility of the active substance and the vehicle; BGP-15 was present in the polymer matrix in dissolved form. The bioavailability of BGP-15 was most significantly enhanced by the combination of Transcutol and Labrasol. The in vitro permeation study confirmed that the formulated patches successfully enabled the transdermal administration of BGP-15.

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Section: Discussionmentioning

confidence: 99%

Formulation and Evaluation of Transdermal Patches Containing BGP-15

Bácskay,

Hosszú,

Budai

et al. 2023

Pharmaceutics

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“…Synergistic effects can be achieved when using certain combinations of penetration enhancers. There are many techniques used to exploit the synergistic behaviour of various penetration enhancers, such as co-solvency; creating eutectic mixtures; using vesicles such as liposomes, transfersomes and niosomes; and creating MEs [71,72]. PG, one of the most commonly used penetration-enhancing agents, is synergistic when combined with terpenes, OA, Azone ® , and IPM [12,63].…”

Section: Synergismmentioning

confidence: 99%

“…Ethanol has demonstrated synergistic behaviour when used with linoleic acid for the TD of lidocaine [73]. A combination of 5% OA and 5% DGME (Transcutol ® P) was able to synergistically enhance the transdermal flux of oxcarbazepine through human skin compared to OA or DGME alone [72]. Synergism has also been demonstrated when CPEs are used in combination with physical penetration-enhancing methods [74], such as iontophoresis [63,[75][76][77], sonophoresis [78], and electroporation [79].…”

Section: Synergismmentioning

confidence: 99%

Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs

Balmanno,

Falconer,

Ravuri

et al. 2024

Pharmaceutics

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The transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has the potential to overcome some of the major disadvantages relating to oral NSAID usage, such as gastrointestinal adverse events and compliance. However, the poor solubility of many of the newer NSAIDs creates challenges in incorporating the drugs into formulations suitable for application to skin and may limit transdermal permeation, particularly if the goal is therapeutic systemic drug concentrations. This review is an overview of the various strategies used to increase the solubility of poorly soluble NSAIDs and enhance their permeation through skin, such as the modification of the vehicle, the modification of or bypassing the barrier function of the skin, and using advanced nano-sized formulations. Furthermore, the simple yet highly versatile microemulsion system has been found to be a cost-effective and highly successful technology to deliver poorly water-soluble NSAIDs.

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“…After the assembled FDCs were allowed to equilibrate for a minimum of 30 min, 500 µL of each formulation was applied to the skin in the donor compartment as described by Virani et al [35,36]. At specific time intervals, a 300 µL sample of the receptor medium was withdrawn, and an equivalent volume of fresh buffer solution was added to the receptor chamber.…”

Section: In Vitro Skin Permeation Studymentioning

confidence: 99%

Effect of Edge Activator Combinations in Transethosomal Formulations for Skin Delivery of Thymoquinone via Langmuir Technique

Mohd,

Dopierała,

Zidar

et al. 2024

Sci. Pharm.

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Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an environment conducive to enhancing TQ’s solubility, stability, and skin permeation. To optimize TQ transethosomal formulations, we introduced a combination of ionic and nonionic surfactants, namely Tween 20 and sodium lauryl sulfate (SLS) or sodium lauroyl glutamate (SLG). Surfactants play a crucial role in stabilizing the formulation, reducing aggregation, improving biocompatibility, and minimizing potential toxicity. We fine-tuned the formulation composition and gained insights into its interfacial behavior using the Langmuir monolayer technique. This method elucidated the interfacial properties and behavior of phospholipids in ethosome and transethosome formulations. Our findings suggest that monolayer studies can serve as the initial step in selecting surfactants for nanocarrier formulations based on their interfacial dilational rheology studies. It was found that the addition of surfactant to the formulation increased the elasticity considering the capability of transethosomes to significantly decrease their radius when permeating the skin barrier. The results of the dilational rheology experiments were most relevant to drug permeation through the skin for the largest amplitude of deformation. The combination of Tween 20 and SLS efficiently modified the rheological behavior of lipids, increasing their elasticity. This conclusion was supported by in vitro studies, where formulation F2 composed of Tween 20 and SLS demonstrated the highest permeation after 24 h (300.23 µg/cm2). Furthermore, the F2 formulation showed the highest encapsulation efficiency (EE) of 94%, surpassing those of the control and ethosomal formulations. Additionally, this transethosomal formulation exhibited antimicrobial activity against S. aureus, with a zone of inhibition of 26.4 ± 0.3 mm. Importantly, we assessed the cytotoxicity of both ethosomes and transethosomes at concentrations ranging from 3.5 µM to 50 µM on HaCaT cell lines and found no cytotoxic effects compared to TQ hydroethanolic solution. These results suggest the potential safety and efficacy of TQ transethosomal formulations.

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Effect of Penetration Enhancers on Transdermal Delivery of Oxcarbazepine, an Antiepileptic Drug Using Microemulsions

Cited by 26 publications

References 50 publications

Formulation and Evaluation of Transdermal Patches Containing BGP-15

Formulation and Evaluation of Transdermal Patches Containing BGP-15

Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs

Effect of Edge Activator Combinations in Transethosomal Formulations for Skin Delivery of Thymoquinone via Langmuir Technique

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