Simultaneous penetration monitoring of oil component and active drug from fluorinated nanoemulsions

Binder, Lisa; Jatschka, Johannes; Kulovits, Eva Maria; Seeböck, Simone; Kählig, Hanspeter; Valenta, Claudia

doi:10.1016/j.ijpharm.2018.10.012

Cited by 8 publications

(5 citation statements)

References 34 publications

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“…Nanoemulsions have shown to improve the topical delivery of DFS as they show excellent solubilization capacities. Higher oil content in the nanoemulsion system leads to higher penetration of DFS, which was due to the occlusive effect [12]. Systemic delivery of DFS can also be achieved by a combination of nanoemulsion and microneedles; the nanoemulsion improved the bioavailability of DFS [13].…”

Section: Introductionmentioning

confidence: 99%

Improved Analgesic and Anti-Inflammatory Effect of Diclofenac Sodium by Topical Nanoemulgel: Formulation Development—In VitroandIn VivoStudies

Alhakamy

Aldawsari

et al. 2020

Journal of Chemistry

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The present study aimed to develop diclofenac sodium nanoemulgel for managing pain and inflammation using the low-energy emulsification technique. Nanoemulsion of diclofenac was formulated using clove oil with adequate amount of surfactants and cosurfactants, and it was converted to hydrogel form using Carbopol 980 as the gelling agent. The droplet size of the oil globules in the nanoemulsion was found to be 64.07 ± 2.65 nm with a low polydispersity index (0.238 ± 0.02) along with high negative zeta potential (−39.06 mV). The developed nanoemulgel exhibited non-Newtonian and pseudoplastic behavior. The in vitro release profile of the developed nanoemulgel was higher as compared to marketed and conventional gel. The carrageenan-induced paw edema test was performed in rats to evaluate the anti-inflammatory activity of developed nanoemulgel. The developed nanoemulgel showed significantly higher (p<0.01) effect in reducing pain and inflammation symptoms as compared to marketed as well as conventional gel of diclofenac. The overall findings of the study suggest that the developed nanoemulgel formulation of diclofenac can be used as a potential approach for the management of pain and inflammation.

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Section: Introductionmentioning

confidence: 99%

Improved Analgesic and Anti-Inflammatory Effect of Diclofenac Sodium by Topical Nanoemulgel: Formulation Development—In VitroandIn VivoStudies

Alhakamy

Aldawsari

et al. 2020

Journal of Chemistry

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“…All the strips (except the first one) and skin pieces were transferred to a conical tube with 10 mL methanol and clotrimazole was extracted by sonicating in an ultrasonic water bath for 30 min and left to stand overnight at 4 °C. After extraction, the resulting solution was centrifuged for 30 min at 15,000 rpm and the drug content in the supernatant was analyzed using HPLC [18,44,50,51].…”

Section: Methodsmentioning

confidence: 99%

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

et al. 2019

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Global incidence of superficial fungal infections caused by dermatophytes is high and affects around 40 million people. It is the fourth most common cause of infection. Clotrimazole, a broad spectrum imidazole antifungal agent is widely used to treat fungal infections. Conventional topical formulations of clotrimazole are intended to treat infections by effective penetration of drugs into the stratum corneum. However, drawbacks such as poor dermal bioavailability, poor penetration, and variable drug levels limit the efficiency. The present study aims to load clotrimazole into ufosomes and evaluate its topical bioavailability. Clotrimazole loaded ufosomes were prepared using cholesterol and sodium oleate by thin film hydration technique and evaluated for size, polydispersity index, and entrapment efficiency to obtain optimized formulation. Optimized formulation was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). Skin diffusion studies and tape-stripping were performed using human skin to determine the amount of clotrimazole accumulated in different layers of the skin. Results showed that the optimized formulation had vesicle size <250 nm with ~84% entrapment efficiency. XRD and DSC confirmed the entrapment of clotrimazole into ufosomes. No permeation was observed through the skin up to 24 h following the permeation studies. Tape-stripping revealed that ufosomes led to accumulation of more clotrimazole in the skin compared to marketed formulation (Perrigo). Overall, results revealed the capability of ufosomes in improving the skin bioavailability of clotrimazole.

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“…In a recent study characterizing nanoemulsions consisting of 20% or 40% perfluorohexyloctane (F6H8) as disperse phase loaded with the active pharmaceutical ingredient (API) diclofenac sodium and stabilized with soya lecithin (S75), a promising penetration behavior was shown in the tape stripping experiments investigated [29]. The total percentage of diclofenac sodium penetrated was about ten-times higher than that of F6H8, regardless of the formulation.…”

Section: Sfas For Topical Drug Delivery On the Skinmentioning

confidence: 99%

“…Rat buccal mucosa is highly keratinized in contrast to the nonkeratinized pig buccal mucosa, which shows penetration behavior similar to humans [106]. Since SFAs seem to increase permeation of drugs in (keratinized) skin [29,30], this in vivo study included both rats and minipigs to emphasize the potential different extents of keratinization. Surprisingly, F4H5/propofol reached high systemic bioavailability after buccal administration in both species.…”

Section: Sfas For Topical Drug Delivery On the Skinmentioning

confidence: 99%

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Semifluorinated Alkanes as New Drug Carriers—An Overview of Potential Medical and Clinical Applications

Tsagogiorgas

Otto

2023

Pharmaceutics

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Fluorinated compounds have been used in clinical and biomedical applications for years. The newer class of semifluorinated alkanes (SFAs) has very interesting physicochemical properties including high gas solubility (e.g., for oxygen) and low surface tensions, such as the well-known perfluorocarbons (PFC). Due to their high propensity to assemble to interfaces, they can be used to formulate a variety of multiphase colloidal systems, including direct and reverse fluorocarbon emulsions, microbubbles and nanoemulsions, gels, dispersions, suspensions and aerosols. In addition, SFAs can dissolve lipophilic drugs and thus be used as new drug carriers or in new formulations. In vitreoretinal surgery and as eye drops, SFAs have become part of daily clinical practice. This review provides brief background information on the fluorinated compounds used in medicine and discusses the physicochemical properties and biocompatibility of SFAs. The clinically established use in vitreoretinal surgery and new developments in drug delivery as eye drops are described. The potential clinical applications for oxygen transport by SFAs as pure fluids into the lungs or as intravenous applications of SFA emulsions are presented. Finally, aspects of drug delivery with SFAs as topical, oral, intravenous (systemic) and pulmonary applications as well as protein delivery are covered. This manuscript provides an overview of the (potential) medical applications of semifluorinated alkanes. The databases of PubMed and Medline were searched until January 2023.

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Simultaneous penetration monitoring of oil component and active drug from fluorinated nanoemulsions

Cited by 8 publications

References 34 publications

Improved Analgesic and Anti-Inflammatory Effect of Diclofenac Sodium by Topical Nanoemulgel: Formulation Development—In VitroandIn VivoStudies

Improved Analgesic and Anti-Inflammatory Effect of Diclofenac Sodium by Topical Nanoemulgel: Formulation Development—In VitroandIn VivoStudies

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Semifluorinated Alkanes as New Drug Carriers—An Overview of Potential Medical and Clinical Applications

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