article · Drug Development and Industrial Pharmacy
Treating joint conditions such as osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis often requires frequent oral doses of aceclofenac. To provide an alternative delivery route, an aceclofenac-loaded transfersomal gel was developed and assessed for transdermal delivery. Elastic lipid vesicles were fabricated using film hydration and optimized by varying the lipid concentration, edge activator levels, and hydration acidity. The optimized vesicles exhibited high drug entrapment and uniform nanoscale dimensions, with scanning electron microscopy confirming spherical morphology. When incorporated into a carbopol polymer gel, the resulting formulation matched the flow behaviour of an existing commercial gel. In ex vivo skin permeation tests, the transfersome gel achieved a fourteen-fold improvement in drug permeation compared to the marketed reference, indicating superior capability for delivering aceclofenac across the skin barrier.
Managing chronic inflammatory joint disorders typically requires frequent oral pain medication, which can lead to unwanted systemic side effects. Delivering anti-inflammatory drugs directly through the skin offers a less disruptive route that could lower oral dosing frequency. By substantially enhancing skin penetration, this formulation technique presents a practical route to improving the effectiveness of non-invasive, topical pain therapies.
The research presents an applied, laboratory-tested topical gel that could be adopted by pharmaceutical manufacturers developing topical pain treatments for arthritis. The formulation relies on established gel matrices and shows markedly higher skin permeation than a current commercial alternative. However, having only completed ex vivo permeation testing, the formulation remains at an early developmental stage and will require formal clinical validation prior to commercial release.
AI-generated from the published abstract. Always read the original work before citing.
The present investigation focused mainly on the development of aceclofenac (AF) loaded transfersomal gel (AF-TG) to minimize the frequency of oral dosing during the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. AF-loaded transfersomes (AF-TS) were prepared by using the film hydration method. The effect of drug loading, pH of hydration medium, edge activator (EA) and lipid concentration on the properties of the AF-TS were studied and optimized. Optimized AF-TS converted into AF-TG by the addition of carbopol 934. Morphology and compatibility studies of AF-TS were observed with scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). AT-TG formulation was evaluated further for <i>ex vivo</i> skin permeation studies compared with marketed Hifenac 30 g gel. Optimized AF-TS showed vesicle size, PDI, and zeta potential of 111.1 ± 3.2 nm, 0.19 ± 0.02, and -29.6 ± 1.2 mV, respectively. Entrapment efficiency of 74.1 ± 1.8% with pH 5.8 phosphate buffer as a hydration medium and 17.1 ± 0.9 elasticity at 0.15%w/v EA and 1%w/v lipid concentration were observed. SEM and DSC studies revealed the spherical shape and no incompatibilities in the AF-TS formulation. The permeability of the AF from AF-TG was enhanced by 14-folds with similar rheological properties compared with marketed gel. Overall, TG containing AF was superior to marketed AF gel formulation for enhanced skin delivery. Therefore, TS and TG formulation could be considered as an alternative delivery approach for the enhanced transdermal application of AF.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.1080/03639045.2020.1788069
Is something wrong with this record? Report it or request removal.
Discussion
Have you built on this work, tried to replicate it, or seen it applied in practice? Share what you know. Verified researchers and MARATTO™ domain experts can open a discussion, and any member can reply. Contributions are reviewed before they appear.
No discussion yet. Open the first thread.
New to MARATTO™? Create a free account.
