The effect of terpenes on percutaneous absorption of tiaprofenic acid gel

Abstract

Tiaprofenic acid is a potent analgesic and nonsteroidal anti-inflammatory drug (NSAID) and like any other nonsteroidal anti-inflammatory drug, oral administration of the conventional dosage forms of tiaprofenic acid invariably causes gastrointestinal side effects. In an effort to eliminate these side effects while enhancing the drug concentration at the target tissue, an epidermal application of tiaprofenic acid seems to be an effective alternative drug delivery modality. This study attempts to demonstrate the influence of different terpenes (d-limonene, menthol and nerolidol) in various combinations of preparations on the percutaneous penetration of tiaprofenic acid from Carbopol(®) 940 based gel formulations (1%) in an ex vivo experiment using Franz-type diffusion cells. The enhancement effect of terpenes on skin absorption of tiaprofenic acid was further evaluated by an in vivo method in rats. Amongst the terpenes used, d-limonene was the most outstanding penetration enhancer that was reference to penetration of tiaprofenic acid through rat skin ex vivo. In vivo penetration study shows that the AUC₀(-)₄₈(h) was increased by about 10 fold by the addition of 5% d-limonene to the formulation. Histological studies show that d-limonene causes disruption on the skin surface and is responsible for enhanced penetration of tiaprofenic acid. Since tiaprofenic acid is known to cause gastrointestinal disturbances following systemic administration, topical formulations of tiaprofenic acid in gel form including 5% d-limonene could be suggested as an alternative.

Gold Nanoparticle Penetration and Reduced Metabolism in Human Skin by Toluene

“…Aside from occupational health issues, studying the behavior of nanoparticles with the skin barrier is a very important basic research approach for later application in designing topical drug delivery systems with optimal parameters. This is especially true when solvents like terpenes are used in topical formulations (38). Our experimental design was congruent with previous gold nanoparticle skin penetration studies with similar exposure times and use of static Franz cells.…”

Copaiba oil enhances in vitro/in vivo cutaneous permeability and in vivo anti-inflammatory effect of celecoxib

“…Studies on the percutaneous absorption of different drugs in the presence of terpenes have suggested that the effects of the latter are related to their concentration and chemical characteristics …”

“…Compounds that can reversibly change the SC barrier properties have been widely described as penetration enhancers (P.Es). Terpenes are naturally occurring compounds found in essential oils that have been explored as skin penetration enhancers (P.E); that is, they can improve the penetration of drugs into the skin by altering the composition or organization of the lipid membrane, thus allowing the diffusion of the drug through the skin . Their effects depend on both the drug and terpene lipophilicity, and they may promote the permeability of hydrophilic or lipophilic drugs …”

Topical Delivery of Aceclofenac: Challenges and Promises of Novel Drug Delivery Systems

“…It is also reported that topical NSAIDs require overall less active drug vis-à-vis the dosage of systemic NSAIDs. Therefore, topical therapy is not only promising on the safety and efficacy fronts but also on the economic fronts too [38]. The various advantages of topical delivery are enlisted in Table 1.…”

“…The physicochemical factors of drug like log P , pK a , solubility, and molecular mass also play an important role in the selection of components for the topical delivery vehicle [36, 40]. For acidic and unstable drugs like ACE, special consideration has to be made on the excipient selection for topical vehicle which will not only mask the irritation potential of ACE due to acidic group but also provide milieu for effective topical delivery and maintenance of chemical integrity [35, 38]. Figure 3 highlights the various challenges offered by ACE while developing an ideal topical formulation.…”