Abstract
Purpose: To achieve percutaneous delivery of trolamine salicylate to muscle and joints for the treatment of inflammatory muscle, tendon and joint diseases.Methods: Trolamine salicylate permeability parameters through rat skin were evaluated with and without chemical enhancers - Transcutol, eucalyptus oil, oleic acid and sodium lauryl sulfate – using the permeability cell technique.Results: The main barrier for trolamine salicylate permeability was the epidermis layer of the skin. Also, partitioning from the aqueous donor phase into the skin was the rate-limiting step for drug flux. Transcutol and eucalyptus oil were the most effective enhancers as they increased flux 11-fold. Sodium lauryl sulfate disrupted the lipid structure of the skin and thus increased diffusion coefficient 3-fold. Supersaturation technique did not increase flux. Propylene glycol in cosolvent system increased drug solubility in donor phase and partitioning.Conclusion: Trolamine salicylate exhibited less flux and diffusion coefficient through rat skin than salicylic acid due to its hydrophilic property. Partitioning from vehicle into skin was the rate-limiting step for trolamine salicylate permeability through rat skin.Keywords: Trolamine salicylate, Percutaneous absorption, Chemical enhancers, Supersaturation technique, Differential scanning calorimetryTropical Journal of Pharmaceutical Research December 2010; 9 (6): 541-548
Highlights
Permeation of drugs through the skin is the basis of transdermal delivery [1]
The results showed that the flux of trolamine salicylate through epidermis was significantly higher (p < 0.05) than through whole skin but Tlag was significantly lower (p < 0.05)
The effect of chemical enhancers on trolamine salicylate permeability is presented in Table 2 as ERflux and ERD
Summary
Permeation of drugs through the skin is the basis of transdermal delivery [1]. Transdermal drug delivery is associated with some advantages such as controlled drug delivery, continuous drug delivery (which is important for drugs with short biological halflife and low therapeutic indices), first-pass intestinal and hepatic bypass, avoidance of the gastrointestinal irritation (which is common with oral medications such as salicylates), and facilitation of drug localization at target site [1] Percutaneous delivery of salicylates to muscle and joints is the goal in the treatment of inflammatory muscle, tendon and joint diseases tendon and joint diseases [2].The two main steps in skin penetration are partitioning and diffusion through the stratum corneum, partitioning and diffusion to the viable epidermis, passage into the dermis and systemic absorption or penetration into deeper tissues. Permeation of drugs through the skin is the basis of transdermal delivery [1]. The greatest barrier to drug penetration is the stratum corneum, the outermost layer of the skin [3]. The stratum corneum poses a formidable challenge to drug delivery systems. Several approaches have been used to improve entry of drugs into lower skin layer and deeper tissues. Chemical and physical permeation enhancers have been designed to facilitate delivery of high drug concentrations across the skin into systemic circulation or deeper tissues [4]. Increased drug diffusivity in the skin, stratum corneum lipid fluidization, increase in thermodynamic activity of drug in the skin and vehicle, as well as effect on drug partition coefficient, are the most common modes of action of chemical enhancers
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