Unsaturated cyclic ureas as new non-toxic biodegradable transdermal penetration enhancers. II. Evaluation study
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Cited by (46)
Penetration enhancers
2012, Advanced Drug Delivery ReviewsCitation Excerpt :As urea itself possesses only marginal penetration enhancing activity, attempts have been made to synthesis analogues containing more potent enhancing moieties. Thus Wong and co-workers synthesised cyclic urea analogues and found them to be as potent as Azone for promoting indomethacin across shed snake skin and hairless mouse skin [46]. A series of alkyl and aryl urea analogies were moderately effective as enhancers for 5-flourouracil when applied in PG to human skin in vitro, though urea itself was ineffective [47].
The effect of terpene concentrations on the skin penetration of diclofenac sodium
2007, International Journal of PharmaceuticsCitation Excerpt :With the safety of permeation enhancers being of a prime consideration, the search continues for an ideal enhancer that is pharmacologically inactive, non-irritant, non-damaging for the skin, potent, and cosmetically acceptable (Pfister et al., 1990). Many of the chemical enhancers such as dimethyl sulfoxide (Kurihara-Begstrom et al., 1987), surfactants (Ashton et al., 1986; Shokri et al., 2001; Nokhodchi et al., 2003), alcohols (Tsuzuki et al., 1988), and urea and its derivatives (Wong et al., 1989) have been screened for their penetration enhancement. The adverse effects caused by some of these enhancers restrict their widespread use.
Penetration enhancers
2004, Advanced Drug Delivery ReviewsNew oligoethylene ester derivatives of 5-iodo-2′-deoxyuridine as dermal prodrugs: Synthesis, physicochemical properties, and skin permeation studies
2002, Journal of Pharmaceutical SciencesCitation Excerpt :These findings suggest that hydrolytic cleavage of esters 9–13 occurs preferentially at the 3′‐O‐ester linkage. Because an essential prerequisite for the successful use of dermal prodrugs is their reconversion into the parent drug within the skin, we assessed the enzymatic cleavage of esters 9–13 with porcine liver esterases, which are regarded as good models for skin esterase enzymatic activity.10,24,25 As may be noted in Table 1, all the esters were susceptible to undergoing enzymatic hydrolysis by porcine liver esterase with t1/2 ranging from ∼2 to 4.5 h.
In vitro and in vivo evaluation of polyoxyethylene esters as dermal prodrugs of ketoprofen, naproxen and diclofenac
2001, European Journal of Pharmaceutical Sciences