The purpose of the present study was to assess by in vitro means the effect of poly (methylmethacrylate) nanoparticles and poly (butylcyanoacrylate) nanoparticles on transdermal drug delivery. Methanol and octanol were chosen as test permeants. In order to distinguish between thermodynamic effect and those due to biological consequences, two different membranes were employed, i.e., full thickness hairless mouse skin and silicone elastomer sheeting (175 microns). It is evident that poly (methylmethacrylate) nanoparticles and poly (butylcyanoacrylate) nanoparticles increase the permeability of methanol through hairless mouse skin by a factor of 1.2-2. The permeability of lipophilic octanol is either unaffected by nanoparticles or decreases as a function of nanoparticle concentration depending on the lipophilicity of the polymer material.
"The other approach is to modify the formulation of the vehicle which plays an important role in the percutaneous absorption (Nannipieri et al., 1990; Loth, 1991). Recently, particulate systems such as liposomes and nanoparticles have been investigated as vehicles for the transdermal absorption of drugs (Knepp et al., 1990; Cappel and Kreuter, 1991; Lasch et al., 1991). Microemulsions, characterized as thermodynamically stable and clear isotropic systems, have also been proposed in pharmaceutical applications (Gallarate et al., 1988; Iwamoto et al., 1991). "
[Show abstract][Hide abstract] ABSTRACT: A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol:ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.
Archives of Pharmacal Research 04/2004; 27(3):351-6. DOI:10.1007/BF02980072 · 2.05 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Thesis (Ph. D.)--University of Notre Dame, 2006. Thesis directed by Agnes E. Ostafin for the Department of Chemical and Biomolecular Engineering. "March 2006." Includes bibliographical references (leaves 280-319). Electronic reproduction.
[Show abstract][Hide abstract] ABSTRACT: The influence of various penetration enhancers including propylene glycol, oleic acid, Azone®, isopropyl myristate, valine, and nanoparticles on the permeation coefficient for the permeation of amino acids through hairless mouse skin as well as a dialysis membrane was assessed in vitro. The two different types of membranes were employed in order to distinguish between effects due to thermodynamic parameters and those due to barrier resistance. Furthermore, the influence of these penetration enhancers on the amount of amino acids remaining within the skin was determined. Oleic acid was found to be the most efficient enhancer for amino acids (enhancement factor (EF) of 176 for histidine) followed by Azone® (EF of 45 for phenylalanine). All other penetration enhancers failed to exert any significant effect on the skin permeation of amino acids. The fact that the enhancement effects of oleic acid and Azone® are not reversible and that the enhancers exhibited no influence with dialysis membranes clearly indicate that both penetration enhancers induce their effects on the basis of changes in skin morphology. Choosing arginine, histidine and phenylalanine as test permeants enabled a correlation between the enhancement effects and the degree of ionization of the test permeant. Histidine is the only amino acid which is unionized at pH 7.4 due to its isoelectric point. This might be the reason why the permeation enhancement induced by valine was only detectable with histidine, and not with the other two amino acids. Neither penetration enhancer resulted in any significant effect on the amount of the amino acid accumulated in the skin.
International Journal of Pharmaceutics 09/1992; 85(1-3):7-17. DOI:10.1016/0378-5173(92)90128-O · 3.65 Impact Factor
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