| Abstract [eng] |
The aim of work: to design and prepare self-adhesive films for topical delivery of dexpanthenol and evaluate in vitro release profiles and ex vivo permeation through non-ablative laser pretreated skin. Main tasks: to select adhesive and firm E100 and RL100 polymer films depending on the amount of plasticizer ATBC in the composition; to evaluate the stability and residue of the organic solvent, acetone, in the formed E100 and RL100 polymer film compositions; to evaluate the in vitro release of dexpanthenol from selected E100 and RL100 polymer films; to perform an adhesion test with selected E100 and RL100 polymer films; to evaluate the permeation of dexpanthenol ex vivo, depending on the structural changes induced by the non-ablative laser. Methods: production of experimental polymeric films; quantification of the residual solvent; stability assessment of polymer films; in vitro release of dexpanthenol and spectrophotometric dose determination; adhesion testing of polymer films loaded with dexpanthenol; laser exposure method for skin samples; ex vivo permeation study of dexpanthenol and ultra-high performance liquid chromatography method for the quantification of dexpanthenol. Results: 6 different polymer film compositions of E100 and RL100 were formed, which were sufficiently adhesive, flexible, homogeneous and firm. 2 hours after films preparation, the amount of solvent in the E100 compositions decreased by 98.0–98.5%, and in the RL100 compositions by 99.0–99.8%. It was found that when stored at room temperature (22-23 ° C), the films absorb 0.5% moisture from the enviroment. Films loaded with 5% of dexpanthenol, reported that after 24 h 13.7 - 17.5 percent of API were released in vitro from the E100 polymer film, and after 24 h 82.7 - 87.8 percent of API were released from the RL100. During the first 2 h, the RL100 1:1 composition releases 50% of initial dose in vitro. E100 1:0.5 polymer film has the highest adhesion and requires a force of 1.87 N to peel off the surface of the probe. When evaluating RL100 polymer compositions, it was found that a force of 0.5 N was required to detach the probe from the 1:1 film, twice as high as in the composition with a higher amount of ATBC. In an ex vivo study, the flux of dexpanthenol through the intact skin into the epidermis was 1.6 and 1.3 fold higher than at 65 J / cm2 and 195 J / cm2 fluence, respectively from the E100 1:0.5 polymer film, and the flux to the dermis 6 and 2.0 times higher. In the case of RL100 1:1, the flow through intact skin to the epidermis was 2.8 and 2.9 times higher than with laser exposure at 65 J / cm2 and 195 J / cm2, respectively, and the flow into the dermis did not differ significantly. Conclusions: The flexibility, adhesivness and firmness of polymeric films are ensured by the plasticizer ATBC, by changing the relative amount of ATBC in the composition, the desired properties can be obtained; During the the drying process of the polymer film, the solvent, acetone evaporates, and after 24 hours. its balance becomes vanishingly small; A relatively stable polymeric film was obtained which did not tend to absorb moisture from the environment; RL100 polymer film with dexpanthenol was found to have better in vitro release than E100 due to the quaternary ammonium groups in its structure; it was observed that in the case of E100 polymer film better adhesion is due to the higher amount of plasticizer ATBC, in contrast to RL100 polymer film; the effect of the Nd: YAG laser on the skin is thought to lead to lower flux of dexpanthenol ex vivo. |
