| Abstract [eng] |
The aim of the study: to model a polymer film with lidocaine hydrochloride for coating on microneedles to achieve effective penetration of the lidoacaine hydrochloride into the skin. Research object : polymer-coated microneedles. Relevance: traditional methods of injecting lidocaine hydrochloride into the body cause pain to patients, mechanically damage to tissues and risk of microbial infection. To use of polymer-coated microneedles is considered a rational alternative to injections and means to achieve an effective delivery of drugs to the skin and such studies are considered relevant. Methods: polymer films production by solvent casting method; evaluation of physical – chemical and mechanical properties (mass, thickiness, time of dissolution, pH, humidity, stickiness, tensile force, distance to rupture point); determination penetration of the lidocaine hydrochloride into the skin by ultra high-performance liquid chromatography method. Main tasks: to form a polymer film from polyvinyl alcohol, carboxymethylcellulose sodium salt and plasticizer; to study the physical – chemical and mechanical properties of polymer films with lidocaine hydrochloride and to select the most one suitable for coating on microneedle; to evaluate the effect of different microneedles on the dermal penetration (ex vivo) of lidocaine hydrochloride from polymer solutions; to determine the dermal penetration (ex vivo) of lidocaine hydrochloride using polymer-coated microneedles. Results: formed a polymeric film from polyvinyl alcohol, carboxymethylcellulose sodium salt in a ratio 1:3 with propylene glycol in a ratio 1:20. Diffferent concentrations of 5 %, 7 % and 10 % lidocaine hydrochloride were added to the selected polymer films and the physicochemical and mechanical properties of the polymer films were investigated. Weight of the polymer films from 0,135 to 0,142 g, thickness from 154,200 to 161,800 µm, time of dissolution from 5,170 to 5,375 min humidity from 6,118 to 6,626 %, pH value from 6,397 to 6,521, top stickiness from 0,614 to 0,856 N, bottom from 0,590 to 0,956 N, tensile force from 7,259 to 8,105 N, the distance to the rupture point from 7,992 to 8,317 mm. After testing these properties a polymer film with 10 % lidocaine hydrochloride was selected according to the highest top (0,856 N) and bottom (0,956 N) stickiness, humidity (6,626 %) and tensile force (8,105 N), the distance to the rupture point (8,317 mm). The highest penetration of lidocaine hydrochloride from polymer solutions into the skin was using 800 µm lenght and 400 µm width and 600 µm lenght and 600 µm lenght and 200 µm width microneedles. The minimum penetration of lidocaine hydrochloride was using 400 µm lenght and 200 µm width microneedles. The highest dermal penetration of lidocaine hydrochloride was using 600 µm lenght and 200 µm width polymer-coated microneedles. The minimum dermal penetration of lidocaine hydrochloride was using 800 µm lenght and 400 µm width microneedles. Conclusions: the polymer film formed from polyvinyl alcohol and carboxymethylcellulose sodium salt with propylene glycol was with suitable properties for the incorporation of the model drug–lidocaine hydrochloride. After incorporating different amounts of lidocaine hydrochloride into the polymer films and investigated their physicochemical and mechanical properties, properties of the polymer films have changed. A polymer film with 10 % lidocaine hydrochloride was selected after evaluation of stickiness, humidity, tensile force, the distance to the rupture point. The highest penetration of lidocaine hydrochloride into the skin (ex vivo) from polymer solutions was using 800 µm lenght and 400 µm width and 600 µm lenght and 200 µm width microneedles. Minimum penetration of lidocaine hydrochloride from the damaged skin was using 400 lenght and 200 µm width microneedles. After evaluating the results of lidocaine hydrochloride for film coating were selected 800 µm lenght and 400 µm width and 600 µm lenght and 200 µm width microneedles. The amount of drug penetrated into the dermis after skin damage with 600 µm lenght and 200 µm lenght microneedles did not differ statistically significiantly, penetration was not affected by the lenght of the microneedles. |
