کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1400378 | 1501362 | 2015 | 10 صفحه PDF | دانلود رایگان |
• A highly potent preactivated thiolated gelatin was synthesised with a coupling rate of 138 ± 15 μmol MNA per gram polymer.
• Dynamic viscosity could be increase up to 400-fold and instantaneous gelation was observed.
• Thermal stability increased with concentration and modification degree of gelatin.
• The preactivated thiolated gelatin has highly mucoadhesive features with an increased maximal detachment force (MDF) as well as total work of adhesion (TWA) and a prolonged residence time on porcine mucosa of up to 5 days.
The aim of this study was to synthesise preactivated thiolated gelatin with potential mucoadhesive and cohesive properties.Gelatin from bovine skin (MW: approximately 50 kDa) was derivatised in two consecutive steps with iminothiolane followed by 2-mercaptonicotinic acid (MNA). The resulting preactivated thiolated gelatin (gelatin–TBA–MNA) was evaluated with respect to its physico-chemical properties such as isoelectric point (pI), viscosity, sol–gel transition and melting point and for its cytotoxicity. Muco-interactive features were investigated by tensile and rotating cylinder studies.Gelatin–TBA–MNA showed a preactivation rate of 138 ± 15 μmol MNA per gram polymer and a pI of 5.7 ± 0.3. The dynamic viscosity was increased up to 400-fold in comparison to unmodified control (p < 0.01 ∗ 10−5). In addition, gelatin–TBA–MNA displayed instantaneous gelation and an increase in melting point of up to 5 °C in comparison to control. According to cytotoxicity screening the novel gelatin derivative showed no toxic effect for up to 6 h. Total work of adhesion (TWA) of up to 71-fold (p < 0.01 ∗ 10−3) for gelatin–TBA–MNA in comparison to control was evident, as well as an up to 70-times extended residence time of the novel gelatin derivative on small intestinal porcine mucosa was recorded (p < 0.02 ∗ 10−9).Being highly mucoadhesive and showing excellent instantaneous gelling properties, the novel gelatin derivative might be a promising tool for the design of mucoadhesive drug delivery systems.
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Journal: European Polymer Journal - Volume 73, December 2015, Pages 268–277