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Study on Intelligent Drug Delivery System of pH Sensitive Hydrogel Loaded Carvedilol

Author: MengXun
Tutor: LiPing
School: Lanzhou University
Course: Drug analysis
Keywords: Intelligent drug delivery system pH sensitivity Hydrogel Chitosan N-succinyl chitosan Carvedilol
CLC: R943
Type: Master's thesis
Year: 2009
Downloads: 90
Quote: 0
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Abstract


Firstly, using chitosan, N-succinyl chitosan (NSC) and alginate as main intelligent carriers, pH sensitive chitosan-alginate hydrogel beads loaded carvedilol and NSC/alginate hydrogel beads loaded carvedilol were prepared respectively by the ionic gelation method in the first time.Secondly, the optimum preparation technique was investigated respectively by single factor design and orthogonal test. The physical and chemical characterizations of the two kinds of hydrogels beads were performed by SEM and FTIR.Finally, swelling behavior and release properties of the two kinds of hydrogel beads in various pH phosphate buffer solutions were investigated, and the release mechanism in vitro was researched.The results showed that the surface morphology of chitosan-alginate hydrogel beads loaded carvedilol and NSC/alginate hydrogel beads loaded carvedilol were spherical and regular, in vitro release behavior presented excellent pH sensitivity. The release of carvedilol from the chitosan-alginate hydrogel beads at pH 1.5 was relatively low (26.7%), while this value approached 89.4% at pH 7.4 within 16h. The release results in imitating gastroenteric environments indicated that carvedilol released from chitosan-alginate hydrogel beads was 21.1% within 2h in SGF (pH1.5). Meanwhile, the amount of carvedilol released approximately 81.7% after 23 hour at pH7.4. The carvedilol released from the NSC/alginate hydrogel beads at pH 2.5 was relatively low (31.40%), while this value approached 87.85% at pH 7.4 within 16h, the release in imitating gastroenteric environments from NSC/alginate bead was 26.93% within 3h in SGF (pH1.5). However, the release of carvedilol increased significantly at pH7.4, approximately 95.03% after 23 hour. The release of carvedilol from two kinds of hydrogel beads at various pH phosphate buffer solutions was analyzed by a semi-empirical equation, and it was found that the drug release mechanism was "anomalous transport" at 1.5-5.0. However, the release was due to polymer relaxation during hydrogel swelling at pH6.8-8.0.In a summary, chitosan-alginate hydrogel beads loaded carvedilol and NSC/alginate hydrogel beads loaded carvedilol can deliver carvedilol to the intestinal tract, and keep the drug release slowly and persistently. Therefore, they can be employed as promising vehicle for oral intelltgent drug delivery in the intestinal tract, minimize the possibility of side effects of carvedilol, decrease administration times and prolong administration frequency, play a good role in cardiovascular diseases.

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CLC: > Medicine, health > Pharmacy > Pharmacy > Pharmaceutics
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