Synthesis, Characterization, In Silico Analysis, and Pharmacological Evaluation of Metoprolol-Modified Saccharide Conjugates for Cardiovascular Targeting

Autor: Smita T. Kumbhar, Manish S. Bhatia, Shitalkumar Shivgonda Patil
Rok vydání: 2021
Předmět:
Zdroj: Journal of Pharmaceutical Innovation. 17:921-930
ISSN: 1939-8042
1872-5120
Popis: Targeted drug delivery to selective cell has emerged as one of the most significant areas of biomedical engineering research today, so to optimize the therapeutic efficacy of a drug by localizing strictly its pharmacological action to a pathophysiologically relevant tissue system. The current study is aimed to develop saccharide conjugates for targeted delivery of metoprolol, the cardio-selective β-blocker. The examination was done in two significant steps. The initial step includes synthesis of modified saccharides (MS). These MS were used for synthesis of metoprolol-modified saccharide conjugates (MET-MS). The chemical modification of saccharides was evaluated for its swellability and HLB followed by FTIR and DSC. The affirmation of conjugate synthesis was finished by melting point and TLC as primary parameters followed by HR-MS, FTIR, DSC, and [1] H NMR study. Drug release analysis and cellular uptake study examination were completed utilizing H9c2 cell lines. Brine shrimp lethality bioassay was done to research the cytotoxicity of synthesized conjugates. The rate lethality and LC50 values were dictated by contrasting the mean enduring hatchlings of the test and control tubes. In silico examination was performed to evaluate the possible binding of the developed conjugates with the GLUT-4. Homology model of the GLUT-4 was created utilizing SWISS MODEL server.
Databáze: OpenAIRE
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