{"title":"Synthesis and Characterization of Baicalein-loaded Aquasomes: An <i>In vitro</i> and <i>In silico</i> Perspective for Diabetes Mellitus.","authors":"Vinay Goyal, Bhavna Kumar, Diwya Kumar Lal, Poorvi Varshney, Vijay Singh Rana","doi":"10.2174/0115701638263815231226171108","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Millions of individuals worldwide suffer from metabolic abnormalities induced by diabetes. Baicalein, a flavonoid, has shown several properties in various treatments with potential properties, including anti-inflammatory, antioxidant, and anti-diabetic properties. Practically, its application is hindered due to low solubility in aqueous media. Overcoming this challenge, aquasomes can offer an effective approach for delivering drugs and bioactive molecules to target various diseases.</p><p><strong>Objective: </strong>The study aimed to develop and evaluate baicalein-loaded aquasomes for improving solubility and comparing their antidiabetic properties to acarbose through <i>in silico</i> docking.</p><p><strong>Methods: </strong>Baicalein-loaded aquasomes were prepared through a three-step process: core preparation, lactose coating, and drug loading. The evaluation included assessing particle size, drug-excipient interactions, drug entrapment efficiency, loading capacity, <i>in vitro</i> drug release, and the kinetics of drug release. <i>In silico</i> docking and <i>in vitro</i> α-amylase inhibition activity was evaluated to assess the anti-diabetic potential of baicalein.</p><p><strong>Results: </strong>The baicalein-loaded aquasomes were spherical with sizes ranging from 300-400 nm. FTIR analysis indicated no interaction between the components. The formulation exhibited drug entrapment efficiency of 94.04±0 4.01% and drug loading of 17.60 ± 01.03%. Drug release study showed sustained and complete (97.30 ± 02.06%) release, following first-order kinetics. Docking analysis revealed comparable binding affinity to acarbose, while the α-amylase inhibition assay showed greater inhibition potential of the aquasomes compared to the baicalein solution.</p><p><strong>Conclusion: </strong>Aquasomes offer an alternative approach to conventional delivery methods. The selfassembling characteristics of aquasomes greatly simplify their preparation process, adding to their appeal as a drug delivery system.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":"e250124226209"},"PeriodicalIF":0.0000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current drug discovery technologies","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0115701638263815231226171108","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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Abstract
Background: Millions of individuals worldwide suffer from metabolic abnormalities induced by diabetes. Baicalein, a flavonoid, has shown several properties in various treatments with potential properties, including anti-inflammatory, antioxidant, and anti-diabetic properties. Practically, its application is hindered due to low solubility in aqueous media. Overcoming this challenge, aquasomes can offer an effective approach for delivering drugs and bioactive molecules to target various diseases.
Objective: The study aimed to develop and evaluate baicalein-loaded aquasomes for improving solubility and comparing their antidiabetic properties to acarbose through in silico docking.
Methods: Baicalein-loaded aquasomes were prepared through a three-step process: core preparation, lactose coating, and drug loading. The evaluation included assessing particle size, drug-excipient interactions, drug entrapment efficiency, loading capacity, in vitro drug release, and the kinetics of drug release. In silico docking and in vitro α-amylase inhibition activity was evaluated to assess the anti-diabetic potential of baicalein.
Results: The baicalein-loaded aquasomes were spherical with sizes ranging from 300-400 nm. FTIR analysis indicated no interaction between the components. The formulation exhibited drug entrapment efficiency of 94.04±0 4.01% and drug loading of 17.60 ± 01.03%. Drug release study showed sustained and complete (97.30 ± 02.06%) release, following first-order kinetics. Docking analysis revealed comparable binding affinity to acarbose, while the α-amylase inhibition assay showed greater inhibition potential of the aquasomes compared to the baicalein solution.
Conclusion: Aquasomes offer an alternative approach to conventional delivery methods. The selfassembling characteristics of aquasomes greatly simplify their preparation process, adding to their appeal as a drug delivery system.
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