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Current Drug Discovery Technologies

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ISSN (Print): 1570-1638
ISSN (Online): 1875-6220

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Research Article

Synthesis and Characterization of Baicalein-loaded Aquasomes: An In vitro and In silico Perspective for Diabetes Mellitus

Author(s): Vinay Goyal, Bhavna Kumar*, Diwya Kumar Lal, Poorvi Varshney and Vijay Singh Rana

Volume 21, Issue 5, 2024

Published on: 25 January, 2024

Article ID: e250124226209 Pages: 9

DOI: 10.2174/0115701638263815231226171108

Price: $65

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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.

Graphical Abstract

[1]
Kharroubi AT, Darwish HM. Diabetes mellitus: The epidemic of the century. World J Diabetes 2015; 6(6): 850-67.
[http://dx.doi.org/10.4239/wjd.v6.i6.850] [PMID: 26131326]
[2]
Dilworth L, Facey A, Omoruyi F. Diabetes mellitus and its metabolic complications: The role of adipose tissues. Int J Mol Sci 2021; 22(14): 7644.
[http://dx.doi.org/10.3390/ijms22147644] [PMID: 34299261]
[3]
Theyamma J, Jacquline CV. diabetes : a silent killer: A threat for cardiorespiratory fitness. In: cardiorespiratory fitness. IntechOpen 2022.
[4]
Westman EC. Type 2 diabetes mellitus: A pathophysiologic perspective. Front Nutr 2021; 8: 707371.
[http://dx.doi.org/10.3389/fnut.2021.707371] [PMID: 34447776]
[5]
Tan SY, Mei Wong JL, Sim YJ, et al. Type 1 and 2 diabetes mellitus: A review on current treatment approach and gene therapy as potential intervention. Diabetes Metab Syndr 2019; 13(1): 364-72.
[http://dx.doi.org/10.1016/j.dsx.2018.10.008] [PMID: 30641727]
[6]
Dirir AM, Daou M, Yousef AF, Yousef LF. A review of alpha glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes. Phytochem Rev 2022; 21(4): 1049-79.
[http://dx.doi.org/10.1007/s11101-021-09773-1] [PMID: 34421444]
[7]
Li K, Yao F, Xue Q, et al. Inhibitory effects against α-glucosidase and α-amylase of the flavonoids-rich extract from Scutellaria baicalensis shoots and interpretation of structure–activity relationship of its eight flavonoids by a refined assign-score method. Chem Cent J 2018; 12(1): 82.
[http://dx.doi.org/10.1186/s13065-018-0445-y] [PMID: 30003449]
[8]
Mechchate H, Es-safi I, Louba A, et al. In vitro alpha-amylase and alpha-glucosidase inhibitory activity and in vivo antidiabetic activity of Withania frutescens L. Foliar Extract. Molecules 2021; 26(2): 293.
[http://dx.doi.org/10.3390/molecules26020293] [PMID: 33430115]
[9]
Thilagam E, Parimaladevi B, Kumarappan C, Chandra Mandal S. α-Glucosidase and α-amylase inhibitory activity of senna surattensis. J Acupunct Meridian Stud 2013; 6(1): 24-30.
[http://dx.doi.org/10.1016/j.jams.2012.10.005] [PMID: 23433052]
[10]
Khoo CM. International Encyclopedia of Public Health. (2nd ed.). Oxford: Academic Press 2017; pp. 288-93.
[http://dx.doi.org/10.1016/B978-0-12-803678-5.00108-9]
[11]
Oyedemi SO, Oyedemi BO, Ijeh II, Ohanyerem PE, Coopoosamy RM, Aiyegoro OA. Alpha-amylase inhibition and antioxidative capacity of some antidiabetic plants used by the traditional healers in southeastern nigeria. ScientificWorldJournal 2017; 2017: 1-11.
[http://dx.doi.org/10.1155/2017/3592491] [PMID: 28367491]
[12]
Palanisamy S, Yien E, Shi L, et al. Systematic review of efficacy and safety of newer antidiabetic drugs approved from 2013 to 2017 in controlling HbA1c in diabetes patients. Pharmacy 2018; 6(3): 57.
[http://dx.doi.org/10.3390/pharmacy6030057] [PMID: 29954090]
[13]
Kim DH, Hossain MA, Kang YJ, et al. Baicalein, an active component of Scutellaria baicalensis Georgi, induces apoptosis in human colon cancer cells and prevents AOM/DSS-induced colon cancer in mice. Int J Oncol 2013; 43(5): 1652-8.
[http://dx.doi.org/10.3892/ijo.2013.2086] [PMID: 24008356]
[14]
Fu Y, Luo J, Jia Z, et al. Baicalein protects against type 2 diabetes via promoting islet β -cell function in obese diabetic mice. Int J Endocrinol 2014; 2014: 1-13.
[http://dx.doi.org/10.1155/2014/846742] [PMID: 25147566]
[15]
Varsha K, Sharma A, Kaur A, et al. Natural plant-derived anticancer drugs nanotherapeutics: A review on preclinical to clinical success.Nanostructures for Cancer Therapy. Elsevier 2017; pp. 775-809.
[http://dx.doi.org/10.1016/B978-0-323-46144-3.00028-3]
[16]
Kwak HJ, Yang D, Hwang Y, Jun HS, Cheon HG. Baicalein protects rat insulinoma INS-1 cells from palmitate-induced lipotoxicity by inducing HO-1. PLoS One 2017; 12(4): e0176432.
[http://dx.doi.org/10.1371/journal.pone.0176432] [PMID: 28445528]
[17]
Yang JR, Luo JG, Kong LY. Determination of α-glucosidase inhibitors from ScutScutellaria baicalensis using liquid chromatography with quadrupole time of flight tandem mass spectrometry coupled with centrifugal ultrafiltration. Chin J Nat Med 2015; 13(3): 208-14.
[http://dx.doi.org/10.1016/S1875-5364(15)30006-6] [PMID: 25835365]
[18]
Gu C, Zhang H, Putri CY, Ng K. Evaluation of α-amylase and α-glucosidase inhibitory activity of flavonoids. Int J Food Nutr Sci 2015; 2(2): 174-9.
[19]
Aliakbari F, Shabani AA, Bardania H, et al. Formulation and anti-neurotoxic activity of baicalein-incorporating neutral nanoliposome. Colloids Surf B Biointerfaces 2018; 161: 578-87.
[http://dx.doi.org/10.1016/j.colsurfb.2017.11.023] [PMID: 29149763]
[20]
Ziyan C, Chunhong L, Fucun W, Shihua Q. Research progress of active ingredients of Chinese medicine for the treatment of insulin resistance in type 2 diabetes mellitus. Hunan J Tradit Chin Med 2019; 35(12): 127-9.
[21]
Yingrui W, Zheng L, Guoyan L, Hongjie W. Research progress of active ingredients of Scutellaria baicalensis in the treatment of type 2 diabetes and its complications. Biomed Pharmacother 2022; 148: 112690.
[http://dx.doi.org/10.1016/j.biopha.2022.112690] [PMID: 35158145]
[22]
Xu X, Shi F, Wei Z, Zhao Y. Nanostructured lipid carriers loaded with baicalin: An efficient carrier for enhanced antidiabetic effects. Pharmacogn Mag 2016; 12(47): 198-202.
[http://dx.doi.org/10.4103/0973-1296.186347] [PMID: 27601850]
[23]
Jain S S, Jagtap P S, Dand N M, Jadhav K R, Kadam V J. Aquasomes: A novel drug carrier J App Pharmac Sci 2012; 184-92.
[24]
Umashankar MS, Sachdeva RK, Gulati M. Aquasomes: A promising carrier for peptides and protein delivery. Nanomedicine 2010; 6(3): 419-26.
[http://dx.doi.org/10.1016/j.nano.2009.11.002] [PMID: 19931422]
[25]
Damera DP, Kaja S, Janardhanam LSL, Alim S, Venuganti VVK, Nag A. Synthesis, detailed characterization, and dual drug delivery application of BSA Loaded Aquasomes. ACS Appl Bio Mater 2019; 2(10): 4471-84.
[http://dx.doi.org/10.1021/acsabm.9b00635] [PMID: 35021407]
[26]
Asfour MH. Advanced trends in protein and peptide drug delivery: A special emphasis on aquasomes and microneedles techniques. Drug Deliv Transl Res 2021; 11(1): 1-23.
[http://dx.doi.org/10.1007/s13346-020-00746-z] [PMID: 32337668]
[27]
Banerjee S, Sen KK. Aquasomes: A novel nanoparticulate drug carrier. J Drug Deliv Sci Technol 2018; 43: 446-52.
[http://dx.doi.org/10.1016/j.jddst.2017.11.011]
[28]
Haranath C, Reddy JL, Ahad HA, Reshma T, Shubha BN. Aquasomes: A novel approach for the delivery of bioactive molecules. J med pharmac all sci 2022; 11(5): 5325-30.
[http://dx.doi.org/10.55522/jmpas.V11I5.4110]
[29]
Kutlehria A, Kaushik P, Sharma S, Kaur A. International research. J Pharm 2018; 9(8): 123-9.
[30]
Vengala DP. Carbohydrate stabilized ceramic nanoparticles for the delivery of a poorly soluble drug, lornoxicam. Asian J Pharm 2017; 11(03)
[31]
Ranjitha VR, Ravishankar VR. Extracellular synthesis of selenium nanoparticles from an actinomycetes streptomyces griseoruber and evaluation of its cytotoxicity on HT-29 Cell Line. Pharm Nanotechnol 2018; 6(1): 61-8.
[http://dx.doi.org/10.2174/2211738505666171113141010] [PMID: 29141577]
[32]
Monsef R, Salavati-Niasari M. Hydrothermal architecture of Cu5V2O10 nanostructures as new electro-sensing catalysts for voltammetric quantification of mefenamic acid in pharmaceuticals and biological samples. Biosens Bioelectron 2021; 178: 113017.
[http://dx.doi.org/10.1016/j.bios.2021.113017] [PMID: 33493895]
[33]
Lopes CE, Langoski G, Klein T, Ferrari PC, Farago PV. A simple HPLC method for the determination of halcinonide in lipid nanoparticles: development, validation, encapsulation efficiency, and in vitro drug permeation. Braz J Pharm Sci 2017; 53(2)
[http://dx.doi.org/10.1590/s2175-97902017000215250]
[34]
Lin PC, Lin S, Wang PC, Sridhar R. Techniques for physicochemical characterization of nanomaterials. Biotechnol Adv 2014; 32(4): 711-26.
[http://dx.doi.org/10.1016/j.biotechadv.2013.11.006] [PMID: 24252561]
[35]
Weng J, Tong HHY, Chow SF. In Vitro release study of the polymeric drug nanoparticles: Development and validation of a novel method. Pharmaceutics 2020; 12(8): 732.
[http://dx.doi.org/10.3390/pharmaceutics12080732] [PMID: 32759786]
[36]
Kim Y, Park EJ, Kim TW, Na DH. Recent progress in drug release testing methods of biopolymeric particulate system. Pharmaceutics 2021; 13(8): 1313.
[http://dx.doi.org/10.3390/pharmaceutics13081313] [PMID: 34452274]
[37]
Bohrey S, Chourasiya V, Pandey A. Polymeric nanoparticles containing diazepam: preparation, optimization, characterization, in-vitro drug release and release kinetic study. Nano Converg 2016; 3(1): 3.
[http://dx.doi.org/10.1186/s40580-016-0061-2] [PMID: 28191413]
[38]
Tagami T, Yamashita K, Okuyama M, Mori H, Yao M, Kimura A. Molecular basis for the recognition of long-chain substrates by plant α-glucosidases. J Biol Chem 2013; 288(26): 19296-303.
[http://dx.doi.org/10.1074/jbc.M113.465211] [PMID: 23687304]
[39]
Maurus R, Begum A, Williams LK, et al. Alternative catalytic anions differentially modulate human α-amylase activity and specificity. Biochemistry 2008; 47(11): 3332-44.
[http://dx.doi.org/10.1021/bi701652t] [PMID: 18284212]
[40]
Trott O, Olson AJ. AutoDock Vina: Improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading. J Comput Chem 2010; 31(2): 455-61.
[http://dx.doi.org/10.1002/jcc.21334] [PMID: 19499576]
[41]
Visvanathan R, Qader M, Jayathilake C, Jayawardana BC, Liyanage R, Sivakanesan R. Critical review on conventional spectroscopic α ‐amylase activity detection methods: Merits, demerits, and future prospects. J Sci Food Agric 2020; 100(7): 2836-47.
[http://dx.doi.org/10.1002/jsfa.10315] [PMID: 32031680]
[42]
Paun G, Neagu E, Albu C, Savin S, Radu GL. In Vitro evaluation of antidiabetic and anti-inflammatory activities of polyphenolic-rich extracts from Anchusa officinalis and Melilotus officinalis. ACS Omega 2020; 5(22): 13014-22.
[http://dx.doi.org/10.1021/acsomega.0c00929] [PMID: 32548486]
[43]
Zhou Y, Dong W, Ye J, et al. A novel matrix dispersion based on phospholipid complex for improving oral bioavailability of baicalein: preparation, in vitro and in vivo evaluations. Drug Deliv 2017; 24(1): 720-8.
[http://dx.doi.org/10.1080/10717544.2017.1311968] [PMID: 28436702]

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