Development and evaluation of sodium alginate-basil seeds mucilage beads as a suitable carrier for controlled release of metformin

Yari, Kasra; Akbari, Iman; Yazdi, Seyed Ali Vaziri

doi:10.1016/j.ijbiomac.2020.04.111

Cited by 17 publications

(4 citation statements)

References 31 publications

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“…The diversity in functionalities such as NH 2 , COOH, and OH groups, allowance of chemical alteration in regards to the target site, and potential for enzymatic modification makes coupling of alginate with mucilage efficacious in terms of desired biochemical and mechanical characteristics, in addition to regulating apt drug release and swelling. 15 Cydonia oblonga mucilage (COM) is extruded from quince seed coats, traditionally known as baihi-dana. It is a hydrogel in nature with an increased manifold swelling index in comparison with that of various other medicinally revered polysaccharides such as guar gum.…”

Section: Introductionmentioning

confidence: 99%

“…A popular current practice prevailing is the blending of alginate microspheres with suitable mucoadhesive biopolymers by ionotropic gelation. , To increase the drug delivery intelligence of these delivery tools and make them more stable, the use of plant mucilage seems to be a way. The diversity in functionalities such as NH 2 , COOH, and OH groups, allowance of chemical alteration in regards to the target site, and potential for enzymatic modification makes coupling of alginate with mucilage efficacious in terms of desired biochemical and mechanical characteristics, in addition to regulating apt drug release and swelling …”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl

et al. 2023

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In recent years, attention has shifted toward the utilization of natural polymers for encapsulation and sustained release of health-hazardous drugs. The purpose of this work is to define and assess the sustained delivery potential and mucoadhesive potential of a Cydonia oblonga mucilage (COM) and sodium alginate (Na-Alg)-constituting polymeric delivery carrier of antidiabetic drugs with a specific end goal to retain metformin HCl in the stomach while expanding the drug’s bioavailability. Metformin HCl was encapsulated in mucoadhesive microspheres by an ionic gelation method. Polymers with different combinations were tried, and the resulting mucoadhesive COM/Na-Alg microspheres were assessed for particle size (mm) PS/Y1, drug encapsulation efficiency DEE (%)/Y2, and in vitro percentage cumulative drug release R12h/Y3 using Drug Design Expert software version 10. The response surface methodology by a 32-central composite design predicted optimal synthesis parameters for the microspheres to be 295 mg for COM and 219 mg for Na-Alg. An optimized formulation was prepared under these conditions and used to evaluate the micrometric properties, morphology and structural characteristics, swelling behavior, in vitro drug release, and kinetics. Acute toxicity studies were carried out on blank COM/Na-Alg microspheres to deem them safe for in vivo studies. The DEE (%) was calculated to be 85.8 ± 1.67, whereas scanning electron microscopy (SEM) showed a coarse surface with characteristic wrinkles and cracks with an optical microscopic particle size of 0.96 ± 2.45. The ex vivo tests showed great mucoadhesive properties and good swelling behavior with pH-responsive drug release and a significant reduction in in vivo blood glucose levels. The results advocated the use of optimized microspheres to enhance the bioactivity with a possible dose reduction, making it less symptomatic, reducing the expense of the treatment, and subsequently facilitating better patient compliance.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl

et al. 2023

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“…In addition, microparticles, owing to their small size, can spread out over the small intestine, resulting in improving drug absorption, decreasing dose-dumping risk, and allowing preprogrammed GI tract transit [ 11 , 35 , 37 ]. Several natural or synthetic polymeric materials have been investigated for microencapsulation of MTF [ 11 , 33 , 38 , 39 , 40 , 41 , 42 , 43 ]. Of these natural polymers, the polyanionic calcium alginate (ALG) biopolymer, which has been extensively investigated in interesting controlled drug delivery systems owing to its pH-sensitivity, biocompatibility, non-toxicity, and decent muco-adhesion properties [ 11 , 44 , 45 ].…”

Section: Introductionmentioning

confidence: 99%

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

2021

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We developed a dual microencapsulation platform for the type 2 diabetes drug metformin (MTF), which is aimed to increase its bioavailability. We report the use of Lycopodium clavatum sporopollenin (LCS), derived from their natural spores, and raw Phoenix dactylifera L. (date palm) pollens (DPP) for MTF microencapsulation. MTF was loaded into LCS and DPP via a vacuum and a novel method of hydration-induced swelling. The loading capacity (LC) and encapsulation efficiency (EE) percentages for MTF-loaded LCS and MTF-loaded DPP microcapsules were 14.9% ± 0.7, 29.8 ± 0.8, and 15.2% ± 0.7, 30.3 ± 1.0, respectively. The release of MTF from MTF-loaded LCS microcapsules was additionally controlled by re-encapsulating the loaded microcapsules into calcium alginate (ALG) microbeads via ionotropic gelation, where the release of MTF was found to be significantly slower and pH-dependent. The pharmacokinetic parameters, obtained from the in vivo study, revealed that the relative bioavailability of the MTF-loaded LCS-ALG beads was 1.215 times higher compared to pure MTF, following oral administration of a single dose equivalent to 25 mg/kg body weight MTF to streptozotocin (STZ)-induced diabetic male Sprague-Dawley rats. Significant hypoglycemic effect was obtained for STZ-induced diabetic rats orally treated with MTF-loaded LCS-ALG beads compared to control diabetic rats. Over a period of 29 days, the STZ-induced diabetic rats treated with MTF-loaded LCS-ALG beads showed a decrease in the aspartate aminotransferase (AST), alanine aminotransferase (ALT), triglycerides, cholesterol, and low-density lipoprotein-cholesterol (LDL-C) levels, as well as an increase in glutathione peroxidase (GPx) and a recovery in the oxidative stress biomarker, lipid peroxidation (LPx). In addition, histopathological studies of liver, pancreas, kidney, and testes suggested that MTF-loaded LCS-ALG beads improved the degenerative changes in organs of diabetic rats. The LCS-ALG platform for dual encapsulation of MTF achieved sustained MTF delivery and enhancement of bioavailability, as well as the improved biochemical and histopathological characteristics in in vivo studies, opening many other intriguing applications in sustained drug delivery.

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Pharmaceutical Applications of Various Natural Gums and Mucilages

Prajapati¹,

Desai²,

Gandhi³

et al. 2022

Reference Series in Phytochemistry

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Development and evaluation of sodium alginate-basil seeds mucilage beads as a suitable carrier for controlled release of metformin

Cited by 17 publications

References 31 publications

Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl

Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

Pharmaceutical Applications of Various Natural Gums and Mucilages

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