Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

Maestrelli, Francesca; Mura, Paola; González-Rodrı́guez, Marı́a Luisa; Rabasco, A. M.; Mannelli, Lorenzo Di Cesare; Ghelardini, Carla

doi:10.1016/j.ijpharm.2017.07.083

Cited by 46 publications

(14 citation statements)

References 61 publications

(63 reference statements)

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“…The surface morphology of the beads is shown in the SEM images in Figure 5 C–F, where no visible surface cracks, wrinkles, or MTF accumulation were observed, indicative of the effectiveness of the protocol used. This is in contrast to previous studies where such surface issues were often reported in MTF-polymer beads [ 45 , 48 ] and microcapsules [ 49 ] due to the collapse of the polymer network upon drying. Figure 5 E,F represents the beads’ surface at high magnifications, where the individual MTF-loaded LCS microcapsules can be clearly seen, some of them coated by the ALG polymer (indicated by arrows).…”

Section: Resultscontrasting

confidence: 89%

“…For the MTF-loaded LCS-ALG beads, the slowest release of MTF in SGF compared to other formulations could be attributed to the dual encapsulation platform used, where MTF needs to be transported through two layers: the LCS shells where it was initially encapsulated and the second ALG polymer that covered the LCS microcapsules. In addition, it was shown that, for ALG in SGI, water-insoluble alginic acid is formed as a result of the protonation of the carboxylate groups of ALG polymer, resulting in limited swelling of the ALG that in turn impeded the release of the drug [ 38 , 49 ]. The situation was different in SIF where the ionotropically gelled ALG was found to swell and allowed faster drug release as a result of electrostatic repulsion between polymer chains in alkaline media, as reported in other studies [ 38 , 49 , 84 ].…”

Section: Resultsmentioning

confidence: 99%

“…In addition, it was shown that, for ALG in SGI, water-insoluble alginic acid is formed as a result of the protonation of the carboxylate groups of ALG polymer, resulting in limited swelling of the ALG that in turn impeded the release of the drug [ 38 , 49 ]. The situation was different in SIF where the ionotropically gelled ALG was found to swell and allowed faster drug release as a result of electrostatic repulsion between polymer chains in alkaline media, as reported in other studies [ 38 , 49 , 84 ]. Therefore, the optimized MTF-loaded LCS-ALG beads were selected as a composite platform for a potential intestinal-targeted MTF release in the next in vivo study.…”

Section: Resultsmentioning

confidence: 99%

“…Hydrogel microcapsules or beads of ALG can be easily prepared at room temperature using the ionotropic gelation technique, where a divalent cation, usually Ca 2+ , crosslinks the alginate chains via the “egg-box” model [ 46 , 47 ]. However, these microparticles or beads exhibited some concerns such as a fragile structure [ 48 ], the existence of surface wrinkles and cracks, and the accumulation of the loaded drug on their surfaces [ 45 , 49 , 50 ], even when the alginate was blended with other polymers during formulations [ 48 , 51 ].…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Resultscontrasting

confidence: 89%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

2021

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“…Whatman filter paper and following suitable dilution absorbance was measured in UV at 268 nm; to measure the concentration of the drug. The EE (%) was calculated using the following formula: 17…”

Section: Characterization Of Phytosomesmentioning

confidence: 99%

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2019

IJPSR

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Present work is aimed at development and characterization of phytosomes, novel drug delivery dosage form used to improve the bioavailability of the drug, containing ethanolic, aqueous, dichloromethane and ethyl acetate extract of Citrullus colocynthis to meet the need for better effectiveness and safety. Required phytosomal formulations were developed using different extracts of Citrullus colocynthis and phytosomes formed from the lecithin and cholesterol, then characterized. Characterization involved various parameters, such as Particle size determination, apparent solubility, entrapment efficiency, Scanning Electron Microscope, Fourier-Transform Infrared Spectroscopy, X-ray Diffraction (XRD), and dissolution study (in-vitro drug release). Particle size varied from 250 nm to 0.1 µm depending on the extract. The mean particle size of phytosomal complex of DCM extract of CC was scattered in a narrow range of 254 ± 20.0 nm, and polydispersity index was 0.857 ± 0.055, where phytosomal formulation of DCM extract shows better entrapment then other phytosomal formulation. Photomicrographs revealed that phytosomes were spherical in shape and uniform in size.

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Quantification of BSA-loaded chitosan/oligonucleotide nanoparticles using reverse-phase high-performance liquid chromatography

et al. 2018

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Therapeutic proteins are administered subcutaneously because of their instability in the gastrointestinal tract. Current research suggests that polymeric-based nanoparticles, microparticles and liposomes are ideal nanocarriers to encapsulate proteins for disease management. In order to develop a successful drug delivery system, it is crucial to determine drug release profile and stability. However, the non-active excipients in polymeric formulations can influence the quantification of proteins in analytical techniques. This study investigated the effect of nine common polymers on quantification of bovine serum albumin (BSA) using RP-HPLC method. The technique offers advantages such as short analytical time, high accuracy and selectivity. In the meantime, the technique can be employed to separate proteins including BSA, insulin and pigment epithelium-derived factor (PEDF). Furthermore, the RP-HPLC method was applied to quantify the drug release pattern of a novel BSA-loaded nanoparticulate formulation in simulated gastric and intestinal fluids. The nanoparticles were formulated by natural polymer (chitosan) and oligonucleotide (Dz13Scr) using complex coacervation. The prepared particles were found to have small size (337.87 nm), low polydispersity index (0.338) and be positively charged (10.23 mV). The in vitro drug release patterns were characterised using the validated RP-HPLC method over 12 h. Graphical abstract ᅟ.

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Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

Cited by 46 publications

References 61 publications

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

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

Untitled

Quantification of BSA-loaded chitosan/oligonucleotide nanoparticles using reverse-phase high-performance liquid chromatography

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