Controlled Release of Metformin Hydrochloride from Core-Shell Nanofibers with Fish Sarcoplasmic Protein

Background and Objectives: A coaxial electrospinning technique was used to produce core/shell nanofibers of a polylactic acid (PLA) as a shell and a polyvinyl alcohol (PVA) containing metformin hydrochloride (MH) as a core. Materials and Methods: Fish sarcoplasmic protein (FSP) was extracted from fresh bonito and incorporated into nanofiber at various concentrations to investigate the influence on properties of the coaxial nanofibers. The morphology, chemical structure and thermal properties of the nanofibers were studied. Results: The results show that uniform and bead-free structured nanofibers with diameters ranging from 621 nm to 681 nm were obtained. A differential scanning calorimetry (DSC) analysis shows that FSP had a reducing effect on the crystallinity of the nanofibers. Furthermore, the drug release profile of electrospun fibers was analyzed using the spectrophotometric method. Conclusions: The nanofibers showed prolonged and sustained release and the first order kinetic seems to be more suitable to describe the release. MTT assay suggests that the produced drug and protein loaded coaxial nanofibers are non-toxic and enhance cell attachment. Thus, these results demonstrate that the produced nanofibers had the potential to be used for diabetic wound healing applications.

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Stability and Influence of Storage Conditions on Nanofibrous Film Containing Tooth Whitening Agent

Pharmaceutics ◽

10.3390/pharmaceutics13040449 ◽

2021 ◽

Vol 13 (4) ◽

pp. 449

Author(s):

Siriporn Okonogi ◽

Adchareeya Kaewpinta ◽

Pisaisit Chaijareenont

Keyword(s):

Water Absorption ◽

Storage Condition ◽

Storage Conditions ◽

Scanning Calorimetry ◽

Adhesive Properties ◽

Tooth Whitening ◽

Electrospinning Technique ◽

Long Term Storage ◽

Whitening Agent ◽

Nanofibrous Structure

Carbamide peroxide (CP), a tooth whitening agent, is chemically unstable. The present study explores stability enhancement of CP by loading in a nanofibrous film (CP-F) composed of polyvinyl alcohol/polyvinylpyrrolidone/silica mixture, using an electrospinning technique. Kept at a temperature range of 60–80 °C for 6 h, CP in CP-F showed significantly higher stability than that in a polymer solution and in water, respectively. Degradation of CP in CP-F could be described by the first order kinetics with the predicted half-life by the Arrhenius equation of approximately 6.52 years. Physicochemical properties of CP-F after long-term storage for 12 months at different temperatures and relative humidity (RH) were investigated using scanning electron microscopy, X-ray diffractometry, differential scanning calorimetry, and Fourier transform infrared spectroscopy. It was found that high temperature and high humidity (45 °C/75% RH) could enhance water absorption and destruction of the nanofibrous structure of CP-F. Interestingly, kept at 25 °C/30% RH, the nanofibrous structure of CP-F was not damaged, and exhibited no water absorption. Moreover, the remaining CP, the mechanical properties, and the adhesive properties of CP-F were not significantly changed in this storage condition. It is concluded that the developed CP-F and a suitable storage condition can significantly improve CP stability.

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Biocompatibility studies of polyurethane electrospun membranes based on arginine as chain extender

Journal of Materials Science Materials in Medicine ◽

10.1007/s10856-021-06581-z ◽

2021 ◽

Vol 32 (9) ◽

Author(s):

Georgina Alejandra Venegas-Cervera ◽

Andrés Iván Oliva ◽

Alejandro Avila-Ortega ◽

José Manuel Cervantes-Uc ◽

Leydi Maribel Carrillo-Cocom ◽

...

Keyword(s):

Fourier Transforms ◽

Cell Attachment ◽

Human Fibroblasts ◽

Gel Permeation Chromatography ◽

Electrospinning Process ◽

Chain Extender ◽

Cellular Interaction ◽

Scanning Calorimetry ◽

Polyurethane Membranes ◽

Electrospun Membranes

AbstractElectrospun polymers are an example of multi-functional biomaterials that improve the material-cellular interaction and aimed at enhancing wound healing. The main objective of this work is to fabricate electrospun polyurethane membranes using arginine as chain extender (PUUR) in order to test the fibroblasts affinity and adhesion on the material and the polymer toxicity. Polyurethane membranes were prepared in two steps: (i) the polyurethane synthesis, and ii) the electrospinning process. The membranes were characterized by scanning electron microscopy (SEM), Fourier transforms infrared spectroscopy, gel permeation chromatography, and differential scanning calorimetry techniques. The evaluation of PUUR as a scaffolding biomaterial for growing and developing of cells on the material was realized by LIVE/DEAD staining. The results show that the fluorescent surface area of human fibroblasts (hFB), was greater in control dense membranes made from Tecoflex than in electrospun and dense PUUR. From SEM analysis, the electrospun membranes show relatively uniform attachment of cells with a well-spread shape, while Tecoflex dense membranes show a non-proliferating round shape, which is attributed to the fiber’s structure in electrospun membranes. The cell morphology and the cell attachment assay results reveal the well spreading of hFB cells on the surface of electrospun PUUR membranes which indicates a good response related to cell adhesion.

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Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-020-00139-6 ◽

2020 ◽

Vol 6 (1) ◽

Author(s):

Chukwuebuka H. Ozoude ◽

Chukwuemeka P. Azubuike ◽

Modupe O. Ologunagba ◽

Sejoro S. Tonuewa ◽

Cecilia I. Igwilo

Keyword(s):

Controlled Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Carrier ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Metformin Hydrochloride ◽

Scanning Calorimetry ◽

Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

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In Situ Vapor Polymerization of Poly(3,4-ethylenedioxythiophene) Coated SnO2-Fe2O3 Continuous Electrospun Nanotubes for Rapid Detection of Iodide Ions

Materials ◽

10.3390/ma11112084 ◽

2018 ◽

Vol 11 (11) ◽

pp. 2084 ◽

Cited By ~ 3

Author(s):

Xiuru Xu ◽

Wei Wang ◽

Bolun Sun ◽

Xue Zhang ◽

Rui Zhao ◽

...

Keyword(s):

In Situ Polymerization ◽

Fast Response ◽

Core Shell ◽

Current Response ◽

Electrospinning Technique ◽

Iodide Ions ◽

Wide Range ◽

Vapor Phase Polymerization ◽

Fe2o3 Nanotubes

In this work poly(3,4-ethylenedioxythiophene) (PEDOT) coated SnO2-Fe2O3 continuous nanotubes with a uniform core–shell structure have been demonstrated for rapid sensitive detection of iodide ions. The SnO2-Fe2O3 nanotubes were firstly fabricated via an electrospinning technique and following calcination process. An in situ polymerization approach was then performed to coat a uniform PEDOT shell on the surface of as-prepared SnO2-Fe2O3 nanotubes by vapor phase polymerization, using Fe2O3 on the surface of nanotubes as an oxidant in an acidic condition. The resultant PEDOT@SnO2-Fe2O3 core-shell nanotubes exhibit a fast response time (~4 s) toward iodide ion detection and a linear current response ranging from 10 to 100 μM, with a detection limit of 1.5 μM and sensitivity of 70 μA/mM/cm2. The facile fabrication process and high sensing performance of this study can promote a wide range of potential applications in human health monitoring and biosensing systems.

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FORMULATION AND EVALUATION OF FUROSEMIDE LIQUISOLID COMPACT

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i6.21458 ◽

2017 ◽

Vol 9 (6) ◽

pp. 39

Author(s):

Zainab E. Jassim

Keyword(s):

Dissolution Rate ◽

Content Uniformity ◽

Drug Release Profile ◽

Scanning Calorimetry ◽

Polyethylene Glycol 400 ◽

Coating Materials ◽

Disintegration Time ◽

Weight Variation ◽

R Ratio

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.

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Development and Characterization of pH-Dependent Cellulose Acetate Phthalate Nanofibers by Electrospinning Technique

Nanomaterials ◽

10.3390/nano11123202 ◽

2021 ◽

Vol 11 (12) ◽

pp. 3202

Author(s):

Gustavo Vidal-Romero ◽

Virginia Rocha-Pérez ◽

María L. Zambrano-Zaragoza ◽

Alicia Del Real ◽

Lizbeth Martínez-Acevedo ◽

...

Keyword(s):

Cellulose Acetate ◽

Polymer Concentration ◽

Process Efficiency ◽

Fickian Diffusion ◽

Solvent Mixtures ◽

Cellulose Acetate Phthalate ◽

Scanning Calorimetry ◽

Electrospinning Technique ◽

Ph Dependent ◽

Release Profiles

The aim of this work was to obtain pH-dependent nanofibers with an electrospinning technique as a novel controlled release system for the treatment of periodontal disease (PD). Cellulose acetate phthalate (CAP) was selected as a pH-sensitive and antimicrobial polymer. The NF was optimized according to polymeric dispersion variables, polymer, and drug concentration, and characterized considering morphology, diameter, entrapment efficiency (EE), process efficiency (PE), thermal properties, and release profiles. Two solvent mixtures were tested, and CHX-CAP-NF prepared with acetone/ethanol at 12% w/v of the polymer showed a diameter size of 934 nm, a uniform morphology with 42% of EE, and 55% of PE. Meanwhile, CHX-CAP-NF prepared with acetone/methanol at 11% w/v of polymer had a diameter of 257 nm, discontinuous nanofiber morphology with 32% of EE, and 40% of PE. EE and PE were dependent on the polymer concentration and the drug used in the formulation. Studies of differential scanning calorimetry (DSC) showed that the drug was dispersed in the NF matrix. The release profiles of CHX from CHX-CAP-NF followed Fickian diffusion dependent on time (t0.43−0.45), suggesting a diffusion–erosion process and a matrix behavior. The NF developed could be employed as a novel drug delivery system in PD.

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Identification of the Glimepiride and Metformin Hydrochloride Physical Interaction in Binary Systems

Borneo Journal of Pharmacy ◽

10.33084/bjop.v4i2.1826 ◽

2021 ◽

Vol 4 (2) ◽

pp. 110-116

Author(s):

Fitrianti Darusman ◽

Taufik Muhammad Fakih ◽

Gina Fuji Nurfarida

Keyword(s):

Binary Systems ◽

Type Ii Diabetes Mellitus ◽

Computational Approach ◽

Metformin Hydrochloride ◽

Physical Interaction ◽

Class Iii ◽

Scanning Calorimetry ◽

Physical Interactions ◽

Dynamics Simulations ◽

Metformin Hcl

Glimepiride is often combined with metformin HCl as an oral antidiabetic in type II diabetes mellitus, which provides a complementary and synergistic effect with multiple targets for insulin secretion. Glimepiride includes class II of BCS, which solubility practically insoluble in water but high permeability, which will impact the drug's small bioavailability. In contrast, metformin HCl includes class III of BCS, which has a high solubility in water, but low permeability is absorbed approximately 50-60% in the digestive tract given orally. The co-crystallization method can be used to improve the glimepiride solubility properties and the permeability properties of metformin HCl by interrupting glimepiride with metformin HCl physically. This study aims to identify the physical interactions between glimepiride and metformin HCL using a thermal analysis of Differential Scanning Calorimetry (DSC) and then confirmed by a computational approach. Identifying the physical interactions between glimepiride and metformin HCL was carried out by plotting the melting points generated from the endothermic peaks of the DSC thermogram at various compositions versus the mole ratios of the two were further confirmed by the computational approach using PatchDock. The results of the phase diagram analysis of the binary system between glimepiride and metformin HCl show a congruent pattern, which indicates the formation of co-crystal or molecular compounds at a 1 : 1 mole ratio at 228°C. Computational approach results showed that the interaction between glimepiride and metformin HCl did not form new compounds but heterosinton formation that was stable in molecular dynamics simulations.

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Poly(L-Lactic Acid-Co-Aspartic Acid): Interactive Polymers for Tissue Engineering

MRS Proceedings ◽

10.1557/proc-394-77 ◽

1995 ◽

Vol 394 ◽

Cited By ~ 3

Author(s):

Jeffrey S. Hrkach ◽

Jean Ou ◽

Noah Lotan ◽

Robert Langer

Keyword(s):

Tissue Engineering ◽

Lactic Acid ◽

Cell Growth ◽

Aspartic Acid ◽

Biodegradable Polymers ◽

Cell Attachment ◽

Biologically Active ◽

Functional Sites ◽

Support Cell ◽

Enhance Cell Attachment

AbstractOne of the challenges in the field of tissue engineering is the development of optimal materials for use as scaffolds to support cell growth and tissue development. For this purpose, we are developing synthetic, biodegradable polymers with functional sites that provide the opportunity to covalently attach biologically active molecules to the polymers, so they can predictably interact with cells in a favorable manner to enhance cell attachment and growth. The preparation of poly(L-lactic acid-co-aspartic acid) comb-like graft copolymers from poly(L-lactic acid-co-β-benzyl-L-aspartate), and the casting of polymer films by solvent evaporation were carried out.

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Formulation and Characterization of Aceclofenac-Loaded Nanofiber Based Orally Dissolving Webs

Pharmaceutics ◽

10.3390/pharmaceutics11080417 ◽

2019 ◽

Vol 11 (8) ◽

pp. 417 ◽

Cited By ~ 12

Author(s):

Emese Sipos ◽

Nóra Kósa ◽

Adrienn Kazsoki ◽

Zoltán-István Szabó ◽

Romána Zelkó

Keyword(s):

Oral Absorption ◽

Vinyl Pyrrolidone ◽

Drug Dissolution ◽

In Vitro Dissolution ◽

Drug Release Profile ◽

Scanning Calorimetry ◽

Ft Ir ◽

Fast Dissolution ◽

Poly Vinyl Pyrrolidone

Aceclofenac-loaded poly(vinyl-pyrrolidone)-based nanofiber formulations were prepared by electrospinning to obtain drug-loaded orally disintegrating webs to enhance the solubility and dissolution rate of the poorly soluble anti-inflammatory active that belongs to the BCS Class-II. Triethanolamine-containing ternary composite of aceclofenac-poly(vinyl-pyrrolidone) nanofibers were formulated to exert the synergistic effect on the drug-dissolution improvement. The composition and the electrospinning parameters were changed to select the fibrous sample of optimum fiber characteristics. To determine the morphology of the nanofibers, scanning electron microscopy was used. Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) were applied for the solid-state characterization of the samples, while the drug release profile was followed by the in vitro dissolution test. The nanofibrous formulations had diameters in the range of few hundred nanometers. FT-IR spectra and DSC thermograms indicated the amorphization of aceclofenac, which resulted in a rapid release of the active substance. The characteristics of the selected ternary fiber composition (10 mg/g aceclofenac, 1% w/w triethanolamine, 15% w/w PVPK90) were found to be suitable for obtaining orally dissolving webs of fast dissolution and potential oral absorption.

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Special Issue: Novel Advances and Approaches in Biomedical Materials Based on Calcium Phosphates

Materials ◽

10.3390/ma12030405 ◽

2019 ◽

Vol 12 (3) ◽

pp. 405 ◽

Cited By ~ 4

Author(s):

Michael Mucalo

Keyword(s):

Calcium Phosphate ◽

Cell Attachment ◽

Calcium Phosphates ◽

Wide Spectrum ◽

Special Issue ◽

Dolomitic Marble ◽

Biomedical Materials ◽

Surface Contaminants ◽

Innovative Solutions ◽

Enhance Cell Attachment

Research on calcium phosphate use in the development and clinical application of biomedical materials is a diverse activity and is genuinely interdisciplinary, with much work leading to innovative solutions for improvement of health outcomes. This Special Issue aimed to summarize current advances in this area. The nine papers published cover a wide spectrum of topical areas, such as (1) remineralisation pastes for decalcified teeth, (2) use of statins to enhance bone formation, (3) how dolomitic marble and seashells can be processed into bioceramic materials, (4) relationships between the roughness of calcium phosphate surfaces and surface charge with the effect on human MRC osteogenic differentiation and maturation being investigated, (5) rheological and mechanical properties of a novel injectable bone substitute, (6) improving strength of bone cements by incorporating reinforcing chemically modified fibres, (7) using adipose stem cells to stimulate osteogenesis, osteoinduction, and angiogenesis on calcium phosphates, (8) using glow discharge treatments to remove surface contaminants from biomedical materials to enhance cell attachment and improve bone generation, and (9) a review on how classically brittle hydroxyapatite based scaffolds can be improved by making fibre-hydroxyapatite composites, with detailed analysis of ceramic crack propagation mechanisms and its prevention via fibre incorporation in the hydroxyapatite.

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