scholarly journals Controlled Release of Chlorogenic Acid from Polyvinyl Alcohol/Poly(γ-Glutamic Acid) Blended Electrospun Nanofiber Mats with Potential Applications in Diabetic Foot Treatment

Polymers ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 2943
Author(s):  
Isela Sandoval-Herrera ◽  
Jorge Romero-García ◽  
Antonio Ledezma-Pérez ◽  
Carmen Alvarado-Canché ◽  
Román Torres-Lubian ◽  
...  
Keyword(s):  
Polyvinyl Alcohol ◽  
Glutamic Acid ◽  
Chlorogenic Acid ◽  
Diabetic Foot ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Electrospun Nanofibers ◽  
Potential Applications ◽  
Release Analysis

This work biosynthesized poly(γ-glutamic acid) (γ-PGA) produced by Bacillus licheniformis ATCC-9945a. This material was utilized to prepare electrospun nanofibers with solutions of 10% polyvinyl alcohol (PVA) (w/v) mixed with γ-PGA at 5 and 10% w/v, intended as a wound dressing for diabetic foot treatment. These solutions were loaded with chlorogenic acid (CGA), an active hypoglycemic agent. Morphological analysis showed a decrease in size of the fibers with the combination of PVA/γ-PGA compared to pure PVA nanofibers, which was attributed to the hydrogen bonding interactions between the glutaraldehyde vapors, γ-PGA, and PVA that permitted nanofiber cross-linking and allowed CGA release. The in vitro release analysis showed that the PVA membranes reached 28% delivery after the first 24 h. Notably, the nanofiber mat with PVA blended with 5% γ-PGA reached 57% delivery, and the PVA nanofiber with 10% γ-PGA reached 66% release after the same amount of time. The rate constant for the release kinetics showed that PVA with 5% γ-PGA had a higher value than that of the other samples, reaching saturation first.

scholarly journals Fabrication and Sustained Release of Chlorogenic Acid from Poly(vinyl alcohol)/Poly(γ-glutamic Acid) Blends Electrospun Mats

2020 ◽  
Author(s):  
I. E. Sandova-Herrera ◽  
A. Ledezma-Pérez ◽  
A. De-León ◽  
C. Alvaro-Canche ◽  
R. Torres-Lubian ◽  
...  
Keyword(s):  
Polyvinyl Alcohol ◽  
Glutamic Acid ◽  
Chlorogenic Acid ◽  
Diabetic Foot ◽  
Release Kinetics ◽  
Electrospun Fiber ◽  
Diffusion Mechanism ◽  
Poly Vinyl Alcohol ◽  
Fiber Mats

Abstract Background: Diabetic foot is a condition that is caused by high levels of glucose in the blood. Poly (γ-glutamic acid) [γ-PGA]/polyvinyl alcohol [PVA] electrospun biopolymers and their use in the release of chlorogenic acid (CGA) is a promising system, thanks to their biocompatibility and the use of (CGA) in the treatment of certain symptoms of diabetic conditions. The use of CGA was reported in 2005 as a capable substance in the treatment of lesions caused by diabetic foot ulcers, thanks to the fact that it has no toxic effects.Methods: In this work, was carried out the bio-synthesis of γ-PGA producing by the Bacillus liqueniformis ATCC-9945a. This material was utilized in the preparation of electrospun nanofibers with solutions of polyvinyl alcohol [PVA] to 10% p/v mixed with γ-PGA to 5 and 10% p/v. These solutions were loaded with chlorogenic acid (CGA) like an active hypoglycemic agent.Results: The morphological analysis shows a size decrease for the fiber with PVA/ γ -PGA, compared to PVA nanofibers; this could be attributed to the hydrogen bonding interactions between γ-PGA and PVA. The use of glutaraldehyde vapors permit the nanofibers crosslinking to maintain a stable structure and allows the CGA release. The in vitro release analysis shows that the PVA membranes reach 28% of delivery after the first 24 hours. Instead of, for the nanofiber mat with PVA blended with γ-PGA at 5% goes up to 57% and nanofiber PVA/γ-PGA at 10% reach to 66% in the same time, the rate constant for release kinetics shows that PVA/γ-PGA at 5% it's higher than the others, being the first in reach the saturation.Conclusions: Biodegradable polymer meshes were fabricated by electrospinning of PVA and PVA/γ-PGA polymer and loaded with CGA. The presence of γ-PGA into PVA solutions increases the in vitro drug release from electrospun fiber mats. The maximal release of CGA was reached at 10% of γ-PGA introduced in the PVA solution, which was 82% release from the electrospun polymer fiber mats. Finally, the use of Peppas and Weibull models indicates the released kinetics of CGA from PVA, PVA/γ-PGA 5, and PVA/γ-PGA 10 electrospun fiber mats are driven by diffusion mechanism.

Preparation, characterization, and in vitro release kinetics of doxorubicin-loaded magnetosomes

2021 ◽  
pp. 088532822110605
Author(s):  
Shuang Zhang ◽  
Xinxin Fan ◽  
Guojing Zhang ◽  
Weidong Wang ◽  
Lei Yan
Keyword(s):  
Particle Size ◽  
Physical Adsorption ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Mechanism ◽  
Target Drug Delivery ◽  
Target Drug ◽  
Potential Applications ◽  
Release Data

The doxorubicin (DOX) was successfully coupled to the magnetosomes from Acidithiobacillus ferrooxidans ( At. ferrooxidans) by genipin bridging. The parameters (magnetosome concentration, DOX concentration, genipin concentration-, and cross-link time) expected for temperature significantly influenced the coupling rate. Bacterial magnetosome-doxorubicin complexes (BMDCs) were characterized by transmission electron microscope (TEM), particle size analyzer and Fourier transform infrared spectroscopy. Results indicated that BMDCs exhibited a mean particle size of 83.98 mm and displayed a negative charge. The chemical reaction occurring between CO and NH group and the physical adsorption predominated by electrostatic interaction were found to involve in coupling. BMDCs can release 40% of DOX in simulated gastrointestinal conditions within 38 h. Kinetic models including Higuchi, Korsmeyer–Peppas, Zero order, First order, Hixon-Crowell, Baker-Lonsdale, and Weibull and Gompertz were utilized to explore the release mechanism of DOX from BMDCs. All models were found to fit well (r2 ≥ 0.8144) with the release data and the Gompertz was the best fit model (r2 = 0.9742), implying that the complex mechanisms involving Fickian and Gompertz diffusion contributed to the release. These findings suggested that magnetosomes from At. ferrooxidans have great potential applications in biomedical and clinical fields as the carrier of target drug delivery systems in the future.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

scholarly journals Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia Catechu Extracts: Microencapsulation and In Vitro Release Study

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1655
Author(s):  
Zvezdelina Yaneva ◽  
Donika Ivanova ◽  
Nikolay Popov
Keyword(s):  
Composite System ◽  
Release Kinetics ◽  
Spectral Characteristics ◽  
In Vitro Release ◽  
Medium Ph ◽  
Release Capacity ◽  
Bioactive Substance ◽  
Acacia Catechu ◽  
Vitro Release

The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich Acacia catechu extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

scholarly journals Design and characterization of 3D printed, neomycin-eluting poly-L-lactide mats for wound-healing applications

2021 ◽  
Vol 32 (4) ◽  
Author(s):  
Mahima Singh ◽  
Sriramakamal Jonnalagadda
Keyword(s):  
Release Kinetics ◽  
Biological Properties ◽  
In Vitro Dissolution ◽  
3D Printer ◽  
Topical Antibiotic ◽  
Young’S Moduli ◽  
Base Polymer ◽  
Potential Applications ◽  
3D Printed

AbstractThis study evaluates the suitability of 3D printed biodegradable mats to load and deliver the topical antibiotic, neomycin, for up to 3 weeks in vitro. A 3D printer equipped with a hot melt extruder was used to print bandage-like wound coverings with porous sizes appropriate for cellular attachment and viability. The semicrystalline polyester, poly-l-lactic acid (PLLA) was used as the base polymer, coated (post-printing) with polyethylene glycols (PEGs) of MWs 400 Da, 6 kDa, or 20 kDa to enable manipulation of physicochemical and biological properties to suit intended applications. The mats were further loaded with a topical antibiotic (neomycin sulfate), and cumulative drug-release monitored for 3 weeks in vitro. Microscopic imaging as well as Scanning Electron Microscopy (SEM) studies showed pore dimensions of 100 × 400 µm. These pore dimensions were achieved without compromising mechanical strength; because of the “tough” individual fibers constituting the mat (Young’s Moduli of 50 ± 20 MPa and Elastic Elongation of 10 ± 5%). The in vitro dissolution study showed first-order release kinetics for neomycin during the first 20 h, followed by diffusion-controlled (Fickian) release for the remaining duration of the study. The release of neomycin suggested that the ability to load neomycin on to PLLA mats increases threefold, as the MW of the applied PEG coating is lowered from 20 kDa to 400 Da. Overall, this study demonstrates a successful approach to using a 3D printer to prepare porous degradable mats for antibiotic delivery with potential applications to dermal regeneration and tissue engineering.

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

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.

scholarly journals Antimicrobial Properties and Release Profile of Ampicillin from Electrospun Poly(εepsilon;-caprolactone) Nanofiber Yarns

2010 ◽  
Vol 5 (4) ◽  
pp. 155892501000500 ◽  
Author(s):  
Hang Liu ◽  
Karen K. Leonas ◽  
Yiping Zhao
Keyword(s):  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Fiber Surface ◽  
Electrospun Nanofibers ◽  
Release Profile ◽  
Burst Release ◽  
Spun Yarns ◽  
Surgical Sutures ◽  
Release Model

Poly(εepsilon;-caprolactone) (PCL) electrospun fibers containing ampicillin sodium salt have been produced and twisted into nanofiber yarns. The fiber diameters and crystallinity, the in vitro antimicrobial properties of the yarns, and the in vitro release of ampicillin from yarns containing various ampicillin concentrations are studied. Decreased fiber diameters and reduced diameter variation are observed with the addition of ampicillin salt into the polymer solution. The results from the zone of inhibition test of the yarns against both gram-positive Staphylococcus aureus and gram-negative Klebsiella pneumoniae indicate that the released ampicillin retains its effectiveness after the production processes, therefore the as-spun yarns are antimicrobial active. A burst release of ampicillin from the yarns has been observed in the first hour, and the release is almost completed in 96 hours. The burst release is believed to be due to the low compatibility of ampicillin with PCL, the accumulation of ampicillin on fiber surface and the small fiber diameters. An empirical release model is developed to describe the release profile. The results indicate that the electrospun nanofibers yarns will have a great potential to be used for biomaterials, such as surgical sutures, to decrease the surgical site infection rate.

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