scholarly journals A Novel Design of Tri-Layer Membrane with Controlled Delivery of Paclitaxel and Anti-Biofilm Effect for Biliary Stent Applications

Nanomaterials ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 486
Author(s):  
Abdelrahman I. Rezk ◽  
Jeesoo Park ◽  
Joon Yeon Moon ◽  
Sunny Lee ◽  
Chan Hee Park ◽  
...  
Keyword(s):  
Sustained Release ◽  
Antibacterial Effect ◽  
Release Profile ◽  
Biliary Stent ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Dual Function ◽  
Electrospinning Technique ◽  
Layer Membrane

Here, we developed a novel biliary stent coating material that is composed of tri-layer membrane with dual function of sustained release of paclitaxel (PTX) anticancer drug and antibacterial effect. The advantages of using electrospinning technique were considered for the even distribution of PTX and controlled release profile from the nanofiber mat. Furthermore, film cast method was utilized to fabricate AgNPs-immobilized PU film to direct the release towards the tumor site and suppress the biofilm formation. The in vitro antibacterial test conducted against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria species showed excellent antibacterial effect. The in vitro drug release study confirmed the sustained release of PTX from the tri-layer membrane and the release profile fitted first order with correlation coefficient of R2 = 0.98. Furthermore, the release mechanism was studied using Korsmeyer–Peppas model, revealing that the release mechanism follows Fickian diffusion. Based on the results, this novel tri-layer membrane shows curative potential in clinical development.

scholarly journals Evaluation of in vitro release kinetics of Capsaicin-loaded chitosan nanoparticles using DDSolver

2020 ◽  
Vol 11 (3) ◽  
pp. 4555-4559
Author(s):  
Narissara Kulpreechanan ◽  
Feuangthit Niyamissara Sorasitthiyanukarn
Keyword(s):  
Gastrointestinal Tract ◽  
Sustained Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
Circulatory System ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Release Study ◽  
Kinetics Of

The present aim is to evaluate the release profile and its release kinetics of encapsulated capsaicin from chitosan nanoparticles using the software DDSolver. The release study was performed by using a dialysis technique in PBS solutions with different pHs (1.2, 6.8 and 7.4) to mimics the different gastrointestinal tract and circulatory system pH ranges as a releasing medium. The nanoparticles were prepared using o/w emulsification and ionotropic gelation technique under optimal condition obtained from response surface methodology (RSM) design as described in our previous study. These nanoparticles were around 180 nm in average hydrodynamic size and encapsulation efficiency percentage around 70%, respectively. In vitro drug release study suggested that the chitosan nanoparticles can potentially use to controlled and sustained release of capsaicin over at least 96. The kinetic release analysis results by DDSolver software indicated that Weibull model was suggested to be the best dynamic models with highest R2adjusted and model selection criteria (MSC) and lowest Akaike information criterion (AIC), respectively, for capsaicin loaded chitosan nanoparticles. The release mechanism of capsaicin from nanoparticles was found to be Fickian diffusion. The results suggest that the chitosan nanoparticles can be applied for the controlled and sustained release of capsaicin in the gastrointestinal tract and circulatory system.

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Chitosan-miRNA functionalized microporous titanium oxide surfaces via a layer-by-layer approach with a sustained release profile for enhanced osteogenic activity

2020 ◽  
Vol 18 (1) ◽  
Author(s):  
Kaimin Wu ◽  
Mengyuan Liu ◽  
Nan Li ◽  
Li Zhang ◽  
Fanhui Meng ◽  
...  
Keyword(s):  
Sustained Release ◽  
Osteogenic Differentiation ◽  
Sodium Hyaluronate ◽  
Release Profile ◽  
Titanium Implants ◽  
Layer By Layer ◽  
Matrix Mineralization ◽  
In Vitro Transfection

Abstract Background The biofunctionalization of titanium implants for high osteogenic ability is a promising approach for the development of advanced implants to promote osseointegration, especially in compromised bone conditions. In this study, polyelectrolyte multilayers (PEMs) were fabricated using the layer-by-layer approach with a chitosan-miRNA (CS-miRNA) complex and sodium hyaluronate (HA) as the positively and negatively charged polyelectrolytes on microarc-oxidized (MAO) Ti surfaces via silane-glutaraldehyde coupling. Methods Dynamic contact angle and scanning electron microscopy measurements were conducted to monitor the layer accumulation. RiboGreen was used to quantify the miRNA loading and release profile in phosphate-buffered saline. The in vitro transfection efficiency and the cytotoxicity were investigated after seeding mesenchymal stem cells (MSCs) on the CS-antimiR-138/HA PEM-functionalized microporous Ti surface. The in vitro osteogenic differentiation of the MSCs and the in vivo osseointegration were also evaluated. Results The surface wettability alternately changed during the formation of PEMs. The CS-miRNA nanoparticles were distributed evenly across the MAO surface. The miRNA loading increased with increasing bilayer number. More importantly, a sustained miRNA release was obtained over a timeframe of approximately 2 weeks. In vitro transfection revealed that the CS-antimiR-138 nanoparticles were taken up efficiently by the cells and caused significant knockdown of miR-138 without showing significant cytotoxicity. The CS-antimiR-138/HA PEM surface enhanced the osteogenic differentiation of MSCs in terms of enhanced alkaline phosphatase, collagen production and extracellular matrix mineralization. Substantially enhanced in vivo osseointegration was observed in the rat model. Conclusions The findings demonstrated that the novel CS-antimiR-138/HA PEM-functionalized microporous Ti implant exhibited sustained release of CS-antimiR-138, and notably enhanced the in vitro osteogenic differentiation of MSCs and in vivo osseointegration. This novel miRNA-functionalized Ti implant may be used in the clinical setting to allow for more effective and robust osseointegration.

scholarly journals Sustained Release of Linezolid from Prepared Hydrogels with Polyvinyl Alcohol and Aliphatic Dicarboxylic Acids of Variable Chain Lengths

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 982
Author(s):  
Gustavo Carreño ◽  
Adolfo Marican ◽  
Sekar Vijayakumar ◽  
Oscar Valdés ◽  
Gustavo Cabrera-Barjas ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Polyvinyl Alcohol ◽  
Sustained Release ◽  
Release Kinetics ◽  
Dicarboxylic Acids ◽  
Release Profile ◽  
Significant Activity ◽  
Crosslinking Degree ◽  
Aliphatic Dicarboxylic Acids

A series of hydrogels with a specific release profile of linezolid was successfully synthesized. The hydrogels were synthesized by cross-linking polyvinyl alcohol (PVA) and aliphatic dicarboxylic acids, which include succinic acid (SA), glutaric acid (GA), and adipic acid (AA). The three crosslinked hydrogels were prepared by esterification and characterized by equilibrium swelling ratio, infrared spectroscopy, thermogravimetric analysis, mechanical properties, and scanning electron microscopy. The release kinetics studies of the linezolid from prepared hydrogels were investigated by cumulative drug release and quantified by chromatographic techniques. Mathematical models were carried out to understand the behavior of the linezolid release. These data revealed that the sustained release of linezolid depends on the aliphatic dicarboxylic acid chain length, their polarity, as well as the hydrogel crosslinking degree and mechanical properties. The in vitro antibacterial assay of hydrogel formulations was assessed in an Enterococcus faecium bacterial strain, showing a significant activity over time. The antibacterial results were consistent with cumulative release assays. Thus, these results demonstrated that the aliphatic dicarboxylic acids used as crosslinkers in the PVA hydrogels were a determining factor in the antibiotic release profile.

scholarly journals Formulation and Evaluation of Acyclovir Microspheres

2018 ◽  
Vol 27 (1) ◽  
pp. 1-7
Author(s):  
Pavani S ◽  
Mounika K ◽  
Naresh K
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Natural Polymers

The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride.   The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.

scholarly journals Design and Development of Antibacterial/Anti-inflammatory Dual Drug-Loaded Nanofibrous Inserts for Ophthalmic Sustained Delivery of Gentamicin and Methylprednisolone: In Vitro Bioassay, Solvent, and Method Effects’ Evaluation

2021 ◽  
Author(s):  
Shahla Mirzaeei ◽  
Donya Barfar
Keyword(s):  
Mechanical Properties ◽  
Sustained Release ◽  
In Vitro Release ◽  
Core Shell ◽  
Solvent Mixtures ◽  
Antibacterial Efficacy ◽  
Electrospinning Technique ◽  
Dual Drug ◽  
Release Profiles

Purpose: To overcome the challenges caused by the use of conventional ophthalmic dosage forms such as the fast elimination of the drug from the surface of the eye, in this study, dual drug-loaded nanofibers were developed for sustained ophthalmic delivery of Gentamicin (GNT) and Methylprednisolone (MP). Moreover, the solvent effects, polymer mixtures, and method of preparation on the release profile of the prepared nanofibers, were evaluated. Methods: The nanofibers were prepared using Polycaprolactone, Poly (lactic-co-glycolic acid), and Polyvinyl alcohol using electrospinning technique. Thereafter, seven optimized formulations were developed with different solvent mixtures and polymer concentrations using various electrospinning methods. The physicochemical and mechanical properties of nanofibers were also evaluated, and the morphology of formulations was observed. The antibacterial efficacy was investigated and the in vitro release amounts of GNT and MP from nanofibers were estimated using the bioassay and Ultraviolet-visible spectroscopy. Results: The developed G1, G4, G5, G6, and G7 had suitable mechanical properties and morphologies with diameter ranging between 70-350 nm. The 1:1 v/v ratio of DMF/DCM in the solvent mixture and using core-shell technique for the preparation, formed nanofibers with more favorable release profiles. The optimized formulations indicated sustained-release manner for both drugs during 3-9 days and the antibacterial efficacy against Staphylococcus aureus. Conclusion: Among all the prepared formulations, the nanofiber with core-shell structure possessed the best sustained-release profiles of GNT and MP. The obtained results suggest that these nanofibers have a potential to be used as an insert in the eye for long-term release of the drug.

scholarly journals EMULSOMES FOR LIPOPHILIC ANTICANCER DRUG DELIVERY: DEVELOPMENT, OPTIMIZATION AND IN VITRO DRUG RELEASE KINETIC STUDY

2021 ◽  
pp. 114-121
Author(s):  
S. DUBEY ◽  
S. P. VYAS
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Particle Diameter ◽  
Release Profile ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and characterize paclitaxel (Ptx) loaded sterically stabilized emulsomes to provide non-toxic and biocompatible carriers with high Ptx loading efficiency. Methods: Plain (P-Es) and sterically stabilized emulsomes (SS-Es) were prepared by a modified solvent evaporation method using tristearin as solid lipid and optimized for lipid to (DSPC+CHOL+DSPE-PEG)/ tristearin ratio, lipid/lipid-PEG (DSPC+CHOL/DSPE-PEG) molar ratio, solid lipid concentration, phospholipid concentration, organic to aqueous phase volume and homogenization time based on their effect particle size and entrapment efficiency. Optimized emulsomes were characterized for morphological features, in vitro drug release kinetics and protection from plasma protein. Results: The emulsomes so formed were uniform in size with a mean particle diameter of 275±5.52 and 195±6.4 nm for P-Es and SS-Es respectively. All the formulations showed pH dependent drug release with a slow and sustained release profile. Slower drug release was observed from sterically stabilized emulsomes than the plain emulsomes. The drug release profile followed the Higuchi model with the Fickian diffusion pattern. The Pegylation of emulsomes significantly reduced the in vitro protein absorption. Conclusion: The sterically stabilized emulsome can serve as a novel non-toxic platform with longer circulatory time for the delivery of Paclitaxel and other poorly water-soluble drugs as well.

scholarly journals 5-Fluorouracil Release from Chitosan-Based Matrix.Experimental and Theoretical Aspects

2020 ◽  
Vol 57 (3) ◽  
pp. 180-188
Author(s):  
Roxana Iancu ◽  
Stefan Andrei Irimiciuc ◽  
Maricel Agop ◽  
Mihail Frasila ◽  
Maria-Alexandra Paun ◽  
...  
Keyword(s):  
Drug Release ◽  
Polarized Light ◽  
Crosslinking Density ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Morphological Aspects ◽  
Drug Release Mechanism ◽  
The Matrix

A series of four drug release formulations based on 5-fluorouracil encapsulated into a chitosan-based matrix were prepared by in situ hydrogelation with 3,7-dimethyl-2,6-octadienal. The formulations were investigated from structural and morphological aspects by FTIR spectroscopy, polarized light microscopy and scanning electron microscopy. It was established that 5-fluorouracil was anchored into the matrix as crystals, whose dimension varied as a function of the crosslinking density. The in vitro drug release simulated into a media mimicking the physiological environment revealed a progressive release of the 5-fluorouracil, in close interdependence with the crosslinking density. In the context of Pharmacokinetics behavioral analysis, a new mathematical procedure for describing drug release dynamics in polymer-drug complex system is proposed. Assuming that the dynamics of polymer-drug system�s structural units take place on continuous and nondifferentiable curves (multifractal curves), we show that in a one-dimensional hydrodynamic formalism of multifractal variables the drug release mechanism (Fickian diffusion, non-Fickian diffusion, etc) are given through synchronous dynamics at a differentiable and non-differentiable scale resolutions. Finally, the model is confirmed by the empirical data.

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