Effect of Organogelator Concentration on Gelation Kinetics and Drug Release Behaviour of Paracetamol-Loaded Soybean Oleogels

Organogelators induce 3-D networked structures in apolar solvent molecules via cross-linking of non-covalent self-assembled aggregates below the gelation temperature. The objective of the present investigation was to evaluate the effects of different Span 40 concentrations on gelation kinetics and drug release behaviour of topical soybean oleogels. An inversely proportional relationship was observed between gelation time, melt flow index and concentration of Span 40 in soybean oleogels. Gompertz model was employed on gelation kinetics data to determine organogelator and oil parameters which are assumed to be associated with thermal stability and gel flexibility respectively. Formulation OGS2 (18% W/V Span 40) formed less viscous, thermally stable and presumably more flexible oleogel compared to other formulations. Nearly ideal zero-order release of paracetamol was achieved from OGS*2 following Fickian diffusion. However, slow drug release profiles, higher t50 values were observed with oleogels having 20-24% w/v Span 40 which followed Korsmeyer-Peppas kinetics with non-Fickian diffusion.

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OLEOGELS OF OLIVE OIL AND SOYBEAN OIL FOR TOPICAL DRUG DELIVERY: A COMPARATIVE ANALYSIS

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2019v11i8.34040 ◽

2019 ◽

pp. 4-10

Author(s):

DIPANJANA ASH ◽

SUTAPA BISWAS MAJEE ◽

GOPA ROY BISWAS

Keyword(s):

Drug Release ◽

Soybean Oil ◽

Olive Oil ◽

Tween 80 ◽

Melt Flow Index ◽

Release Profile ◽

Flow Index ◽

Drug Release Profile ◽

Organoleptic Evaluation ◽

Ft Ir

Objective: The objective of the present investigation was to develop olive and soybean oil-based oleogels with Span 40 and/or Tween 80 (as gelator and/or surfactant) and determine the critical gelator concentration (CGC), characterise and compare the rheological, thermal properties and drug release profile of the gels formed for topical delivery. Methods: Olive and soybean oil-based Span 40 and Span 40/Tween 80 oleogel formulations were prepared by solid fiber mechanism and subjected to organoleptic evaluation, FT-IR spectroscopy, thermal analysis, rheological study, kinetic modeling of gelation and drug release. Results: The critical gelator (Span 40) concentration was found to be lower for olive oil (12% w/v) and depend on the type of oil. Tween 80 reduced CGC of soybean oleogels only. Soybean oil-based oleogel containing 18% w/v Span 40 was found to form more flexible, less viscous and thermally less stable formulation with better release of paracetamol as evident from lower melt flow index, Tg value, lower β and higher α value compared to olive oil-based oleogel with 12% w/v Span 40 (CGC). Surfactant addition can be assumed to modify the microarchitecture of the oleogels to a great extent to produce more flexible and thermally stable gels with even better drug release profile. Span-Tween based soybean oleogel formed a gel-matrix whereas matrix in olive oil-based oleogels containing Span only became slightly flexible to release the drug in zero-order fashion on the addition of surfactant cogelator. Conclusion: Nature of oil exerts profound influence on the rheological, thermal and release profile of oleogels containing Span 40 as gelator and/or Tween 80 as surfactant cogelator.

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Design and Evaluation of Lovastatin Solid Dispersions Incorporated Trilayer Matrix Tablets

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2020.120409 ◽

2020 ◽

pp. 368-376

Author(s):

Chinthala Shanthi Priya ◽

Tummaluru Ramamohan Reddy

Keyword(s):

Drug Release ◽

Solid Dispersions ◽

Extended Period ◽

Matrix Tablets ◽

Drug Dissolution ◽

Fickian Diffusion ◽

Release Formulation ◽

Extended Release Formulation ◽

Zero Order Release ◽

Evaporation Technique

The current work is aimed to design, prepare and evaluate the trilayer matrix tablets incorporated with lovastatin solid dispersion (SD) for extend drug release. The lovastatin SD prepared by using solvent evaporation technique with varying amounts of polymers (GMS II, Soluplus, Kolliphor ELP, PEG 2000 and Urea) for enhancing the drug solubility. All the formulations examined for physicochemical parameters are within the permissible limits. The optimized SD formulation was incorporated into trilayer matrix tablets which were prepared using different polymers (HPMC 15M & K100M, Chitosan, xanthan gum) by direct compression method for sustaining the drug release. The drug dissolution of optimized lovastatin SD formulation SD15 (drug, soluplus and SLN) was 99.88±5.32% within 60 min which is higher than pure drug 47.33±2.25% and other formulations. The FT-IR, XRD and SEM data assure the compatibility of drug and excipients and amorphous nature of lovastatin. The solid dispersions were further incorporated in to trilayer matrix tablets with active layer and barrier layers. Eight formulations of lovastatin trilayer matrix tablets (AF9-HF9) designed and checked for pre compression parameters. Formulation GF9 demonstrated highest drug release of 99.41±5.28% for 24 hours sustainably over an extended period of time and excellent flow properties. The release order kinetics data indicate the zero order release with highest R2 of 0.9957 for GF9, superior than market extended release formulation (R2=0.9934). All the formulations showed best fit to Higuchi model and Korsmeyer-Peppa’s model indicating diffusion and non-Fickian diffusion process of drug release. GF90 was found to be stable for 180 days at accelerated conditions. Hence the solubility, dissolution rate of lovastatin was enhanced by SD technique further incorporated in to trilayer matrix tablets for sustainable extended drug release upto 24 h.

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Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.3.8 ◽

1970 ◽

Vol 9 (3) ◽

pp. 3318-3329

Author(s):

Kranthi Kumar Kotta ◽

L. Srinivas

Keyword(s):

Controlled Release ◽

Drug Release ◽

Xanthan Gum ◽

Diffusion Mechanism ◽

Matrix Tablets ◽

Fickian Diffusion ◽

Content Uniformity ◽

In Vitro Drug Release ◽

Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

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Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

Current Computer - Aided Drug Design ◽

10.2174/1573409916666201224153414 ◽

2020 ◽

Vol 16 ◽

Author(s):

Anjali P.B ◽

Jawahar N. ◽

Jubie S. ◽

Neetu Yadav ◽

Selvaraj A. ◽

...

Keyword(s):

Drug Release ◽

Phospholipase A2 ◽

Release Kinetics ◽

Entrapment Efficiency ◽

Structural Analog ◽

Fickian Diffusion ◽

Release Kinetic ◽

Nanostructured Lipid Carrier ◽

Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

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Nanostructured Ketorolac-Tromethamine/MCF: Synthesis, Characterization and Application in Drug Release System

Current Nanoscience ◽

10.2174/1573413714666180222134742 ◽

2018 ◽

Vol 14 (5) ◽

pp. 432-439 ◽

Cited By ~ 1

Author(s):

Juliana M. Juarez ◽

Jorgelina Cussa ◽

Marcos B. Gomez Costa ◽

Oscar A. Anunziata

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Therapeutic Efficacy ◽

Drug Delivery Systems ◽

Controlled Drug Release ◽

Delivery Systems ◽

The Body ◽

Fickian Diffusion ◽

Ketorolac Tromethamine

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.

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Laboratory Study of the Ultraviolet Radiation Effect on an HDPE Geomembrane

Membranes ◽

10.3390/membranes11060390 ◽

2021 ◽

Vol 11 (6) ◽

pp. 390

Author(s):

Fernando Luiz Lavoie ◽

Marcelo Kobelnik ◽

Clever Aparecido Valentin ◽

Érica Fernanda da Silva Tirelli ◽

Maria de Lurdes Lopes ◽

...

Keyword(s):

Ultraviolet Radiation ◽

Morphological Changes ◽

Field Performance ◽

Melt Flow Index ◽

Flow Index ◽

Test Results ◽

Upward Trend ◽

Scanning Calorimetry ◽

Ultraviolet Exposure ◽

Brittle Behavior

High-density polyethylene (HDPE) geomembranes are polymeric geosynthetic materials usually applied as a liner in environmental facilities due to their good mechanical properties, good welding conditions, and excellent chemical resistance. A geomembrane’s field performance is affected by different conditions and exposures, including ultraviolet radiation, thermal and oxidative exposure, and chemical contact. This article presents an experimental study with a 1.0 mm-thick HDPE virgin geomembrane exposed by the Xenon arc weatherometer for 2160 h and the ultraviolet fluorescent weatherometer for 8760 h to understand the geomembrane’s behavior under ultraviolet exposure. The evaluation was performed using the melt flow index (MFI) test, oxidative-induction time (OIT) tests, tensile test, differential scanning calorimetry (DSC) analysis, and Fourier transform infrared spectroscopy (FTIR) analysis. The sample exposed in the Xenon arc equipment showed a tendency to increase the MFI values during the exposure time. This upward trend may indicate morphological changes in the polymer. The tensile behavior analysis showed a tendency of the sample to lose ductility, without showing brittle behavior. The samples’ OIT test results under both device exposures showed faster antioxidant depletion for the standard OIT test than the high-pressure OIT test. The DSC and FTIR analyses did not demonstrate the polymer’s changes.

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Enhancement of mechanical, thermal and water uptake performance of TPU/jute fiber green composites via chemical treatments on fiber surface

e-Polymers ◽

10.1515/epoly-2020-0015 ◽

2020 ◽

Vol 20 (1) ◽

pp. 133-143 ◽

Cited By ~ 6

Author(s):

Tuffaha Fathe Salem ◽

Seha Tirkes ◽

Alinda Oyku Akar ◽

Umit Tayfun

Keyword(s):

Water Absorption ◽

Water Uptake ◽

Mechanical Test ◽

Fiber Surface ◽

Melt Flow Index ◽

Jute Fiber ◽

Morphological Properties ◽

Flow Index ◽

Melt Flow ◽

Treatment Type

AbstractChopped jute fiber (JF) surfaces were modified using alkaline, silane and eco-grade epoxy resin. Surface characteristics of jute fibers were confirmed by FTIR and EDX analyses. JF filled polyurethane elastomer (TPU) composites were prepared via extrusion process. The effect of surface modifications of JF on mechanical, thermo-mechanical, melt-flow, water uptake and morphological properties of TPU-based eco-composites were investigated by tensile and hardness tests, dynamic mechanical analysis (DMA), melt flow index (MFI) test, water absorption measurements and scanning electron microscopy (SEM) techniques, respectively. Mechanical test results showed that silane and epoxy treated JF additions led to increase in tensile strength, modulus and hardness of TPU. Glass transition temperature (Tg) of TPU rose up to higher values after JF inclusions regardless of treatment type. Si-JF filled TPU exhibited the lowest water absorption among composites. Surface treated JFs displayed homogeneous dispersion into TPU and their surface were covered by TPU according to SEM micro-photographs.

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Green TPUs from Prepolymer Mixtures Designed by Controlling the Chemical Structure of Flexible Segments

International Journal of Molecular Sciences ◽

10.3390/ijms22147438 ◽

2021 ◽

Vol 22 (14) ◽

pp. 7438

Author(s):

Paulina Kasprzyk ◽

Ewa Głowińska ◽

Paulina Parcheta-Szwindowska ◽

Kamila Rohde ◽

Janusz Datta

Keyword(s):

Chemical Structure ◽

Melt Flow Index ◽

Molar Ratio ◽

Flow Index ◽

Step Method ◽

Elongation At Break ◽

Molecular Weights ◽

Trimethylene Glycol ◽

Hard Segments ◽

A Chain

This study concerns green thermoplastic polyurethanes (TPU) obtained by controlling the chemical structure of flexible segments. Two types of bio-based polyether polyols—poly(trimethylene glycol)s—with average molecular weights ca. 1000 and 2700 Da were used (PO3G1000 and PO3G2700, respectively). TPUs were prepared via a two-step method. Hard segments consisted of 4,4′-diphenylmethane diisocyanates and the bio-based 1,4-butanodiol (used as a chain extender and used to control the [NCO]/[OH] molar ratio). The impacts of the structure of flexible segments, the amount of each type of prepolymer, and the [NCO]/[OH] molar ratio on the chemical structure and selected properties of the TPUs were verified. By regulating the number of flexible segments of a given type, different selected properties of TPU materials were obtained. Thermal analysis confirmed the high thermal stability of the prepared materials and revealed that TPUs based on a higher amount of prepolymer synthesized from PO3G2700 have a tendency for cold crystallization. An increase in the amount of PO3G1000 at the flexible segments caused an increase in the tensile strength and decrease in the elongation at break. Melt flow index results demonstrated that the increase in the amount of prepolymer based on PO3G1000 resulted in TPUs favorable in terms of machining.

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Halloysite Nanotubes and Silane-Treated Alumina Trihydrate Hybrid Flame Retardant System for High-Performance Cable Insulation

Polymers ◽

10.3390/polym13132134 ◽

2021 ◽

Vol 13 (13) ◽

pp. 2134

Author(s):

Sandra Paszkiewicz ◽

Izabela Irska ◽

Iman Taraghi ◽

Elżbieta Piesowicz ◽

Jakub Sieminski ◽

...

Keyword(s):

Mechanical Properties ◽

Polymer Blend ◽

Hybrid System ◽

Reference Sample ◽

Melt Flow Index ◽

Halloysite Nanotubes ◽

Flow Index ◽

Scanning Calorimetry ◽

Limiting Oxygen Index ◽

Alumina Trihydrate

The effect of the presence of halloysite nanotubes (HNTs) and silane-treated alumina trihydrate (ATH-sil) nanofillers on the mechanical, thermal, and flame retardancy properties of ethylene-vinyl acetate (EVA) copolymer/low-density polyethylene (LDPE) blends was investigated. Different weight percentages of HNT and ATH-sil nanoparticles, as well as the hybrid system of those nanofillers, were melt mixed with the polymer blend (reference sample) using a twin-screw extruder. The morphology of the nanoparticles and polymer compositions was studied using scanning electron microscopy (SEM) and energy dispersive spectroscopy (EDS). The mechanical properties, hardness, water absorption, and melt flow index (MFI) of the compositions were assessed. The tensile strength increases as a function of the amount of HNT nanofiller; however, the elongation at break decreases. In the case of the hybrid system of nanofillers, the compositions showed superior mechanical properties. The thermal properties of the reference sample and those of the corresponding sample with nanofiller blends were studied using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). Two peaks were observed in the melting and crystallization temperatures. This shows that the EVA/LDPE is an immiscible polymer blend. The thermal stability of the blends was improved by the presence of HNTs and ATH-sil nanoparticles. Thermal degradation temperatures were shifted to higher values by the presence of hybrid nanofillers. Finally, the flammability of the compositions was assessed. Flammability as reflected by the limiting oxygen index (OI) was increased by the presence of HNT and ATH-sil nanofiller and a hybrid system of the nanoparticles.

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Mechanical, Thermal and Rheological Properties of Polyethylene-Based Composites Filled with Micrometric Aluminum Powder

Materials ◽

10.3390/ma13051242 ◽

2020 ◽

Vol 13 (5) ◽

pp. 1242

Author(s):

Olga Mysiukiewicz ◽

Paulina Kosmela ◽

Mateusz Barczewski ◽

Aleksander Hejna

Keyword(s):

Mechanical Properties ◽

Melt Flow Index ◽

Tensile Tests ◽

Mechanical Analysis ◽

Flow Index ◽

Scanning Calorimetry ◽

Metal Composites ◽

Pre Treatment ◽

The Impact ◽

Properties Of Composites

Investigations related to polymer/metal composites are often limited to the analysis of the electrical and thermal conductivity of the materials. The presented study aims to analyze the impact of aluminum (Al) filler content (from 1 to 20 wt%) on the rarely investigated properties of composites based on the high-density polyethylene (HDPE) matrix. The crystalline structure, rheological (melt flow index and oscillatory rheometry), thermal (differential scanning calorimetry), as well as static (tensile tests, hardness, rebound resilience) and dynamic (dynamical mechanical analysis) mechanical properties of composites were investigated. The incorporation of 1 and 2 wt% of aluminum filler resulted in small enhancements of mechanical properties, while loadings of 5 and 10 wt% provided materials with a similar performance to neat HDPE. Such results were supported by the lack of disturbances in the rheological behavior of composites. The presented results indicate that a significant content of aluminum filler may be introduced into the HDPE matrix without additional pre-treatment and does not cause the deterioration of composites’ performance, which should be considered beneficial when engineering PE/metal composites.

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