Design of atrazine containing polysaccharide based slow release formulations to control environmental hazards

Atrazine is more reliable, flexible, effective and less expensive herbicide than any other available weed control approaches. However, easy leaching of atrazine is a matter of great environmental and health concern which limits its strong recommendation for practical applicability. Hence, controlled release formulations of atrazine, specially based on natural polysaccharide, are required for delivery and resolve the problems associated with conventional formulations. In the present work, slow release atrazine containing alginate-agar based bead formulations have been prepared and characterized by scanning electron micrography, Fourier transform infrared spectroscopy and swelling studies. The release of atrazine from the beads occurred through non-Fickian diffusion mechanism. The release of atrazine from the beads in the soil has been observed slower and lesser in soil as compared to the in vitro release. Besides providing the slow release of atrazine, these formulations after degradation may enhance the fertility of the soil.

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

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39965 ◽

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.

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EFFECT OF HYDROPHILIC POLYMERS ON CONTROLLED RELEASE MATRIX TABLETS OF ACYCLOVIR

INDIAN DRUGS ◽

10.53879/id.50.01.p0042 ◽

2013 ◽

Vol 50 (01) ◽

pp. 42-49

Author(s):

P Ashok Kumar ◽

◽

S. Damodar Kumar

Keyword(s):

Controlled Release ◽

Diffusion Mechanism ◽

In Vitro Release ◽

Matrix Tablets ◽

Hydrophilic Polymers ◽

Fickian Diffusion ◽

Sem Images ◽

Weight Variation ◽

Karaya Gum

Acyclovir was formulated as oral controlled release matrix tablets using natural and synthetic polymers separately or in combinations. Tablets were prepared by direct compression method. The tablets were evaluated to thickness, weight variation test, drug content, hardness, friability and in vitro release studies.All the formulations showed compliance with pharmacopoeal standards. The tablets prepared with various combination of hydroxy propyl methylcellulose (HPMC K100), locust bean gum (LBG) and karaya gum (KG) failed to produce the desired controlled release. Dissolution studies indicated that formulation F5 was most successful of the study. The formulation F5 exhibited anomalous (non-Fickian) diffusion mechanism. Based on the results of in-vitro studies it was concluded that the hydrophilic polymers canbe used as an effective matrix former to provide controlled release of acyclovir. SEM images of tablet after dissolution showed pore formation. FT-IR and DSC study did not show any possibility of interaction between acyclovir and excipients.

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Sinomenine-loaded microcapsules fabricated by phase reversion emulsification-drying in liquid method: An evaluation of process parameters, characterization, and released properties

Journal of Bioactive and Compatible Polymers ◽

10.1177/0883911517751159 ◽

2017 ◽

Vol 33 (4) ◽

pp. 382-396 ◽

Cited By ~ 1

Author(s):

Wen Zhang ◽

Yan Gao ◽

Ning Yang ◽

Hua Zhang ◽

Feng Zhang ◽

...

Keyword(s):

Biological Activities ◽

Drug Loading ◽

Diffusion Mechanism ◽

In Vitro Release ◽

Spherical Shape ◽

Fickian Diffusion ◽

Anti Cancer ◽

Methyl Thiazolyl Tetrazolium Assay ◽

Natural Alkaloid

Sinomenine is a natural alkaloid with important biological activities (e.g. anti-cancer, anti-inflammatory, and anti-allergic). However, the unstability and short half-life absolutely limited its application to foods. Microencapsulation technology can offer a way to solve these issues. In this study, polylactic acid microcapsules loading sinomenine hydrochloride were fabricated by phase inversion emulsification-drying in liquid technique. The results showed that microcapsules had nice spherical shape, uniform particle size, and free flowing. The encapsulation efficiency was 89.2% and drug loading was 8.9% under the optimal conditions. In vitro release assays demonstrated that release of sinomenine from microcapsules was sustained and slow. Moreover, it was found that the sinomenine release fitted Fickian diffusion mechanism. The results of cytotoxicity study showed that sinomenine-loaded microcapsules were biocompatible. Sinomenine-loaded microcapsules could inhibit the growth of MDA-MB-231 cells using methyl thiazolyl tetrazolium assay. In summary, polylactide microcapsules exhibit excellent properties for sinomenine that can be used in drug or food industry.

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Hollow Mesoporous Spheres with Cubic Pore Network as a Potential Carrier for Drug Storage and its In Vitro Release Kinetics

Journal of Materials Research ◽

10.1557/jmr.2005.0035 ◽

2005 ◽

Vol 20 (1) ◽

pp. 54-61 ◽

Cited By ~ 64

Author(s):

Yu-Fang Zhu ◽

Jian-Lin Shi ◽

Yong-Sheng Li ◽

Hang-Rong Chen ◽

Wei-Hua Shen ◽

...

Keyword(s):

Release Kinetics ◽

Diffusion Mechanism ◽

In Vitro Release ◽

Pore Network ◽

Fickian Diffusion ◽

Step Method ◽

Release Process ◽

Drug Molecules ◽

Mcm 41

The hollow mesoporous spheres (HMS) with cubic pore network have been synthesized via a simple two-step method. Two drugs of different molecules size, Aspirin and Gentamicin, were tested by one simple adsorption process. Up to 336 mg Aspirin molecules can be stored in 1.0 g HMS, while Gentamicin molecules of much larger size are much more difficult to be introduced into the pore channels of HMS. The same results can be obtained by using MCM-48 and MCM-41 as comparative mesoporous carriers. The HMS shows significantly higher storage amount of Aspirin than conventional MCM-48 and MCM-41 due to its hollow core structure. The release process of HMS-Aspirin, MCM-48-Aspirin and MCM-41-Aspirin are found to have a sustained-release property and follow a Fickian diffusion mechanism. Moreover, the HMS is suitable for storage of drug molecules of much smaller size.

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Preparation and Characterization of Aminoglycoside-Loaded Chitosan/Tripolyphosphate/Alginate Microspheres against E. coli

Polymers ◽

10.3390/polym13193326 ◽

2021 ◽

Vol 13 (19) ◽

pp. 3326

Author(s):

Estefanía Tiburcio ◽

Eduardo García-Junceda ◽

Leoncio Garrido ◽

Alfonso Fernández-Mayoralas ◽

Julia Revuelta ◽

...

Keyword(s):

Pathogenic Bacteria ◽

Bacterial Resistance ◽

Diffusion Mechanism ◽

In Vitro Release ◽

Antibacterial Properties ◽

Fickian Diffusion ◽

Burst Release ◽

E Coli ◽

Gel Beads

Although aminoglycosides are one of the common classes of antibiotics that have been widely used for treating infections caused by pathogenic bacteria, the evolution of bacterial resistance mechanisms and their inherent toxicity have diminished their applicability. Biocompatible carrier systems can help sustain and control the delivery of antibacterial compounds while reducing the chances of antibacterial resistance or accumulation in unwanted tissues. In this study, novel chitosan gel beads were synthesized by a double ionic co-crosslinking mechanism. Tripolyphosphate and alginate, a polysaccharide obtained from marine brown algae, were employed as ionic cross-linkers to prepare the chitosan-based networks of gel beads. The in vitro release of streptomycin and kanamycin A was bimodal; an initial burst release was observed followed by a diffusion mediated sustained release, based on a Fickian diffusion mechanism. Finally, in terms of antibacterial properties, the particles resulted in growth inhibition of Gram-negative (E. coli) bacteria.

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Cubosomes Dispersions as Enhanced Indomethacin Oral Delivery Systems: In vitro and Stability Evaluation

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i25a31449 ◽

2021 ◽

pp. 24-35

Author(s):

Iman M. Alfagih ◽

Bushra AlQuadeib ◽

Basmah Aldosari ◽

Alanood Almurshedi ◽

Mohamed M. Badran ◽

...

Keyword(s):

Oral Delivery ◽

Diffusion Mechanism ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Poloxamer 407 ◽

Fickian Diffusion ◽

The Stability ◽

Oral Delivery Systems ◽

Kinetics Of

Aims: To improve the dissolution of indomethacin through developing liquid indomethacin loaded cubosomes dispersion for oral delivery. Methodology: Glyceryl monooleate based indomethacin loaded cubosomes dispersion were prepared using Taguchi design to study the effect of indomethacin to the disperse phase ratio and poloxamer 407 (PLX%) concentrations on the particle size and entrapment efficiency (%EE). Furthermore, in vitro release in phosphate buffer (pH 6.8), and morphology were investigated. Also, the stability of indomethacin loaded cubosomes dispersions was examined after 6 months storage at 25°C in the dark. Results: The prepared indomethacin cubosomes dispersions were in the nanoscale (184.53±0.7 to 261.33±0.8 nm) with reasonable %EE (49.30±2.6 to 95.55±3.4 %). Moreover, a biphasic release profile was predominant for all formulations, up to 50% of payload released after 2h followed by a second continuous sustained release phase over 24h. The kinetics of indomethacin release was best explained by Higuchi model and the mechanism of drug release from these cubosomes dispersions was by fickian diffusion mechanism. In general, the indomethacin loaded cubosomes dispersions were stable after 6 months storage at 25°C in the dark. Conclusion: Indomethacin loaded cubosomes dispersions proved to be a successful platform to encapsulate and enhance the release of indomethacin with a good stability profile over 6 months.

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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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Electrospun Janus Beads-On-A-String Structures for Different Types of Controlled Release Profiles of Double Drugs

Biomolecules ◽

10.3390/biom11050635 ◽

2021 ◽

Vol 11 (5) ◽

pp. 635

Author(s):

Ding Li ◽

Menglong Wang ◽

Wen-Liang Song ◽

Deng-Guang Yu ◽

Sim Wan Annie Bligh

Keyword(s):

Controlled Release ◽

Combined Therapy ◽

Diffusion Mechanism ◽

Amorphous State ◽

Electrospinning Process ◽

Fickian Diffusion ◽

In Vitro Dissolution ◽

Sem Images ◽

Release Profiles

A side-by-side electrospinning process characterized by a home-made eccentric spinneret was established to produce the Janus beads-on-a-string products. In this study, ketoprofen (KET) and methylene blue (MB) were used as model drugs, which loaded in Janus beads-on-a-string products, in which polyvinylpyrrolidone K90 (PVP K90) and ethyl cellulose (EC) were exploited as the polymer matrices. From SEM images, distinct nanofibers and microparticles in the Janus beads-on-a-string structures could be observed clearly. X-ray diffraction demonstrated that all crystalline drugs loaded in Janus beads-on-a-string products were transferred into the amorphous state. ATR-FTIR revealed that the components of prepared Janus nanostructures were compatibility. In vitro dissolution tests showed that Janus beads-on-a-string products could provide typical double drugs controlled-release profiles, which provided a faster immediate release of MB and a slower sustained release of KET than the electrospun Janus nanofibers. Drug releases from the Janus beads-on-a-string products were controlled through a combination of erosion mechanism (linear MB-PVP sides) and a typical Fickian diffusion mechanism (bead KET-EC sides). This work developed a brand-new approach for the preparation of the Janus beads-on-a-string nanostructures using side-by-side electrospinning, and also provided a fresh idea for double drugs controlled release and the potential combined therapy.

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

Advanced Pharmaceutical Bulletin ◽

10.15171/apb.2019.026 ◽

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.

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α-Mangostin Hydrogel Film Based Chitosan–Alginate for Recurrent Aphthous Stomatitis

Applied Sciences ◽

10.3390/app9235235 ◽

2019 ◽

Vol 9 (23) ◽

pp. 5235 ◽

Cited By ~ 2

Author(s):

Nasrul Wathoni ◽

Nia Yuniarsih ◽

Arief Cahyanto ◽

Muhctaridi Muhctaridi

Keyword(s):

In Vitro Release ◽

Recurrent Aphthous Stomatitis ◽

Aphthous Stomatitis ◽

Fickian Diffusion ◽

Garcinia Mangostana ◽

Scanning Calorimetry ◽

Main Compound ◽

Discovery Studio ◽

Hydrogel Film

Many antiseptic drugs, local anaesthetics, and corticosteroids have been used for effective therapy of recurrent aphthous stomatitis (RAS). However, these drugs have harmful side effects. α-mangostin (α-M), a main compound of mangosteen (Garcinia mangostana L.) peel, has been known as a wound healing agent. In addition, hydrogel film as dressings designed to separate mucosal lesions from the oral environment, and improve the effectiveness of RAS therapy. The purpose of this study was to develop α-M hydrogel film based chitosan–alginate (ChAlg/α-M HF) for RAS. The in silico study by Discovery studio visualizer and AutoDock confirmed that hydrogen bonding between Ch, Alg, and α-M occurred. The results of physicochemical characterizations by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) indicated that the ChAlg/α-M HF had a lower crystalline form compared to pure α-M. In addition, ChAlg/α-M HF significantly improved the swelling ratio and tensile strength compared to that of ChAlg HF. Moreover, the existence of Alg increased the degradability of Ch, and closely related to the release of α-M from ChAlg HF. The in vitro release study confirmed that the release of α-M from ChAlg/α-M HF was the Fickian diffusion model. Finally, the mucoadhesive study revealed that ChAlg/α-M HF had a good mucoadhesive property. These results suggest that hydrogel film-based chitosan–alginate have the potential as carriers of α-M for RAS therapy.

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