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

2005 ◽  
Vol 20 (1) ◽  
pp. 54-61 ◽  
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.

Formulation and Evaluation of Dispersible tablets of a Model Anti-Parasitic Drug

2021 ◽  
pp. 2824-2828
Author(s):  
S. Preethi ◽  
S. Padmapriya ◽  
A. N. Rajalakshmi
Keyword(s):  
Release Kinetics ◽  
Diffusion Mechanism ◽  
Stability Study ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Weight Variation ◽  
Dispersible Tablets ◽  
In Vitro Disintegration

The study was aimed to formulate and evaluate dispersible tablets of a model anti-parasitic drug (XXX) with an objective to produce fast dispersion of tablets by reducing the disintegration time using three superdisintegrants like Sodium Starch Glycolate (SSG), Crospovidone (PVP K30) and Croscarmellose sodium (CCS) and also diluents namely MCC and Lactose by changing their concentrations in each formulations. Totally six formulations (F1-F6) were prepared by direct compression method and evaluated for hardness, thickness, weight variation, friability, wetting volume, wetting time, water absorption ratio, uniformity of dispersion, in-vitro disintegration time, Drug content, in-vitro dissolution test and release kinetics study. FTIR studies was carried out to see possible drug excipients interaction. The stability studies were performed as per ICH guidelines. Among the formulations F6 formulation was found to be promising as it showed better results than other five formulations with In-vitro disintegration time, percentage drug release and dispersion time of 16 ± 0.93 seconds, 98.32±0.54% and 66±1.30 seconds respectively. Further the FTIR results revealed that there was no interactionF between drug and excipients. Stability study of formulation showed no significant changes in tablet properties and the drug follows Higuchi release kinetics with Fickian diffusion mechanism.

EFFECT OF HYDROPHILIC POLYMERS ON CONTROLLED RELEASE MATRIX TABLETS OF ACYCLOVIR

INDIAN DRUGS ◽  
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.

Formulation and In vitro Evaluation of Floating Microspheres of Misoprostol

2017 ◽  
Vol 10 (1) ◽  
pp. 3608-3615
Author(s):  
K Vanitha ◽  
M. Mohan Varma ◽  
Ramesh Alluri
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Chemical Interaction ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
Methyl Cellulose ◽  
Ultra Violet ◽  
Fickian Diffusion ◽  
Polymer Ratio

Misoprostol is a synthetic prostaglandin PGE1 analogue, which has proved to be an effective anti-secretory agent for oral use. The major indications of Misoprostol are in the prevention and treatment of NSAID-induced gastric and duodenal ulcers. Its half-life is 20-40 minutes. More than one third of patients with ulcers are resistant to H2 antagonists. So, these patients can be healed on Misoprostol. The objective of the present study was to formulate gastroretentive floating drug delivery system of an antiulcer drug Misoprostol. Floating microspheres of Misoprostol were prepared by an emulsification solvent evaporation technique using hydroxy propyl methyl-cellulose (HPMC K 100M) and ethyl cellulose. The percentage yield and drug entrapment efficiencies of these floating microspheres were within the range between: 70 ± 2.8 to 98 ± 2.9 % and 39.27 to 82.39 %, respectively. The determined mean particle size for all the microspheres were 250 ± 7.28 to 400 ± 2.32 µm. The flowability of these microspheres was found good. A high performance liquid chromatography (HPLC) method with ultra-violet (UV) detection was selected for the method of analysis.  The drug release was found to delay for 12 hours with the increasing drug to polymer ratio. The drug release kinetics followed Korsemeyer-Peppas and Higuchi model with anomalous (non-Fickian) diffusion mechanism for the drug release. The FTIR and DSC studies showed that there was an absence of chemical interaction between the drug and the excipients. The in vitro drug release from Misoprostol floating microspheres showed the drug release was dependent on the drug to polymer ratio. The drug release was found delayed with the increasing drug to polymer ratio.  

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

2017 ◽  
Vol 33 (4) ◽  
pp. 382-396 ◽  
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.

scholarly journals Characteristics, Cryoprotection Evaluation and In Vitro Release of BSA-Loaded Chitosan Nanoparticles

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 315
Author(s):  
Qinying Yan ◽  
Jiaqi Weng ◽  
Xieqi Wu ◽  
Weiwei Wang ◽  
Qingliang Yang ◽  
...  
Keyword(s):  
Electrostatic Interactions ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Spectroscopic Techniques ◽  
Release Process ◽  
Dynamic High Pressure Microfluidization ◽  
High Consistency ◽  
And Function

Chitosan nanoparticles (CS-NPs) are under increasing investigation for the delivery of therapeutic proteins, such as vaccines, interferons, and biologics. A large number of studies have been taken on the characteristics of CS-NPs, and very few of these studies have focused on the microstructure of protein-loaded NPs. In this study, we prepared the CS-NPs by an ionic gelation method, and bovine serum albumin (BSA) was used as a model protein. Dynamic high pressure microfluidization (DHPM) was utilized to post-treat the nanoparticles so as to improve the uniformity, repeatability and controllability. The BSA-loaded NPs were then characterized for particle size, Zeta potential, morphology, encapsulation efficiency (EE), loading capacity (LC), and subsequent release kinetics. To improve the long-term stability of NPs, trehalose, glucose, sucrose, and mannitol were selected respectively to investigate the performance as a cryoprotectant. Furthermore, trehalose was used to obtain re-dispersible lyophilized NPs that can significantly reduce the dosage of cryoprotectants. Multiple spectroscopic techniques were used to characterize BSA-loaded NPs, in order to explain the release process of the NPs in vitro. The experimental results indicated that CS and Tripolyphosphate pentasodium (TPP) spontaneously formed the basic skeleton of the NPs through electrostatic interactions. BSA was incorporated in the basic skeleton, adsorbed on the surface of the NPs (some of which were inlaid on the NPs), without any change in structure and function. The release profiles of the NPs showed high consistency with the multispectral results.

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

2017 ◽  
Vol 1 (1) ◽  
Author(s):  
Baljit Singh ◽  
Devender Kumar Sharma ◽  
Abhishek Dhiman
Keyword(s):  
Slow Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Health Concern ◽  
Natural Polysaccharide ◽  
Scanning Electron Micrography ◽  
Controlled Release Formulations ◽  
Swelling Studies

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.

scholarly journals FORMULATION AND EVALUATION OF METOCLOPRAMIDE HCL RECTAL SUPPOSITORIES

2019 ◽  
Author(s):  
Deborah Ejiogu Chioma ◽  
Felix Sunday Yusuf
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Weight Variation ◽  
Rectal Suppositories ◽  
Vitro Release

Metoclopramide hydrochloride is a dopamine receptor antagonist, used mostly for stomach and esophageal problems as it is a prokinetic agent. The aim of the present study was to design and evaluate the suppositories of Metoclopramide HCl.  Six different, rectal suppositories were developed by fusion (pour-moulding) method by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent.  Metoclopramide HCl suppositories were evaluated for appearance, weight variation, drug content uniformity, liquefaction time and temperature, micro-melting range, disintegration and in-vitro release study.  The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism. Optimum formulation of batch S1 has shown 83.427% Metoclopramide HCl in a study of 2 hrs. These drug release results are supported by the disintegration time of suppositories. Lesser the disintegration time faster the drug release. All formulations has shown zero, first and Higuchi release kinetics. The result suggests that the Metoclopramide HCl suppositories can be prepared by employing hydrophilic and hydrophobic polymers.

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

Polymers ◽  
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.

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

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.

scholarly journals Preparation and Evaluation of Multi-Particulate System (Pellets) of Prasugrel Hydrochloride

2015 ◽  
Vol 2 (1) ◽  
pp. 74-80 ◽  
Author(s):  
Navjot Kanwar ◽  
Rakesh Kumar ◽  
V.R. Sinha
Keyword(s):  
Moisture Content ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Narrow Particle Size Distribution ◽  
Crystalline Cellulose ◽  
Flow Properties ◽  
Drug Content

Multiparticulate systems (pellets) of prasugrel hydrochloride were prepared by extrusion spheronization method using MCC (micro crystalline cellulose). Optimum spheronization time and method of drying were selected as the process parameters for the preparation of final batches. Various pellet properties were evaluated like size & shape analysis, flow properties, bulk & tapped density, friability, moisture content, drug content, in vitro release rate and in vivo pharmacodynamic studies. All pellet batches showed a narrow particle size distribution, good sphericity and excellent flow properties. Drug content and moisture content of different pellet batches were found in specified limits. The release kinetics of drug loaded MCC pellets followed Peppas model with Fickian diffusion of prasugrel from the pellets. In vivo pharmacodynamic studies exhibited improved bleeding time in pellet group when compared with the marketed tablet formulation.

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