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

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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DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2022v14i1.43353 ◽

2022 ◽

pp. 156-163

Author(s):

RASHAD M. KAOUD ◽

EMAN J. HEIKAL ◽

TAHA M. HAMMADY

Keyword(s):

Physical Stability ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Stability Study ◽

Molar Ratios ◽

Tween 40 ◽

A New Technique ◽

The Stability ◽

Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

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BENAZEPRIL HYDROCHLORIDE LOADED NIOSOMAL FORMULATION FOR ORAL DELIVERY: FORMULATION AND CHARACTERIZATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i5.27564 ◽

2018 ◽

Vol 10 (5) ◽

pp. 66

Author(s):

Ameerah A. Radhi

Keyword(s):

Zeta Potential ◽

Oral Delivery ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Potential Range ◽

Transmission Electron ◽

Study Results ◽

Span 60 ◽

A Charge

Objective: The objective of the present study was to formulate niosomal formulations of benazepril hydrochloride in an attempt to overcome the hurdles associated with itʼs poor oral absorption.Methods: Nine formulations were prepared with various ratios of sorbitan monostearate (span 60), sorbitan monopalmitate (span 40) and polyoxyethylene 2 stearyl ether (brij 72) as non-ionic surfactants, cholesterol as a stabilizing agent and soya lecithin as a charge imparting agent. Then, they were characterized for vesicle size, polydispersity (PDI), entrapment efficiency (EE %), release profile, zeta (ζ) potential and transmission electron microscopy (TEM).Results: Niosomal formulations exhibited an efficient entrapment range between (80.4-97.8) percent, vesicles size analyses revealed the formation of homogenously dispersed vesicles having a size range of (3.9±1.7-8.72±4.4) micrometers. The in vitro release studies revealed that all formulations displayed sustained release in comparison with the pure drug. Formulations prepared with span 60 and span 40 possessed adequate stability according to zeta potential analysis, whereas brij 72 failed the test and possessed inadequate zeta potential range. TEM images of the optimized formulations (F7 and F8) have confirmed the formation of vesicles with spherical shapes.Conclusion: Based on the study results, niosomal formulations seem to be attractive alternatives to conventional delivery for benazepril hydrochloride.

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Clarithromycin-Loaded Poly (Lactic-co-glycolic Acid) (PLGA) Nanoparticles for Oral Administration: Effect of Polymer Molecular Weight and Surface Modification with Chitosan on Formulation, Nanoparticle Characterization and Antibacterial Effects

Polymers ◽

10.3390/polym11101632 ◽

2019 ◽

Vol 11 (10) ◽

pp. 1632 ◽

Cited By ~ 8

Author(s):

A. Alper Öztürk ◽

Evrim Yenilmez ◽

Mustafa Güçlü Özarda

Keyword(s):

Oral Delivery ◽

Glycolic Acid ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Test Method ◽

Molecular Weights ◽

Antibiotic Group ◽

Surface Modified

Clarithromycin (CLR) is a member of the macrolide antibiotic group. CLR has low systemic oral bioavailability and is a drug of class II of the Biopharmaceutical Classification System. In many studies, using nanoparticles (NPs) as a drug delivery system has been shown to increase the effectiveness and bioavailability of active drug substances. This study describes the development and evaluation of poly (lactic-co-glycolic acid) (PLGA) NPs and chitosan (CS)-coated PLGA NPs for oral delivery of CLR. NPs were obtained by nanoprecipitation technique and characterized in detail, and the effect of three molecular weights (Mw1: 7.000–17.000, Mw2: 38.000–54.000, Mw3: 50.000–190.000) of PLGA and CS coating on particle size (PS), zeta potential (ZP), entrapment efficiency (EE%), and release properties etc. were elucidated. Gastrointestinal stability and cryoprotectant effect tests were performed on the NPs. The PS of the prepared NPs were in the range of 178 to 578 nm and they were affected by the Mw and CS coating. In surface-modified formulations with CS, the ZP of the NPs increased significantly to positive values. EE% varied from 62% to 85%, depending upon the Mw and CS coating. In vitro release studies of CLR-loaded NPs showed an extended release up to 144 h. Peppas–Sahlin and Weibull kinetic model was found to fit best for CLR release from NPs. By the broth microdilution test method, the antibacterial activity of the formulations was determined on Staphylococcus aureus (ATCC 25923), Listeria monocytogenes (ATCC 1911), and Klebsiella pneumoniae (ATCC 700603). The structures of the formulations were clarified by thermal (DSC), FT-IR, and 1H-NMR analysis. The results showed that PS, ZP, EE%, and dissolution rates of NPs were directly related to the Mw of PLGA and CS coating.

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

Prayogik Rasayan ◽

10.53023/p.rasayan-201702211 ◽

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.

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Formulation and Evaluation of Eudragit Rl100 Polymeric Drug Loaded Microsponge for Ophthalmic Use

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i24b31440 ◽

2021 ◽

pp. 45-51

Author(s):

Rajashri B. Ambikar ◽

Ashok V. Bhosale

Keyword(s):

Particle Size ◽

Controlled Release ◽

Drug Release ◽

Delivery System ◽

Diffusion Mechanism ◽

Diclofenac Sodium ◽

Entrapment Efficiency ◽

Fickian Diffusion ◽

Drug Content

Aims: The aim of this work is the formulation of Eudragit RL100 polymeric microsponges. The Microsponge Delivery System is a patented technique in which there is a polymeric system consisting of porous particles. Methodology: The ratio of Diclofenac sodium and eudragit RL100 varied from 1:1 to 13: 1 to formulate microsponge. Dichloromethane was used as internal phase and polyvinylalcohol was used as an external phase. The formed microsponges were characterized for particle size, entrapment efficiency, drug content, in vitro drug release and SEM. Results: With increase in drug: polymer ratio there is increase in production yield from 20.04% to 72.14%, and entrapment efficiency from 20.11% to 70.77%. Drug content of formed microsponge varied between 50.18% to 91.09% whereas particle size ranged from 1.41 µm to 17.66 µm. Microsponge formulations F3, F4 and F5 showed desired particle size hence studied for further evaluation. Formulation F3, F4 and F5 showed controlled release of 89.54%, 98.5% and 98.76% respectively up to 6 hr. F3 showed more controlled release at the end of 6 hr. The drug release from microsponges was best fitted to Higuchi’s diffusion kinetics for all microsponge formulations with non-Fickian diffusion mechanism. The formed microsponge particles have spherical porous structure. Conclusion: Study showed significance of Microsponge Delivery System for ophthalmic administration.

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Polymeric Nanoparticles Loaded with Acyclovir: Formulation, Characterization and In-Vitro Drug Prolonged-Release Study

Current Nanomedicine ◽

10.2174/2468187310999200701215154 ◽

2020 ◽

Vol 10 (3) ◽

pp. 271-279

Author(s):

Tran Thi Hai Yen ◽

Nguyen Tran Linh ◽

Vu Thi Thu Giang ◽

Hoang Lan Anh

Keyword(s):

Particle Size ◽

Drug Release ◽

Diffusion Mechanism ◽

Antiviral Drug ◽

Entrapment Efficiency ◽

Fickian Diffusion ◽

Prolonged Release ◽

In Vitro Drug Release ◽

Release Study

Objectives: Acyclovir (ACV) is an antiviral drug, which requires frequent dosing regimen because of poor oral bioavailability and short half-life. In this study, ACV nanoparticles were formulated using ammonium methacrylates copolymers such as Eudragit RS 100 (Eud RS) and Eudragit RL 100 (Eud RL) to prolong release drug, and increase bioavailability. Methods: ACV loaded nanoparticles were prepared by the solvent replacement technique and then were characterized by particle size, distribution, entrapment efficiency, differential scanning calorimeter, transmission electron microscope, and in-vitro drug release. Results: It was found that as drug:polymer ratio changed from 1:2 to1:5, particle size and drug entrapment efficiency increased significantly. ACV– Eud RS loaded nanoparticles had a larger mean diameter of 363 nm in comparison to 200 nm of ACV- Eud RL nanoparticles. DSC results showed that in the prepared ACV-Eud RS nanoparticles, the drug was presented in the amorphous phase and may have been molecularly dispersed in the polymer matrix, but in the ACV-Eud RL nanoparticles, the drug was presented in the particles and homogeneously dispersed in the polymeric matrix. The entrapment efficiency of AVC-Eud RS nanoparticles was higher than that of ACV-Eud RL nanoparticles. In vitro drug release study showed that the ratios of released drug from ACV-Eud RS nanoparticles in the range from 58±3.8 to 62.9±4.6%, which was lower than those from ACV-Eud RL nanoparticles, in the range from 73.3±4.9 to 77.9±2.9%. The release was found to follow the Weibull model with a Fickian diffusion mechanism for both ACVEud RS and ACV- Eud RL nanoparticles. Conclusion: These results suggest that ACV nanoparticles based on Eud RS100 and Eud RL100 could prolong the release of the drug.

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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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