Development, Optimization and Characterization of Eudraguard®-Based Microparticles for Colon Delivery

Development of pH-dependent systems for colon delivery of natural active ingredients is an attractive area of research in the field of nutraceutical products. This study was focused on Eudraguard® resins, that are methacrylate copolymers approved as “food grade” by European Commission and useful for the production of food supplements. In particular, Eudraguard® Biotic (EUG-B), characterized by a pH-dependent solubility and Eudraguard® Control (EUG-C), whose chemical properties support a prolonged release of the encapsulated compounds, were tested. To obtain EUG microparticles, different preparation techniques were tested, in order to optimize the preparation method and observe the effect upon drug encapsulation and specific colonic release. Unloaded microparticles were initially produced to evaluate the influence of polymer characteristics on the formulation process; subsequently microparticles loaded with quercetin (QUE) as a low solubility model drug were prepared. The characterization of microparticles in the solid-state (FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry) indicated that QUE was uniformly dispersed in a non-crystalline state in the polymeric network, without strong signs of chemical interactions. Finally, to assess the ability of EUG-C and EUG-B to control the drug release in the gastric environment, and to allow an increased release at a colonic level, suitable in vitro release tests were carried out by simulating the pH variations along the gastro-intestinal tract. Among the evaluated preparation methods, those in which an aqueous phase was not present, and in particular the emulsion-solvent evaporation method produced the best microparticle systems. The in vitro tests showed a limited drug release at a gastric level and a good specific colon release.

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DESIGN AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PHENFORMIN HYDROCHLORIDE

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2017v9i6.23437 ◽

2017 ◽

Vol 9 (6) ◽

pp. 90

Author(s):

Pratik Swarup Das ◽

Puja Saha

Keyword(s):

Drug Release ◽

Diffusion Mechanism ◽

Skin Irritation ◽

In Vitro Release ◽

Chemical Properties ◽

In Vitro Dissolution ◽

Release Mechanism ◽

Transdermal Patches ◽

The Matrix

Objective: In present work was designed to develop suitable transdermal matrix patches of Phenformin hydrochloride using various hydrophilic (HPMC) and hydrophobic (EUDRAGID) polymers as matrix formers.Methods: Transdermal patches containing Phenformin hydrochloride were prepared by the solvent casting evaporation technique.Results: Revealed that prepared patches showed good physical characteristics, no drug-polymer interaction and no skin irritation was observed. The in vitro release study revealed that F3 formulation showed maximum release in 24 h. Formulation F3 was subjected for accelerated stability studies. The F3 formulation was found to be stable as there was no drastic change in the Physico-chemical properties of the patches, which was also confirmed by FTIR.Conclusion: Thus conclusion can be made that stable transdermal patches of Phenformin hydrochloride has been developed. F1, F2, F3, F4 formulations showed highest cumulative percentage drug release of 98.13%, 95.50%, 98.65%, 97.21% were obtained during in vitro drug release studies after 24 h. The release of Phenformin hydrochloride appears to be dependent on lipophilicity of the matrix. Moderately lipophillic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. Based upon the in vitro dissolution data the F3 formulation was concluded as optimized formulation.

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FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE COATED MATRIX GRANULES OF METFORMIN HYDROCHLORIDE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i7.24996 ◽

2018 ◽

Vol 11 (7) ◽

pp. 387

Author(s):

Radha Rani Earle ◽

Kiran Kumar Bandaru ◽

Lakshmi Usha A

Keyword(s):

Drug Release ◽

Sustained Release ◽

In Vitro Release ◽

Methyl Cellulose ◽

Metformin Hydrochloride ◽

Scanning Calorimetry ◽

Diabetes Mellitus Type Ii ◽

Drug Content ◽

Percentage Yield

Objective: Metformin hydrochloride is a biguanide antihyperglycemic agent which is a generally recommended first-line drug for the treatment of diabetes mellitus (Type II). The purpose of this investigation is to prepare sustained release matrix granules of metformin hydrochloride which are coated to extend the drug release over a longer time period.Methods: Metformin hydrochloride granules were prepared by mixing all the dry powders in a V-cone blender and wetting the powder mix with aqueous solution of hydroxypropyl methyl cellulose K100. The prepared granules (MG1-MG5) were investigated for drug release. The batch of granules which exhibited extended release for up to 4 h was coated in a standard coating pan with blends of Eudragit RS and RL to further enhance release period. These were marked as coated metformin granules (CMG3) and CMG4 which were later filled into empty capsules. The granules were characterized for micromeritic properties, percentage yield, particle size distribution, percentage of drug content, and in vitro release of the drug.Results: All the formulations showed percentage yield in the range of 77.66–82.86% and drug content in the range of 78.23–96.62%. CMG3 showed drug release of 97.02% for 12 h. Fourier-transform infrared spectroscopy and differential scanning calorimetry studies indicated that no possible interaction existed between the drug and the polymers used. Scanning electron microscopy images revealed that the granules were spherical in shape with smooth surface and completely covered with a coating of polymer. Kinetic analysis of drug release confirmed that drug release followed zero-order kinetics where it is independent of the concentration.Conclusion: From the results, it was analyzed that design of coated granules employing the polymers used in the present work can produce a sustained release of the drug over a period of 12 h.

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Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique

Journal of Pharmaceutics ◽

10.1155/2013/315902 ◽

2013 ◽

Vol 2013 ◽

pp. 1-9 ◽

Cited By ~ 4

Author(s):

V. J. Kapure ◽

V. V. Pande ◽

P. K. Deshmukh

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Water Soluble ◽

Dissolution Enhancement ◽

Content Uniformity ◽

Scanning Calorimetry ◽

Weight Variation ◽

Liquisolid Compacts ◽

Rosuvastatin Calcium

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

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In Vitro Release Characterization of Tetracycline Hydrochloride from PLGA/Tetracycline Hydrochloride Electrospun Nanofiber Mats

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.785-786.339 ◽

2013 ◽

Vol 785-786 ◽

pp. 339-345 ◽

Cited By ~ 1

Author(s):

Jian Fei Xie ◽

Chun Yan Li ◽

Shu Han Hong ◽

Yu Rong Yan

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Tetracycline Hydrochloride ◽

Release Behavior ◽

In Vitro Drug Release ◽

Hydrophilic Drugs ◽

Release Ratio ◽

Nanofiber Mats

In order to study in vitro release behavior of hydrophilic drugs in polymer nanofibers and establish a fast characterization method, tetracycline hydrochloride-loaded poly (lacticacid-co-glycolic acid) nanofiber mats with varied tetracycline hydrochloride contents and different lacticacid to glycolic ratios in PLGA were preparied by electrospinning. Accroding to Chinese Pharmacopoeia, a basic and an improved test devices and processes were compared and their validity were commented by using an UV-visible spectrophotometer method. Results showed that the improved method can be used to estimate in vitro drug release behavior of drug-loaded mats and the results was better than the basic method. When temperature affected cumulative release ratio under controlled error, flotation method can replace the centrifugation method during the first stage of drug release testing process. Parallel experiments were carried out and results indicated that nanofibres on different part of mats had a relative stable result and repeat experimental error was kept below 4%.

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DEVELOPMENT AND CHARACTERIZATION OF NOVEL SITE SPECIFIC FLOATING-MUCOADHESIVE TABLETS BEARING 5-FLOUROURACIL FOR STOMACH TARGETING.

INDIAN DRUGS ◽

10.53879/id.51.09.10140 ◽

2014 ◽

Vol 51 (09) ◽

pp. 23-30

Author(s):

P Bhardwaj ◽

◽

R Singh ◽

A Swarup

Keyword(s):

Drug Release ◽

Methyl Cellulose ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Wet Granulation ◽

Prolonged Release ◽

Mucoadhesive Tablets

Object of present investigation was to develop and characterize such a gastroretentive tablet, which provides the synergism effect of adhesiveness and floating property for prolonged release of 5-flourouracil within the stomach. The floating mucoadhesive tablets were prepared by the wet granulation method using different ratios of hydroxy propyl methyl cellulose (HPMC K4MCR) and Carbopol 934P as polymers. The prepared floating-mucoadhesive tables were characterized for hardness, detachment stress, floating properties, swelling index and surface morphology by SEM. The in vitro drug release and floating behaviour were studied in simulated gastric fluid (SGF) at pH 1.2. Different kinetic models for drug release were as well applied. Formulations of T-9 batch were furthermore subjected to stability and in vivo radiographic studies.

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Development and Characterization of Water-in-Oil Microemulsion for Transdermal Delivery of Eperisone Hydrochloride

Applied Clinical Research Clinical Trials and Regulatory Affairs ◽

10.2174/2213476x06666190318120522 ◽

2020 ◽

Vol 7 (1) ◽

pp. 45-64

Author(s):

Monika D. Kumbhar ◽

Manisha S. Karpe ◽

Vilasrao J. Kadam

Keyword(s):

Drug Release ◽

Zeta Potential ◽

Droplet Size ◽

Ex Vivo ◽

In Vitro Release ◽

Tween 80 ◽

Physical Parameters ◽

Scanning Calorimetry ◽

Spontaneous Emulsification

Background: Eperisone hydrochloride possesses short biological half-life due to first pass metabolism resulting in low bioavailability and short duration of response with toxic effects, ultimately limits its utilization for treatment of muscle spasm. Objective: In view of this background, current study was designed for the development of Eperisone hydrochloride-loaded microemulsion and Eperisone hydrochloride-loaded microemulsion based cream for topical delivery and compared it with conventional cream. Methods: Firstly, water-in-oil microemulsion was prepared by spontaneous emulsification method. The concentration of components was found out from existence of microemulsion region by constructing pseudoternary phase diagram. The oil was selected on the basis of drug solubility effect on the drug release, whereas surfactant and cosurfactant were screened on the basis of their efficiency to form microemulsion region. The influence of components on microemulsion formation, drug release capacity, permeation was studied by differential scanning calorimetry, X-ray diffraction, in-vitro release and ex-vivo drug permeation studies respectively. By using microemulsion, the cream was prepared for proving optimum structure for topical application. Microemulsion was evaluated for droplet size, zeta potential, pH, viscosity and conductivity. Besides the cream was characterized for pH, rheology and stability. Permeation of EPE from microemulsion across the rat skin was evaluated and compared with conventional cream. Results: The microemulsion consisting Isopropyl Myristrate/Water/Span 80:Tween 80 (50/8/42% by weight) possessed droplet size of 95.77nm, zeta potential of −5.23 mV with 7.25 pH and conductivity near to zero (<0.05mScm-1). Physical parameters of the cream were satisfactory, also 2.33-fold higher permeation and 1.57-fold higher release observed as compared to conventional cream. Conclusion: It can be concluded that Eperisone hydrochloride-loaded microemulsion and its cream is being effectively used for muscle spasticity by topical route.

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Ciprofloxacin-Collagen-Based Materials with Potential Oral Surgical Applications

Polymers ◽

10.3390/polym12091915 ◽

2020 ◽

Vol 12 (9) ◽

pp. 1915

Author(s):

Daniel-Cristian Ioan ◽

Ileana Rău ◽

Mădălina Georgiana Albu Kaya ◽

Nicoleta Radu ◽

Marinela Bostan ◽

...

Keyword(s):

Drug Release ◽

Cytotoxic Drug ◽

Synthesis And Characterization ◽

In Vitro Tests

We report in this paper the synthesis and characterization of a new collagen-based material. This material was obtained in a spongy form and was functionalized with an antibiotic, ciprofloxacin. The targeted applications of these kind of materials concern the post-operative prophylaxis. The in vitro tests (antimicrobial, cytotoxic, drug release) showed that sponges with a concentration of 0.75 g of ciprofloxacin per gram of collagen could be beneficial for the desired applications.

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PREPARATION AND CHARACTERIZATION OF METFORMIN LOADED STEARIC ACID COUPLED F127 NANOPARTICLES

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i8.26444 ◽

2018 ◽

Vol 11 (8) ◽

pp. 212

Author(s):

Vipan Kumar Kamboj ◽

Prabhakar Kumar Verma

Keyword(s):

Drug Release ◽

Zeta Potential ◽

Stearic Acid ◽

In Vitro Release ◽

Particle Diameter ◽

Class Iii ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Scanning Calorimetry

Objective: The objective of this study was to prepare and evaluate metformin nanoparticles (MN) using stearic acid-coupled F127 (SAF127) copolymer and polyvinyl alcohol by emulsion solvent evaporation technique.Method: Metformin is the first-line drug for the treatment of type II diabetes mellitus belongs to Biopharmaceutical Classification System Class III. The prepared MN was characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment, percentage yield, in vitro drug release, and stability studies. The compatibility studies were performed by Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The crystallographic and surface properties were studied by X-ray diffractometry and scanning electron microscopy, respectively.Results: The mean particle diameter of prepared nanoparticles ranged from 207.8 to 977.64 nm, PDI value ranged from 0.146 to 0.694, and zeta potential ranged from −20.5 to −6.97 mV. The drug entrapment efficiency of these nanoparticles varies between 18.81 to 69.01 %. The drug to SAF127 copolymer (10/30 w/w) ratio (MN3) showed optimum results. The MN3 had spherical morphology with semi-amorphous nature. The results of FTIR and DSC analysis showed that there was no significant interaction between drug and excipients. The prepared polymeric nanoparticles were stable at 5±3°C up to 3 months. In vitro release of drug from MN3 was 20.52% in the first 1 h and remaining drug was released up to 30 h.Conclusion: The results of this study confirmed the sustained drug release profile of metformin loaded SAF127 copolymer nanoparticles. These nanoparticles can be best stored up to 3 months.

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Release of Aspirin from Biodegradable Polyesterurethane Networks

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.79-82.1431 ◽

2009 ◽

Vol 79-82 ◽

pp. 1431-1434 ◽

Cited By ~ 7

Author(s):

Ya Kai Feng ◽

Shi Feng Zhang ◽

Li Zhang ◽

Jin Tang Guo ◽

Yong Shen Xu

Keyword(s):

Drug Release ◽

Release Rate ◽

In Vitro Release ◽

Degradation Process ◽

Crosslinking Density ◽

Release Mechanism ◽

Scanning Calorimetry ◽

Model Drug ◽

Phosphate Buffered Saline

In this paper, the release of model drug aspirin (ASP) from biodegradable polyesterurethane networks was studied. Poly(D,L-lactide-co-glycolide)urethane (PULG) networks were prepared from hydroxyl telechelic star-shaped oligo(D,L-lactide-co-glycolide) coupled with 1,6-diisocyanate-2,2,4-trimethylhexane and 1,6-diisocyanate-2,4,4-trimethylhexane or isophorone diisocyanate. PULG networks turned from transparent to opaque after ASP loading. PULG networks with lower crosslinking density always resulted in higher drug loaded content. The results of differential scanning calorimetry (DSC) and scanning electron microscope (SEM) measurements demonstrated that ASP was uniformly distributed in the networks. The drug release courses of ASP from PULG networks in phosphate buffered saline pH = 7.0 at 37 °C could be divided into three stages. Firstly, ASP release was at approximately uniform rate from PULG networks; Secondly, the release rate obviously increased for the degradation of the PULG networks; Thirdly, the release rate decreased gradually because most of the ASP had diffused out of the PULG networks. The crosslinking density of polyesterurethane networks also affected drug release rate. The in vitro release test revealed that ASP accelerated the degradation process of PULG, which exhibited a typical erosion-controlled release mechanism.

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Evaluation of Transdermal Formulations of Metoclopramide Prepared Using Arachis Oil and Liquid Paraffin as Permeation Enhancers

Pharmaceutical and Biomedical Research ◽

10.18502/pbr.v6i3.4648 ◽

2020 ◽

Author(s):

Sylvester O. Eraga ◽

Matthew I. Arhewoh ◽

Ogochukwu A. Meko

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Release Kinetics ◽

Liquid Paraffin ◽

In Vitro Release ◽

Methyl Cellulose ◽

Tween 80 ◽

Patient Acceptance ◽

Scanning Calorimetry

Background: The study aimed to evaluate the effect of arachis oil and liquid paraffin on metoclopramide release from transdermal films. Objectives: Batches of metoclopramide films were prepared with hydroxypropyl methyl cellulose (HPMC), arachis oil or liquid paraffin and Tween 80 as plasticizer. The films were evaluated for their physiochemical properties, in vitro and ex vivo drug release and drug release kinetics. Drug-excipient interactions were investigated using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy. Methods: The transdermal films had a weight range of 0.22-0.24 g, folding endurance of 300-306, percentage moisture content and uptake of 2%-10% and 19%-110%, respectively and drug content of 98%-104%. There was similar condition in vitro release profile for the films but their ex vivo profiles exhibited variable drug release with the P3 (30% arachis oil) giving the highest drug (almost 100%) release. Results: The release kinetics of metoclopramide followed the first order and Korsemeyer-Peppas models more closely as seen in their correlation coefficients (R2) of 0.9832 and 0.9560, respectively. Drug-excipient compatibility studies showed no interactions between excipients and metoclopramide. Conclusion: The formulated transdermal films showed controlled drug release over a period of 12 h. Arachis oil and liquid paraffin showed similar permeation enhancing ability. These enhanced permeation properties of the films could be helpful in the development of alternative route for metoclopramide administration in the management of emesis with improved patient acceptance.

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