Preparation, characterization, and in vitro release kinetics of doxorubicin-loaded magnetosomes

The doxorubicin (DOX) was successfully coupled to the magnetosomes from Acidithiobacillus ferrooxidans ( At. ferrooxidans) by genipin bridging. The parameters (magnetosome concentration, DOX concentration, genipin concentration-, and cross-link time) expected for temperature significantly influenced the coupling rate. Bacterial magnetosome-doxorubicin complexes (BMDCs) were characterized by transmission electron microscope (TEM), particle size analyzer and Fourier transform infrared spectroscopy. Results indicated that BMDCs exhibited a mean particle size of 83.98 mm and displayed a negative charge. The chemical reaction occurring between CO and NH group and the physical adsorption predominated by electrostatic interaction were found to involve in coupling. BMDCs can release 40% of DOX in simulated gastrointestinal conditions within 38 h. Kinetic models including Higuchi, Korsmeyer–Peppas, Zero order, First order, Hixon-Crowell, Baker-Lonsdale, and Weibull and Gompertz were utilized to explore the release mechanism of DOX from BMDCs. All models were found to fit well (r2 ≥ 0.8144) with the release data and the Gompertz was the best fit model (r2 = 0.9742), implying that the complex mechanisms involving Fickian and Gompertz diffusion contributed to the release. These findings suggested that magnetosomes from At. ferrooxidans have great potential applications in biomedical and clinical fields as the carrier of target drug delivery systems in the future.

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Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

10.20944/preprints201807.0165.v1 ◽

2018 ◽

Author(s):

Barkat Khan ◽

Faheem Haider ◽

Kifayat Shah ◽

Bushra Uzair ◽

Kaijian Hou ◽

...

Keyword(s):

Controlled Release ◽

Drug Release ◽

Release Kinetics ◽

Immediate Release ◽

Matrix Tablets ◽

Release Mechanism ◽

In Vitro Drug Release ◽

Solubility Study ◽

Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

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DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v7i6.559 ◽

2018 ◽

Vol 7 (6) ◽

Author(s):

Mohini Sihare ◽

Rajendra Chouksey

Keyword(s):

Drug Release ◽

Release Kinetics ◽

In Vitro Release ◽

Release Profile ◽

Matrix Tablets ◽

In Vivo Studies ◽

Release Mechanism ◽

In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

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DEVELOPMENT, CHARACTERIZATION AND IN VITRO RELEASE KINETIC STUDIES OF IBANDRONATE LOADED CHITOSAN NANOPARTICLES FOR EFFECTIVE MANAGEMENT OF OSTEOPOROSIS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i6.42697 ◽

2021 ◽

pp. 120-125

Author(s):

S. PATHAK ◽

S. P. VYAS ◽

A. PANDEY

Keyword(s):

Electron Microscopy ◽

Particle Size ◽

Sodium Tripolyphosphate ◽

Release Kinetics ◽

Ph Effect ◽

Chitosan Nanoparticles ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Release Kinetic

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR). Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.

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FLUCONAZOLE NANOGEL: FABRICATION AND IN VITRO EVALUATION FOR TOPICAL APPLICATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i4.40531 ◽

2021 ◽

pp. 272-277

Author(s):

DIVYA ◽

INDERBIR SINGH ◽

UPENDRA NAGAICH

Keyword(s):

Particle Size ◽

Drug Release ◽

Release Kinetics ◽

Seborrheic Dermatitis ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Tween 80 ◽

Flow Index ◽

In Vitro Evaluation

Objective: The aim of this study is to develop and in vitro evaluation of prepared fluconazole nanogel for seborrheic dermatitis Methods: Fluconazole nanogel was formulated to act against seborrheic dermatitis. The fluconazole nanoparticles were prepared by a simplified evaporation method and evaluated for particle size, entrapment efficiency, and percent in vitro drug release. The nanogel was also characterized based on parameters like particle size, percent entrapment efficiency, shape surface morphology, rheological properties, in vitro release R² = 0.9046, and release kinetics. Results: The nanoparticle with a combination of Eudragit RS and Tween 80 showed the best result with particle size in the range of 119.0 nm to 149.5 nm, with a cumulative percent drug release of 95 % up to 18 h. The formulated nanogel with optimum concentration of HPMC authenticate with particle size 149.50±0.5 with maximum drug release (92.13±0.32) %. Conclusion: Different percentages of polymers (ethyl-cellulose, eudragit, and tween 80) are used as variable components in the formulation of nanogel. The optimized batch showed good physical properties (flow index, spreadability, and viscosity) along with rapid drug release. Therefore, it can be concluded that nanogel containing fluconazole has potential application in topical delivery.

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An Innovative Formulation Based on Nanostructured Lipid Carriers for Imatinib Delivery: Pre-Formulation, Cellular Uptake and Cytotoxicity Studies

Nanomaterials ◽

10.3390/nano12020250 ◽

2022 ◽

Vol 12 (2) ◽

pp. 250

Author(s):

Evren Gundogdu ◽

Emine-Selin Demir ◽

Meliha Ekinci ◽

Emre Ozgenc ◽

Derya Ilem-Ozdemir ◽

...

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Cellular Uptake ◽

Enzyme Inhibitor ◽

Release Kinetics ◽

In Vitro Release ◽

Nanostructured Lipid Carrier ◽

Loading Capacity ◽

Cytotoxicity Studies

Imatinib (IMT) is a tyrosine kinase enzyme inhibitor and extensively used for the treatment of gastrointestinal stromal tumors (GISTs). A nanostructured lipid carrier system (NLCS) containing IMT was developed by using emulsification–sonication methods. The characterization of the developed formulation was performed in terms of its particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, loading capacity, sterility, syringeability, stability, in vitro release kinetics with mathematical models, cellular uptake studies with flow cytometry, fluorescence microscopy and cytotoxicity for CRL-1739 cells. The particle size, PDI, loading capacity and zeta potential of selected NLCS (F16-IMT) were found to be 96.63 ± 1.87 nm, 0.27 ± 0.15, 96.49 ± 1.46% and −32.7 ± 2.48 mV, respectively. F16-IMT was found to be stable, thermodynamic, sterile and syringeable through an 18 gauze needle. The formulation revealed a Korsmeyer–Peppas drug release model of 53% at 8 h, above 90% of cell viability, 23.61 µM of IC50 and induction of apoptosis in CRL-1739 cell lines. In the future, F16-IMT can be employed to treat GISTs. A small amount of IMT loaded into the NLCSs will be better than IMT alone for therapy for GISTs. Consequently, F16-IMT could prove to be useful for effective GIST treatment.

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Release Kinetics Study of Azithromycin from Bi-layered Tablets

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v20i1.32094 ◽

2017 ◽

Vol 20 (1) ◽

pp. 54-63

Author(s):

FM Shah Noman Ul Bari ◽

Muhammad Rashedul Islam ◽

Md Mizanur Rahman Moghal ◽

Israt Jahan Ira

Keyword(s):

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Pharmaceutical Journal ◽

High Viscosity ◽

Release Mechanism ◽

Low Viscosity ◽

Release Studies ◽

Vitro Release

The objective of this study was to analysis in vitro release kinetics of Azithromycin from bi-layer tablets prepared by direct compression using high viscosity to low viscosity grades of hydroxypropyl methyl cellulose (HPMC K15M, HPMC K4M, HPMC 50 cps), Carbopol 934p and Carbopol 974p. In addition, it also includes evaluating the effect of formulation variables like polymer proportion and polymer viscosity on the release of Azithromycin. In vitro release studies were performed using USP Type-II (Rotating paddle method) at 100 rpm. The dissolution medium consisted of 0.1N HCl (900 ml) for the first 2 hr and the phosphate buffer (pH 6.0) from 3rd to 10th hour. From twenty five different formulations (F-1 to F-25) based on polymer variation, model-dependent and independent methods were used for data analysis and the best results were observed for HPMC 50cps in Korsmeyer- Peppas (R2=0.995 on F-23) kinetic model. The release mechanism of all formulations was Fickian.Bangladesh Pharmaceutical Journal 20(1): 54-63, 2017

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Effect of Polymers nature and Stirring Speeds on Physicochemical Properties and the Controlled Release of Allopurinol-loaded Microspheres

Journal of the Mexican Chemical Society ◽

10.29356/jmcs.v66i1.1583 ◽

2021 ◽

Vol 66 (1) ◽

Author(s):

Karima Badis ◽

Haouaria Merine ◽

Youssef Ramli ◽

OumCheikh Larbi ◽

Cherifa Hakima Memou

Keyword(s):

Fourier Transforms ◽

Release Kinetics ◽

Drug Loading ◽

In Vitro Release ◽

Release Mechanism ◽

Release Studies ◽

Fourier Transforms Infrared Spectroscopy ◽

The Mean ◽

Solvent Evaporation Process

Abstract. Allopurinol is an antigout drug therapy, commonly used in the treatment of chronic gout or hyperuricaemia associated with treatment of diuretic conditions. In the present study, new formulations based on Allopurinol, have been prepared with the microencapsulation by solvent evaporation process. Microspheres were prepared using pure Allopurinol and polymeric matrices (ethylcellulose EC, poly (ε-caprolactone) PCL, β-cyclodextrin CD and hydroxypropylmethylcellulose HPMC) at different compositions and stirring speeds to investigate the effect of these parameters on loading efficiency and drug release kinetics. The formulations produced were characterized by various methods : Fourier transforms infrared spectroscopy (FTIR), X-ray powder diffractometry, optical microscopy, surface morphology by scanning electron microscopy (SEM) and drug loading, as well as in vitro release studies in the simulated stomach tract. Depending on the stirring speed and the composition of the microparticles, the active ingredient loading is in a range from 10.46 ± 1.45 to 46.40 ± 0.5%. The microspheres are spherical and the mean Sauter diameter (d32) of the microparticles obtained is smaller and is in the range of 47.71 to 151.01 µm. Different release profiles were obtained and show that the release rate is strongly influenced by the characteristics of the microparticles ; namely, the stirring rates and the composition of the microparticles. The release mechanism was identified by modelling using Higuchi and Korsmeyer-Peppas models. Resumen. Alopurinol es una droga terapéutica para tratar la gota, y se utiliza en el tratamiento de gota crónica o hiperuricemia asociada con el tratamiento de condiciones diuréticas. En este estudio, nuevas formulaciones basadas en Alopurinol se prepararon mediante microencapsulación por el proceso de evaporación de disolvente. Microesferas se prepararon usando Alopurinol puro y diferentes matrices poliméricas (etil-celulosa EC, poli(-caprolactona) PCL, β-cyclodextrina CD e hidroxipropil-metil-celulose HPMC) en diferentes composiciones y velocidades de agitación, para investigar el efecto de estos parámetros en la eficiencia de carga y en la cinética de liberación del fármaco. Las formulaciones obtenidas fueron caracterizadas por diferentes técnicas : Espectroscopía infrarroja de transformadas de Fourier (FTIR), difractometría de rayos X de polvos, microscopía óptica, morfología de superficies mediante microscopía electrónica de barrido electrónico, y la eficiencia de carga del fármaco, así como estudios de liberación in vitro en tracto estomacal simulado. Dependiendo de la velocidad de agitación y la composición de las micropartículas, la carga del ingrediente activo se encuentra en el rango de 10.46 ± 1.45 a 46.40 ± 0.5%. Las microesferas son esféricas y el diámetro medio de Sauter (d32) de las micropartículas obtenidas es menor, y se encuentra en el rango de 47.71 a 151.01 µm. Se obtuvieron diferentes perfiles de liberación y se observa que la velocidad de liberación está influenciada principalmente por las características propias de la producción de las micropartículas ; en particualr, las velocidades de agitación y las composición de las micropartículas. El mecanismo de liberación se ajusta mejor a los modelos matemáticos de Higuchi and Korsmeyer-Peppas.

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Formulation and Ex-vivo Evaluation of Glipizide Buccal Tablets

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2014.7.2.10 ◽

2014 ◽

Vol 7 (2) ◽

pp. 2487-2493

Author(s):

Sudarshan Singh ◽

Sandip G Maru ◽

Sunil Bothara B

Keyword(s):

Guar Gum ◽

Chemical Interaction ◽

Ex Vivo ◽

Release Kinetics ◽

In Vitro Release ◽

Aloe Vera ◽

Release Mechanism ◽

Drug Release Profile ◽

Buccal Tablets

Bioadhesive materials are agents which adhere to the mucous membrane due to specific properties and release the drug at the site of action in controlled manner. Since the biodegradability of the synthetic polymer is at some instance hesitant. In this exploration, a bioadhesive polymer has been developed which was isolated from leaves of Aloe vera (L.) Burm. f. The mucilage isolated from A. vera were used as a bioadhesive polymer in tablet formulation and evaluated for the parameters such as swelling, pH, and bioadhesive property like bioadhesive strength, record of adherence and ex-vivo residence time. The buccal bioadhesive tablet was prepared using glipizide as model drug. The prepared tablet was evaluated against existing bioadhesive polymer such as guar gum and hydroxyl propyl cellulose. Swelling index and surface pH was found to be 13.12-18.06% and 6.5-6.9 respectively. The drug permeation through goat buccal mucosa was found to be 60.21 ± 0.06 % in the end of 7 h with a Jss of 0.24 mg h-1 cm-2. The stability studies were performed on optimized formulation as per ICH guideline, result showed that there was no significant change in physical characteristic, adhesive strength and in vitro release. It was observed that as the concentration of mucilage increases swelling index also increases. Results of pH showed that mucilage is slightly near to neutral in nature. Formulations were evaluated for preformulation parameters, in vitro drug release profile and release kinetics. The formulations were found to have good preformulation characteristics. FTIR spectroscopy showed no significant chemical interaction within drug and excipients. The release mechanism of glipizide from buccal tablets indicated anomalous (non-fickian) transport mechanism and followed zero order kinetics. It was concluded that the mucilage of A. vera can be used as a pharmaceutical excipient in buccal bioadhesive drug delivery systems.

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Preparation and characterization of microcapsules of Pterodon pubescens Benth. by using natural polymers

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502014000400028 ◽

2014 ◽

Vol 50 (4) ◽

pp. 919-930 ◽

Cited By ~ 7

Author(s):

Alexandre Espada Reinas ◽

Jaqueline Hoscheid ◽

Priscila Miyuki Outuki ◽

Mara Lane Carvalho Cardoso

Keyword(s):

Molecular Weight ◽

Release Kinetics ◽

In Vitro Release ◽

Chemical Degradation ◽

Release Mechanism ◽

Natural Polymers ◽

Alcohol Extract ◽

Polymeric Systems ◽

Formulation Parameters

An oleaginous fraction obtained from an alcohol extract of the fruit of Pterodon pubescensBenth. (FHPp) was microencapsulated in polymeric systems. These systems were developed using a complex coacervation method and consisted of alginate/medium-molecular-weight chitosan (F1-MC), alginate/chitosan with greater than 75% deacetylation (F2-MC), and alginate/low-molecular-weight chitosan (F3-MC). These developed systems have the potential to both mask the taste of the extract, and to protect its constituents against possible chemical degradation. The influence of the formulation parameters and process were determined by chemical profiling and measurement of the microencapsulation efficiency of the oleaginous fraction, and by assessment of microcapsule morphology. The obtained formulations were slightly yellow, odorless, and had a pleasant taste. The average diameters of the microcapsules were 0.4679 µm (F2-MC), 0.5885 µm (F3-MC), and 0.9033 µm (F1-MC). The best formulation was F3-MC, with FHPp microencapsulation efficiency of 61.01 ± 2.00% and an in vitro release profile of 75.88 ± 0.45%; the content of vouacapans 3-4 was 99.49 ± 2.80%. The best model to describe the release kinetics for F1-MC and F3-MC was that proposed by Higuchi; however, F2-MC release displayed first-order kinetics; the release mechanism was of the supercase II type for all formulations.

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Preparation and in vitro release kinetics of ivermectin sustained-release bolus optimized by response surface methodology

PeerJ ◽

10.7717/peerj.5418 ◽

2018 ◽

Vol 6 ◽

pp. e5418 ◽

Cited By ~ 1

Author(s):

Xiangchun Ruan ◽

Xiuge Gao ◽

Ying Gao ◽

Lin Peng ◽

Hui Ji ◽

...

Keyword(s):

Response Surface Methodology ◽

Sustained Release ◽

Response Surface ◽

Release Kinetics ◽

In Vitro Release ◽

Information Criterion ◽

Quadratic Model ◽

Dissolution Time ◽

Release Mechanism

Sustained-release formulations of ivermectin (IVM) are useful for controlling parasitic diseases in animals. In this work, an IVM bolus made from microcrystalline cellulose (MCC), starch and low-substituted hydroxypropyl cellulose (LS-HPC) was optimized by response surface methodology. The bolus was dissolved in a cup containing 900 mL of dissolution medium at 39.5 °C, under with stirring at 100 rpm. A quadratic model was formulated using analysis of variance according to the dissolution time. The optimized formulation of the bolus contained 8% MCC, 0.5% starch, and 0.25% LS-HPC. The length, width, and height of the prepared IVM bolus were 28.12 ± 0.14, 16.1 ± 0.13, and 13.03 ± 0.05 mm, respectively. The bolus weighed 11.4842 ± 0.1675 g (with a density of 1.95 g/cm3) and contained 458.26 ± 6.68 mg of IVM. It exhibited in vitro sustained-release for over 60 days, with a cumulative amount and percentage of released IVM of 423.72 ± 5.48 mg and 92.52 ± 1.20%, respectively. The Korsmeyer–Peppas model provided the best fit to the dissolution release kinetics, exhibiting anR2value close to 1 and the lowest Akaike Information Criterion among different models. The parametern(0.5180) of the Korsmeyer–Peppas model was between 0.45 and 0.89. It was demonstrated that the release mechanism of the IVM bolus followed a diffusive erosion style.

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