Controlled release of amoxicillin from PMMA and poly(butylsuccinate) microspheres

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Release Kinetics ◽  
Tween 80 ◽  
Water Emulsion ◽  
Polymeric Systems ◽  
Evaporation Technique ◽  
Polybutylene Succinate ◽  
Oil Water

This work focus on the study and the elaboration of microspheres based on amoxicillin (AMO), those microspheres were prepared through the oil/water emulsion evaporation technique. Polybutylene succinate (PBS) and Poly(methylmethacrylate) (PMMA) polymeric matrix were used with Tween 80 (T80) and Polyvinyl alcohol (PVA) as emulsifiers. These polymeric systems were analyzed by SEM, FTIR and optical microscopy. The conditions of the microspheres forming were varied and the preparation was performed by changing different parameters such as: the nature of the polymer, the stirring speed, organic solvent, surfactant nature, and concentration, which allows the study of their effect on encapsulation efficiency and drug release kinetics. These parameters affect strongly the size of microspheres, the drug content and the drug release, the latter is settled in an artificially reconstituted media of pH = 1.2 transcribed from the stomachal medium.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

Evaluation of Kollicoat SR 30D and Kollicoat EMM 30D as Matrix Former for Controlled Release Drug Delivery

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mohammad Salim Hossain ◽  
Reza-ul Jalil ◽  
Selim Reza ◽  
Mohiuddin Abdul Quadir ◽  
CF Hossain
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Matrix Effects ◽  
Release Kinetics ◽  
Polymeric Systems ◽  
Release Drug ◽  
The Matrix ◽  
Kinetics Of ◽  
Order Pattern ◽  
Drug Liberation

Efficiency of kollicoat EMM 30 D and SR 30D as matrix forming material was investigated. It was found that, theophylline loaded granules prepared with these two polymers could not sustain drug release for a significant period of time. However, compression of these granules into tablets retarded drug release for up to 8 hours. Release was faster from EMM 30D polymeric system than that from SR 30D matrix. Effects of fillers and rate modifiers on drug liberation have been assessed. Incorporation of Avicel RC 591 and starch caused substantial release of theophylline from both the polymeric systems. Avicel PH 101 intensified the retardation effect of both EMM 30D and SR 30D on theophylline release. HPMC 50 cps, when added to the matrix, caused the release of theophylline to follow near zero order pattern. Increasing the content of HPMC in both EMM 30D and SR 30D compressed tablets decreased the rate and extent of theophylline release. In the presence of excipients, no significant differences between rate and extent of drug release from EMM 30D and SR 30D systems were found. Biexponential equation was applied to explore and explain drug release kinetics. It was found that drug release followed Fickian or case I kinetics from EMM 30D compressed tablet while anomalous or non-fickian kinetics of drug release was observed for SR 30D system. Key words: Kolliocoat SR 30D, Kollicoat EMM 30D, Theophylline, Matrix system, Controlled release Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals ENCAPSULATION OF IBUPROFEN INTO SOLID LIPID NANOPARTICLES FOR CONTROLLED AND SUSTAINED RELEASE USING EMULSIFICATION SOLVENT EVAPORATION TECHNIQUE

2019 ◽  
pp. 74-81
Author(s):  
WESLEY N OMWOYO ◽  
MAKWENA J MOLOTO
Keyword(s):  
Fourier Transform ◽  
Infrared Spectroscopy ◽  
Controlled Release ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Release Kinetics ◽  
Lipid Nanoparticles ◽  
The Matrix ◽  
Evaporation Technique ◽  
Emulsification Solvent Evaporation

Objective: The objective of the study was to encapsulate ibuprofen (IBU) into solid lipid nanoparticles (SLNs) for enhanced dissolution and achieving a sustained and controlled release of the drug from the nanocarrier. Methods: IBU loaded nanoparticles were prepared by emulsification solvent evaporation technique and characterized by Fourier Transform Infrared spectroscopy, Thermogravimetric Analysis, X-ray diffraction (XRD), and transmission electron microscopy. Release kinetics on the drug-loaded nanoparticles was carried out in phosphate buffer pH 6.8 using pharma test dissolution apparatus adopting shaking basket method at 37°C. Results: The optimized IBU-loaded SLNs had a particle size of 76.40 nm, polydispersity index of 0.275, and zeta potential of −41.3 mV. The encapsulation efficiency (EE) and DL were 99.73% and 2.31%, respectively. The Fourier transform infrared spectroscopy (FTIR) spectra confirmed successful encapsulation of the drug inside the nanocarrier as only peaks responsible for the emulsifier and the binder could be identified. This corroborated well with XRD spectra which showed a completely amorphous state of the drug-loaded nanoparticles as compared to the crystalline nature of the pure drug. The IBU-SLNs showed a release profile of up to 8 h which is a great improvement from other reported works. The drug release pattern of IBU-SLNs was best fitted with Higuchi square root model and followed the Higuchi drug release kinetics. Korsmeyer-Peppas model confirmed a non-Fickian diffusion model for the release of the drug from the matrix system. Conclusion: IBU-loaded SLNs were successfully prepared which had a sustained and controlled release. It was observed that the release of the drug from the matrix was diffusion controlled and time dependent.

scholarly journals Preparation and Evaluation of In Vitro Release Kinetics of Theophylline Loaded Matrix Tablet Based on Eudragit NE 30 D and Eudragit RS 30 D

1970 ◽  
Vol 8 (2) ◽  
pp. 153-159
Author(s):  
Mohammad Borhan Uddin ◽  
Jakir Ahmed Chowdhury ◽  
Kazi Rashidul Azam ◽  
Reza-ul Jalil ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Matrix Tablet ◽  
Matrix System ◽  
Polymeric Systems ◽  
Eudragit Rs ◽  
Kinetics Of ◽  
Preparation And Evaluation

In the present study efficiency of Eudragit NE 30 D and RS 30 D as matrix forming materials was investigated. It was found that theophylline loaded granules prepared with these two polymers could not sustain drug release for a significant period of time. However, compression of these granules into tablets retarded drug release for up to 7 hours. Release was similar with both of the polymers. Effects of fillers and rate modifiers on drug release have been assessed. Incorporation of lactose and starch caused substantial release of theophylline from both the polymeric systems. Avicel PH 101 intensified the retardation effect of both NE 30 D and RS 30 D on theophylline release. Hydrophobic excipients also show retardation of release from both NE 30 D and RS 30 D. Key words: Eudragit RS 30 D; Eudragit NE 30 D; Theophylline; Matrix system; Controlled release DOI: 10.3329/dujps.v8i2.6030 Dhaka Univ. J. Pharm. Sci. 8(2): 153-159, 2009 (December)

scholarly journals Multiparticulate Drug Delivery System for Gastrointestinal Tuberculosis

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
Monica RP Rao ◽  
Mayuri K. Magar
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Glycol Succinate ◽  
Moderate Increase ◽  
32 Factorial Design

Drug solubility poses numerous challenges in design of formulations for drugs with poor aqueous solubility. Ethionamide is an antitubercular drug belonging to biopharmaceutical classification system class II drug having less aqueous solubility. Nanosuspensions were prepared by using various solvents such as methanol, ethanol, acetone and chloroform and it was prepared using anti-solvent precipitation technique by using probe sonication. Various stabilizers such as tocopherolpolythytlene glycol succinate, polyvinylpyrrolidone and tween 80 singly or in combination were studied. A 32 factorial design was employed to study the effect of independent variables, concentration of stabilizers and stirring speed on particle size and cumulative percent drug release. The particle size of the optimized batch was 97.54 ± 8.47 nm with polydispersity index of 0.36 and zeta potential -10.1 ± 2.3 mV. The cumulative percent drug release of optimized batch was found to be 95.01 ± 1.16% in 60 min. Optimized batch was ultracentrifuged and evaluated for saturation solubility studies, stability and powder X-ray Diffraction studies. Optimized nanosuspension was loaded on Espheres by spraying in a coating pan and then coating of Eudragit controlled release polymers. The coated Espheres were evaluated for drug content, friability, scanning electron microscopy, ex-vivo permeation studies and drug release kinetics studies. The friability value for primary coated sphere was found to be 0.8 ± 0.12% and for secondary was 1% and the best fit model was found to be Korsmeyer-Peppas model which is indicative of diffusion controlled release. Ex vivo diffusion studies revealed a moderate increase in permeability.

scholarly journals Effect of the formulation parameters on the encapsulation efficiency and release behavior of p-aminobenzoic acid-loaded ethylcellulose microspheres

2016 ◽  
Vol 81 (10) ◽  
pp. 1183-1198 ◽  
Author(s):  
Meryem Mouffok ◽  
Abderrezzak Mesli ◽  
Ilham Abdelmalek ◽  
Etienne Gontier
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Aminobenzoic Acid ◽  
The Mean ◽  
Formulation Parameters ◽  
Release Data

In the current study, p-aminobenzoic acid-loaded ethylcellulose microspheres were prepared under various conditions by solvent evaporation method (o/w). This preparation was carried out with different p-aminobenzoic acid:ethylcellulose (PABA:EC) ratios, stirring speed, surfactant nature and concentration in order to investigate their effect on encapsulation efficiency and drug release kinetics. Scanning Electron Microscopy (SEM) studies showed spherical microspheres with a porous surface and different structures. The mean diameter of Sauter (d32) of these microparticles is in the range from 47 to 165 ?m with PVA and from 793 to 870 ?m with Tween 80 by adjusting process parameters. However, the encapsulation efficiency varied from 37.52 to 79.05 % suitable for the adjustment of a p-aminobenzoic acid with pro-longed release. Microspheres were characterized by FTIR, DSC and XRD. The release of cation of p-aminobenzoic acid was performed in simulated gastric medium at pH 1.2 and 37?0.5?C by UV-VIS analysis to estimate its content. The release data were best fitted to Higuchi model with high correlation coefficient (r?) and the obtained values of n from Korsmeyer-Peppas showed that the drug release follows the Fickian diffusion mechanism.

Optimization Study to Develop Once-a-day Controlled Release Formulation of Metoclopramide with Predictable Design Space

1970 ◽  
Vol 1 (1) ◽  
pp. 71-76
Author(s):  
Rajesh Dubey ◽  
Udaya K. Chowdary ◽  
Venkateswarlu V.
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Design Space ◽  
Release Kinetics ◽  
Release Profile ◽  
Release Formulation ◽  
Linear Effect ◽  
Controlled Release Formulation ◽  
The Difference ◽  
Face Centered

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile

scholarly journals DESIGN AND EVALUATION OF CONTROLLED-RELEASE OCULAR INSERTS OF BRIMONIDINE-TARTRATE AND TIMOLOL MALEATE

2016 ◽  
Vol 9 (1) ◽  
pp. 79 ◽  
Author(s):  
Preethi G. B. ◽  
Prashanth Kunal
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Release Kinetics ◽  
Water Soluble ◽  
Moisture Loss ◽  
Timolol Maleate ◽  
Brimonidine Tartrate

<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.<strong></strong></p><p><strong>Methods: </strong>Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and <em>in vitro </em>release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.<strong></strong></p><p><strong>Results: </strong>It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. <strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, <em>in vitro</em> drug release and stability.</p>

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

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.

scholarly journals PREPARATION, PHYSICAL CHARACTERIZATION, AND PHARMACOKINETIC STUDY OF DOCETAXEL NANOCRYSTALS

2019 ◽  
pp. 238-244
Author(s):  
ARVIND GANNIMITTA ◽  
PRATHIMA SRINIVAS ◽  
VENKATESHWAR REDDY A ◽  
PEDIREDDI SOBHITA RANI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Water Solubility ◽  
Release Kinetics ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Sustained Drug Release ◽  
Egg Lecithin

Objective: The main objective of this study was to prepare and evaluate the nanocrystal formulation of docetaxel. Methods: Docetaxel nanocrystals were formulated to improve the water solubility. Docetaxel nanocrystals were prepared by nanoprecipitation method using Tween 80, egg lecithin, and povidone C-12 as stabilizers and poly(lactic-co-glycolic acid) (PLGA) as polymer in acceptable limits. A total of 16 formulations were prepared by changing stabilizer and polymer ratios. The prepared nanocrystals were characterized by particle size, zeta potential, crystalline structure, surface morphology, assay, saturation solubility, and in vitro drug release. Results: Based on particle size, polydispersity index, and zeta potential data, four formulations were optimized. The formulation containing Tween 80 as stabilizer has shown lowest particle size and better drug release than the formulations containing egg lecithin and povidone C-12 as stabilizers. The formulation containing Tween 80 and PLGA has shown still lower sized particles than the Tween 80 alone and exhibited prolonged sustained drug release. The release kinetics of formulations containing Tween 80 and PLGA followed zero-order release kinetics and formulations containing egg lecithin and povidone C-12 followed Higuchi diffusion (non-Fickian). Conclusion: From the study, we concluded that as the type and concentration of stabilizer changed the size and shape of the crystals were also changed and the formulations showed sustained drug release with non-Fickian diffusion.

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