Optimization of ciprofloxacin release kinetics of novel Nano-bioactive glasses: Effect of glass modifier content on drug loading and release mechanism

2019 ◽  
Vol 521 ◽  
pp. 119471 ◽  
Author(s):  
Abeer M. El-Kady ◽  
Manar M. Ahmed ◽  
Bothaina M. Abd El-Hady ◽  
Ashraf F. Ali ◽  
Alaa M. Ibrahim
2019 ◽  
Vol 9 (04) ◽  
pp. 704-710
Author(s):  
Tutiek Purwanti ◽  
Maimuna Syamsuar ◽  
Dewi Melani Hariyadi ◽  
Tristiana Erawati

Gentamicin sulfate is a broad-spectrum aminoglycoside antibiotic that can be used for primary and secondary infections of the skin. Microspheres can be used to extend drug release on the skin; the resulting therapeutic effect is constant and has a longer duration of action. Therefore it can reduce the frequency of use and increase patient compliance. This study investigated the appropriate profile and release kinetics model of gentamicin sulfate microspheres entrapped on the emulgel base. Gentamicin-alginate microspheres were made by the ionotropic gelation method with aerosolization technique, using 2.5% Na-alginate low viscosity, CaCl2 solution of 1.5M as a crosslinker, maltodextrin as lyoprotectant and were dried using the freeze-drying method. The result of microspheres characterization, gentamicin microsphere was spherical with smooth surface structure and had particle diameter of 3.021 ± 0.017μm. Gentamicin microspheres had moisture content 2.89%, and maximum swelling index was 2625 ± 21.70% was achieved within 5 hours. The drug loading of microspheres was 1.75 ± 0.11%, and entrapment efficiency was 10.96 ± 0.19%. The release evaluation during 720 minutes showed that the amount of gentamicin release from alginate microspheres on emulgel base was 14.857 ± 0.816%, and gentamicin release on emulgel conventional was 49.239 ± 5.954%. The model of release kinetics of gentamicin microspheres on emulgel was Higuchi model that showed the release of the active ingredient through the diffusion process. While the model of release kinetics of gentamicin on emulgel base was first order, that showed the release of active agent depends on remaining concentration.


Processes ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 1350
Author(s):  
Sidra Bashir ◽  
Nadiah Zafar ◽  
Noureddine Lebaz ◽  
Asif Mahmood ◽  
Abdelhamid Elaissari

The study aims to prepare a smart copolymeric for controlled delivery of Galantamine hydrobromide. The synthesis of the hydrogel was executed through free radical polymerization using HPMC (Hydroxypropyl methylcellulose) and pectin as polymers and acrylic acid as monomer. Cross-linking was performed by methylene bisacrylamide (MBA). HPMC-pectin-co-acrylic acid hydrogel was loaded with Galantamine hydrobromide (antidementia drug) as a model drug for treatment of Alzheimer based dementia. Formulated hydrogels (SN1–SN9) were characterized for Fourier transform-infrared spectroscopy, differential scanning calorimetry, thermogravimetric analysis, X-ray diffraction, and energy dispersive X-ray. Drug loading efficiency, gel fraction, measurements of porosity, and tensile strength were reported. Swelling and release studies were performed at pH 1.2 and 7.4. Drug liberation mechanism was evaluated by applying different release kinetic models. Galantamine hydrobromide was released from prepared hydrogels by Fickian release mechanism. Swelling, gel fraction, porosity, and drug release percentages were found to be dependent on hydroxypropyl methylcellulose, pectin, acrylic acid, and methylene bisacrylamide concentrations. By increasing HPMC amount, swelling was increased from 76.7% to 95.9%. Toxicity studies were conducted on albino male rabbits for a period of 14 days. Hematological and histopathological studies were carried out to evaluate safety level of hydrogel. Successfully prepared HPMC-pectin-co-acrylic acid hydrogel showed good swelling and release kinetics, which may help greatly in providing controlled release drug effect leading to enhanced patient compliance for dementia patients.


2012 ◽  
Vol 62 (3) ◽  
pp. 383-394 ◽  
Author(s):  
Mohammed S. Khan ◽  
Gowda D. Vishakante ◽  
H. G. Shivakumar

The present investigation was undertaken to fabricate porous nanoparticles of metoprolol tartrate by spray-drying using ammonium carbonate as pore former. Prepared nanoparticles were coated with Eudragit S100 polymer in order to prevent the release of metoprolol tartrate in the upper GI tract. It was shown that nanoparticles with low size ranges can be obtained with a low feed inlet rate. Micromeritic studies confirmed that nanoparticle batches are discrete and free flowing. Effects of the pore former on drug loading, porosity and in vitro release were studied. It was found that there was an increase in drug loading and porosity with increasing the amount of pore former. In vitro drug release studies showed that an increase in pore former made drug release faster. Release kinetics proved that nanoparticles follow a zero-order release mechanism.


2012 ◽  
Vol 584 ◽  
pp. 465-469 ◽  
Author(s):  
S. Malathi ◽  
S. Balasubramanian

Nanoparticles-based drug delivery systems have considerable potential for the treatment of tuberculosis (TB). A series of PLGA polymers with different molar feed ratios (P2:87/13, P3:83/17, P5:63/37, P6:76/24, P9:53/47) were synthesized by direct melt poly condensation method. The resulting biodegradable polymers were characterized by FTIR and 1H NMR spectroscopy. The preparation of the drug (Pyrazinamide (PZA)) encapsulated PLGA polymers were carried out by double emulsion – solvent evaporation technique. The drug loaded PLGA-NPs were analyzed by UV-visible spectroscopy and scanning electron microscopy. The drug loading efficiency and drug release kinetics varies in the following order: P9>P5>P6>P3>P2. Among the formulations, PP9 showed a uniform as well as sustained drug release. The drug release kinetics has been evaluated by Zero-order, First order, Higuchi and Koresmeyer- Peppas models and the release mechanism has also been investigated


2020 ◽  
Vol 11 (3) ◽  
pp. 4555-4559
Author(s):  
Narissara Kulpreechanan ◽  
Feuangthit Niyamissara Sorasitthiyanukarn

The present aim is to evaluate the release profile and its release kinetics of encapsulated capsaicin from chitosan nanoparticles using the software DDSolver. The release study was performed by using a dialysis technique in PBS solutions with different pHs (1.2, 6.8 and 7.4) to mimics the different gastrointestinal tract and circulatory system pH ranges as a releasing medium. The nanoparticles were prepared using o/w emulsification and ionotropic gelation technique under optimal condition obtained from response surface methodology (RSM) design as described in our previous study. These nanoparticles were around 180 nm in average hydrodynamic size and encapsulation efficiency percentage around 70%, respectively. In vitro drug release study suggested that the chitosan nanoparticles can potentially use to controlled and sustained release of capsaicin over at least 96. The kinetic release analysis results by DDSolver software indicated that Weibull model was suggested to be the best dynamic models with highest R2adjusted and model selection criteria (MSC) and lowest Akaike information criterion (AIC), respectively, for capsaicin loaded chitosan nanoparticles. The release mechanism of capsaicin from nanoparticles was found to be Fickian diffusion. The results suggest that the chitosan nanoparticles can be applied for the controlled and sustained release of capsaicin in the gastrointestinal tract and circulatory system.


2021 ◽  
Vol 66 (1) ◽  
Author(s):  
Karima Badis ◽  
Haouaria Merine ◽  
Youssef Ramli ◽  
OumCheikh Larbi ◽  
Cherifa Hakima Memou

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.


Química Nova ◽  
2021 ◽  
Author(s):  
Renata Neves ◽  
Erika Bronze-Uhle ◽  
Pâmela Santos ◽  
Paulo Lisboa-Filho ◽  
Aroldo Magdalena

The controlled release of Salicylic Acid (SA) influences the concentration and collateral effects of the drug. This release refers to the matrix in which the SA is incorporated. Among the matrices, Fe3O4 nanoparticles (NPs) stand out, for transporting drugs to specific sites. The functionalization of Fe3O4 by bovine serum albumin (BSA) can improve colloidal and chemical stability, in addition to increasing interactions with drugs. Thus, understanding the release kinetics of the AS incorporated in Fe3O4-BSA is essential to improve the controlled release. The study aimed the synthesis, characterization and release of the SA into the Fe3O4-BSA NPs. The results showed the functionalization of the Fe3O4-BSA NPs was effective and the average size was below 30 nm. The NPs showed colloidal stability above the pH of 7.5 which can be used as a drug carrier in blood plasma. Drug encapsulation into the NPs system was efficient (~91%) with about 30% of drug loading capability. The kinetic results showed the SA release mechanism was controlled by diffusion. The conclusion is that the incorporation of SA in Fe3O4-BSA NPs led to a release of SA in the first six hours, reaching equilibrium at 0.265 mg mL-1 and 1.83 mg.


Author(s):  
Baiyrkhanova A. ◽  
Ismailova A. ◽  
Botabekova T. ◽  
Enin E. ◽  
Semenova Y.

5-Fluorouracil (5-FU)-loaded chitosan (Ch) film for chemotherapy were prepared applying a superhydrophobic surfacebased encapsulation technology. The aim of this study was to develop polymeric film with glutaraldehyde (GA) of controlled drug delivery systems for 5 – fluorouracil (FU) as a model drug for the treatment of proliferative vitreoretinopathy. Polymer film of chitosan and polyvinyl alcohol (PVA in 75:25 ratios were prepared and treated with GA. FTIR spectra of 5-FU, Ch/5-FU and Ch/PVA film loaded 5-FU were studied. Physical characteristics such as thickness and swelling coefficient of the film were performed. The thermal of the Ch/PVA film was studied with thermogravimethric analysis. The drug loading efficiency, film size and chemical compositions of the film loaded drug were confirmed by UV–vis spectrophotometer and Fourier transform infrared spectroscopy. In vitro release kinetics of drug from the polymeric films was investigated to determine the drug release properties. In vivo study of PVR was showed the efficacy and no toxicity of this formulation. Further uses of the film loaded 5 - fluorouracil may provide an efficiency deliverable for ophthalmic administration.


1970 ◽  
Vol 6 (2) ◽  
pp. 99-103 ◽  
Author(s):  
Irin Dewan ◽  
Md Elias-Al-Mamun ◽  
Reza-ul Jalil

In situ implants containing Progesterone (PRG) were prepared by using biodegradable Poly (DLlactide- co-glycolide) polymer. Dimethyl sulfoxide (DMSO) was used as an aprotic solvent in this implant formulation. This system was prepared by dissolving a water insoluble and biodegradable polymer (PLGA) in a biocompatible organic solvent (DMSO) and then the drug progesterone was added to the polymer solution to produce the drug solution. When the PLGA-PRG solution (0.5 ml) was injected subcutaneously into rat (weight 130g), the solvent dissipated into the surrounding tissue leading phase separation and subsequent coagulation of the polymer & drug to form an implant in situ. The implants were removed from the rat after one hour and stored in freezing condition. The digital photographs of the in-situ formed implants obtained after 1hour shows the evidence of the formation of the implants. Two formulations of implants were made. One contained 10% of progesterone and the other 20%. In vitro dissolution studies of progesterone was performed at static condition in ethanol-water mixture (30:70) at 37°C for 30 days. The implants of 20% progesterone loading showed about 65% release and the implants of 10% loading showed 56% release within 30 days. The release mechanism from these implants resembles closely to Higuchian pattern and first order. The release rate was found faster from the implants with higher drug loading of 20% progesterone, compared to implants of 10% drug loading. Key words: Biodegradable; Implant; Biocompatible; Sustained Release Dhaka Univ. J. Pharm. Sci. 6(2): 99-103, 2007 (December)


2016 ◽  
Vol 19 (1) ◽  
pp. 58-67
Author(s):  
Paroma Arefin ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza

The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016


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