Immobilization and Release Studies of Triazole Derivatives from Grafted Copolymer Based on Gellan-Carrying Betaine Units

New polymer-bioactive compound systems were obtained by immobilization of triazole derivatives onto grafted copolymers and grafted copolymers carrying betaine units based on gellan and N-vinylimidazole. For preparation of bioactive compound, two new types of heterocyclic thio-derivatives with different substituents were combined in a single molecule to increase the selectivity of the biological action. The 5-aryl-amino-1,3,4 thiadiazole and 5-mercapto-1,2,4-triazole derivatives, each containing 2-mercapto-benzoxazole nucleus, were prepared by an intramolecular cyclization of thiosemicarbazides-1,4 disubstituted in acidic and basic medium. The structures of the new bioactive compounds were confirmed by elemental and spectral analysis (FT-IR and 1H-NMR). The antimicrobial activity of 1,3,4 thiadiazoles and 1,2,4 triazoles was tested on gram-positive and gram-negative bacteria. The triazole compound was chosen to be immobilized onto polymeric particles by adsorption. The Langmuir, Freundlich, and Dubinin–Radushkevich adsorption isotherm were used to describe the adsorption equilibrium. Also, the pseudo-first and pseudo-second models were used to elucidate the adsorption mechanism of triazole onto grafted copolymer based on N-vinylimidazole and gellan (PG copolymer) and grafted copolymers carrying betaine units (PGB1 copolymer). In vitro release studies have shown that the release mechanism of triazole from PG and PGB1 copolymers is characteristic of an anomalous transport mechanism.

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FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39965 ◽

2021 ◽

pp. 206-215

Author(s):

DHARMENDER PALLERLA ◽

SUMAN BANOTH ◽

SUNKARI JYOTHI

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Controlled Drug Release ◽

Fickian Diffusion ◽

Simulated Gastric Fluid ◽

Release Mechanism ◽

Release Studies ◽

Swelling Studies ◽

Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

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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 EVALUATION OF TRANSDERMAL PATCHES OF PANTOPRAZOLE SODIUM

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i5.42175 ◽

2021 ◽

pp. 287-291

Author(s):

M. R. SHIVALINGAM ◽

ARUL BALASUBRAMANIAN ◽

KOTHAI RAMALINGAM

Keyword(s):

In Vitro Release ◽

Skin Permeability ◽

Release Mechanism ◽

Content Uniformity ◽

Prolonged Release ◽

Peptic Ulcers ◽

Transdermal Patches ◽

Release Studies ◽

Vitro Release

Objective: The present study was an attempt to develop an alternative dosage form for the existing conventional oral, parenteral proton pump inhibitor (PPI) as transdermal patches for treating peptic ulcers. Methods: Transdermal patches of PPI were prepared using HPMC E5 with PVP K 30 and HPMC E5 with Eudragit L100 polymers in different ratios by a solvent evaporation method. All the formulated patches were subjected to various evaluation parameters such as thickness, folding endurance, weight uniformity, content uniformity, swelling index, percentage moisture content, moisture uptake, surface pH and in vitro release studies. Results: All patches exhibited satisfactory characteristics regarding integrity, flexibility, dispersion of drug, and other quality control parameters. In the in vitro release studies of transdermal patches, formulation F1 showed the prolonged release of drug (98.99 %) for 24 h, which indicates the maximum availability of the drug, and the in vitro skin permeability studies also showed that 96.26 % of drug Pantoprazole sodium permeated through the rat abdominal skin in 24 h. The kinetic studies were carried out and it was found that all the formulations follow zero-order and the release mechanism of drugs was found to be diffusion rate-limited, Non-Fickian mechanism which was confirmed by Korsmeyer–Peppas model. Conclusion: This suggests the transdermal application of Pantoprazole sodium holds the promised controlled release of the drug for an extended period of time.

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Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.3.9 ◽

1970 ◽

Vol 1 (3) ◽

pp. 257-266

Author(s):

Nagda C. D. ◽

Chotai N. P. ◽

Patel S. B. ◽

Soni T. J ◽

Patel U. L

Keyword(s):

Drug Loading ◽

In Vitro Release ◽

Phenyl Acetic Acid ◽

Solvent Evaporation Method ◽

Elimination Half ◽

Release Studies ◽

Differential Scanning Colorimetry ◽

Polymer Interactions ◽

Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

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Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-020-00130-1 ◽

2020 ◽

Vol 6 (1) ◽

Author(s):

Charu Bharti ◽

Upendra Nagaich ◽

Jaya Pandey ◽

Suman Jain ◽

Neha Jain

Keyword(s):

Particle Size ◽

Desirability Function ◽

In Vitro Release ◽

Entrapment Efficiency ◽

In Vitro Drug Release ◽

Release Studies ◽

Percentage Yield ◽

Vitro Release ◽

Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

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Inclusion of hydroxytyrosol in ethyl cellulose microparticles: In vitro release studies under digestion conditions

Food Hydrocolloids ◽

10.1016/j.foodhyd.2018.06.009 ◽

2018 ◽

Vol 84 ◽

pp. 104-116 ◽

Cited By ~ 13

Author(s):

Filipa Paulo ◽

Lúcia Santos

Keyword(s):

Ethyl Cellulose ◽

In Vitro Release ◽

Release Studies ◽

Vitro Release

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Sodium alginate nanoparticles as a new transdermal vehicle of glucosamine sulfate for treatment of osteoarthritis

European Journal of Nanomedicine ◽

10.1515/ejnm-2017-0008 ◽

2017 ◽

Vol 9 (3-4) ◽

Cited By ~ 2

Author(s):

Asmaa S. El-Houssiny ◽

Azza A. Ward ◽

Dina M. Mostafa ◽

Salwa L. Abd-El-Messieh ◽

Kamal N. Abdel-Nour ◽

...

Keyword(s):

Side Effects ◽

Surface Charge ◽

Ex Vivo ◽

In Vitro Release ◽

Glucosamine Sulfate ◽

Suspension Stability ◽

Rat Skin ◽

Release Studies ◽

Vitro Release

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.

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