scholarly journals Formulation and invitro evaluation of oral extended release microspheres of aceclofenac using various natural polymers

2019 ◽  
Vol 1 (2) ◽  
pp. 58-66
Author(s):  
Syed abid ali ◽  
Syed mujtaba pasha ◽  
Omair sohail ahmed ◽  
Omer wasiq ◽  
Mohammed mukaram ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Oral Route ◽  
Aqueous System ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Drug Release Mechanism ◽  
Microsphere Method

In the present work, bioadhesive microspheres of Aceclofenac using Sodium alginate along with Carbopol 934, Carbopol 971, HPMC K4M as copolymers were formulated to deliver Aceclofenac via oral route. The results of this investigation indicate that ionic cross-linking technique Ionotropic gelation method can be successfully employed to fabricate Aceclofenac microspheres. The technique provides characteristic advantage over conventional microsphere method, which involves an “all-aqueous” system, avoids residual solvents in microspheres. FT-IR spectra of the physical mixture revealed that the drug is compatible with the polymers and copolymers used. Micromeritic studies revealed that the mean particle size of the prepared microspheres was in the size range of 512-903µm and are suitable for bioadhesive microspheres for oral administration. The in-vitro mucoadhesive study demonstrated that microspheres of Aceclofenac using sodium alginate along with Carbopol934 as copolymer adhered to the mucus to a greater extent than the microspheres of Aceclofenac using sodium alginate along with Carbopol 971 and HPMC K4M as copolymers. The invitro drug release decreased with increase in the polymer and copolymer concentration. Analysis of drug release mechanism showed that the drug release from the formulations followed non-Fickian diffusion and the best fit model was found to be Korsmeyer-Peppas. Based on the results of evaluation tests formulation coded T4 was concluded as best formulation.

scholarly journals 5-Fluorouracil Release from Chitosan-Based Matrix.Experimental and Theoretical Aspects

2020 ◽  
Vol 57 (3) ◽  
pp. 180-188
Author(s):  
Roxana Iancu ◽  
Stefan Andrei Irimiciuc ◽  
Maricel Agop ◽  
Mihail Frasila ◽  
Maria-Alexandra Paun ◽  
...  
Keyword(s):  
Drug Release ◽  
Polarized Light ◽  
Crosslinking Density ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Morphological Aspects ◽  
Drug Release Mechanism ◽  
The Matrix

A series of four drug release formulations based on 5-fluorouracil encapsulated into a chitosan-based matrix were prepared by in situ hydrogelation with 3,7-dimethyl-2,6-octadienal. The formulations were investigated from structural and morphological aspects by FTIR spectroscopy, polarized light microscopy and scanning electron microscopy. It was established that 5-fluorouracil was anchored into the matrix as crystals, whose dimension varied as a function of the crosslinking density. The in vitro drug release simulated into a media mimicking the physiological environment revealed a progressive release of the 5-fluorouracil, in close interdependence with the crosslinking density. In the context of Pharmacokinetics behavioral analysis, a new mathematical procedure for describing drug release dynamics in polymer-drug complex system is proposed. Assuming that the dynamics of polymer-drug system�s structural units take place on continuous and nondifferentiable curves (multifractal curves), we show that in a one-dimensional hydrodynamic formalism of multifractal variables the drug release mechanism (Fickian diffusion, non-Fickian diffusion, etc) are given through synchronous dynamics at a differentiable and non-differentiable scale resolutions. Finally, the model is confirmed by the empirical data.

Formulation and Evaluation of Sustained Release Floating Tablets of an Antihypertensive Diltiazem

2017 ◽  
Vol 10 (5) ◽  
pp. 3844-3852
Author(s):  
Gururaj S Kulkarni ◽  
Prabhansh P Chaudhary ◽  
Shivakumar Swamy
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Angle Of Repose ◽  
Polymeric Chain ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Floating Tablets ◽  
Higuchi Model

The aim of the present study was to develop and evaluate sustained release floating tablets of Diltiazem hydro-chloride, an antihypertensive agent. The sustained release floating tablets were prepared by direct compression method and formulated using different polymer combinations, formulations such as F1 to F9. Natural polymer Sodium alginate and synthetic polymer HPMC K4M were used. Developed formulations were evaluated for the pre compression parameters i.e., drug- excipients compatibility by FTIR, bulk density, compressibility, and angle of repose etc. Post compression parameters i.e. weight variation; full factorial design was applied to optimize the developed formulation. SA and HPMC K4M were selected as independent variable at three different concentrations. The in-vitro drug release study revealed that formulation F8 combination of both synthetic (HPMC) and natural polymers (sodium alginate) was the most successful formulation of the study, all tablets but one exhibited gradual and near complete sustained release for diltiazem HCl (90-100%) that extended the drug release up to 8 hours, with satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile.  Model equations of zero and first order, Higuchi, Hixson-Crowell and Peppas, intended to elucidate the drug release mechanism, and were fitted to the release data. Mathematical modelling of in-vitro dissolution data indicated the best-fit release kinetics was achieved with Higuchi model with r2 vales of 0.994 in its semi log plot. The ‘n’ value in Higuchi model was >0.89 which indicated, Super Case-II transport of drug from polymer sustained, i.e., diffusion with relaxation of polymeric chain. In conclusion, the results indicated that the prepared sustained-release tablets of Diltiazem hydrochloride could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance.     

scholarly journals FABRICATION OF SODIUM ALGINATE/GUM GHATTI IPN MICROBEADS INTERCALATED WITH KAOLIN NANO CLAY FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 233-241
Author(s):  
D. GANESH ◽  
P. SURESH ◽  
G. SRINIVAS RAO
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
In Vitro Release ◽  
Kinetic Equations ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Nano Clay ◽  
Gum Ghatti

Objective: The objective of this study is to fabricate sodium alginate (SA)/gum ghatti (GG) microbeads intercalated with Kaolin (KA) nano clay for the sustained release of curcumin (CUR). Methods: The microbeads were prepared by a simple ionotropic gelation technique. The developed beads 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). Swelling studies and in vitro release studies were investigated under both pH 7.4 and pH 1.2 at 37 °C. Results: The developed microbeads were characterized by FTIR, which confirms the interaction between CUR, polymeric matrix and KA. DSC and XRD analysis reveals that the CUR has molecularly dispersed in the polymer matrix. In vitro results illustrated that microbeads were influenced by the pH of test media, which might be suitable for intestinal drug delivery. The drug release mechanism was analyzed by fitting the release data into different kinetic equations and n values are obtained in the range of 0.609-0.640, suggesting that the developed microbeads showed the non-Fickian diffusion type drug release. Conclusion: These results clearly illustrated that the developed KA intercalated polymeric microbeads are potential drug carriers for the controlled release of CUR.

scholarly journals Formulation and in-vitro Evaluation of Carvedilol Gastroretentive Capsule as (Superporous Hydrogel)

2021 ◽  
Vol 30 (2) ◽  
pp. 196-207
Author(s):  
Haider Mohammed Jihad ◽  
Entidhar J. Al- Akkam
Keyword(s):  
Drug Release ◽  
Tween 80 ◽  
Oral Route ◽  
Fickian Diffusion ◽  
Poly Vinyl Alcohol ◽  
Release Mechanism ◽  
Gastric Residence Time ◽  
Gas Blowing ◽  
Superporous Hydrogel

  The preferred route of drug administration is the oral route, but drugs with narrow absorption window in the gastrointestinal tract are still challenging. The ability to extend and monitor the gastric emptying time is a valuable tool for processes remaining in the stomach longer than other traditional dosage forms. The purpose of this study was to formulate and evaluate gastroretentive superporous hydrogel (SPH) of carvedilol with view to improve its solubility and increase gastric residence time in order to get sustained release formulas via utilization of various kinds and concentrations of hydrophilic polymers then after, incorporate the best prepared formula into capsules.  Sixteenth formulae of SPH hybrid were prepared by gas blowing technique from the following materials; monomers (Poly vinyl alcohol, and Acrylamide), cross-linkers (Methylene bisacrylamide, and glutaraldehyde), hybrid agent (Chitosan), foaming agent (NaHCO3) and foam stabilizer (Tween 80). Different amounts or concentrations of these materials were utilized to investigate their effect on SPH properties (density, porosity, floating, drug content, drug release, swelling time, and swelling ratio). The soaking procedure was utilized for loading of carvedilol into SPH hybrid (6.25mg/2.5g SPH).  After analysis the results statistically and application the similarity factor (f2) equation, formula F8 was selected as the best formula and incorporated into capsules.  The drug release data were applied to different mathematical kinetics and the results were shown to be fitted to Higuchi model and the release mechanism was (non fickian) diffusion. The overall results suggested that the proposed SPH hybrid drug delivery system is encouraging for carvedilol specific delivery to the stomach.

DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 71-73
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
J Vijaya Ratna ◽  
R. B. Srinivasa
Keyword(s):  
Drug Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Gastric Residence Time ◽  
Drug Release Mechanism ◽  
The Matrix ◽  
Gastro Retentive

The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.

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

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.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals FORMULATION AND EVALUATION OF RAMIPRIL MOUTH DISSOLVING FILMS

2019 ◽  
pp. 124-129
Author(s):  
Jasvanth E ◽  
Teja D ◽  
Mounika B ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Release Mechanism ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Preparation And Evaluation ◽  
Pvp K30

Objective: The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of Ramipril to enhance patient convenience, compliance and to improve bioavailability. Methods: MDFs with 0.5% w/w Ramipril were prepared by a solvent casting method using a wet film applicator. The effects of film formers, wetting/solubilizing, saliva stimulating agents and film modifiers on the physicomechanical and in vitro Ramipril release from MDFs were evaluated. Results: The MDFs prepared were transparent, smooth and showed no re-crystallization upon storage. MDFs casted with hydroxypropyl methylcellulose (HPMC) E3 as film former and polyethylene glycol (PEG-400) as plasticizer showed superior Ramipril release rates and good physicomechanical properties when compared to MDFs with E5 and E15 as film formers. HPMC E3 MDFs with polyvinyl pyrrolidone K30 (PVP K30) and sodium lauryl sulphate (SLS) gave superior drug release properties than MDFs without PVP K30 and SLS. The HPMC E3 MDFs with citric acid (CA) as saliva stimulating and xylitol as soothing agent gave significantly superior in vitro drug release than the MDFs without CA and xylitol. Release kinetics data reveals diffusion as a drug release mechanism. Conclusion: From the obtained results, it can be concluded that the administration of Ramipril as MDF may provide a quick onset of action with enhanced oral bioavailability and therapeutic efficacy.

scholarly journals Formulation and Evaluation of Acyclovir Microspheres

2018 ◽  
Vol 27 (1) ◽  
pp. 1-7
Author(s):  
Pavani S ◽  
Mounika K ◽  
Naresh K
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Natural Polymers

The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride.   The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.

scholarly journals Fabrication and Characterization of Anticancer Drug Loaded Double Walled Microspheres

2019 ◽  
Vol 9 (4-A) ◽  
pp. 79-85
Author(s):  
Elangovan Nagarajan ◽  
B Rama ◽  
M Swetha ◽  
G.S Sharma ◽  
L Jyothi Rani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Guar Gum ◽  
Diffusion Mechanism ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Breast Cancer Patients

In the present work, double walled microspheres of Tamoxifen (antiestrogenic drug) using Sodium alginate, Hydroxy propyl methyl cellulose (HPMC) K100,Guar gum, Xanthun gum were formulated to deliver Tamoxifen (TMX) through  oral route to treat breast cancer patients. Details regarding the preparation and evaluation of the formulations have been discussed in results. From the study following conclusions could be drawn. The results of this investigation indicate that Ion gelation method can be successfully employed to fabricate TMX microspheres. FT-IR spectra of the physical mixture revealed that the drug is compatible with the polymers and copolymer used. Microspheres containing sodium alginate along with HPMC in 1:1 ratio had a least size range of 610µm. Increase in the polymer concentration led to increase in % Yield, % Drug entrapment efficiency, Particle size. The  invitro drug release decreased with increase in the polymer and copolymer concentration. Among all formulations F7 shows Maximum drug release in 12 th hr  when compared with other formulations. Analysis of drug release mechanism showed that the drug release from the formulations followed the Non fickian diffusion mechanism and follows zero order kinectics. Based on the results of evaluation tests formulation coded F7 was concluded as best formulation. Keywords : Tamoxifen, sodium alginate, HPMC, Microspheres, Diffusion, Copolymers,  Entrapment efficiency.

Sign in / Sign up

Export Citation Format

Share Document