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.

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 Oral Formulations of diclofenac beads and their Characterization

2019 ◽  
Author(s):  
Bushra Alquadeib
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Ph Value ◽  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
In Vitro Dissolution ◽  
Ulcer Bleeding ◽  
Scanning Calorimetry

Diclofenac sodium (DS) is an effective non-steroidal anti-inflammatory drug (NSAID) agent. However, DS has short half life and adverse effects (e.g., ulcer bleeding or perforation of intestinal wall). The objectives of this study were to improve the oral bioavailability by loading DS in sodium alginate beads. The feasibility of different concentration and stabilizers on the mean particle size (MPS) and entrapment efficiency were also investigated.Materials and methods: DS-floating alginate or pectin beads were prepared by extrusion congealing technique. Physicochemical properties and particle size characterization were evaluated using Fourier Transform Infra-Red spectroscopy (FTIR), differential scanning calorimetry. Moreover, in vitro dissolution profiles were performed for all formulated DS loaded beads. Results: MPS of the prepared spherical beads of DS ranged from 568.3 ± 193 to 1791.3 ± 592 nm. and decreasing in sodium alginate or pectin concentration to the hydroxylpropylmethlycellulose ratio favored DS beads with a smaller MPS. There was a significant reduction in MPS, increment in drug content and drug release, with reduction of sodium alginate or pectin concentrations in the formulated beads. Both DSC and FTIR spectroscopy demonstrated a some sort of interaction between the drug and polymer used. Under conditions mimicking those in the stomach, a small amount of drug was released. The DS beads showed a release behavior dependent on pH value and alginate or pectin to hydroxypropylmethylcellulose ratio.

scholarly journals Design and Evaluation of Microspheres Loaded With Pirenzepine

2018 ◽  
Vol 10 (02) ◽  
Author(s):  
A. Aparna ◽  
C. M. Shalina ◽  
D.V.R.N. Bhikshapathi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Calcium Chloride ◽  
Entrapment Efficiency ◽  
Oral Route ◽  
Cross Linking ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Ich Guidelines

The current objective of the investigation was to fabricate Pirenzepine loaded microspheres for the treatment of gastritis delivered through oral route. The microspheres were prepared by ionotropic gelation technique using sodium as alginate polymer and calcium chloride as cross-linking agent. The effect of polymer and cross-linking agent on particle size, shape, % yield, entrapment efficiency, and drug release were studied. The prepared microspheres morphology and physicochemical properties of were investigated by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Among the total S14 formulations, S7 formulation was optimized at 2.2% of sodium alginate, 7% of calcium chloride maintained100rpm for 10 min at room temperature. The optimized S7 formulation displayed the %EE 94.10%, particle size 82.45 ± 0.09μm, % yield 96.30% and swelling index of 95.13%. From In vitro drug release studies S7 shown 97.17 ± 0.28% up to 12 h in 0.1N HCl, and the drug release followed the zero order and Korsmeyer- Peppas model (R2 = 0.987, 0.995) respectively, indicating the possible drug release mechanism to be by erosion and diffusion. The marketed product showed the drug release of 95.23 ± 0.21% within 1 h. The optimized S7 formulation subjected to stability studies for 6months as per ICH guidelines, no appreciable difference was observed hence the S7 formulation found stable. The data obtained thus suggest that a micro particulate system can be successfully designed for sustained delivery of Pirenzepine and to improve its bioavailability

scholarly journals Optimization of Site-Specific Drug Delivery System of Tyrosine Kinase Inhibitor Using Response Surface Methodology

2021 ◽  
pp. 273-286
Author(s):  
S. Parimala Krishnan ◽  
Cinnayyagari Mahesh Reddy ◽  
Challa Balashekar Reddy
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Site Specific ◽  
Box Behnken Design ◽  
Specific Formulation

Aims: The aim of present study was to develop a stomach specific formulation of Imatinibmesylate to increase the fraction of drug absorbed in stomach. Study Design: Development and Optimization of Microspheres for site specific delivery.. Place and Duration of Study: The study was carried out in Department of Pharmacy, Annamalai University, between October 2020 and July 2021. Methodology: Ionotropic gelation method with Sodium alginate and Chitosan were used to formulate the mucoadhesive microspheres with calcium chloride. The formulation was optimized using Box – Behnken design to study the effect of independent variables, Amount of Sodium Alginate (X1), Amount of Chitosan (X2) and concentration of Calcium Chloride (X3) on dependent variables Particle Size (Y1), Entrapment Efficiency (Y2) and In-vitro drug release (Y3). Results: Particle size of prepared microspheres varied from 458.25 to 810.75 μm, entrapment efficiency from 64.87 to 82.63% and in-vitro release from 69.22 to 83.50%. The optimized formulation was found using point prediction, and formulation showed optimum results. The drug release was controlled for more than 12 h. Conclusion: Stomach specific formulation of Imatinibmesylate was successfully optimized by a three-factor, three level Box – Behnken design.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

scholarly journals FORMULATION AND CHARACTERIZATION OF GASTRORETENTIVE FLOATING MICROBALLOONS OF POORLY WATER-SOLUBLE DRUG DIACEREIN

2021 ◽  
Vol 15 (5) ◽  
pp. 8-12
Author(s):  
Kajal Tomer ◽  
Dilip Kumar Gupta
Keyword(s):  
Particle Size ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Acrylic Polymer ◽  
Water Soluble Drug ◽  
Technological Advances ◽  
S 100

The drug can be released in a controlled manner using a gastro retentive dosage type. The main focus on the novel technological advances in the floating drug delivery method for gastric retention. The preparation of diacerein micro balloon is done by solvent diffusion method, using acrylic polymer like Eudragit S 100 and HPMC K4 M. The various evaluation of the prepared floating microsphere like its % yield, drug entrapment efficiency, particle size in-vitro dissolution, buoyancy, was studied. The floating microsphere was found to be spherical and range from 85 μm - 192 μm. Whereas the buoyancy in gastric mucosa between the range 30.5% -49.5%. The % yield and % entrapment efficiency were found under the range 61% - 82% and 45.1–84.1% respectively. The microsphere showed favorable in-vitro dissolution 76.8 to 94.45. The optimized formulation was found based on evaluation of floating micro-balloons, Formulation (M3E3) showed the best result as particle size 192 μm, DDE 84.1%, in vitro drug release 94.5%, and in vitro buoyancy 49.5%. all the formulations showed controlled release up to 24 hours.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

2017 ◽  
Vol 10 (5) ◽  
pp. 285
Author(s):  
S Shanmugam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Kinetic ◽  
Natural Polymers ◽  
In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 

scholarly journals Development and Evaluation of Floating Microspheres of Sumatriptan Succinate using Ethyl Cellulose and Mucilage Extracted from Vigna Mungo

2021 ◽  
pp. 24-36
Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Vigna Mungo ◽  
Average Particle ◽  
Sumatriptan Succinate

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.

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