Stavudine Loaded Microcapsules using various Cellulose Polymers: Preparation and In-Vitro Evaluation

2009 ◽  
Vol 2 (2) ◽  
pp. 551-556
Author(s):  
Narayana R. Padala ◽  
Prakash K. ◽  
C. S. Reddy Bonepally ◽  
Krishnaveni B. ◽  
Shantakumari K. ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Liquid Paraffin ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Electron Microscopic ◽  
Accelerated Stability ◽  
Scanning Electron

The objective of the present study was to prepare and characterize the microcapsules for the controlled release of Stavudine using cellulose acetate butyrate (CAB), ethyl cellulose (EC), hydroxy propyl methyl cellulose phthalate (HPMCP). The microcapsules were prepared by solvent evaporation method using acetone and liquid paraffin as a drug dispersion and liquid manufacturing phase, respectively. The prepared microcapsules were characterized for particle size distribution (PSD), percent drug content, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared microcapsules were filled in hard gelatin capsules and kept for accelerated stability study as per ICH guidelines for about 3 months. The prepared microcapsules were spherical and free flowing. The entrapment efficiency was found to be 25-45%. The release of drug from the microcapsules was extended upto 12 hours and more. FTIR and DSC thermo graphs showed stable character of stavudine. Scanning electron microscopic study revealed that then microcapsules were spherical and porous in nature. The release kinetics study revealed that the prepared microcapsules were best fitted to the Higuchi model, first order and followed by Zero order and indicating that the drug release was diffusion controlled. The release was mainly influenced by the type of polymer and its viscosity. The DSC study revealed that there is no drug to polymer interaction and showed the stable character of the drug which was further confirmed by the assay of accelerated stability of microcapsules.

scholarly journals Formulation and evaluation of Zidovudine alginate microspheres

2019 ◽  
Vol 9 (5-s) ◽  
pp. 57-64
Author(s):  
Pingali Srinivasa Rao ◽  
Kanakam Vijayabhaskar
Keyword(s):  
Controlled Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Ionic Gelation ◽  
Ftir Studies ◽  
Diffusion Controlled ◽  
Accelerated Stability ◽  
Characterization Studies

The objective of the  present  study  was  to  prepare  and  evaluate  microspheres  for  the controlled release of Zidovudine from the prepared microspheres using different polymers. The microspheres were prepared by ionic gelation method. The prepared microspheres were characterized for FTIR, scanning electron microscopy (SEM), the percentage drug content, entrapment efficiency, and in vitro dissolution studies. Accelerated stability studies were also carried out for the formulations. The microspheres were spherical in shape and free flowing. The entrapment efficiency was varying from 76 to 86%. The release of drug  from  the  microspheres was extended up to  8  to  12  hours. FTIR studies showed the stable character of Zidovudine in the microspheres. SEM studies revealed that the microspheres were  porous  in  nature.  The release kinetics studies revealed that the prepared microspheres were best  fitted  to  the  zero  order for all eight formulations and peppa’s model. The release kinetics data and characterization studies indicated that the drug release from microspheres was diffusion – controlled and the microspheres were stable in nature. Keywords: Zidovudine, microspheres, controlled release, stability, ionic gelation, entrapment efficiency.

scholarly journals Evaluation of Transdermal Formulations of Metoclopramide Prepared Using Arachis Oil and Liquid Paraffin as Permeation Enhancers

2020 ◽  
Author(s):  
Sylvester O. Eraga ◽  
Matthew I. Arhewoh ◽  
Ogochukwu A. Meko
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Liquid Paraffin ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Tween 80 ◽  
Patient Acceptance ◽  
Scanning Calorimetry

Background: The study aimed to evaluate the effect of arachis oil and liquid paraffin on metoclopramide release from transdermal films. Objectives: Batches of metoclopramide films were prepared with hydroxypropyl methyl cellulose (HPMC), arachis oil or liquid paraffin and Tween 80 as plasticizer. The films were evaluated for their physiochemical properties, in vitro and ex vivo drug release and drug release kinetics. Drug-excipient interactions were investigated using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy. Methods: The transdermal films had a weight range of 0.22-0.24 g, folding endurance of 300-306, percentage moisture content and uptake of 2%-10% and 19%-110%, respectively and drug content of 98%-104%. There was similar condition in vitro release profile for the films but their ex vivo profiles exhibited variable drug release with the P3 (30% arachis oil) giving the highest drug (almost 100%) release.  Results: The release kinetics of metoclopramide followed the first order and Korsemeyer-Peppas models more closely as seen in their correlation coefficients (R2) of 0.9832 and 0.9560, respectively. Drug-excipient compatibility studies showed no interactions between excipients and metoclopramide. Conclusion: The formulated transdermal films showed controlled drug release over a period of 12 h. Arachis oil and liquid paraffin showed similar permeation enhancing ability. These enhanced permeation properties of the films could be helpful in the development of alternative route for metoclopramide administration in the management of emesis with improved patient acceptance.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals Formulation and evaluation of gas powered systems of cefdinir tablets for controlled release

2020 ◽  
Vol 10 (5) ◽  
pp. 182-187
Author(s):  
Manoj R. Chincholikar ◽  
Jagdish Rathi
Keyword(s):  
Controlled Release ◽  
Sodium Bicarbonate ◽  
Ethyl Cellulose ◽  
Guar Gum ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Magnesium Stearate ◽  
Stability Study ◽  
In Vitro Dissolution

The  present  work  is  aimed  to  formulate  Cefdinir  floating  tablets  using different  hydrophilic  and  hydrophobic  polymers  like  HPMC,  Ethyl  cellulose, Xanthum gum, guar gum and gas generating agent Sodium bicarbonate. The develop gastro retentive dosage form thatcould  retain  the  agent  namely  Cefdinir  in  the  stomach  for  longer periods of time delivering the drug to the site of action, i.e., stomach. HPMC  is  used  as  a  swelling  agent,  Guar  gum  and  Xanthum  gum  is used as binding agent. Ethyl cellulose is used as matrix form agent.  PVP is used as a suspending agent. Sodium bicarbonate is used as a gas forming agent. MCC is used as a disintergrant and diluent. Magnesium stearate is used as a lubricant. The  prepared  Cefdinir  tablets  will  be  evaluated  for  drug  content,  entrapment efficiency, post compression studies, In-vitro buoyancy studies, swelling index studies, in-vitro dissolution studies, release kinetics, stability studies.All these parameters were found to be within the pharmacopoeial limits. Formulation F5 was selected for drug release and stability study on the basis of appropriate results of post compression study.In vitro dissolution study was carried out and showed controlled release pattern. Keywords: Gas Powered Systems, Cefdinir, Controlled release, Floating drug delivery.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

scholarly journals “EFFECT OF CROSSLINKING AGENT ON DEVELOPMENT OF GASTRORETENTIVE MUCOADHESIVE MICROSPHERES OF RISEDRONATE SODIUM”

2018 ◽  
Vol 10 (4) ◽  
pp. 133 ◽  
Author(s):  
Shweta Gedam ◽  
Pritee Jadhav ◽  
Swati Talele ◽  
Anil Jadhav
Keyword(s):  
Differential Scanning Calorimetry ◽  
Particle Size ◽  
Drug Release ◽  
Calcium Chloride ◽  
Crosslinking Agent ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Scanning Electron ◽  
Polymer Ratio

Objective: The present investigation was undertaken to develop and evaluate a gastroretentive mucoadhesive microspheres of anti-osteoporosis drug risedronate sodium to enhance the residence time and drug release by studying the effect of the crosslinking agent to obtain the best formulation with reduced particle size and good in vitro mucoadhesion strength.Methods: Selected drug risedronate sodium is a potent pyridinyl bisphosphonate used for the treatment of osteoporosis, and other bone disorders. Microspheres using sodium alginate as a polymer and calcium chloride solution as a cross-linker were prepared successfully by the emulsification crosslinking method. The 23 factorial design was used to study the effects of various variables like a drug: polymer ratio, crosslinking agent concentration and crosslinking time on the particle size and in vitro mucoadhesion strength. All these formulations were evaluated for entrapment efficiency, percentage yield and cumulative drug release. F1 batch was selected as best formulation and evaluated for scanning electron microscopy, fourier transforms infrared spectroscopy, differential scanning calorimetry, stability study.Results: Design batches were evaluated for percent yield (61.29-89.33%), % entrapment efficiency (42.25±0.620-62.58±0.330), mucoadhesion strength (68.15±0.37-82.24±0.72%) and drug release at 12 h (67-84%). Among the microspheres formulation, an F1 batch of (0.5:1) drug: polymer concentration and at 4% concentration of calcium chloride as a crosslinker was considered best formulation with reduced particle size 32.85±0.774μm, % intro mucoadhesion. 82.24±0.72. In vitro mucoadhesion strength was increased with the increasing crosslinking time from 5 min to 10 min. The fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) study showed no interaction between drug and polymer. X-ray diffraction (XRD) spectrum of microspheres indicates that drug particles are dispersed at the molecular level in the polymer matrices so no indication of the crystalline nature of the drug nature. Scanning electron microscopic (SEM) study showed that microspheres were spherical in shape with a smooth surface. F1 batch shows percentage cumulative drug release 84.07%. In vitro dissolution studies indicates that percent cumulative drug release from microspheres follows zero order kinetics plot which indicates controlled-release drug-delivery for 12 h which leads to control of plasma concentration.Conclusion: The results show that the formulation that contains (0.5:1) drug: polymer ratio, calcium chloride in 4% concentration and crosslinking time 10 min is the best one and can be utilized to formulate risedronate sodium mucoadhesive microspheres to enhance gastric residence time, improved patient compliance and reduction in the frequency of drug administration.

scholarly journals Formulation Development and in vitro Evaluation of Drug Release Kinetics from Sustained Release Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

2012 ◽  
Vol 11 (1) ◽  
pp. 37-43 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Madhabi Lata Shuma ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index ◽  
Originator Brand

The objective of the present study was to develop a once-daily sustained release matrix tablet of Aceclofenac using hydroxypropyl methyl cellulose (Methocel K 100M CR) as release controlling factor and to  evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct  compression method. The powder blends were evaluated for angle of repose, loose bulk density, tapped bulk density,  compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 24  hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus in phosphate buffer (pH 7.4). The powder blends showed satisfactory flow properties, compressibility index and drug content etc. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-3 (40% Methocel K100M CR of total weight of tablet) could extend the drug release up to 24 hours and the total release pattern was very close to the theoretical release profile. By comparing the dissolution profiles with the originator brand of Arrestin SR, the formulation F-3 exhibited drug release profile like originator brand. From this study, a decrease in release kinetics of the drug was observed by  increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which  was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion  mechanism in all cases. The drug release from the formulation (F-3) was satisfactory after 3 months storage in 400C  and 75% RH. Besides, this study explored both of the optimum concentration and effect of polymer(s) on  Aceclofenac release pattern from the tablet matrix for 24 hour period. The matrix tablet of Aceclofenac using HPMC  with molecular weight of K100M controlled the drug release effectively for 24 hours; hence the formulation can be  considered as a once daily sustained release tablet of Aceclofenac in order to improve patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12485 Dhaka Univ. J. Pharm. Sci. 11(1): 37-43, 2012 (June)

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 FORMULATION AND EVALUATION OF ESOMEPRAZOLE FAST DISSOLVING BUCCAL FILMS

2018 ◽  
Vol 11 (10) ◽  
pp. 193 ◽  
Author(s):  
Balakrishna T ◽  
Vidyadhara S ◽  
Murthy Tegk ◽  
Ramu A ◽  
Sasidhar Rlc
Keyword(s):  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Effective Treatment Option ◽  
Electron Microscopic ◽  
Polyethylene Glycol 400 ◽  
Film Forming ◽  
Microscopic Studies ◽  
Dispersion Test ◽  
Buccal Films

Objective: The present study deals with the formulation and evaluation of fast dissolving buccal films for effective treatment option in the gastroesophageal reflux disease.Methods: Esomeprazole fast dissolving buccal films are a convenient formulation of which can be taken with or without water. In the present investigation, polyvinyl alcohol and polyvinylpyrrolidone were used as film-forming agents and polyethylene glycol 400 is taken as plasticizer. Solvent evaporation method was used for the preparation of fast dissolving buccal films.Results: The films were prepared and evaluated for film thickness, folding endurance, dispersion test, drug content, and dissolution. The in vitro dissolution studies were carried out using simulated salivary fluid (pH 6.8 phosphate buffer).Conclusion: Among all the formulations, Formulation E7 was released up to 99.6% of the drug from the film within 5 min of time which exhibits faster absorption and also shows desirable characteristics of the film. The drug-excipient interaction studies WERE carried out by Fourier-transform infrared studies, differential scanning calorimetry analysis-X-diffraction studies, and scanning electron microscopic studies and the results revealed that there were no major interactions between the drugs and excipients used for the preparation of films.

scholarly journals DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

2019 ◽  
pp. 109-115
Author(s):  
AHMED GARDOUH ◽  
Samar H. Faheim ◽  
Samar M. Solyman
Keyword(s):  
Zeta Potential ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Homogenization Method ◽  
Nanostructured Lipid Carriers ◽  
Scanning Calorimetry ◽  
Release Study ◽  
Vitro Release

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

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