scholarly journals IBUPROFEN LOADED ORGANOGEL: DEVELOPMENT AND CHARACTERIZATION

2021 ◽  
pp. 224-227
Author(s):  
CHANDRA PRABHA UPADHYAY ◽  
MEENAKSHI BHARKATIYA
Keyword(s):  
Transdermal Delivery ◽  
In Vitro Release ◽  
Stability Study ◽  
Elastic Behavior ◽  
In Vitro Drug Release ◽  
Sorbitan Esters ◽  
And Storage ◽  
Vitro Release ◽  
Water Contents

Objective: This study aimed to develop and in vitro characterize an organogel (OG) loaded Ibuprofen. Methods: Organogel (OG) composed of water, isooctane, sorbitan esters, sorbitan monopalmitate (Span-40), and poly(oxyethylene) sorbitan monostearate (Polysorbate-60) was loaded with Ibuprofen. The partial phase behavior of ibuprofen OG was studied to optimize the formulation composition. 1.0% w/w Ibuprofen loaded OG were characterize for rheological, in vitro release and stability study. Results: Phase diagram showed an isotropic gel region at low water contents, which converted to emulsion on increasing water quantity. The rheological properties of the OG incorporating 1.0% w/w Ibuprofen shows the presence of two Tg’s and elastic behavior of gel, reflects the presence of an entangled network of aqueous tubules. The fractal dimension df value of 2.1 and 2.3 was obtained for the two curves (elastic and storage modulus), which is indicative of the formation of the densest gel structure. The diffusional release exponent (n) was found to be ~0.7 (0.5<n<1), which is indicative of non-Fickian, anomalous diffusion of the drug from the OG. The in vitro drug release exhibited release @ 7.04%/h 0.7/cm2 from the OG. Ibuprofen containing OG was stable for 28 d in terms of chemical potency and gel stiffness at 4 °C and room temperature (~25 °C). Conclusion: The study indicates the potential of OG for improved transdermal delivery of Ibuprofen.

scholarly journals FORMULATION AND EVALUATION OF SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF ETORICOXIB

2017 ◽  
Vol 10 (7) ◽  
pp. 367 ◽  
Author(s):  
Surendra Singh Saurabh ◽  
Roshan Issarani ◽  
Nagori Bp
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
In Vitro Release ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
In Vitro Permeation ◽  
Globule Size ◽  
Vitro Release ◽  
As Solubility

Objective: In the present dissertation work, the aim was to prepare self-emulsifying drug delivery systems (SEDDS) of etoricoxib to improve its solubility with a view to enhance its oral bioavailability.Methods: The prepared SEDDS was the concentrate of drug, oil, surfactants, and cosurfactant. The formulation was evaluated for various tests such as solubility, globule size, thermodynamic stability study, pH determination, ease of dispersibility, uniformity index, drug content, in-vitro release study, and in-vitro permeation study.Results: The optimized formulation F6 showed drug release (79.21±2.73%), droplet size (0.546 μm). In vitro drug release of the F6 was highly significant (p<0.05) as compared to the plain drug.Conclusion: All formulations of etoricoxib SEDDS were showed faster dissolution than plain drug (p<0.05), mean bioavailability of etoricoxib increase in respect to the plain drug. The F6 can be further used for the preparation of various solid SEDDS formulations.

scholarly journals DEVELOPMENT AND EVALUATION OF TIOCONAZOLE LOADED EMULGEL

2017 ◽  
Vol 9 (5) ◽  
pp. 83
Author(s):  
Shailendra Kumar Sah ◽  
Ashutosh Badola ◽  
Sayantan Mukhopadhyay
Keyword(s):  
Kinetic Analysis ◽  
In Vitro Release ◽  
Physical Appearance ◽  
Stability Study ◽  
Fickian Diffusion ◽  
Hydrophobic Drug ◽  
In Vitro Drug Release ◽  
Release Data ◽  
Vitro Release

Objective: The objective of the present work was to develop, characterize and evaluate the tioconazole loaded emulgel and to prove that emulgel can be the best alternative for delivery of hydrophobic drug topically.Methods: for the preparation of stable Emulgel, firstly gels were prepared using different polymers as carbopol 934 and xanthan gum, followed by preparation of emulsions and finally mixed together (table 1). Emulgel was evaluated for physical appearance, pH, spreadability, extrudability, viscosity, swelling index, dilution test, centrifuge test, drug content, in vitro release study, kinetic analysis of release data, antifungal activity and stability study for 3 mo. A comparative study was also performed between prepared emulgels with available marketed antifungal cream.Results: All evaluation parameters were in acceptable range with good physical appearance and the pH in the range of 5.5 to 6.8. The results show that the extrudability was in the range 15.63 to 35.27 g/cm2; with spreadability in range of 6.6 to 8.833 cm. swelling index of F3 was seen a maximum in 3 h of about 75.13%. The viscosity was in the range of 15240 to 56340 cps at 10 RPM. During in vitro release of all formulations, F1 and F5 showed a maximum in vitro drug release of 59.11% and 55.11% respectively in 8 h. The kinetic analysis of fitting the data in different model shows that the best formulation of F1 fits in the Higuchi model with regression coefficient (R2) of 0.998 and show non-fickian diffusion. The formulations were found stable. F1 and F5 provide a similar zone of inhibition like to market cream.Conclusion: Tioconazole emulgel provide the better platform for delivery of hydrophobic drug for topical route and so able to produce better patient compliance. 

Development and Evaluation of Floating Tablets of Lamivudine

2021 ◽  
pp. 2593-2597
Author(s):  
Chinmaya Keshari Sahoo ◽  
Amiyakanta Mishra ◽  
Amaresh Prusty ◽  
S. Ram Mohan Rao ◽  
Jimidi Bhaskar
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Stability Study ◽  
Compression Method ◽  
Short Term ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Vitro Release

The present study was undertaken to develop floating tablets of lamivudine. The tablets were prepared by direct compression method. The prepared tablets were evaluated for pre compression parameters, post compression parameters, in vitro drug release study and in vitro buoyancy study. Among the prepared formulations F4 batch show 90.98% drug release in 12 h. The in vitro release kinetics were analyzed for different batches by different pharmacokinetic models such as zero order, first order, Higuchi, and Korsmeyer Peppas. The result of optimized formulation releases drug up to 12 h in a controlled manner and follows Higuchi kinetics. Short term stability study at 40±2ºC/75±5% RH for three months on the best formulation was performed showing no significant changes in thickness, hardness, friability, drug content and in vitro drug release.

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

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.

scholarly journals Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

2010 ◽  
Vol 13 (2) ◽  
pp. 286 ◽  
Author(s):  
Tailane Sant´Anna Moreira ◽  
Valéria Pereira De Sousa ◽  
Maria Bernadete Riemma Pierre
Keyword(s):  
Oleic Acid ◽  
Rheological Behavior ◽  
Transdermal Delivery ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Penetration Enhancer ◽  
Release Studies ◽  
Vitro Release ◽  
Gel Transition

Abstract PURPOSE: Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (Tsol-gel) were also carried out in these systems. METHODS: In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm2) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm2. h -1. The determination of viscosity was carried out at different shear rates (γ) between 0.1- 1000 S-1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine Tsol-gel. RESULTS: Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% compared to other concentrations of the penetration enhancer. Tsol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. CONCLUSIONS: Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics. Novelty of the work: A transdermal delivery of non-steroidal antinflammatory drugs like lumiracoxib (LM) can be an interesting alternative to the oral route of this drug, since it was recently withdraw of the market due to the liver damage when systemically administered in tablets as dosage form. There are no transdermal formulations of LM and it could be an alternative to treat inflammation caused by arthritis or arthrosis. Then, an adequate delivery system to LM is necessary in order to release the drug properly from the PBDS as well as have good characteristics related to semi-solid preparations for transdermal application, which were evaluated through in vitro release studies and rheological behavior in this paper, respectively.

scholarly journals DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

2018 ◽  
Vol 8 (5-s) ◽  
pp. 235-239
Author(s):  
NILESH M MAHAJAN ◽  
Kalyanee Wanaskar ◽  
Yogesh Bhutada ◽  
Raju Thenge ◽  
Vaibhav Adhao
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Tablet Properties ◽  
Vitro Release

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC

scholarly journals Design and evaluation of Pulsatile drug delivery of Losartan Potassium

2014 ◽  
Vol 12 (2) ◽  
pp. 119-123
Author(s):  
MS Ashwini ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
In Vitro Release ◽  
Losartan Potassium ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Release Studies ◽  
The Stability ◽  
Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

scholarly journals SOLUBILITY ENHANCEMENT OF CELECOXIB BY SOLID DISPERSION TECHNIQUE AND INCORPORATION INTO TOPICAL GEL

2019 ◽  
pp. 294-300
Author(s):  
AMRIN SHAIKH ◽  
PRASHANT BHIDE ◽  
REESHWA NACHINOLKAR
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Peg 6000 ◽  
Topical Gel ◽  
Drug Content ◽  
Vitro Release

Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux. Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release. Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol. Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.

scholarly journals FORMULATION OF TETRANDRINE BEADS USING IONIC GELATION METHOD CA-PECTINATE COATED PH-SENSITIVE POLYMERS AS COLON-TARGETED DOSAGE FORM

2017 ◽  
Vol 10 (10) ◽  
pp. 90
Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Cindy Espreancelly Sandiata ◽  
Sisilia Triani ◽  
Santi Purna Sari ◽  
...  
Keyword(s):  
Targeted Drug Delivery ◽  
In Vitro Release ◽  
Chloride Concentration ◽  
In Vitro Drug Release ◽  
Eudragit L100 ◽  
Calcium Pectinate ◽  
Release Study ◽  
Vitro Release

Objectives Pectin, a natural polysaccharide, can be used as colon targeted drug delivery systems. Ionotropic gelation of pectin in the presence of certain divalent cations, such as calcium ions, protects drugs by producing insoluble hydrogels that can be used as a colon-targeted drug delivery carrier. In this study, calcium pectinate beads containing tetrandrine were made and were evaluated for in-vitro drug release and in-vivo study.Methods: Calcium pectinate beads were prepared by ionic gelation method with varied calcium chloride concentration (5%, 10%, and 15%). The best formula was coated with pH sensitive polymers, i.e. Eudragit L100-55, Eudragit L100, HPMCP (Hydroxypropylmethyl Cellulose Phthalate) HP-55 or CAP (Cellulose Acetate Phthalate).Results: Characterization results showed that the beads produced were quite spherical and have yellow-brownish color. After the coating process, beads were used in in-vitro drug release and targeted test. From in-vitro release study, beads coated with Eudragit L100 10% has shown good colon targeted dosage form with percent cumulative release 57.87%. This result also confirmed with the in-vivo test. Beads which were coated by Eudragit L100 10% could be found in the rat intestine.Conclusion: Formula 1 (5% calcium chloride concentration) was chosen as the best beads characterization. Formula 1C (5% beads coated with 10% Eudragit L100) showed an optimal protection from gastric acid in the in-vitro release study and able to deliver the beads to the intestine in the in-vivo targeted test.

scholarly journals Microencapsulation of Thymol in Poly(lactide-co-glycolide) (PLGA): Physical and Antibacterial Properties

Materials ◽  
2019 ◽  
Vol 12 (7) ◽  
pp. 1133 ◽  
Author(s):  
Zhu Zhu ◽  
Tiantian Min ◽  
Xueji Zhang ◽  
Yongqiang Wen
Keyword(s):  
Storage Stability ◽  
In Vitro Release ◽  
Antibacterial Properties ◽  
Spherical Shape ◽  
Food Preservative ◽  
And Storage ◽  
Fast Release ◽  
Vitro Release ◽  
And Staphylococcus Aureus

Thymol has been shown to be a safe and effective broad-spectrum antimicrobial agent that can be used as a food preservative. However, its volatile characteristics and strong odor limit its use in food products. The microencapsulation of this essential oil in biopolymers could overcome these disadvantages. In this work, thymol-loaded poly(lactide-co-glycolide) (PLGA) microparticles were successfully prepared and the optimal encapsulation efficiency was obtained at 20% (w/w) thymol. Microparticles containing thymol presented a spherical shape and smooth surface. Microencapsulation significantly improved the thermal and storage stability of thymol. In vitro release profiles demonstrated an initial fast release followed by a slow and sustained release. Thymol-loaded microparticles had strong antibacterial activity against Escherichia coli and Staphylococcus aureus, and the effectiveness of their antibacterial properties was confirmed in a milk test. Therefore, the thymol-loaded microparticles show great potential for use as an antimicrobial and as preservation additives in food.

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