Evaluation of Anti-inflammatory Activity and In Vitro Drug Release of Ibuprofen-Loaded Nanoparticles Based on Sodium Alginate and Chitosan

2020 ◽  
Vol 45 (9) ◽  
pp. 7599-7609
Author(s):  
Sarra Bensouiki ◽  
Fouzia Belaib ◽  
Michèle Sindt ◽  
Pierre Magri ◽  
Sandrine Rup-Jacques ◽  
...  
INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 87-92
Author(s):  
C Sushmitha ◽  
◽  
M.P. Kusuma ◽  
J Archana

Emulgels (emulsion gels) are a class of biphasic semi-solid formulations, having aqueous and non-aqueous phases, delivering both hydrophilic and lipophilic agents. The main advantage of an emulgel is that lipophilic drugs can be easily formulated as emulgels. Rutin trihydrate is an herbal drug used for topical treatment of inflammation. However, its poor water solubility (0.125 mg/ml) presents a hindrance for its local bioavailability and limits effective anti-inflammatory activity. The aim of the current study was to formulate and optimize rutin trihydrate emulgel to enhance its efficacy and stability. 28 formulations were developed with various types of gelling agents like Carbapol 934 (0.8 and 1% w/v), Xanthum gum (1.5 and 2% w/v), HPMCk15 (2, 2.5 and 3% w/v),HPMC K100 (2, 2.5% w/v), guar gum (1, 1.5 and 2% w/v), badam gum (1% w/v) and using various permeation enhancers like clove oil, eucalyptus oil and oil of orange (10 and12.5% v/v). The optimised formulation (f8) was yellow in colour, homogeneous with good consistency, possessed pH of 6.51±0.04 that is very close to that of normal skin (6-7), drug content of 98.7%, viscosity of 14,680cps at 30rpm, spreadability 13.5gm.cm/sec and extrudability 36.2% and in vitro drug release of 79.3% for 7 hrs, ex vivo drug release of 70.08% was stable for 3 months and was having comparable anti inflammatory activity with that of marketed formulation.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Praveen Kumar Gaur ◽  
Shikha Mishra ◽  
Suresh Purohit

Diclofenac sodium loaded solid lipid nanoparticles (SLNs) were formulated using guggul lipid as major lipid component and analyzed for physical parameters, permeation profile, and anti-inflammatory activity. The SLNs were prepared using melt-emulsion sonication/low temperature-solidification method and characterized for physical parameters, in vitro drug release, and accelerated stability studies, and formulated into gel. Respective gels were compared with a commercial emulgel (CEG) and plain carbopol gel containing drug (CG) for ex vivo and in vivo drug permeation and anti-inflammatory activity. The SLNs were stable with optimum physical parameters. GMS nanoparticle 1 (GMN-1) and stearic acid nanoparticle 1 (SAN-1) gave the highest in vitro drug release. Guggul lipid nanoparticle gel 3 (GLNG-3) showed 104.68 times higher drug content than CEG in receptor fluid. The enhancement ratio of GLNG-3 was 39.43 with respect to CG. GLNG-3 showed almost 8.12 times higherCmaxthan CEG at 4 hours. The AUC value of GLNG-3 was 15.28 times higher than the AUC of CEG. GLNG-3 showed edema inhibition up to 69.47% in the first hour. Physicochemical properties of major lipid component govern the properties of SLN. SLN made up of guggul lipid showed good physical properties with acceptable stability. Furthermore, it showed a controlled drug release profile along with a promising permeation profile.


Author(s):  
Bipul Nath ◽  
Santimoni Saikia

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.


2020 ◽  
Vol 10 (4-s) ◽  
pp. 92-99
Author(s):  
Ankur Vasoya ◽  
Sunil Kumar Shah ◽  
C K Tyagi ◽  
Prabhakar Budholiya ◽  
Harish Pandey

The purpose of this research work was to formulate raft-forming chewable bilayer tablets of sodium alginate using a raft-forming agent along with gas-generating agents. Tablets were prepared by wet granulation and evaluated for raft strength, acid neutralization capacity, weight variation, % drug content, thickness, hardness, friability and in vitro drug release. Various raft-forming agents were used in preliminary screening. The amount of sodium alginate, amount of calcium carbonate and amount sodium bicarbonate were selected as variables. Raft strength, acid neutralization capacity and drug release at 30 min were selected as responses.Tablets containing sodium alginate were having maximum raft strength as compared with other raft-forming agents. Acid neutralization capacity and in vitro drug release of all factorial batches were found to be satisfactory. Prepared tablets were found to be pharmaceutically equivalent to the marketed product. It was concluded that raft-forming chewable bilayer tablets prepared using an optimum amount of sodium alginate, calcium carbonate and sodium bicarbonate could be an efficient dosage form in the treatment of gastro oesophageal reflux diseases. Keywords: Chewable bilayer tablet, Sodium alginate, Raft forming agent, Acid Neutralizing capacity


2021 ◽  
Vol 11 (1) ◽  
pp. 72-76
Author(s):  
Mahesh Umbarkar ◽  
Swapnil Thakare ◽  
Tanaji Surushe ◽  
Amol Giri ◽  
Vaibhav Chopade

Liposomes are the most advance formulation for targeting and controlled drug delivery system. These liposomes are generally administered by intra-venous route. In this work the liposome was prepared by using thin film hydration method. The formulated liposome is evaluated or characterised by using zeta sizer, Encapsulation efficiency, Entrapment efficiency, In vitro drug release. Main things are drug which are used for formulation of liposome was Diclofenac sodium, it having anti-inflammatory and anti-pyretic effect. The Diclofenac sodium having several adverse effects, such as depression of renal function, Liver failure for repeated administration, Local mucosal irritation, gastritis. To avoid this adverse effect Diclofenac sodium are incorporate in liposomal formulation. By formulating liposomal formulation, the bioavailability of Diclofenac sodium increase. In conventional dosage form bioavailability of diclofenac sodium is 50℅. But in liposomal formulation bioavailability of this drug increase. The final result includes that diclofenac liposome formulation shows more sustained and prolong anti-inflammatory activity. Keywords: Diclofenac sodium, Liposome, Anti-inflammatory activity.


2019 ◽  
Vol 11 (1) ◽  
pp. 198
Author(s):  
Shailaja Pashikanti ◽  
Jyothsna B.

Objective: The objective of the study was to develop floating in situ gel formulations of Ciprofloxacin that has a narrow absorption window and mainly absorbed in the proximal areas of GIT. These formulations increases the targeted action on bacteria for a longer time that can be used in the treatment of Helicobacter pylori (H. pylori) infections and urinary tract infections.Methods: In situ gel formulations were prepared by varying concentrations of sodium alginate as in situ gel forming bio-degradable polymer and calcium carbonate as a cross-linking agent. The formulations were evaluated for Physical appearance, pH, in vitro drug release, viscosity, in vitro floating behaviour, in vitro gelling capacity and drug content. FTIR was conducted for Ciprofloxacin, excipients used and optimized formulation.Results: All the formulations showed an optimum viscosity that will allow ease of administration and swallowing. Floating lag time of all formulations was between 32-70 seconds and floated for>12 h. The in vitro gelling capacity increased with increasing the polymer and gelling agent concentrations. Increase in polymer concentration decreased the rate and extent of the drug release. Among all the formulations, F4 containing 4% w/v of sodium alginate and 4% w/v of calcium carbonate showed sustained in vitro drug release (95.6%) over an extended period of 12 h. FTIR studies revealed no interaction between drug and excipients used. Drug release from the formulations followed First order kinetics with Fickian diffusion.Conclusion: Ciprofloxacin was successfully formulated as a pH-triggered floating in situ gelling system using sodium alginate.


Author(s):  
MANJULA D ◽  
ABHISHEK RAJ ◽  
JOSEPHINE LENO JENITA J ◽  
SHANAZ BANU

Objective: The current research work has been carried out with the aim to develop a transdermal gel formulation of fenoprofen (a nonsteroidal anti-inflammatory drug used to treat pain associated in arthritis) which would overcome the gastrointestinal-related problems associated with oral administration of the drug. The present study aims at formulating transdermal gels using different concentrations of Carbopol, hydroxypropyl methylcellulose (HPMC), sodium alginate, and guar gum. Methods: The formulated gels were subjected for various evaluation tests such as clarity, homogeneity, viscosity, drug content, pH, spreadability, and in vitro permeation studies. Drug–polymer interaction was studied by Fourier transmission infrared (FTIR) and differential scanning calorimetry (DSC). The in vitro permeation studies were performed in phosphate buffer 7.4 using Franz diffusion cell. Results: The FT-IR and DSC studies showed no chemical interaction between drug and polymers used. All the formulated gels showed acceptable physical properties with respect to clarity, homogeneity, viscosity, drug content, pH, and spreadability. Among all the gel formulations, Carbopol gels containing fenoprofen showed good drug release compared to HPMC, sodium alginate, and guar gum. Optimized formulation was further subjected to kinetic studies which showed Higuchi model of drug release. The same formulation showed significant anti-inflammatory and analgesic activity, tested in Wistar albino rats. No signs of erythema, edema, flushing, and papules were observed when skin irritation test was performed. Stability studies under accelerated condition showed satisfactory results for the optimized formulation. Conclusions: Thus, it was concluded from the results that the optimized formulation showed controlled and slow drug delivery. Animal studies were significant at p<0.05 and 0.001. The selected formulation was stable at various ambient temperatures.


2014 ◽  
Vol 2014 ◽  
pp. 1-9
Author(s):  
Nicholas C. Obitte ◽  
Kenneth C. Ofokansi ◽  
Franklin C. Kenechukwu

In this study, goat fat (Capra hircus) and melon oil were extracted and used to formulate self-nanoemulsifying drug delivery systems (SNEDDS) based on either goat fat alone or its admixture with melon oil by employing escalating ratios of oil(s), surfactant blend (1 : 1 Tween 60 and Tween 80), and cosurfactant (Span 85), with or without carbosil, a glidant, for the delivery of indomethacin. The formulations were encapsulated in hard gelatin capsules and then assessed using isotropicity test, aqueous dilution stability and precipitation propensity, absolute drug content, emulsification time, in vitro drug release, and anti-inflammatory activity. The SNEDDS exhibited low precipitation propensity and excellent stability on copious dilution, as well as high drug release in vitro and in vivo. The inhibition produced by the SNEDDS was comparable to that of indomethacin injection (positive control) for much of the 5 h test period, indicating a high degree of bioavailability of the administered SNEDDS. The absolute drug contents and emulsification times fell within narrow limits. This study has shown that a 1 : 1 ratio of melon oil and goat fat could confer favourable properties with respect to drug release and anti-inflammatory activity on SNEDDS for the delivery of indomethacin, thus encouraging further development of the formulations.


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