scholarly journals In vitro and in vivo evaluation of sustained release ketoprofen-loaded nanoparticles

2013 ◽  
Vol 16 (1) ◽  
pp. 15-25
Author(s):  
Tuyen Thi Phuong Dao ◽  
Nhan Ngoc Thanh Le ◽  
Anh Tuan Nguyen ◽  
Khai Tan Tran ◽  
Dam Duy Le ◽  
...  
Keyword(s):  
Spray Drying ◽  
In Vitro Dissolution ◽  
Drying Method ◽  
In Vivo Evaluation ◽  
The Matrix ◽  
Nanoparticle Formulation ◽  
Electron Microscopes ◽  
Size And Morphology

The purpose of this study is to i) fabricate a biodegradable nanoparticle formulation of Ketoprofen, ii) evaluate its characteristics, iii) investigate its in vitro dissolution and in vivo pharmaceutical property. The nanoparticle formulation was prepared by spray drying method using Eudragit L100 as the matrix polymer. Size and morphology of drug-loaded nanoparticles were characterized with the electron microscopes (TEM, SEM). These successfully prepared nanoparticles by spray drying method are spherical in shape and quite homologous with diameter size of 100 – 200 nm. The in vitro dissolution studies were conducted at pH 1.2 and 7.4. The results indicated that there is a significant increase in Keto concentration at pH 7.4 compared to pH 1.2. For the in vivo assessment, our Keto-loaded nanoparticles and referential Profenid were administered by oral gavages to rabbits. The results implied that Keto-loadednanoparticles remarkably increased AUC compared to Profenid.

scholarly journals Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1210
Author(s):  
Xieguo Yan ◽  
Shiqiang Wang ◽  
Kaoxiang Sun
Keyword(s):  
Drug Loading ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
In Vivo Evaluation ◽  
Long Term Treatment ◽  
Long Acting

Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the optimized formulation by stepwise regression. We also assessed the crystalline changes, residual solvents, solubility and stability after sterilization, in-vivo polymer degradation, pharmacokinetics, and tissue inflammation in the case of the optimized formulation. The surface of the optimized RIS microspheres was small and hollow with 134.4 ± 3.5 µm particle size, 1.60 SPAN, 46.7% ± 2.3% implant drug loading, and 93.4% entrapment efficiency. The in-vitro dissolution behavior of RIS-IM had zero-order kinetics and stable blood concentration; no lag time was released for over three months. Furthermore, the RIS-IM was not only non-irritating to tissues but also had good biocompatibility and product stability. Long-acting RIS-IMs with microspheres and film coatings can provide a new avenue for treating schizophrenia.

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

Optimization, in vitro–in vivo Evaluation, and Short-term Tolerability of Novel Levofloxacin-loaded PLGA Nanoparticle Formulation

2012 ◽  
Vol 101 (6) ◽  
pp. 2165-2176 ◽  
Author(s):  
Gaurav Kumar ◽  
Sadhna Sharma ◽  
Nusrat Shafiq ◽  
Gopal Krishan Khuller ◽  
Samir Malhotra
Keyword(s):  
Short Term ◽  
In Vivo Evaluation ◽  
Term Tolerability ◽  
Nanoparticle Formulation ◽  
Plga Nanoparticle

scholarly journals FORMULATION OF ATOVAQUONE TABLET USING BIOSURFACTANT IN A TERNARY SOLID DISPERSION SYSTEM: IN VITRO AND IN VIVO EVALUATION

2019 ◽  
pp. 44-49
Author(s):  
UDAYKUMAR B. BOLMAL ◽  
PRAMOD H. J.
Keyword(s):  
Ternary System ◽  
Solid Dispersion ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Enhanced Dissolution ◽  
Bioavailability Study

Objective: The goal of the present investigation was to improve the solubility and bioavailability of atovaquone tablet, using in-house biosynthesized biosurfactant in the ternary system of solid dispersion containing hydrophilic polymers with varying concentrations of biosurfactant. Atovaquone is an anti-malarial agent and belongs to biopharmaceutical classification system class IV. Methods: The solid dispersion of binary and ternary mixture was prepared using hydroxyl propyl methyl cellulose (HPMC) and biosurfactant respectively by a solvent evaporation method. All the atovaquone tablet formulations were prepared by incorporation of physical mixture, binary and ternary solid dispersed products with excipients by direct compression method. Pre-compression and post-compression parameters of atovaquone tablets were evaluated. In vivo bioavailability study was performed using female albino rabbits. Results: In vitro dissolution profile of binary and ternary system of solid dispersion products showed 8.65% and 34.64% respectively. Precompression and post-compression values of all atovaquone tablets formulations were within the specified limits. In vitro dissolution efficiency of F2 and F5 were 1.44 fold and 6.62 fold respectively, in accordance to the F1. In vivo study revealed that bioavailability of optimized formulation F5 was increased by 2.5 times and time to reach peak concentration was reduced to 1.4 h, in accordance to pure atovaquone suspension. Conclusion: Potential application of biosurfactant in the solid dosage form of atovaquone tablet was proved for enhanced dissolution rate and bioavailability of atovaquone for malaria treatment.

scholarly journals Formulation, In Vitro and In Vivo Evaluation of Gefitinib Solid Dispersions Prepared Using Different Techniques

Processes ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 1210
Author(s):  
Sultan Alshehri ◽  
Abdullah Alanazi ◽  
Ehab M. Elzayat ◽  
Mohammad A. Altamimi ◽  
Syed S. Imam ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
In Vivo Evaluation ◽  
Significant Release

Gefitinib (Gef) is a poorly water-soluble antitumor drug, which shows poor absorption/bioavailability after oral administration. Therefore, this study was carried out to develop Gef solid dispersions (SDs) using different carriers and different techniques in order to enhance its dissolution and oral absorption/bioavailability. Various SD formulations of Gef were established using fusion and microwave methods utilizing Soluplus, Kollidone VA64, and polyethylene glycol 4000 (PEG 4000) as the carriers. Developed SDs of Gef were characterized physicochemically and evaluated for in vitro dissolution and in vivo pharmacokinetic studies. The physicochemical evaluation revealed the formation of Gef SDs using fusion and microwave methods. In vitro dissolution studies indicated significant release of Gef from all SDs compared to the pure Gef. Optimized SD of Gef (S2-MW) presented significant release of Gef (82.10%) compared with pure Gef (21.23%). The optimized Gef SD (S2) was subjected to in vivo pharmacokinetic evaluation in comparison with pure Gef in rats. The results indicated significant enhancement in various pharmacokinetic parameters of Gef from an optimized SD S2 compared to the pure Gef. In addition, Gef-SD S2 resulted in remarkable improvement in bioavailability compared to the pure Gef. Overall, this study suggested that the prepared Gef-SD by microwave method showed marked enhancement in dissolution and bioavailability.

scholarly journals GASTRO-FLOATING TABLETS OF REPAGLINIDE: PREPARATION AND IN VIVO EVALUATION

2018 ◽  
Vol 11 (7) ◽  
pp. 291
Author(s):  
Poornima P ◽  
Abbulu K ◽  
Mukkanti K
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Effective Management ◽  
Drug Bioavailability ◽  
In Vivo Evaluation ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Evaluation Parameters

Objective: Current research concerns the expansion of repaglinide matrix floating tablets, which are designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects.Methods: Different formulations of repaglinide floating tablets were prepared with different grades of hydroxypropyl methylcellulose (HPMC) and other agents. Evaluation parameters and in vivo bioavailability studies were conducted in the suitable model.Results: Among all the formulations, F21 containing HPMC K1500 PH PRM, Polyox WSR 303, and sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physicochemical properties, floating lag time (36 s), and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24 h whereas 95.09±5.01% of the drug was released from the marketed product within 1 h.Conclusion: From in vitro and in vivo bioavailability studies repaglinide floating tablets expected to give a new choice for safe, economical, and increased bioavailability for effective management of diabetes mellitus.

scholarly journals Microspheres prepared with biodegradable PHBV and PLA polymers as prolonged-release system for ibuprofen: in vitro drug release and in vivo evaluation

2012 ◽  
Vol 48 (4) ◽  
pp. 773-780 ◽  
Author(s):  
Giovana Carolina Bazzo ◽  
Aline Teixeira de Macedo ◽  
Janine Paula Crenca ◽  
Virgínia Emiliana Silva ◽  
Eduardo Manoel Pereira ◽  
...  
Keyword(s):  
Drug Release ◽  
Maximum Level ◽  
Immediate Release ◽  
Spherical Particles ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
In Vivo Evaluation ◽  
Evaporation Technique

In this study, poly(hydroxybutyrate-co-hydroxyvalerate) (PHBV) and poly(l-lactide) (PLA) microspheres containing ibuprofen were prepared with the aim of prolonging the drug release. The oil-in-water (O/W) emulsion solvent evaporation technique was used, varying the polymer ratio. All formulations provided spherical particles with drug crystals on the surface and a porous and rough polymeric matrix when PHBV was used and smooth external surface when prepared with PLA. The in vitro dissolution profiles show that the formulation containing PHBV/PLA at the proportion of 30/70 presented the best results in terms of prolonging the ibuprofen release. The analysis of the concentration of ibuprofen in the blood of rats showed that maximum levels were achieved at between one and two hours after administration of the immediate-release form (pure drug), while the prolonged microspheres led to a small amount of the drug being released within the first two hours and reached the maximum level after six hours of administration. It was concluded that it is possible to prolong the release of ibuprofen through its incorporation into PHBV/PLA microspheres.

Development and In Vitro – In Vivo Evaluation of Gastro-retentive Floating Tablets Containing Repaglinide

2018 ◽  
Vol 11 (2) ◽  
pp. 4026-4036
Author(s):  
Poornima P ◽  
Abbulu K ◽  
Mukkanti K
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Drug Bioavailability ◽  
In Vivo Evaluation ◽  
Gastric Residence Time

The present investigation concerns the development of the repaglinide floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K1500 PH PRM, Polyox WSR-303 and Sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physico chemical properties, floating lag time (36 sec) and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24h whereas 95.09±5.01% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non-Fickian transport by coupled diffusion and erosion. In vivo experiments supported the expectations in prolonging the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time for the tested tablets was 270 min±60. This result is encouraging, because a longer gastric residence time is an important condition for higher bioavailability of the drugs included in the prolonged or controlled release dosage forms.

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