scholarly journals Formulation and In-Vitro evaluation of Nanocrystal formulation of poorly soluble drugs

2020 ◽  
Vol 9 (4-s) ◽  
pp. 1183-1190
Author(s):  
Arvind Sharma ◽  
Alok Pal Jain ◽  
Sandeep Arora
Keyword(s):  
Particle Size ◽  
In Vitro Study ◽  
Physicochemical Characteristics ◽  
Precipitation Method ◽  
Drug Candidate ◽  
Poorly Soluble Drugs ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Poorly Soluble

Introduction:-Poor solubility of drug compounds which accounts for 40% of new molecules investigated at present is an issue of great concern in pharmaceutical industry and reducing particle size (i,e to reduce below 1000 nm )of drug candidate to be investigated is one of the simplest and efficient ways to overcome this challenge. Drug nanocrystals, solid nanosized drug particles are defined as formulation having 100% drug, which are covered by a stabilizer layer. In this study attempt was made to formulate and evaluate nanocrystals of poorly soluble drugs having low oral bioavailability. Material and method:- Nanocrystals were prepared successfully by varying concentration of different stabilizers by anti-solvent precipitation method. The formulated nanocrystals were evaluated by determining physicochemical characteristics such as physical appearance, Differential Scanning Calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffractometry, solubility studies, particle size distribution, zeta potential, and in vitro drug release profile studies. Results:- An in-vitro study was performed on the successful formulation in comparison to drug powder using dissolution apparatus The particle size of RVT and PSNC-3 was found to be 1975.3 nm and 790.1 nm respectively. Conclusion: Precipitated Nanocrystals formulated with different stablizer’s method resultedin formation of small and uniform RVT nanocrystals with an improved saturation solubility, dissolution rate. Keywords: Nanocrystal, poorly soluble drugs

scholarly journals FABRICATION AND IN VITRO CHARACTERIZATION OF A NOVEL NANOSUSPENSION OF TELMISARTAN: A POORLY SOLUBLE DRUG PREPARED BY ANTISOLVENT PRECIPITATION TECHNIQUE USING 33 FACTORIAL DESIGN

2020 ◽  
pp. 286-294
Author(s):  
PRASANTA KUMAR MOHAPATRA ◽  
SIREESHA ◽  
VAIBHAV RATHORE ◽  
HARISH CHANDRA VERMA ◽  
BIBHUTI PRASAD RATH ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
Release Kinetics ◽  
Precipitation Method ◽  
Lauryl Sulfate ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Objective: The motivation behind the current examination was to build the solvency and dissolution rate of an antihypertensive drug telmisartan by the planning of nanosuspension by precipitation method at the research facility scale. We researched the nanoparticle manufacture of telmisartan employing a 33 factorial experimental configuration considering the impacts of nanosuspension on the physical, morphological, and dissolution properties of telmisartan. Methods: To get ready, nanosuspension particles of an ineffectively dissolvable drug are moreover of a drug solution to the anti-solvent leads to abrupt supersaturation and precipitation the making of nanoparticles. The nanosuspension particles of a poorly soluble drug loaded with urea and surfactants (sodium lauryl sulfate (SLS), poloxamer 188, Tween 80) have been prepared by a precipitation method. The nanosuspension particles were characterized for particle size, zeta potential, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), in vitro drug release, and release kinetics. Results: The readily optimized batch nanosuspension particles evaluated and exhibited the particle size (750 nm), zeta potential (-24.33 mV), differential scanning calorimetry (DSC) drug exhibited a change in crystalline form to amorphous, in vitro dissolution (F12 was higher 95% within 5 min) and drug release kinetics. The formulation parameter of surfactant concentration is optimized. Conclusion: The formulation of the nanosuspension approach has been shown to substantial improvement in the dissolution rate, thereby enhancing the oral bioavailability with the future development of this technology.

Formulation and Characterization of Nateglinide Nanosuspension by Precipitation Method

2014 ◽  
Vol 7 (4) ◽  
pp. 2685-2691
Author(s):  
Amruta Papdiwal ◽  
Kishor Sagar ◽  
Vishal Pande
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Water Solubility ◽  
Average Particle Size ◽  
Biologically Active ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Average Particle ◽  
Scanning Calorimetry

Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.

scholarly journals PREPARATION, CHARACTERIZATION, AND EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF ETORICOXIB LOADED SOLUPLUS® NANOCOMPOSITES

2018 ◽  
Vol 10 (6) ◽  
pp. 268
Author(s):  
Yogesh Pore ◽  
Madhuri Mane ◽  
Vaishnavi Mangrule ◽  
Atul Chopade ◽  
Pankaj Gajare
Keyword(s):  
Particle Size ◽  
Physicochemical Properties ◽  
Inflammatory Activity ◽  
Log P ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Dissolution Efficiency

Objective: The objective of this study was to prepare and characterize etoricoxib (ECB) loaded Soluplus® nanocomposites to improve its physicochemical properties. The effect of polymer and surfactant concentration on particle size, in vitro percentage dissolution efficiency and the anti-inflammatory activity of nanocomposites were also investigated.Methods: The nanocomposites were prepared by using a freeze-drying technique. The analytical evidence for the formulation of lyophilized nanocomposites in solid state were generated and confirmed by differential scanning calorimetry (DSC), fourier transformation infrared spectroscopy (FTIR), x-ray powder diffractometry (XPRD) and scanning electron microscopy (SEM). The in vitro drug release profile of nanocomposites was compared with pure ECB powder.Results: The nanocomposites of ECB were contained in a nano range with particle size and zeta potential of 63.5 nm and 46.5 mv, respectively. The solubility and dissolution of the nanocomposites were significantly (p<0.001) improved as compared to ECB alone, evidenced by decreased log P values (1.90±0.002) of the nanocomposites. The characterization studies revealed the formation of amorphous nanocomposites of ECB with existence of physical interactions between drug and polymer. The anti-inflammatory activity of nanocomposites evaluated by carrageenan-induced rat paw edema model demonstrated nonsignificant (p>0.05) increase in anti-inflammatory activity as compared to pure ECB.Conclusion: From the results, it could be concluded that the formation of ECB nanocomposites with Soluplus® could be an effective and alternative approach to modify the physicochemical properties of ECB.

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.

scholarly journals The Influence of a Knitted Hydrophilic Prosthesis of Blood Vessels on the Activation of Coagulation System—In Vitro Study

Nanomaterials ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 1600
Author(s):  
Maria Szymonowicz ◽  
Maciej Dobrzynski ◽  
Sara Targonska ◽  
Agnieszka Rusak ◽  
Zbigniew Rybak ◽  
...  
Keyword(s):  
Blood Vessels ◽  
Initial Period ◽  
In Vitro Study ◽  
Vascular Prosthesis ◽  
Coagulation System ◽  
Factor Xii ◽  
Scanning Calorimetry ◽  
Vascular Prostheses ◽  
Control Value

The replacement of affected blood vessels of the polymer material can cause imbalances in the blood haemostatic system. Changes in blood after the implantation of vascular grafts depend not only on the chemical composition but also on the degree of surface wettability. The Dallon® H unsealed hydrophilic knitted vascular prosthesis double velour was assessed at work and compare with hydrophobic vascular prosthesis Dallon®. Spectrophotometric studies were performed in the infrared and differential scanning calorimetry, which confirmed the effectiveness of the process of modifying vascular prostheses. Determination of the parameters of coagulation time of blood after contact in vitro with Dallon® H vascular prosthesis was also carried out. Prolongation of activated thromboplastin time, decreased activity of factor XII, IX and VIII, were observed. The prolonged thrombin and fibrinogen were reduced in the initial period of the experiment. The activity of plasminogen and antithrombin III and protein C were at the level of control value. The observed changes in the values of determined parameters blood coagulation do not exceed the range of referential values for those indexes. The observed changes are the result of considerable blood absorptiveness by the prosthesis of blood vessels and their sealing.

scholarly journals Physicochemical Characteristics of Arginine Enriched NaF Varnish: An In Vitro Study

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2998
Author(s):  
Mohammed Nadeem Bijle ◽  
Manikandan Ekambaram ◽  
Edward Lo ◽  
Cynthia Yiu
Keyword(s):  
Molecular Dynamics ◽  
Physical Properties ◽  
Artificial Saliva ◽  
Chemical Properties ◽  
In Vitro Study ◽  
Physicochemical Characteristics ◽  
Vitro Study ◽  
Physical And Chemical ◽  
Stable Matrix

The in vitro study objectives were to investigate the effect of arginine (Arg) incorporation in a 5% sodium fluoride (NaF) varnish on its physical and chemical properties including F/Arg release. Six experimental formulations were prepared with L-arginine (L-Arg) and L-arginine monohydrochloride at 2%, 4%, and 8% w/v in a 5% NaF varnish, which served as a control. The varnishes were subjected to assessments for adhesion, viscosity, and NaF extraction. Molecular dynamics were simulated to identify post-dynamics total energy for NaF=Arg/Arg>NaF/Arg<NaF concentrations. The Arg/F varnish release profiles were determined in polyacrylic lactate buffer (pH-4.5; 7 days) and artificial saliva (pH-7; 1 h, 24 h, and 12 weeks). Incorporation of L-Arg in NaF varnish significantly influences physical properties ameliorating retention (p < 0.001). L-Arg in NaF varnish institutes the Arg-F complex. Molecular dynamics suggests that NaF>Arg concentration denotes the stabilized environment compared to NaF<Arg (p < 0.001). The 2% Arg-NaF exhibits periodic perennial Arg/F release and shows significantly higher integrated mean F release than NaF (p < 0.001). Incorporating 2% L-arginine in 5% NaF varnish improves its physical properties and renders a stable matrix with enduring higher F/Arg release than control.

Chitosan nanoparticles for tamoxifen delivery and cytotoxicity to MCF-7 and Vero cells

2011 ◽  
Vol 83 (11) ◽  
pp. 2027-2040 ◽  
Author(s):  
Neralakere Ramanna Ravikumara ◽  
Basavaraj Madhusudhan
Keyword(s):  
Particle Size ◽  
Chitosan Nanoparticles ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Correlation Spectroscopy ◽  
Scanning Calorimetry ◽  
Ζ Potential ◽  
Human Red Blood Cells ◽  
Tamoxifen Citrate

In this study, tamoxifen citrate-loaded chitosan nanoparticles (tamoxcL-ChtNPs) and tamoxifen citrate-free chitosan nanoparticles (tamoxcF-ChtNPs) were prepared by an ionic gelation (IG) method. The physicochemical properties of the nanoparticles were analyzed for particle size, zeta (ζ) potential, and other characteristics using photon correlation spectroscopy (PCS), zeta phase analysis light scattering (PALS), scanning electron microscopy (SEM), Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC). The variation in particle size was assessed by changing the concentration of chitosan, pentasodium tripolyphosphate (TPP), and the pH of the solution. The optimized tamoxcL-ChtNPs showed mean diameter of 187 nm, polydispersity of 0.125, and ζ-potential of +19.1 mV. The encapsulation efficiency (EE) of tamoxifen citrate (tamoxc) increased at higher concentrations, and release of tamoxc from the chitosan matrix displayed controlled biphasic behavior. Those tamoxcL-ChtNPs tested for chemosensitivity showed dose- and time-dependent antiproliferative activity of tamoxc. Further, tamoxcL-ChtNPs were found to be hemocompatible with human red blood cells (RBCs) and safe by in vitro cytotoxicity tests, suggesting that they offer promise as drug delivery systems in therapy.

In vitro -in vivo correlation in the effect of cyclodextrin on oral absorption of poorly soluble drugs

2021 ◽  
pp. 120494
Author(s):  
Risa Aihara ◽  
Roman Messerschmid ◽  
Masashi Mizoguchi ◽  
Koichi Wada ◽  
Keiko Minami ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals Poly(δ-valerolactone)/Poly(ethylene-co-vinylalcohol)/β-Tricalcium Phosphate Composite as Scaffolds: Preparation, Properties, and In Vitro Amoxicillin Release

Polymers ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 46
Author(s):  
Mohammed Badwelan ◽  
Mohammed Alkindi ◽  
Osama Alghamdi ◽  
Waseem Sharaf Saeed ◽  
Abdel-Basit Al-Odayni ◽  
...  
Keyword(s):  
Hybrid Materials ◽  
Tricalcium Phosphate ◽  
Drug Carrier ◽  
Human Mesenchymal Stem Cells ◽  
In Vitro Study ◽  
Micro Computed Tomography ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Poly Ethylene

Two poly(δ-valerolactone)/poly(ethylene-co-vinylalcohol)/β-tricalcium phosphate (PEVAL/PDVAL/β-TCP) composites containing an equal ratio of polymer and filled with 50 and 70 wt% of β-TCP microparticles were prepared by the solvent casting method. Interconnected pores were realized using the salt leached technique, and the porosity of the resulted composites was evaluated by the scanning electron microscopy (SEM) method. The homogeneity of the hybrid materials was investigated by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The prepared materials’ SEM images showed interconnected micropores that respond to the conditions required to allow their uses as scaffolds. The porosity of each scaffold was determined from micro computed tomography (micro-CT) data, and the analysis of the mechanical properties of the prepared materials was studied through the stress-strain compressive test. The proliferation test results used human mesenchymal stem cells (MSCs) to grow and proliferate on the different types of prepared materials, reflecting that the hybrid materials were non-toxic and could be biologically acceptable scaffolds. The antibacterial activity test revealed that incorporation of amoxicillin in the specimens could inhibit the bacterial growth of S. aureus. The in vitro study of the release of amoxicillin from the PEVAL/PDVAL/amoxicillin and PEVAL/PDVAL/β-TCP/amoxicillin drug carrier systems in pH media 7.4, during eight days, gave promising results, and the antibiotic diffusion in these scaffolds obeys the Fickian model.

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.

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