Formulation and Evaluation of Nanosuspension of Simvastatin

2015 ◽  
Vol 8 (2) ◽  
pp. 2858-2873
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L Shid
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Factorial Design ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Total Drug ◽  
23 Factorial Design ◽  
Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the  preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin  (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial  design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

Formulation and Evaluation of Nanosuspension Formulation for Drug Delivery of Simvastatin

2014 ◽  
Vol 7 (4) ◽  
pp. 2650-2665
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L. Shid
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
In Vivo Study ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Total Drug ◽  
Poloxamer 188 ◽  
Drug Content

Poor water solubility and slow dissolution rate are issues drug content and polydispersity index. The obtained for the majority of upcoming and existing biologically results showed that particle size (nm) and rate of active compounds. Simvastatin is poorly water-soluble  dissolution has been improved when nanosuspension drug and its bioavailability is very low from its crystalline prepared with the higher concentration of PVPK-30 and form. The purpose of the present investigation was to Poloxamer-188 and lower concentration of SLS. The increase the solubility and dissolution rate of simvastatin by particle size and zeta potential of optimized formulation the preparation of nanosuspension by Emulsification was found to be 258.3 nm and 23.43. The rate of Solvent Diffusion Method at laboratory scale. Prepared dissolution of the optimized nanosuspension was nanosuspension was evaluated for its particle size and enhanced (90.02% in 60min), relative to plain simvastatin in vitro dissolution study and characterized by zeta (21% in 60 min), mainly due to the formation of nanosized potential, differential scanning calorimetry (DSC) and particles. These results indicate the suitability of 23 factorial X-Ray diffractometry (XRD), Motic digital microscopy, design for preparation of simvastatin loaded nanosus- entrapment efficiency, total drug content, saturated pension significantly improved in vitro dissolution rate, solubility study and in vivo study. A 23 factorial design was and thus possibly enhance fast onset of therapeutic drug employed to study the effect of independent variables, effect. In vivo study shows increase in bioavailability in amount of SLS (X1), amount of PVPK-30 (X2) and nanosuspension formulation than the plain simvastatin Poloxamer-188 (X3) and dependent variables are Total drug. 

Development and Characterization of Oral Nanosuspension Using Esomeprazole Magnesium Trihydrate

2020 ◽  
Vol 10 (6) ◽  
pp. 909-917
Author(s):  
Surya Goel ◽  
Vijay Agarwal ◽  
Monika Sachdeva
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
Research Work ◽  
In Vitro Dissolution ◽  
Top Down ◽  
Bottom Up ◽  
Poloxamer 188 ◽  
Esomeprazole Magnesium

Background: Nanosuspension has arisen as a lucrative, remunerative, as well as a potent approach to improve the solubility and dissolution rate of poorly soluble drug entities. Several challenges are still present in this technology which need more research. Objective: The prime aim of this research work is to develop, optimize and characterize the oral nanosuspension using esomeprazole magnesium trihydrate as a drug candidate. Methods: The drug nanosuspensions were prepared using both approaches; Top-down and Bottom-up as the combinational approach. Poloxamer 188 was used as a stabilizer in this study. All the important formulation variables, like concentration of stabilizers that may influence characteristics of the nanosuspensions, were optimized. Formulation screening was performed using the optimization process, and the optimized nanosuspension was evaluated for its particle size, polydispersity index, zeta potential, shape, in vitro drug release and stability. Results: For optimization of drug nanosuspension, the effect of Poloxamer 188 concentration and esomeprazole concentration was investigated and the optimal values were 0.3% w/v and 4 mg/ml, respectively. The particle size of nanosuspensions was in the range of 185 to 1048 nm with varying the zeta potential values from -11.2 to -27.5 mV. The in vitro dissolution rate of esomeprazole was increased up to 3-folds, approximately (92% in 90 min) as compared with crude esomeprazole drug (31% in 90 min) due to the decrease in particle size. Conclusion: The result indicated that the combination of top-down and bottom-up approach used for preparing the oral nanosuspension is a suitable approach for poorly aqueous soluble drug moieties like esomeprazole magnesium.

Formulation and Evaluation of Nanosuspension Delivery System for Simvastatin

2014 ◽  
Vol 7 (2) ◽  
pp. 2459-2475 ◽  
Author(s):  
Rupali Shid L. ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L. Shid L.
Keyword(s):  
Zeta Potential ◽  
Dissolution Rate ◽  
Water Soluble ◽  
In Vivo Study ◽  
Diffusion Method ◽  
Total Drug ◽  
Poloxamer 188 ◽  
Drug Content

Poor water solubility and slow dissolution rate are issues polydispersity index. The obtained results showed that for the majority of upcoming and existing biologically active  particlesize (nm) and rate of dissolution has been improved compounds. Simvastatin is poorly water-soluble drug and  when nanosuspension prepared with the higher its bioavailability is very low from its crystalline form. The  concentration of PVPK-30 with the higher concentration of purpose of the present investigation was to increase the  PVP K-30 and Poloxamer-188 and lower concentration of solubility and dissolution rate of simvastatin by the  SLS. The partical size and zeta potential of optimized preparation of nanosuspension by Emulsification Solvent  formulation was found to be 258.3 nm and 23.43. The rate Diffusion Method at laboratory scale. Prepared nanosus- of dissolution of the optimized nanosuspension was pension was evaluated for its particle size and in vitro  enhanced (90.02% in 60 min), relative to plain simvastatin dissolution study and characterized by zeta potential, (21% in 60 min), mainly due to the formation of nanosized differential scanning calorimetry (DSC) and X-Ray particles. These results indicate the suitability of 23 factorial diffractometry (XRD), motic digital microscopy, entrapment  design for preparation of simvastatin loaded efficiency, total drug content, saturated solubility study and nanosuspension significantly improved in vitro dissolution in vivo study. A 23 factorial design was employed to study  rate, and thus possibly enhance fast onset of therapeutic the effect of independent variables, amount of SLS (X1), drug effect. In vivo study shows increase in bioavailability in amount of PVPK-30 (X2) and Poloxamer-188 (X3) and  nanosuspension formulation than the plain simvastatin dependent variables are total drug content and drug. 

scholarly journals An impact of nanocrystals on dissolution rate of Lercanidipine: Supersaturation and crystallization by addition of solvent to antisolvent

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Dolly Tulsibhai Gadhiya ◽  
Jayvadan K. Patel ◽  
Arti Arjanbhai Bagada
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
High Speed ◽  
Particle Morphology ◽  
In Vitro Dissolution ◽  
Antisolvent Precipitation ◽  
Pvp K30

Abstract Background Nanocrystals of any drug are pure solid drug particles with a mean diameter in nanometer range. Dissolution is a crucial factor for absorption of medicine in case of water-insoluble or poorly soluble drugs. The aim of this study was to develop nanocrystals of a hydrophobic drug, Lercanidipine, by addition of solvent to an antisolvent with high-speed homogenization to achieve dissolution and solubility enhancement. Addition of organic solvent to antisolvent results in genesis of nanosized particles due to fast nucleation process and rapid mixing. The nanosuspension was formulated using PVP K30 as a stabilizer. Further, nanosuspensions were lyophilized to convert into solid nanocrystals using mannitol as a cryoprotectant. The developed nanosuspensions were characterized for particle size, zeta potential, saturation solubility, and in vitro dissolution studies. Lyophilized solid nanocrystals were characterized for FTIR, SEM, XRD, and zeta potential (ζ). Results Central composite design was executed to study influence of amount of stabilizer and solvent to antisolvent ratio (independent variables) on particle size and % drug release at 10 min (dependent variables). The particle size of the developed Lercanidipine nanosuspensions were observed in the range of 302.00 ± 10.58 to 484.33 ± 6.51 nm measured by Zetatrac. A considerable increase was found in the solubility and dissolution rate of the nanocrystals as compared to pure drug. The drug release from Lercanidipine nanosuspensions was increased up to 88.95% within 10 min as compared to pure Lercanidipine which was only 21.53%. The X-ray diffraction study of lyophilized nanocrystals showed sharp and distinct peaks due to an increse in crystallinity of Lercanidipine Particle morphology was studied by scanning electron microscopy revealed that nanoprecipitated particles with lyophilization in the presence of mannitol exhibited dendrite needle-like crystals. Conclusion The nanocrystal development by antisolvent precipitation procedure using methanol as solvent, water as antisolvent, and low amounts of PVP K30 as stabilizer is a very promising and effective method to increase the dissolution rate of Lercanidipine. Graphical abstract

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.

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.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Atorvastatin calcium loaded chitosan nanoparticles: in vitro evaluation and in vivo pharmacokinetic studies in rabbits

2015 ◽  
Vol 51 (2) ◽  
pp. 467-477 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Ranjit Konwar ◽  
Rupa Sengupta
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Oral Bioavailability ◽  
Chitosan Nanoparticles ◽  
Rabbit Model ◽  
Pharmacokinetic Studies ◽  
Release Formulation ◽  
Atorvastatin Calcium

<p>In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, <italic>in vitro</italic> release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva<sup>(r))</sup> in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. <italic>In vitro</italic> release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva<sup>(r))</sup>. Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.</p>

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