scholarly journals Encapsulation of water-insoluble drug by a cross-linking technique: Effect of process and formulation variables on encapsulation efficiency, particle size, and in vitro dissolution rate

AAPS PharmSci ◽  
2004 ◽  
Vol 6 (1) ◽  
pp. 112-119 ◽  
Author(s):  
Pralhad T. Tayade ◽  
Rajendrakumar D. Kale
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Encapsulation Efficiency ◽  
In Vitro Dissolution ◽  
Cross Linking ◽  
Technique Effect ◽  
Water Insoluble Drug ◽  
Formulation Variables

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.

scholarly journals Nanosuspensions of Selexipag: Formulation, Characterization, and in vitro Evaluation

2021 ◽  
Vol 30 (1) ◽  
pp. 144-153
Author(s):  
Rusul M. Alwan ◽  
Nawal A. Rajab
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Antisolvent Precipitation ◽  
Prostacyclin Receptor ◽  
Pulmonary Arterial ◽  
Formulation Parameters ◽  
Long Acting

Selexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm with PDI and Zeta potential value of 0.073 and -47mV, respectively. SLPNS exhibited an increase in the dissolution rate in phosphate buffer pH 6.8 (100% drug release during 60 min) compared to the pure drug ( 40% during the same time). This result indicates that SLPNS is an efficient way of improving the dissolution rate.  

scholarly journals Formulation and evaluation of self nano-emulsifying drug delivery system of ezetimibe for dissolution rate enhancement

2020 ◽  
Vol 11 (2) ◽  
pp. 1294-1301
Author(s):  
Geethanjali K ◽  
Vaiyana Rajesh C
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Dissolution Rate ◽  
Delivery System ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Cinnamon Oil ◽  
Peg 400 ◽  
Solid Form

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was         90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.

scholarly journals Pure Trans-Resveratrol Nanoparticles Prepared by a Supercritical Antisolvent Process Using Alcohol and Dichloromethane Mixtures: Effect of Particle Size on Dissolution and Bioavailability in Rats

Antioxidants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 342 ◽  
Author(s):  
Eun-Sol Ha ◽  
Heejun Park ◽  
Seon-Kwang Lee ◽  
Woo-Yong Sim ◽  
Ji-Su Jeong ◽  
...  
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
In Vitro Dissolution ◽  
Absolute Bioavailability ◽  
Simulated Gastric Fluid ◽  
Mean Particle Size ◽  
Supercritical Antisolvent ◽  
Effect Of Particle Size

The aim of this study was to prepare pure trans-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) using a supercritical antisolvent (SAS) process with alcohol (methanol or ethanol) and dichloromethane mixtures. In addition, in order to investigate the effect of particle size on the dissolution and oral bioavailability of the trans-resveratrol, two microparticles with different sizes (1.94 μm and 18.75 μm) were prepared using two different milling processes, and compared to trans-resveratrol nanoparticles prepared by the SAS process. The solid-state properties of pure trans-resveratrol particles were characterized. By increasing the percentage of dichloromethane in the solvent mixtures, the mean particle size of trans-resveratrol was decreased, whereas its specific surface area was increased. The particle size could thus be controlled by solvent composition. Trans-resveratrol nanoparticle with a mean particle size of 0.17 μm was prepared by the SAS process using the ethanol/dichloromethane mixture at a ratio of 25/75 (w/w). The in vitro dissolution rate of trans-resveratrol in fasted state-simulated gastric fluid was significantly improved by the reduction of particle size, resulting in enhanced oral bioavailability in rats. The absolute bioavailability of trans-resveratrol nanoparticles was 25.2%. The maximum plasma concentration values were well correlated with the in vitro dissolution rate. These findings clearly indicate that the oral bioavailability of trans-resveratrol can be enhanced by preparing pure trans-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) by the SAS process. These pure trans-resveratrol nanoparticles can be applied as an active ingredient for the development of health supplements, pharmaceutical products, and cosmetic products.

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.

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 Formulations of Ramipril using Hydrophilic Polymers

2015 ◽  
Vol 8 (1) ◽  
pp. 2735-2741
Author(s):  
Pankaj P Nerker ◽  
Hitendra Mahajan ◽  
Sagar Deore ◽  
Pradyumn Ige
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Hydrophilic Polymers ◽  
In Vitro Dissolution ◽  
Average Particle ◽  
Antisolvent Precipitation ◽  
Enhanced Dissolution

Nanosuspensions provide convenient formulations for improving the bioavailability and drug delivery. The objective of the investigation was to develop stable nanosuspension formulation of ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavailability. Ramipril is a potent antihypertensive drug, which act by inhibiting the angiotensin-converting enzyme. Nanosuspension was developed by antisolvent precipitation followed by high-pressure homogenization using hydrophilic polymers such as HPMC E5, HPMC E15, PVP K30, PVP K25, and PVA. The resulting nanosuspension was transformed into dry powder by freeze-drying process. Among all five formulations a formulation was choosen on the basis of results obtained from comparative study between different polymers based nanosuspension formulation of ramipril. The nanosuspension prepared was then evaluated for particle size, polydispesivity index, zeta potential, entrapment efficiency, saturated solubility study, scanning electron microscopy, differential scanning colorometry, and X ray diffraction. The combination of soya lecithin and pluronic F-68 as stabilizers yield nanosuspension with the smallest average particle size. The formulation of ramipril based on HPMC E 15 (Formulation B) shown enhanced dissolution rate. In which more than 60% of the drug was dissolved in the first 20 min compared to less than 25% of the pure drug within the same time period. The increase in the in vitro dissolution rate, nano size may favourably affect bioavailability.

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. 

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